Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
139392567 192465 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 C[C@]1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5208674 192465 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 C[C@]1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392567 192465 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 C[C@]1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5208674 192465 0 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 C[C@]1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
155792928 190541 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 CC1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5179782 190541 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 CC1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392897 190475 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C(C)N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5178891 190475 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C(C)N)C2)c1 10.1016/j.bmcl.2022.128807
168269957 189905 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)ccc(F)c3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5169724 189905 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)ccc(F)c3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392897 190475 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C(C)N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5178891 190475 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C(C)N)C2)c1 10.1016/j.bmcl.2022.128807
155792928 190541 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 CC1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5179782 190541 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.2 CC1(N)CCN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
168269957 189905 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)ccc(F)c3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5169724 189905 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)ccc(F)c3[nH]2)C1 10.1016/j.bmcl.2022.128807
16129706 209031 40 None -8 11 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 209031 40 None -8 11 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
139392643 190613 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 448 4 2 5 4.4 CC(N)C1CN(c2c(-c3cc(F)cc(C#N)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5180885 190613 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 448 4 2 5 4.4 CC(N)C1CN(c2c(-c3cc(F)cc(C#N)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392643 190613 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 448 4 2 5 4.4 CC(N)C1CN(c2c(-c3cc(F)cc(C#N)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5180885 190613 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 448 4 2 5 4.4 CC(N)C1CN(c2c(-c3cc(F)cc(C#N)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392666 190202 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5174433 190202 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392666 190202 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5174433 190202 0 None 1 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392711 190331 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 3 2 4 4.8 N[C@H]1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5176490 190331 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 3 2 4 4.8 N[C@H]1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392701 191379 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5192315 191379 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392711 190331 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 3 2 4 4.8 N[C@H]1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5176490 190331 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 3 2 4 4.8 N[C@H]1CCN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cccc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392701 191379 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5192315 191379 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 491 4 2 4 5.5 CC(N)C1CN(c2c(-c3cc(F)cc(C(F)(F)F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392904 191029 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 457 4 2 4 5.1 CC(N)C1CN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5186952 191029 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 457 4 2 4 5.1 CC(N)C1CN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392904 191029 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 457 4 2 4 5.1 CC(N)C1CN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5186952 191029 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 457 4 2 4 5.1 CC(N)C1CN(c2c(-c3cc(F)cc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392693 189941 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 4 2 4 4.6 NCC1CN(c2c(-c3cccc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5170249 189941 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 4 2 4 4.6 NCC1CN(c2c(-c3cccc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392804 191603 1 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5195355 191603 1 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392693 189941 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 4 2 4 4.6 NCC1CN(c2c(-c3cccc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5170249 189941 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 425 4 2 4 4.6 NCC1CN(c2c(-c3cccc(Cl)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392804 191603 1 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5195355 191603 1 None -1 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 3 2 5 4.1 Cc1cccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392859 190834 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 432 3 2 5 4.5 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5184249 190834 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 432 3 2 5 4.5 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392887 192058 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 398 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5202527 192058 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 398 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392887 192058 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 398 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5202527 192058 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 398 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392859 190834 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 432 3 2 5 4.5 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5184249 190834 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 432 3 2 5 4.5 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392614 190419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)ccc1F 10.1016/j.bmcl.2022.128807
CHEMBL5177934 190419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)ccc1F 10.1016/j.bmcl.2022.128807
139392614 190419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)ccc1F 10.1016/j.bmcl.2022.128807
CHEMBL5177934 190419 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)ccc1F 10.1016/j.bmcl.2022.128807
155792947 191910 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1c(F)ccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5200076 191910 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1c(F)ccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
155792947 191910 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1c(F)ccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5200076 191910 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1c(F)ccc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392561 192026 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5201920 192026 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392526 191831 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 3 6 3.2 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CCC(N)(CO)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5198832 191831 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 3 6 3.2 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CCC(N)(CO)C2)c1 10.1016/j.bmcl.2022.128807
139392561 192026 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5201920 192026 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392665 191455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 421 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5193208 191455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 421 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392665 191455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 421 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5193208 191455 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 421 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(Cl)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392524 190600 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5180721 190600 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392524 190600 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5180721 190600 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
152122090 191113 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 3 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5187920 191113 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 3 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392604 191168 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5188855 191168 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392875 192185 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1cc(F)cc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5204225 192185 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1cc(F)cc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392522 191024 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1F 10.1016/j.bmcl.2022.128807
CHEMBL5186865 191024 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1F 10.1016/j.bmcl.2022.128807
168271385 190591 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CCC(N)(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5180466 190591 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CCC(N)(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
139392839 191647 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3ccc(F)cc3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5195986 191647 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3ccc(F)cc3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392839 191647 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3ccc(F)cc3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5195986 191647 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3ccc(F)cc3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392713 190221 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
CHEMBL5174784 190221 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
16737814 85507 0 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227212 85507 0 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL504838 85507 0 None -1 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
139392713 190221 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
CHEMBL5174784 190221 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
139392619 190846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2nc(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)n(C)c12 10.1016/j.bmcl.2022.128807
CHEMBL5184442 190846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2nc(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)n(C)c12 10.1016/j.bmcl.2022.128807
10096510 57428 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity on human somatostatin receptor 5Agonist activity on human somatostatin receptor 5
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL165402 57428 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity on human somatostatin receptor 5Agonist activity on human somatostatin receptor 5
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
139392619 190846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2nc(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)n(C)c12 10.1016/j.bmcl.2022.128807
CHEMBL5184442 190846 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2nc(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)n(C)c12 10.1016/j.bmcl.2022.128807
139392612 191272 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 4 2 5 4.0 Cc1cc(F)cc(-c2cncc(-c3nc4c(C#N)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5190580 191272 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 4 2 5 4.0 Cc1cc(F)cc(-c2cncc(-c3nc4c(C#N)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392612 191272 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 4 2 5 4.0 Cc1cc(F)cc(-c2cncc(-c3nc4c(C#N)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5190580 191272 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 412 4 2 5 4.0 Cc1cc(F)cc(-c2cncc(-c3nc4c(C#N)cccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392737 191928 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 417 5 2 5 4.1 COc1cccc2[nH]c(-c3cncc(-c4cc(C)cc(F)c4)c3N3CC(CN)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5200338 191928 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 417 5 2 5 4.1 COc1cccc2[nH]c(-c3cncc(-c4cc(C)cc(F)c4)c3N3CC(CN)C3)nc12 10.1016/j.bmcl.2022.128807
139392875 192185 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1cc(F)cc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5204225 192185 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 430 3 2 5 4.3 Cc1cc(F)cc2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12 10.1016/j.bmcl.2022.128807
139392604 191168 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5188855 191168 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392654 190665 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5181646 190665 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392732 190838 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C)(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5184298 190838 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C)(CN)C2)c1 10.1016/j.bmcl.2022.128807
11705763 168315 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 168315 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
139392654 190665 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5181646 190665 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392648 190737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 4 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5182636 190737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 4 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392732 190838 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C)(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5184298 190838 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 437 4 2 4 4.8 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(C)(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392648 190737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 4 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5182636 190737 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 4 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
152122090 191113 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 3 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5187920 191113 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 3 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392737 191928 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 417 5 2 5 4.1 COc1cccc2[nH]c(-c3cncc(-c4cc(C)cc(F)c4)c3N3CC(CN)C3)nc12 10.1016/j.bmcl.2022.128807
CHEMBL5200338 191928 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 417 5 2 5 4.1 COc1cccc2[nH]c(-c3cncc(-c4cc(C)cc(F)c4)c3N3CC(CN)C3)nc12 10.1016/j.bmcl.2022.128807
139392635 191150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)c(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5188516 191150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)c(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392635 191150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)c(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5188516 191150 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 4 2 4 4.4 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)c(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392637 192410 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2c1nc(-c1cncc(-c3cc(F)cc(C#N)c3)c1N1CC[C@H](N)C1)n2C 10.1016/j.bmcl.2022.128807
CHEMBL5208031 192410 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2c1nc(-c1cncc(-c3cc(F)cc(C#N)c3)c1N1CC[C@H](N)C1)n2C 10.1016/j.bmcl.2022.128807
44397706 67191 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 67191 0 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
139392751 191402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1ccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)cc1F 10.1016/j.bmcl.2022.128807
CHEMBL5192571 191402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1ccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)cc1F 10.1016/j.bmcl.2022.128807
139392797 192493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.6 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(N)C(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5209017 192493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.6 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(N)C(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
139392554 191959 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3nc4c(F)cc(F)cc4[nH]3)cncc2-c2ccccc2F)C1 10.1016/j.bmcl.2022.128807
CHEMBL5200958 191959 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3nc4c(F)cc(F)cc4[nH]3)cncc2-c2ccccc2F)C1 10.1016/j.bmcl.2022.128807
139392637 192410 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2c1nc(-c1cncc(-c3cc(F)cc(C#N)c3)c1N1CC[C@H](N)C1)n2C 10.1016/j.bmcl.2022.128807
CHEMBL5208031 192410 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 426 3 1 6 4.2 Cc1cccc2c1nc(-c1cncc(-c3cc(F)cc(C#N)c3)c1N1CC[C@H](N)C1)n2C 10.1016/j.bmcl.2022.128807
139392554 191959 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3nc4c(F)cc(F)cc4[nH]3)cncc2-c2ccccc2F)C1 10.1016/j.bmcl.2022.128807
CHEMBL5200958 191959 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3nc4c(F)cc(F)cc4[nH]3)cncc2-c2ccccc2F)C1 10.1016/j.bmcl.2022.128807
139392797 192493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.6 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(N)C(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5209017 192493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 466 3 2 5 4.6 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC(N)C(C(F)(F)F)C2)c1 10.1016/j.bmcl.2022.128807
44397389 124044 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 124044 0 None -3 2 Human 7.4 pEC50 = 7.4 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
139392751 191402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1ccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)cc1F 10.1016/j.bmcl.2022.128807
CHEMBL5192571 191402 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 4.0 N#Cc1ccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2CC[C@H](N)C2)cc1F 10.1016/j.bmcl.2022.128807
150689079 192077 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 414 3 3 6 2.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](O)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5202785 192077 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 414 3 3 6 2.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](O)C2)c1 10.1016/j.bmcl.2022.128807
139392712 191749 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
CHEMBL5197482 191749 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
139392768 189921 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](F)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5169928 189921 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](F)C2)c1 10.1016/j.bmcl.2022.128807
168271712 190404 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 3 2 4 4.6 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5177695 190404 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 3 2 4 4.6 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392598 190726 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5182561 190726 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
139392768 189921 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](F)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5169928 189921 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 416 3 2 5 3.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](F)C2)c1 10.1016/j.bmcl.2022.128807
168271712 190404 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 3 2 4 4.6 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5177695 190404 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 423 3 2 4 4.6 Cc1cc(F)cc(-c2cncc(-c3nc4c(F)cc(F)cc4[nH]3)c2N2CC[C@H](N)C2)c1 10.1016/j.bmcl.2022.128807
139392598 190726 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5182561 190726 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 405 4 2 4 4.3 Cc1cc(F)cc(-c2cncc(-c3nc4cc(F)ccc4[nH]3)c2N2CC(CN)C2)c1 10.1016/j.bmcl.2022.128807
150689079 192077 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 414 3 3 6 2.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](O)C2)c1 10.1016/j.bmcl.2022.128807
CHEMBL5202785 192077 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 414 3 3 6 2.8 N#Cc1cccc(-c2cncc(-c3nc4c(F)cccc4[nH]3)c2N2C[C@@H](N)[C@H](O)C2)c1 10.1016/j.bmcl.2022.128807
139392712 191749 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
CHEMBL5197482 191749 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 428 4 2 6 3.5 CO[C@H]1CN(c2c(-c3cccc(C#N)c3)cncc2-c2nc3c(F)cccc3[nH]2)C[C@H]1N 10.1016/j.bmcl.2022.128807
44397835 67519 0 None -8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL189554 67519 0 None -8 2 Human 7.3 pEC50 = 7.3 Functional
Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptorInhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
139392691 191216 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3cccc(F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5189678 191216 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3cccc(F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
139392691 191216 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3cccc(F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
CHEMBL5189678 191216 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP levelAgonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL 409 4 2 4 4.1 NCC1CN(c2c(-c3cccc(F)c3)cncc2-c2nc3c(F)cc(F)cc3[nH]2)C1 10.1016/j.bmcl.2022.128807
66766052 166901 0 None 34 2 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4286244 166901 0 None 34 2 Human 10.0 pIC50 = 10 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
56847878 128407 0 None 3 2 Mouse 9.5 pIC50 = 9.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL3665800 128407 0 None 3 2 Mouse 9.5 pIC50 = 9.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
89573420 166875 0 None 109 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4285917 166875 0 None 109 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
89583208 166957 0 None 6 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4287248 166957 0 None 6 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
89573523 167084 0 None 42 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
CHEMBL4289661 167084 0 None 42 2 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
89573623 167288 0 None 3 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4293458 167288 0 None 3 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
145981627 166480 0 None 33 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4278328 166480 0 None 33 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
68093280 166406 0 None 13 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4277006 166406 0 None 13 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
49800498 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4282052 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288391 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
49800498 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4282052 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288391 167014 15 None -1 3 Mouse 9.1 pIC50 = 9.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145981179 166518 0 None 20 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
CHEMBL4278915 166518 0 None 20 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
89573623 167288 0 None -3 2 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4293458 167288 0 None -3 2 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
56848075 129219 0 None 15 2 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL3670722 129219 0 None 15 2 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
49800498 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4282052 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288391 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
49800498 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4282052 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288391 167014 15 None 1 3 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
16737814 85507 0 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227212 85507 0 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL504838 85507 0 None -1 5 Human 8.9 pIC50 = 8.9 Functional
Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP productionAgonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
66765321 166655 0 None 6 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4281446 166655 0 None 6 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
56847878 128407 0 None -3 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL3665800 128407 0 None -3 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
66765125 166540 0 None 40 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4279392 166540 0 None 40 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
89583208 166957 0 None -6 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4287248 166957 0 None -6 2 Mouse 8.8 pIC50 = 8.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
137654598 159009 0 None -2 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 490 9 1 6 5.2 CCOc1cc(CN2CC3(CC(c4ccc(CO)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4096502 159009 0 None -2 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 490 9 1 6 5.2 CCOc1cc(CN2CC3(CC(c4ccc(CO)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145991247 166806 0 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284442 166806 0 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
25122324 167100 0 None -6 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4289922 167100 0 None -6 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145990810 166823 0 None -4 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284867 166823 0 None -4 2 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
145982363 166601 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4280432 166601 0 None -12 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
118897726 161128 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4067347 161128 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4117200 161128 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118897690 157991 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4085201 157991 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
90423008 157012 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 539 9 1 7 5.2 CCOc1cc(CN2CC3(CC(N4CCC(CC)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4073378 157012 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 539 9 1 7 5.2 CCOc1cc(CN2CC3(CC(N4CCC(CC)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
86299160 158766 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 525 8 1 7 4.8 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4094029 158766 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 525 8 1 7 4.8 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
137653235 158675 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.7 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4C)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4092944 158675 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.7 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4C)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137649134 157404 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 503 9 1 6 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(N)=O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4078472 157404 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 503 9 1 6 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(N)=O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137649134 157404 0 None -1 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 503 9 1 6 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(N)=O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4078472 157404 0 None -1 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 503 9 1 6 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(N)=O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145980628 166673 0 None -64 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4281783 166673 0 None -64 2 Mouse 4.8 pIC50 = 4.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
86299160 158766 0 None -1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 525 8 1 7 4.8 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4094029 158766 0 None -1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 525 8 1 7 4.8 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
89573523 167084 0 None -42 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
CHEMBL4289661 167084 0 None -42 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
118963835 167012 0 None -61 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4288334 167012 0 None -61 2 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
118897590 158073 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 7 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4086265 158073 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 7 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
145980226 166716 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
CHEMBL4282854 166716 0 None 1 2 Mouse 7.8 pIC50 = 7.8 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
90423008 157012 0 None -1 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 539 9 1 7 5.2 CCOc1cc(CN2CC3(CC(N4CCC(CC)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4073378 157012 0 None -1 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 539 9 1 7 5.2 CCOc1cc(CN2CC3(CC(N4CCC(CC)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
118897803 161060 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4088598 161060 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4116623 161060 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118897591 159486 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CC(C)Oc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4101718 159486 0 None 1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CC(C)Oc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
89573118 167063 0 None 19 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4289325 167063 0 None 19 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
90423996 156784 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4070852 156784 0 None 1 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
46911015 15179 0 None 1 2 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL1210207 15179 0 None 1 2 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145982363 166601 0 None 12 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4280432 166601 0 None 12 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
132576641 157125 0 None 3 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 9 1 7 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cn4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4074952 157125 0 None 3 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 9 1 7 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cn4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118897726 161128 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4067347 161128 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4117200 161128 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 483 8 1 7 3.6 CCOc1cc(CN2CC3(CC(N4CC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137660796 159479 0 None -20 2 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.9 CCOc1cc(C(C)N2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4101641 159479 0 None -20 2 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.9 CCOc1cc(C(C)N2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
56848075 129219 0 None -15 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL3670722 129219 0 None -15 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
68093280 166406 0 None -13 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4277006 166406 0 None -13 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
137653235 158675 0 None 6 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.7 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4C)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4092944 158675 0 None 6 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.7 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4C)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118897690 157991 0 None -1 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4085201 157991 0 None -1 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137629608 161163 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4070285 161163 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4117472 161163 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
132576638 157941 0 None 14 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 456 10 1 6 4.5 CCOc1cc(CN2CC3(CC(CCC(=O)O)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4084575 157941 0 None 14 2 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 456 10 1 6 4.5 CCOc1cc(CN2CC3(CC(CCC(=O)O)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118898153 155921 0 None -3 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 509 7 1 6 4.9 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(CC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4060897 155921 0 None -3 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 509 7 1 6 4.9 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(CC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
89583150 166828 0 None -120 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4284956 166828 0 None -120 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
145989896 167016 0 None -2 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288417 167016 0 None -2 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145981627 166480 0 None -33 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4278328 166480 0 None -33 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
78210294 157337 0 None -4 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 541 6 1 6 5.5 COc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
CHEMBL4077605 157337 0 None -4 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 541 6 1 6 5.5 COc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
118897987 159372 0 None -3 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 555 7 1 6 5.9 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
CHEMBL4100523 159372 0 None -3 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 555 7 1 6 5.9 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
145979224 166605 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 567 9 0 6 5.8 CCOc1cc(CN2CCC3(CC2)CCN(S(=O)(=O)c2cccnc2)CC3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4280531 166605 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 567 9 0 6 5.8 CCOc1cc(CN2CCC3(CC2)CCN(S(=O)(=O)c2cccnc2)CC3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
137645727 157602 0 None 2 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4cccc(C(=O)O)c4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4080924 157602 0 None 2 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4cccc(C(=O)O)c4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145980628 166673 0 None 64 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4281783 166673 0 None 64 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
145980226 166716 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
CHEMBL4282854 166716 0 None -1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
145982284 166472 0 None -1 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4278161 166472 0 None -1 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
132576640 156082 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 460 8 0 5 5.7 CCOc1cc(CN2CC3(CC(c4ccccc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4062911 156082 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 460 8 0 5 5.7 CCOc1cc(CN2CC3(CC(c4ccccc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
89573250 167109 0 None -9 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4290073 167109 0 None -9 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
118897585 157084 0 None -5 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 6 1 5 5.4 CCc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4074342 157084 0 None -5 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 6 1 5 5.4 CCc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
145990504 167011 0 None -10 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288259 167011 0 None -10 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
46911015 15179 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL1210207 15179 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
89573308 166459 0 None 11 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4277991 166459 0 None 11 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
89583150 166828 0 None 120 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4284956 166828 0 None 120 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
118963835 167012 0 None 61 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4288334 167012 0 None 61 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
118897882 155928 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 507 6 1 6 4.9 COc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4060964 155928 0 None 1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 507 6 1 6 4.9 COc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
118897591 159486 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CC(C)Oc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4101718 159486 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CC(C)Oc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
145990810 166823 0 None 4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284867 166823 0 None 4 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
89573250 167109 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4290073 167109 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
118897690 156900 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4072189 156900 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137653284 158753 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 538 9 1 6 6.0 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4Cl)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4093913 158753 0 None 1 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 538 9 1 6 6.0 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4Cl)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
132576638 157941 0 None -14 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 456 10 1 6 4.5 CCOc1cc(CN2CC3(CC(CCC(=O)O)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4084575 157941 0 None -14 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 456 10 1 6 4.5 CCOc1cc(CN2CC3(CC(CCC(=O)O)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
132576639 159096 0 None -3 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4097462 159096 0 None -3 2 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145991247 166806 0 None -2 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284442 166806 0 None -2 2 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
145994083 167394 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4295189 167394 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
145990504 167011 0 None 10 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288259 167011 0 None 10 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
118898105 155822 0 None -5 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1C 10.1016/j.bmc.2017.06.003
CHEMBL4059929 155822 0 None -5 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1C 10.1016/j.bmc.2017.06.003
118897690 156900 0 None -1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4072189 156900 0 None -1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 510 9 1 6 5.5 CCOc1cc(CN2CC3(CC([C@H]4CC[C@H](C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
66765125 166540 0 None -40 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4279392 166540 0 None -40 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
68093096 167253 0 None -48 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
CHEMBL4292738 167253 0 None -48 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
90423996 156784 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4070852 156784 0 None -1 2 Mouse 8.4 pIC50 = 8.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
68254010 166414 0 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4277106 166414 0 None 2 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
118897967 158662 0 None 18 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)c(C2CC2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4092798 158662 0 None 18 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)c(C2CC2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
89573308 166459 0 None -11 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4277991 166459 0 None -11 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
89573118 167063 0 None -19 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4289325 167063 0 None -19 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
137654598 159009 0 None 2 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 490 9 1 6 5.2 CCOc1cc(CN2CC3(CC(c4ccc(CO)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4096502 159009 0 None 2 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 490 9 1 6 5.2 CCOc1cc(CN2CC3(CC(c4ccc(CO)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137653284 158753 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 538 9 1 6 6.0 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4Cl)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4093913 158753 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 538 9 1 6 6.0 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4Cl)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
89573310 166443 0 None -6 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
CHEMBL4277613 166443 0 None -6 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
118897803 161060 0 None 3 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4088598 161060 0 None 3 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4116623 161060 0 None 3 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 497 8 1 7 4.0 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)C4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145981179 166518 0 None -20 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
CHEMBL4278915 166518 0 None -20 2 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
118897585 157084 0 None 5 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 6 1 5 5.4 CCc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4074342 157084 0 None 5 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 6 1 5 5.4 CCc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
89573310 166443 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
CHEMBL4277613 166443 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
118897700 159333 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4100114 159333 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
137645727 157602 0 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4cccc(C(=O)O)c4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4080924 157602 0 None -2 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4cccc(C(=O)O)c4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
89573420 166875 0 None -109 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4285917 166875 0 None -109 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
90423921 156140 20 None -6 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
90423921 156140 20 None -6 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4063587 156140 20 None -6 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4063587 156140 20 None -6 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118898094 157857 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 529 8 1 7 4.5 CCOc1cc(CN2CC3(CC(N4CCC(F)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4083763 157857 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 529 8 1 7 4.5 CCOc1cc(CN2CC3(CC(N4CCC(F)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
66766052 166901 0 None -34 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4286244 166901 0 None -34 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
118898153 155921 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 509 7 1 6 4.9 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(CC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4060897 155921 0 None 3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 509 7 1 6 4.9 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(CC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
118897691 156242 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 495 6 1 6 4.7 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4064789 156242 0 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 495 6 1 6 4.7 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
68254010 166414 0 None -2 3 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4277106 166414 0 None -2 3 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
78210294 157337 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 541 6 1 6 5.5 COc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
CHEMBL4077605 157337 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 541 6 1 6 5.5 COc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
118898105 155822 0 None 5 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1C 10.1016/j.bmc.2017.06.003
CHEMBL4059929 155822 0 None 5 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 535 7 1 6 5.6 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1C 10.1016/j.bmc.2017.06.003
132576641 157125 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 9 1 7 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cn4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4074952 157125 0 None -3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 505 9 1 7 4.8 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cn4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
118897590 158073 0 None -3 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 7 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4086265 158073 0 None -3 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 7 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(OC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
145994083 167394 0 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4295189 167394 0 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
118963840 166926 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 518 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(OC(F)(F)F)c(Cl)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4286833 166926 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 518 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(OC(F)(F)F)c(Cl)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
145989394 167231 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4292255 167231 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145993203 167040 0 None -6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288848 167040 0 None -6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145993203 167040 0 None 6 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288848 167040 0 None 6 2 Mouse 8.2 pIC50 = 8.2 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
118897987 159372 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 555 7 1 6 5.9 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
CHEMBL4100523 159372 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 555 7 1 6 5.9 CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1Cl 10.1016/j.bmc.2017.06.003
118897691 156242 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 495 6 1 6 4.7 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4064789 156242 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 495 6 1 6 4.7 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
25122324 167100 0 None 6 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4289922 167100 0 None 6 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
118897882 155928 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 507 6 1 6 4.9 COc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
CHEMBL4060964 155928 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 507 6 1 6 4.9 COc1cc(-c2ccc(F)cc2)c(C2CC2)cc1CN1CC2(CC(N3CCC(C)(C(=O)O)CC3)=NO2)C1 10.1016/j.bmc.2017.06.003
118897700 159333 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4100114 159333 0 None -1 2 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
16062555 5956 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAntagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
CHEMBL1079874 5956 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAntagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
145981765 166661 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4281620 166661 0 None -3 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
137629608 161163 0 None 2 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4070285 161163 0 None 2 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4117472 161163 0 None 2 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 10 1 6 5.3 CCOc1cc(CN2CC3(CC(c4ccc(CC(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
11848624 89146 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human SST5R expressed in CHO cells assessed as reversal of somatostatin-14 induced cAMP responseAntagonist activity at human SST5R expressed in CHO cells assessed as reversal of somatostatin-14 induced cAMP response
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL236587 89146 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human SST5R expressed in CHO cells assessed as reversal of somatostatin-14 induced cAMP responseAntagonist activity at human SST5R expressed in CHO cells assessed as reversal of somatostatin-14 induced cAMP response
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
145989603 167208 0 None 12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 6 1 4 7.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(-c5ccc(Cl)cc5Cl)c(OC(F)(F)F)c4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4291751 167208 0 None 12 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 6 1 4 7.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(-c5ccc(Cl)cc5Cl)c(OC(F)(F)F)c4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
118898094 157857 0 None -1 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 529 8 1 7 4.5 CCOc1cc(CN2CC3(CC(N4CCC(F)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4083763 157857 0 None -1 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 529 8 1 7 4.5 CCOc1cc(CN2CC3(CC(N4CCC(F)(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
68093096 167253 0 None 48 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
CHEMBL4292738 167253 0 None 48 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
145982284 166472 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4278161 166472 0 None 1 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
118897967 158662 0 None -18 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)c(C2CC2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4092798 158662 0 None -18 2 Mouse 7.1 pIC50 = 7.1 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 521 7 1 6 5.2 CCOc1cc(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)c(C2CC2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
132576639 159096 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4097462 159096 0 None 3 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 504 9 1 6 5.4 CCOc1cc(CN2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
66765321 166655 0 None -6 2 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4281446 166655 0 None -6 2 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
90423921 156140 20 None 6 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
90423921 156140 20 None 6 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4063587 156140 20 None 6 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.003
CHEMBL4063587 156140 20 None 6 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.4 CCOc1cc(CN2CC3(CC(N4CCC(C(=O)O)CC4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
137660796 159479 0 None 20 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.9 CCOc1cc(C(C)N2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4101641 159479 0 None 20 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 518 9 1 6 5.9 CCOc1cc(C(C)N2CC3(CC(c4ccc(C(=O)O)cc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
16062553 6065 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAntagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL1080586 6065 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assayAntagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay
ChEMBL 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
145989896 167016 0 None 2 3 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288417 167016 0 None 2 3 Mouse 7.0 pIC50 = 7.0 Functional
Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assayAntagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
132576640 156082 0 None 2 2 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 460 8 0 5 5.7 CCOc1cc(CN2CC3(CC(c4ccccc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
CHEMBL4062911 156082 0 None 2 2 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assayAntagonist activity at mouse SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay
ChEMBL 460 8 0 5 5.7 CCOc1cc(CN2CC3(CC(c4ccccc4)=NO3)C2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmc.2017.06.007
145989603 167208 0 None -12 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 6 1 4 7.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(-c5ccc(Cl)cc5Cl)c(OC(F)(F)F)c4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4291751 167208 0 None -12 2 Mouse 6.0 pIC50 = 6 Functional
Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assayAntagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay
ChEMBL 592 6 1 4 7.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(-c5ccc(Cl)cc5Cl)c(OC(F)(F)F)c4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
13224 4135 0 None - 1 Human 9.0 pEC50 < 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 4 2 5 3.1 N[C@@H]1CN(CC1)C2=C(C=NC(=C2C3=CC(=CC(=C3)F)F)C#N)C(=O)N[C@H](C(F)(F)F)C None
156065422 4135 0 None - 1 Human 9.0 pEC50 < 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 4 2 5 3.1 N[C@@H]1CN(CC1)C2=C(C=NC(=C2C3=CC(=CC(=C3)F)F)C#N)C(=O)N[C@H](C(F)(F)F)C None
2055 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
383414 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
90488715 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
CHEMBL1680 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
CHEMBL262746 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
DB00104 2907 48 None -23 4 Human 8.1 pIC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
145705877 217736 0 None -1 5 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 1047 17 9 11 3.4 NCCCC[C@@H]1NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)C(NC(=O)[C@@H]2C[C@H](CN2C(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=C(OCC3=CC=CC=C3)C=C2)NC1=O)OC(=O)NCCN)C1=CC=CC=C1 None
2026 654 0 None -3 5 Human 6.9 pIC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2027 655 0 None -12 5 Human 7.1 pIC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2053 2848 0 None -3 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
2041 650 0 None -50 3 Human 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9045884
2012 1375 0 None -5 4 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2042 700 0 None -5 3 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15709181
2013 2180 0 None 1 6 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2018 3007 28 None 6 5 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
9941444 3007 28 None 6 5 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
CHEMBL3349607 3007 28 None 6 5 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717
DB06663 3007 28 None 6 5 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15477717


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
16129706 209031 40 None -9 5 Human 10.2 pEC50 = 10.2 Binding
Effective concentration on human somatostatin receptor 5Effective concentration on human somatostatin receptor 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00051-8
CHEMBL1823872 209031 40 None -9 5 Human 10.2 pEC50 = 10.2 Binding
Effective concentration on human somatostatin receptor 5Effective concentration on human somatostatin receptor 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00051-8
140762500 181733 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at SST5 (unknown origin)Agonist activity at SST5 (unknown origin)
ChEMBL 529 5 1 5 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4777122 181733 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at SST5 (unknown origin)Agonist activity at SST5 (unknown origin)
ChEMBL 529 5 1 5 6.1 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(F)cc(C#N)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762573 182377 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at SST5 (unknown origin)Agonist activity at SST5 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4785112 182377 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at SST5 (unknown origin)Agonist activity at SST5 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)ccc4F)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
56832524 128426 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 578 10 1 7 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(OC)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665819 128426 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 578 10 1 7 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(OC)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848227 128438 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(F)cc2F)cc1C nan
CHEMBL3665831 128438 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(F)cc2F)cc1C nan
86766058 128444 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 580 6 1 5 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(OC(F)(F)F)ccc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665837 128444 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 580 6 1 5 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(OC(F)(F)F)ccc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
66764762 128460 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 476 6 1 6 4.5 COc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cccc12 nan
CHEMBL3665853 128460 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 476 6 1 6 4.5 COc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cccc12 nan
56848224 128439 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 7 1 5 6.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665832 128439 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 7 1 5 6.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
89583208 166957 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4287248 166957 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 552 6 1 4 6.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(-c5ccc(F)cc5F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
89573623 167288 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4293458 167288 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)c(F)c3F)cccc21 10.1021/acsmedchemlett.8b00306
16129706 209031 40 None -9 5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
CHEMBL1823872 209031 40 None -9 5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
56848074 129245 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 553 8 1 6 6.5 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(OCc3ccccc3)cccc21 nan
CHEMBL3670748 129245 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 553 8 1 6 6.5 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(OCc3ccccc3)cccc21 nan
86766059 128445 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 584 8 1 6 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(OC)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665838 128445 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 584 8 1 6 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(OC)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
68092957 128461 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 7 1 6 5.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)ccc(Cl)c12 nan
CHEMBL3665854 128461 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 7 1 6 5.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)ccc(Cl)c12 nan
66765461 128446 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc5c(cc4-c4cc(F)c(F)cc4F)CCC5)CC3)OC2=O)cc1 nan
CHEMBL3665839 128446 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc5c(cc4-c4cc(F)c(F)cc4F)CCC5)CC3)OC2=O)cc1 nan
56848029 129241 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 8 1 7 5.9 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(OCc3ccccc3)ccc21 nan
CHEMBL3670744 129241 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 8 1 7 5.9 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(OCc3ccccc3)ccc21 nan
86766057 128443 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CC(C)Oc1ccc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665836 128443 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CC(C)Oc1ccc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
44569804 175262 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 10 2 4 6.9 NCc1cccc(C[C@@H]2O[C@@H](CC(=O)NCc3ccccc3F)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)c1 10.1021/jm801205x
CHEMBL457245 175262 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 10 2 4 6.9 NCc1cccc(C[C@@H]2O[C@@H](CC(=O)NCc3ccccc3F)C(=O)N(Cc3ccc(-c4ccccc4)cc3)c3ccccc32)c1 10.1021/jm801205x
66766052 166901 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4286244 166901 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 487 6 1 5 5.8 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
56848028 129222 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 464 4 1 5 4.7 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCCC2(C)C nan
CHEMBL3670725 129222 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 464 4 1 5 4.7 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCCC2(C)C nan
56847770 128418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 9 1 8 5.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665811 128418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 9 1 8 5.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56847843 129251 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(-c3ccc(F)c(F)c3F)ccc21 nan
CHEMBL3670754 129251 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 577 6 1 5 7.0 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(-c3ccc(F)c(F)c3F)ccc21 nan
86766056 128425 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 9 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2Cl)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665818 128425 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 9 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2Cl)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
66765305 128454 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 504 7 1 7 4.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-n2cc(C)cn2)cc1C nan
CHEMBL3665847 128454 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 504 7 1 7 4.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-n2cc(C)cn2)cc1C nan
86766060 128448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 7 1 5 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2F)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665841 128448 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 7 1 5 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2F)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
2016 2260 4 None 7 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to sst5 receptorBinding affinity to sst5 receptor
ChEMBL 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 10.1021/jm070886i
5311375 2260 4 None 7 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to sst5 receptorBinding affinity to sst5 receptor
ChEMBL 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 10.1021/jm070886i
CHEMBL252764 2260 4 None 7 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to sst5 receptorBinding affinity to sst5 receptor
ChEMBL 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 10.1021/jm070886i
9937014 190689 26 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 536 11 4 5 5.2 C[C@H](N)COC(=O)[C@@H](CCCCN)NC(=O)Cc1c(-c2ccc3ccccc3c2)[nH]c2c1ccc1ccccc12 10.1021/jm801205x
CHEMBL518199 190689 26 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 536 11 4 5 5.2 C[C@H](N)COC(=O)[C@@H](CCCCN)NC(=O)Cc1c(-c2ccc3ccccc3c2)[nH]c2c1ccc1ccccc12 10.1021/jm801205x
89573523 167084 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
CHEMBL4289661 167084 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 542 6 1 6 6.1 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)ccnc21 10.1021/acsmedchemlett.8b00306
56848175 128441 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 519 7 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)nc2)cc1C nan
CHEMBL3665834 128441 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 519 7 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)nc2)cc1C nan
56848331 128434 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665827 128434 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
86766035 128370 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 5 1 6 5.8 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(Cl)c2)n1 nan
CHEMBL3665763 128370 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 5 1 6 5.8 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(Cl)c2)n1 nan
86766066 128462 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 6 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2cnc(C(F)(F)F)cc12 nan
CHEMBL3665855 128462 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 6 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2cnc(C(F)(F)F)cc12 nan
56848072 128427 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 9 1 6 6.1 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2F)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665820 128427 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 9 1 6 6.1 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2F)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848278 128436 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 564 5 1 4 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665829 128436 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 564 5 1 4 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
86766061 128449 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 588 7 1 5 6.8 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2Cl)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665842 128449 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 588 7 1 5 6.8 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2Cl)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
56848280 128435 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 7 1 5 6.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2C)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
CHEMBL3665828 128435 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 7 1 5 6.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2C)C(=O)O3)c(-c2ccc(F)c(F)c2F)cc1C nan
56848120 128430 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 522 7 1 5 5.7 CCOc1ccc(-c2ccc(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665823 128430 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 522 7 1 5 5.7 CCOc1ccc(-c2ccc(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
56848122 128431 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 522 7 1 5 5.7 CCOc1ccc(-c2ccc(F)c(F)c2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665824 128431 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 522 7 1 5 5.7 CCOc1ccc(-c2ccc(F)c(F)c2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
56848174 128433 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CC(C)Oc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665826 128433 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CC(C)Oc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
56847844 129252 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 5 1 5 5.7 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(Br)ccc21 nan
CHEMBL3670755 129252 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 5 1 5 5.7 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(Br)ccc21 nan
56848172 128432 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 5 5.9 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665825 128432 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 5 5.9 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
25188780 12431 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1185941 12431 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL442605 12431 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 10 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCCc2ccccc2)C1=O 10.1021/jm801205x
86766036 128371 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 5 1 8 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
CHEMBL3665764 128371 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 5 1 8 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
145993203 167040 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288848 167040 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
25189325 12446 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186056 12446 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL447455 12446 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 3.6 NCCCC[C@@H](C(=O)NCCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
66765125 166540 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4279392 166540 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 466 4 1 5 5.2 CC1(C)CCSc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
68092930 128447 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 569 7 1 6 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(C(F)(F)F)nc2)cc1C nan
CHEMBL3665840 128447 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 569 7 1 6 6.2 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(C(F)(F)F)nc2)cc1C nan
CHEMBL264133 210607 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
68092954 128459 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 7 1 6 5.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cc(Cl)cc12 nan
CHEMBL3665852 128459 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 7 1 6 5.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cc(Cl)cc12 nan
145982284 166472 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4278161 166472 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
89573420 166875 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4285917 166875 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 508 5 1 4 5.9 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
66764855 128456 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 490 7 1 6 4.9 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cccc12 nan
CHEMBL3665849 128456 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 490 7 1 6 4.9 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OC)cccc12 nan
66765719 129256 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 535 6 1 7 5.8 COc1ccc(-c2nc(C(C)(C)C)sc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3670759 129256 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 535 6 1 7 5.8 COc1ccc(-c2nc(C(C)(C)C)sc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
66765170 128367 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 608 6 1 6 6.7 CC1(C)C2CCC(C2)C1n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665760 128367 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 608 6 1 6 6.7 CC1(C)C2CCC(C2)C1n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
56847878 128407 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665800 128407 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
13690207 115382 0 None -29 5 Human 9.1 pIC50 = 9.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm960850i
CHEMBL3350037 115382 0 None -29 5 Human 9.1 pIC50 = 9.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm960850i
CHEMBL415860 213206 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL None None None C[C@@H](O)[C@@H](NC(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm960851a
68092935 128428 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 5 5.9 CCOc1ccc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665821 128428 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 5 5.9 CCOc1ccc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
145982284 166472 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4278161 166472 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 580 10 0 5 6.6 CCOc1cc(CN2CCC(C3CCN(S(=O)(=O)c4ccccc4)CC3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
56847878 128407 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL3665800 128407 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
145981627 166480 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4278328 166480 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 485 6 1 4 5.8 CC(C)n1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)c2c(C3CC3)cccc21 10.1021/acsmedchemlett.8b00306
66765212 129243 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 6 1 6 4.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(C(C)C)c2c1 nan
CHEMBL3670746 129243 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 6 1 6 4.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(C(C)C)c2c1 nan
25189052 12672 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1187345 12672 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL499681 12672 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 676 10 5 6 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC(n3c(=O)[nH]c4ccccc43)CC2)C1=O 10.1021/jm801205x
16129706 209031 40 None -9 5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL1823872 209031 40 None -9 5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2018.11.030
56847735 128417 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cn2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665810 128417 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cn2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
86766027 128346 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 6 1 6 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
CHEMBL3665739 128346 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 6 1 6 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
68093086 128457 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 504 8 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OCC)cccc12 nan
CHEMBL3665850 128457 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 504 8 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c(OCC)cccc12 nan
56848176 128440 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)c1 nan
CHEMBL3665833 128440 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 7 1 5 6.2 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)c1 nan
44290734 155835 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1123 15 12 11 1.3 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCNC(=O)CCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL406000 155835 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1123 15 12 11 1.3 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCCNC(=O)CCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
46911015 15179 0 None - 1 Mouse 9.0 pIC50 = 9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL1210207 15179 0 None - 1 Mouse 9.0 pIC50 = 9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL440636 213868 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
56848025 129247 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 7 1 6 4.8 CCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
CHEMBL3670750 129247 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 7 1 6 4.8 CCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
86766062 128451 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 544 5 1 4 6.4 Cc1cc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
CHEMBL3665844 128451 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 544 5 1 4 6.4 Cc1cc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
66765023 128424 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 9 1 6 6.1 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(F)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665817 128424 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 566 9 1 6 6.1 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(F)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
68287850 128422 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2C)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665815 128422 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2C)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL2372713 210284 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
49800498 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4282052 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288391 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
16737814 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL227212 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504838 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
16737814 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227212 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL504838 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
89583150 166828 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4284956 166828 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 578 5 1 4 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
49800498 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4282052 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288391 167014 15 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
16737814 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
CHEMBL227212 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
CHEMBL504838 85507 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL 551 11 4 4 3.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1016/j.ejmech.2018.11.030
56847841 128415 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 9 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(Cl)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665808 128415 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 9 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(Cl)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848027 129224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 484 4 1 5 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
CHEMBL3670727 129224 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 484 4 1 5 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
56848226 128375 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3665768 128375 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
44290766 157956 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1101 15 11 12 2.0 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL408471 157956 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1101 15 11 12 2.0 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
46911015 15179 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL1210207 15179 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
86766063 128452 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 509 5 1 5 5.5 Cc1cc(-c2ccc(F)nc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
CHEMBL3665845 128452 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 509 5 1 5 5.5 Cc1cc(-c2ccc(F)nc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
56848021 128361 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665754 128361 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
56847876 129255 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 561 7 1 7 6.6 COc1ccc(-c2nc(C3CCCCC3)sc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3670758 129255 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 561 7 1 7 6.6 COc1ccc(-c2nc(C3CCCCC3)sc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
25187685 12470 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1186206 12470 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL454202 12470 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 648 11 4 5 3.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C2CCN(C(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
86766055 128410 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)nc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665803 128410 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)nc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56847840 128414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665807 128414 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56847875 129253 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 6 1 6 4.9 COc1ccc2c(c1)c(CN1CCC3(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O3)cn2C(C)C nan
CHEMBL3670756 129253 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 477 6 1 6 4.9 COc1ccc2c(c1)c(CN1CCC3(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O3)cn2C(C)C nan
68092995 128408 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 521 8 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cncc(O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665801 128408 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 521 8 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cncc(O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848276 128437 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4-c4ccc(F)nc4)CC3)OC2=O)cc1 nan
CHEMBL3665830 128437 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4-c4ccc(F)nc4)CC3)OC2=O)cc1 nan
56848075 129219 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL3670722 129219 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
68092968 128453 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 493 7 1 7 4.9 CCOc1ccc(-c2nccs2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665846 128453 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 493 7 1 7 4.9 CCOc1ccc(-c2nccs2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
56848070 128349 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4cccc(C(F)(F)F)c4)CC3)OC2=O)cc1 nan
CHEMBL3665742 128349 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4cccc(C(F)(F)F)c4)CC3)OC2=O)cc1 nan
56848075 129219 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
CHEMBL3670722 129219 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.4 CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
56848071 128350 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 6 1 6 6.3 Cc1ccc(-n2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c(-c3ccc(F)c(F)c3F)n2)c(C)c1 nan
CHEMBL3665743 128350 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 6 1 6 6.3 Cc1ccc(-n2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c(-c3ccc(F)c(F)c3F)n2)c(C)c1 nan
86766039 128379 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 5 1 6 5.7 Cc1cc(C(=O)O)ccc1N1CC2(CCN(Cc3cn(C(C)(C)C)nc3-c3ccc(F)c(F)c3F)CC2)OC1=O nan
CHEMBL3665772 128379 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 5 1 6 5.7 Cc1cc(C(=O)O)ccc1N1CC2(CCN(Cc3cn(C(C)(C)C)nc3-c3ccc(F)c(F)c3F)CC2)OC1=O nan
145989394 167231 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4292255 167231 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
56847774 129262 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 559 5 1 6 6.2 CC(C)(C)c1nc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)s1 nan
CHEMBL3670765 129262 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 559 5 1 6 6.2 CC(C)(C)c1nc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)s1 nan
25187400 12694 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187495 12694 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504930 12694 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 537 10 4 4 3.7 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccccc2)C1=O 10.1021/jm801205x
66765321 166655 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4281446 166655 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C(F)(F)F)c(C5CC5)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
56848330 128357 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccccc1-c1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3665750 128357 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccccc1-c1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
66765178 129225 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.6 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCCC2C nan
CHEMBL3670728 129225 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.6 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCCC2C nan
86766051 128396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cnn(-c5ccccc5)c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3665789 128396 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cnn(-c5ccccc5)c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
86766037 128372 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 5 1 6 5.3 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)cc2F)n1 nan
CHEMBL3665765 128372 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 524 5 1 6 5.3 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)cc2F)n1 nan
16129706 209031 40 None -9 5 Human 8.0 pIC50 = 8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm049519m
CHEMBL1823872 209031 40 None -9 5 Human 8.0 pIC50 = 8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm049519m
CHEMBL407676 212677 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
56848076 128397 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cnn(C5CCCCC5)c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3665790 128397 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cnn(C5CCCCC5)c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
86766041 128383 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 5.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(CC(F)(F)F)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665776 128383 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 568 6 1 6 5.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(CC(F)(F)F)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL2372603 210274 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=2)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=2)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL421493 213278 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@H](C(=O)O)NC1=O 10.1021/jm960850i
CHEMBL421493 213278 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@H](C(=O)O)NC1=O 10.1021/jm960851a
52948577 16989 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 516 11 3 7 3.7 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCN)C(OCc2cccc3ccccc23)[C@@H]1O 10.1021/jm1002777
CHEMBL1253955 16989 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 516 11 3 7 3.7 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCN)C(OCc2cccc3ccccc23)[C@@H]1O 10.1021/jm1002777
CHEMBL3349611 211438 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm970730q
CHEMBL3349618 211444 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3349665 211449 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349666 211450 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349675 211458 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970730q
CHEMBL3350899 211521 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
122179457 121454 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to somatostatin receptor type 5 (unknown origin)Binding affinity to somatostatin receptor type 5 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL3582317 121454 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to somatostatin receptor type 5 (unknown origin)Binding affinity to somatostatin receptor type 5 (unknown origin)
ChEMBL 495 4 3 8 3.7 Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 10.1016/j.bmcl.2016.02.022
CHEMBL263306 210566 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL3349664 211448 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm970730q
66765500 129265 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 420 4 1 6 3.3 Cc1nc2ccccn2c1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3670768 129265 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 420 4 1 6 3.3 Cc1nc2ccccn2c1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
11457521 115459 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350892 115459 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1136 15 14 14 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3349612 211439 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL505496 214193 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1SS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL455435 214003 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H]1CCSSCC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm701445q
CHEMBL412029 212972 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(N)=O)C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm060363v
CHEMBL503596 214170 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
86766067 128463 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 6 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2ccc(C(F)(F)F)nc12 nan
CHEMBL3665856 128463 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 529 6 1 6 5.3 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2ccc(C(F)(F)F)nc12 nan
56847924 129248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 491 8 1 6 5.1 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
CHEMBL3670751 129248 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 491 8 1 6 5.1 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
11343811 115461 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350903 115461 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
90663872 106738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL3144282 106738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL3144284 106738 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1646 26 24 30 -7.4 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL509192 215334 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(N)=O)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
86766048 128393 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4nn(Cc5ccc(Cl)cc5)cc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3665786 128393 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4nn(Cc5ccc(Cl)cc5)cc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL386768 212389 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
66765525 129228 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 424 4 2 5 3.4 O=C(O)c1ccc(N2CC3(CCN(Cc4n[nH]c5ccc(F)cc45)CC3)OC2=O)cc1 nan
CHEMBL3670731 129228 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 424 4 2 5 3.4 O=C(O)c1ccc(N2CC3(CCN(Cc4n[nH]c5ccc(F)cc45)CC3)OC2=O)cc1 nan
CHEMBL3349597 211426 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm970730q
66765618 129254 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 561 6 1 6 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
CHEMBL3670757 129254 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 561 6 1 6 6.5 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
CHEMBL3122130 211108 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
44569760 188651 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 1133 21 12 12 2.6 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N1 10.1021/jm801205x
CHEMBL503472 188651 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 1133 21 12 12 2.6 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)N1 10.1021/jm801205x
49865343 15909 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223228 15909 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
68092994 128369 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 592 7 1 7 6.1 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccc(OC(F)(F)F)cc4)CC3)OC2=O)cc1 nan
CHEMBL3665762 128369 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 592 7 1 7 6.1 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccc(OC(F)(F)F)cc4)CC3)OC2=O)cc1 nan
68093004 129234 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 473 6 1 7 4.0 CCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C#N)cc21 nan
CHEMBL3670737 129234 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 473 6 1 7 4.0 CCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C#N)cc21 nan
68287726 129235 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 491 6 2 7 3.4 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C(N)=O)cc21 nan
CHEMBL3670738 129235 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 491 6 2 7 3.4 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C(N)=O)cc21 nan
86766071 129242 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 534 7 1 8 4.4 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(CC(=O)C(C)(C)C)c2c1 nan
CHEMBL3670745 129242 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 534 7 1 8 4.4 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(CC(=O)C(C)(C)C)c2c1 nan
86766074 129263 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 5 1 6 5.1 O=C(O)c1ccc(N2CC3(CCN(Cc4nc5ccccn5c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3670766 129263 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 5 1 6 5.1 O=C(O)c1ccc(N2CC3(CCN(Cc4nc5ccccn5c4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
66765340 129236 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 473 5 1 7 4.2 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C#N)cc21 nan
CHEMBL3670739 129236 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 473 5 1 7 4.2 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(C#N)cc21 nan
CHEMBL2079626 209197 2 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL3349673 211456 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2011462 209110 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/ml200032v
CHEMBL415359 213185 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371060 210007 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
145979224 166605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 567 9 0 6 5.8 CCOc1cc(CN2CCC3(CC2)CCN(S(=O)(=O)c2cccnc2)CC3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4280531 166605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 567 9 0 6 5.8 CCOc1cc(CN2CCC3(CC2)CCN(S(=O)(=O)c2cccnc2)CC3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145981765 166661 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4281620 166661 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
25188496 12535 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186630 12535 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL473160 12535 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 476 9 3 5 2.5 COC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL216992 209348 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
68093278 128429 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 541 7 1 6 5.3 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
CHEMBL3665822 128429 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 541 7 1 6 5.3 CCOc1ccc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
56847807 129264 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 482 5 1 6 4.7 O=C(O)c1ccc(N2CC3(CCN(Cc4c(-c5ccccc5)nc5ccccn45)CC3)OC2=O)cc1 nan
CHEMBL3670767 129264 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 482 5 1 6 4.7 O=C(O)c1ccc(N2CC3(CCN(Cc4c(-c5ccccc5)nc5ccccn45)CC3)OC2=O)cc1 nan
CHEMBL3349679 211462 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm970730q
66765097 129237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 494 5 1 6 4.9 CC(C)(C)Cn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL3670740 129237 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 494 5 1 6 4.9 CC(C)(C)Cn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL2011466 209114 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)N(C)C1=O 10.1021/ml200032v
CHEMBL406816 212623 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1824055 209039 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL1824055 209039 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL386909 212400 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
68092978 129220 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 4 1 5 5.2 CC1(C)CC(C)(C)c2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
CHEMBL3670723 129220 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 4 1 5 5.2 CC1(C)CC(C)(C)c2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
86766044 128386 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 9 1 6 6.0 CCCCn1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
CHEMBL3665779 128386 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 9 1 6 6.0 CCCCn1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
56847977 128398 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 514 5 1 6 4.6 CC(C)(C)n1cc(CN2CC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665791 128398 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 514 5 1 6 4.6 CC(C)(C)n1cc(CN2CC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
44345981 14694 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 587 14 4 6 2.9 NCCCC[C@@H](NC(=O)CC1SC(c2ccccc2)N([C@@H](Cc2ccc(-c3ccccc3)cc2)C(N)=O)C1=O)C(N)=O 10.1016/s0960-894x(98)00647-7
CHEMBL120607 14694 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 587 14 4 6 2.9 NCCCC[C@@H](NC(=O)CC1SC(c2ccccc2)N([C@@H](Cc2ccc(-c3ccccc3)cc2)C(N)=O)C1=O)C(N)=O 10.1016/s0960-894x(98)00647-7
CHEMBL2111200 209215 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
86766068 129232 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 466 5 1 6 4.4 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL3670735 129232 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 466 5 1 6 4.4 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL3349668 211452 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL502219 214151 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL414446 213131 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2079563 209196 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
68093273 129260 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 463 5 1 6 4.8 Cc1nc(-c2ccccc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)s1 nan
CHEMBL3670763 129260 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 463 5 1 6 4.8 Cc1nc(-c2ccccc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)s1 nan
122179477 121474 5 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SSTR5 receptor (unknown origin)Inhibition of SSTR5 receptor (unknown origin)
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 121474 5 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of SSTR5 receptor (unknown origin)Inhibition of SSTR5 receptor (unknown origin)
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
66765604 129230 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 7 1 7 4.1 CCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
CHEMBL3670733 129230 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 7 1 7 4.1 CCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2ccc(OC)cc21 nan
CHEMBL376703 212254 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm060363v
68254010 166414 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4277106 166414 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL1824055 209039 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL3122129 211107 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)COCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
25187681 12469 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL1186190 12469 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
CHEMBL453412 12469 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 613 11 4 4 5.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(-c3ccccc3)cc2)C1=O 10.1021/jm801205x
49865344 15910 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1031 17 13 12 0.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL1223229 15910 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1031 17 13 12 0.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL2369533 209632 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm010037+
52944903 16996 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 466 11 3 7 2.6 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCN)C(OCc2ccccc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254048 16996 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 466 11 3 7 2.6 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCN)C(OCc2ccccc2)[C@@H]1O 10.1021/jm1002777
52944904 16997 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 480 12 3 7 2.6 COC[C@H]1OC(OCCc2ccccc2)[C@H](NCCN)C(OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254049 16997 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 480 12 3 7 2.6 COC[C@H]1OC(OCCc2ccccc2)[C@H](NCCN)C(OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
56651207 175897 0 None -1 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4586779 175897 0 None -1 2 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
155529288 171397 0 None -1 2 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4462329 171397 0 None -1 2 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
49865346 15912 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223231 15912 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
145991247 166806 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284442 166806 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 448 4 1 4 4.5 CC1(C)CCOc2ccc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL453936 213990 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1CSS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
145994083 167394 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4295189 167394 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 486 5 1 3 5.8 Cc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(C)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL2111257 209216 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H]([C@H](C)c2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
11563877 164720 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 668 9 3 5 5.7 Cc1cc(F)ccc1N1CCN(C(=O)N[C@@H](C(=O)Nc2cc(CN(C)C)ccc2OC(F)(F)F)[C@@H](C)c2c[nH]c3ccccc23)CC1=O 10.1016/j.bmc.2017.09.031
CHEMBL4217405 164720 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting method
ChEMBL 668 9 3 5 5.7 Cc1cc(F)ccc1N1CCN(C(=O)N[C@@H](C(=O)Nc2cc(CN(C)C)ccc2OC(F)(F)F)[C@@H](C)c2c[nH]c3ccccc23)CC1=O 10.1016/j.bmc.2017.09.031
66765477 129229 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 436 5 2 6 3.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)n[nH]c2c1 nan
CHEMBL3670732 129229 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 436 5 2 6 3.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)n[nH]c2c1 nan
CHEMBL3349674 211457 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm970730q
CHEMBL3350357 211475 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL2372712 210283 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C(=O)[C@@H](N)Cc2ccccc2)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
45102042 17031 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254395 17031 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
155528330 171340 0 None -1 2 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4461404 171340 0 None -1 2 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
70689723 73968 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021559 73968 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349667 211451 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349506 211411 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
66765622 129240 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 512 6 1 7 4.7 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(-c3ccccc3)c2c1 nan
CHEMBL3670743 129240 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 512 6 1 7 4.7 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(-c3ccccc3)c2c1 nan
91936729 167578 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL430066 167578 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL3350895 211517 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
145990504 167011 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4288259 167011 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 506 5 1 3 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)c(Cl)cc4C4CC4)CC3)CC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL265846 210667 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(CN)cc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm010037+
86766049 128394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 7 5.1 COc1c(-c2cn(C(C)C)nc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)ccc(F)c1F nan
CHEMBL3665787 128394 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 540 7 1 7 5.1 COc1c(-c2cn(C(C)C)nc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)ccc(F)c1F nan
CHEMBL524327 215602 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL3349680 211463 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1021/jm970730q
CHEMBL2011465 209113 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/ml200032v
CHEMBL3350896 211518 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350896 211518 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL455760 214008 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2c[nH]c(C(=O)O)c2)CCSSCC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701445q
56848119 128353 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 7 1 7 5.2 COc1ccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3665746 128353 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 7 1 7 5.2 COc1ccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
68093113 128366 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(C(F)(F)F)cc4)CC3)OC2=O)cc1 nan
CHEMBL3665759 128366 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 582 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(C(F)(F)F)cc4)CC3)OC2=O)cc1 nan
68092970 128374 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 6 1 7 5.1 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(F)c1 nan
CHEMBL3665767 128374 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 6 1 7 5.1 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(F)c1 nan
56848123 128373 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 558 5 1 6 5.9 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
CHEMBL3665766 128373 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 558 5 1 6 5.9 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
CHEMBL442494 213913 0 None -1 5 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/ml200032v
49800498 167014 15 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4282052 167014 15 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288391 167014 15 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 546 9 1 5 6.0 CCOc1cc(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL442494 213913 0 None -1 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm070886i
89573118 167063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4289325 167063 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(C(F)(F)F)ccc4C4CC4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
68093131 128411 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cncc(C(=O)O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665804 128411 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cncc(C(=O)O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848277 128359 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 6 1 6 5.2 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665752 128359 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 6 1 6 5.2 CC(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
68093082 128352 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2c(F)cc(F)cc2F)n1 nan
CHEMBL3665745 128352 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2c(F)cc(F)cc2F)n1 nan
68093085 128423 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cc(C(=O)O)ccn2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665816 128423 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 549 9 1 7 5.4 CCOc1cc(CN2CCC3(CC2)CN(c2cc(C(=O)O)ccn2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56847975 128345 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665738 128345 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
66765470 128365 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 598 7 1 7 6.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(OC(F)(F)F)cc4)CC3)OC2=O)cc1 nan
CHEMBL3665758 128365 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 598 7 1 7 6.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(C5CCCCC5)nc4-c4ccc(OC(F)(F)F)cc4)CC3)OC2=O)cc1 nan
68092932 128450 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 505 5 1 5 5.7 Cc1ccc(-c2cc(C)c(Cl)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 nan
CHEMBL3665843 128450 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 505 5 1 5 5.7 Cc1ccc(-c2cc(C)c(Cl)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 nan
68092936 128455 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.4 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCC2(C)C nan
CHEMBL3665848 128455 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.4 Cc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc2c1OCC2(C)C nan
CHEMBL1907758 209068 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
CHEMBL1824052 209036 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL442494 213913 0 None -1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm1005868
CHEMBL442494 213913 0 None -1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701618q
118963835 167012 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4288334 167012 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 592 5 1 4 7.7 Cc1cc(-c2ccc(Cl)cc2Cl)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL442494 213913 0 None -1 5 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
68254010 166414 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4277106 166414 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 559 10 2 7 6.6 CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
145989394 167231 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4292255 167231 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 535 9 0 5 6.6 CCOc1cc(CN2CCC3(CC2)CC(Cc2ccc(F)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL442494 213913 0 None -1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701445q
CHEMBL1907758 209068 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm040794i
CHEMBL452157 213976 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
CHEMBL442494 213913 0 None -1 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm801205x
86766029 128351 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(F)cc2F)n1 nan
CHEMBL3665744 128351 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 5 1 6 5.4 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2cc(F)c(F)cc2F)n1 nan
145989896 167016 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288417 167016 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL219375 209413 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm060363v
86766031 128360 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 8 1 6 5.5 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665753 128360 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 542 8 1 6 5.5 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
86766034 128368 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 612 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccc6ccccc6c5)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665761 128368 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 612 6 1 6 6.8 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccc6ccccc6c5)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
56847808 128421 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 616 9 1 6 7.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C(F)(F)F)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665814 128421 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 616 9 1 6 7.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(C(F)(F)F)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
44290718 155888 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1115 15 11 12 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
CHEMBL406051 155888 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL 1115 15 11 12 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
86766028 128347 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 508 6 1 6 5.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccccc4)CC3)OC2=O)cc1 nan
CHEMBL3665740 128347 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 508 6 1 6 5.2 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccccc4)CC3)OC2=O)cc1 nan
56848121 124430 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3639646 124430 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
86766043 128385 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 543 5 1 7 4.8 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cn2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665778 128385 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 543 5 1 7 4.8 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cn2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL1907758 209068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
145993203 167040 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288848 167040 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 514 10 0 5 7.1 CCOc1cc(CN2CCC(COc3cccc4cccnc34)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
25187955 12436 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL1185951 12436 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL443084 12436 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 646 9 4 4 4.9 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCC3(CCc4ccccc43)CC2)C1=O 10.1021/jm801205x
CHEMBL442494 213913 0 None -1 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm801314f
68093280 166406 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4277006 166406 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 525 5 1 5 5.8 Cc1cc(-c2ccncc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL410110 212800 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL3350881 211504 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
52948856 16937 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 494 13 3 7 3.0 COC[C@H]1OC(OCCc2ccccc2)[C@H](NCCCN)C(OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253191 16937 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 494 13 3 7 3.0 COC[C@H]1OC(OCCc2ccccc2)[C@H](NCCCN)C(OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
52941607 17025 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254321 17025 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 522 13 3 7 2.9 COC[C@H]1O[C@H](OCCc2ccccc2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
46902023 17038 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.7 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254476 17038 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.7 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCN)[C@@H](OCc2ccc3ccccc3c2)[C@@H]1O 10.1021/jm1002777
11535351 97052 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 983 17 13 12 -0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CCCC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL267054 97052 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 983 17 13 12 -0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)CCCC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL3349663 211447 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(-c3ccccc3)c2)C(N)=O)NC1=O 10.1021/jm970730q
24777672 94912 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
CHEMBL254210 94912 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 1027 18 12 11 1.0 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccccc2)C(=O)N1 10.1021/jm070886i
86766052 128400 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 5 1 6 5.8 CC(C)(C)n1cc(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665793 128400 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 5 1 6 5.8 CC(C)(C)n1cc(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3349614 211441 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
66765127 129226 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 410 4 1 6 3.1 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc5c(c4)OCO5)CC3)OC2=O)cc1 nan
CHEMBL3670729 129226 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 410 4 1 6 3.1 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc5c(c4)OCO5)CC3)OC2=O)cc1 nan
145981765 166661 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4281620 166661 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 485 9 0 6 5.8 CCOc1cc(CN2CCC(Oc3nccc(Cl)n3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL506892 214216 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1SS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3349508 211413 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
13690207 115382 0 None -29 5 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm050376t
CHEMBL3350037 115382 0 None -29 5 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm050376t
90663873 106739 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144283 106739 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144285 106739 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1498 23 21 25 -5.1 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
44368406 10267 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 10267 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
86766070 129239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 476 6 1 7 4.1 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(C3CC3)c2c1 nan
CHEMBL3670742 129239 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 476 6 1 7 4.1 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(C3CC3)c2c1 nan
CHEMBL452074 213974 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2c[nH]c(C(=O)O)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701445q
45273129 195737 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL557288 195737 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1173 19 14 15 1.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSS[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm801314f
CHEMBL510755 215588 0 None -1 3 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
66764686 128442 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cnc(-c5ccccc5)nc4-c4ccc(F)cc4)CC3)OC2=O)cc1 nan
CHEMBL3665835 128442 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cnc(-c5ccccc5)nc4-c4ccc(F)cc4)CC3)OC2=O)cc1 nan
2055 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
383414 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
90488715 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
CHEMBL1680 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
CHEMBL262746 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
DB00104 2907 48 None -32 14 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human SSTR5 by radioligand binding assayInhibition of human SSTR5 by radioligand binding assay
ChEMBL None None None None 10.1016/j.ejmech.2018.11.030
66765367 128387 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 576 7 1 6 5.8 CC(C)n1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
CHEMBL3665780 128387 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 576 7 1 6 5.8 CC(C)n1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
70689221 77856 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@@H](O)NC1=O 10.1021/jm030243c
CHEMBL2093026 77856 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1033 12 13 14 -0.7 C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)N(C)[C@@H](O)NC1=O 10.1021/jm030243c
CHEMBL3349672 211455 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3350897 211519 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](c1c[nH]c2ccccc12)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
145980628 166673 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
CHEMBL4281783 166673 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 542 6 1 6 6.1 CC(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2c(-c3ccc(F)cc3)cccc21 10.1021/acsmedchemlett.8b00306
86766054 128409 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccccc2C(=O)O)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665802 128409 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccccc2C(=O)O)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL406373 212606 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(I)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL3349608 211436 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL3350912 211530 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
145990810 166823 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4284867 166823 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 482 4 1 4 5.1 CC1(C)CCOc2c(Cl)cc(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL3350905 211524 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3349671 211454 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(-c3ccccc3)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
16737813 142081 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 418 8 3 3 2.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL388069 142081 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 418 8 3 3 2.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL2079559 209195 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2011464 209112 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/ml200032v
CHEMBL3350887 211510 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL451932 213973 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](CC2CCCCC2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL3122127 211105 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)NCC(=O)N[C@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1016/j.ejmech.2013.12.003
25188776 12482 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186427 12482 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL462020 12482 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 551 11 4 4 3.6 NCCCC[C@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL504457 214177 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
56847979 128402 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 7 1 5 6.1 CCOc1ccc(-c2ccc(F)c(F)c2)c(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665795 128402 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 536 7 1 5 6.1 CCOc1ccc(-c2ccc(F)c(F)c2)c(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
56847980 128403 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 532 6 1 7 5.4 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3665796 128403 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 532 6 1 7 5.4 COc1ccc(-c2nn(C(C)(C)C)cc2CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL2011467 209115 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)N(C)C1=O 10.1021/ml200032v
CHEMBL415582 213190 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371100 210012 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL502777 214157 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3349505 211410 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm970730q
CHEMBL447064 213947 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None CC(=O)N[C@H](Cc1ccc([N+](=O)[O-])cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm701618q
70683416 73967 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2021544 73967 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1170 16 9 12 4.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349616 211442 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970730q
44444935 94642 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
CHEMBL252355 94642 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm070886i
49865341 15907 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL1223226 15907 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 981 17 13 12 -0.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C/C=C\C[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm1005868
CHEMBL504087 214173 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1CCSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
86766050 128395 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 7 1 6 5.1 CCCn1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
CHEMBL3665788 128395 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 7 1 6 5.1 CCCn1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
162651887 180271 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4750625 180271 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 924 25 12 12 -0.1 CCC(NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](N)CC(N)=O)C(N)=O 10.1021/acs.jmedchem.6b00164
49865342 15908 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223227 15908 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1147 20 12 13 2.2 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
68092986 129221 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
CHEMBL3670724 129221 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
CHEMBL3349507 211412 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
66765665 128390 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 500 5 1 6 4.2 Cn1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
CHEMBL3665783 128390 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 500 5 1 6 4.2 Cn1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
CHEMBL1823873 209032 9 None -1 4 Human 8.5 pIC50 = 8.5 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
25188220 12491 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186489 12491 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL466609 12491 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL442494 213913 0 None -1 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm701444y
86766033 128363 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 620 6 1 8 5.4 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5cccc6c5OCCO6)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665756 128363 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 620 6 1 8 5.4 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5cccc6c5OCCO6)nc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
25187398 12448 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186066 12448 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448026 12448 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 12 4 4 4.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL263209 210563 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@@H](C(N)=O)[C@H](C)O)NC1=O 10.1021/jm050376t
25189327 12696 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187509 12696 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL505888 12696 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 601 11 4 4 4.7 NCCCC[C@@H](C(=O)NCc1cccc2ccccc12)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm801205x
25189054 12704 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL1187568 12704 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
CHEMBL509513 12704 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 685 11 4 6 3.0 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)N2CCN(S(=O)(=O)c3ccccc3)CC2)C1=O 10.1021/jm801205x
68092939 129223 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 468 4 1 5 4.6 CC1(C)CCOc2c(F)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
CHEMBL3670726 129223 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 468 4 1 5 4.6 CC1(C)CCOc2c(F)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
25187679 12671 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL1187340 12671 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
CHEMBL499398 12671 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 571 10 4 4 4.3 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)c2ccc(Cl)cc2)C1=O 10.1021/jm801205x
56848279 128358 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3665751 128358 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 6 1 6 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
56847771 128419 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 521 8 1 6 5.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(=O)[nH]c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665812 128419 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 521 8 1 6 5.0 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(=O)[nH]c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL1907758 209068 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cc3ccccc3[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030243c
CHEMBL3350886 211509 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL441185 213882 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL3349613 211440 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
56651206 174631 0 None -1 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4557933 174631 0 None -1 2 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL2079559 209195 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2cccc(-c3ccccc3)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2311181 209507 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
68092934 128399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 433 4 1 5 4.3 Cn1ccc2ccc(CN3CCCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
CHEMBL3665792 128399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 433 4 1 5 4.3 Cn1ccc2ccc(CN3CCCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 nan
89573250 167109 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL4290073 167109 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 498 4 1 6 3.8 CC1(C)CCS(=O)(=O)c2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 10.1021/acsmedchemlett.8b00306
CHEMBL263587 210578 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
90663875 106741 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144287 106741 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL499760 214101 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H]2NC(=O)[C@H](NC(=O)[C@H](N)Cc3ccc(Cl)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm701618q
44346098 16428 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 525 13 0 4 5.6 O=C1[C@H](Cc2ccc(OCc3ccccc3)cc2)N(CCCCc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
CHEMBL123190 16428 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 525 13 0 4 5.6 O=C1[C@H](Cc2ccc(OCc3ccccc3)cc2)N(CCCCc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
44346082 113815 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 521 10 0 4 5.0 O=C1[C@H](Cc2ccc(OCc3ccccc3)cc2)N(CCC#Cc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
CHEMBL332512 113815 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 521 10 0 4 5.0 O=C1[C@H](Cc2ccc(OCc3ccccc3)cc2)N(CCC#Cc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
CHEMBL3350891 211514 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
16737812 85506 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL227211 85506 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
25122324 167100 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4289922 167100 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from mouse SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
86766053 128406 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 5 1 6 5.0 CC(C)(C)n1cc(CN2CCC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665799 128406 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 528 5 1 6 5.0 CC(C)(C)n1cc(CN2CCC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
44560876 188776 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1324 21 17 17 -0.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL505628 188776 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1324 21 17 17 -0.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(N)=O)NC1=O 10.1021/jm701618q
90663874 106740 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144286 106740 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144291 106740 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1660 26 24 30 -7.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O[C@@H]4O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]4O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
145980226 166716 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
CHEMBL4282854 166716 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 459 5 1 4 5.2 Cc1cccc2c(CN3CCC4(CC3)CC(=O)N(c3ccc(C(=O)O)cc3)C4)cn(C(C)C)c12 10.1021/acsmedchemlett.8b00306
CHEMBL3349610 211437 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(C)(C)SSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm970730q
CHEMBL2371051 210004 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
44368398 10266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161331 10266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1196 16 15 16 -0.2 C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350893 211515 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350880 211503 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3349598 211427 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm970730q
CHEMBL3351090 211544 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
86766038 128377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 506 5 1 6 5.0 CC(C)(C)c1nn(-c2ccc(F)cc2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3665770 128377 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 506 5 1 6 5.0 CC(C)(C)c1nn(-c2ccc(F)cc2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL2111200 209215 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL3122124 211103 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL3349617 211443 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm970730q
CHEMBL262135 210527 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL437451 213720 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(CN)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm010037+
44368406 10267 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161332 10267 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1022 9 11 12 1.1 C[C@@H]1NC(=O)N(C)[C@H](O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350908 211527 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](c1c[nH]c2ccccc12)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030245x
158782 157834 20 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
ChEMBL 1421 26 17 22 -3.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL408350 157834 20 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
ChEMBL 1421 26 17 22 -3.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL2371059 210006 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
44345936 110423 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 465 7 0 3 4.6 O=C1[C@H](Cc2cccc3ccccc23)N(CCC#Cc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
CHEMBL324511 110423 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 465 7 0 3 4.6 O=C1[C@H](Cc2cccc3ccccc23)N(CCC#Cc2ccccc2)C(=O)N1CCN1CCCC1 10.1016/s0960-894x(98)00647-7
56848332 128356 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 592 5 1 6 6.6 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(Cl)c2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
CHEMBL3665749 128356 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 592 5 1 6 6.6 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(Cl)c2)C(=O)O3)c(-c2cc(F)c(Cl)cc2F)n1 nan
89573308 166459 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4277991 166459 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 474 5 1 4 5.3 O=C(O)c1ccc(N2CC3(CCN(Cc4ccc(C5CC5)c(C(F)(F)F)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
44311889 96984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm960850i
CHEMBL266469 96984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm960850i
44311889 96984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm960851a
CHEMBL266469 96984 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL 1000 17 13 13 -1.4 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm960851a
16129706 209031 40 None -9 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
CHEMBL1823872 209031 40 None -9 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
16129706 209031 40 None -9 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL1823872 209031 40 None -9 5 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.ejmech.2013.12.003
CHEMBL2372667 210280 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)C(NC(=O)[C@@H](N)Cc2ccccc2)CSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
56848068 128348 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 502 7 1 7 4.6 COc1ccc(-c2nn(C3CC3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3665741 128348 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 502 7 1 7 4.6 COc1ccc(-c2nn(C3CC3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
66764848 128376 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 560 6 1 6 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
CHEMBL3665769 128376 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 560 6 1 6 6.0 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccccc5)nc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
86766042 128384 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 560 5 1 6 5.6 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(F)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
CHEMBL3665777 128384 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 560 5 1 6 5.6 CC(C)(C)n1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)c(F)c2)C(=O)O3)c(-c2ccc(F)c(F)c2F)n1 nan
56848330 128357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccccc1-c1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3665750 128357 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 518 6 1 7 5.0 COc1ccccc1-c1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3350911 211529 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL262379 210538 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm049520l
68092931 128364 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 7 1 7 5.2 COc1cccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
CHEMBL3665757 128364 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 538 7 1 7 5.2 COc1cccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1 nan
49865347 15913 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1197 20 12 13 3.4 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223232 15913 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1197 20 12 13 3.4 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccc3ccccc23)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(OC(=O)c3ccccc3)cc2)C(=O)N1 10.1021/jm1005868
145982363 166601 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
CHEMBL4280432 166601 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 576 5 1 3 6.8 Cc1cc(-c2ccc(F)c(F)c2F)c(CN2CCC3(CC2)CC(=O)N(c2ccc(C(=O)O)cc2)C3)cc1C(F)(F)F 10.1021/acsmedchemlett.8b00306
44311848 168703 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm960850i
CHEMBL436783 168703 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR5
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm960850i
44311848 168703 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm960851a
CHEMBL436783 168703 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)compound was tested for the inhibition of human somatostatin receptor 5 (hSSTR5)
ChEMBL 999 17 13 13 -2.0 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm960851a
56847978 128401 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.4 CCOc1cc(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665794 128401 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 562 9 1 6 6.4 CCOc1cc(CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
56848077 128388 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 576 8 1 6 5.6 CCCn1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
CHEMBL3665781 128388 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 576 8 1 6 5.6 CCCn1nc(Cc2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c1Cl nan
CHEMBL1824050 209034 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
44325273 207308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)
ChEMBL 554 7 2 4 5.4 NCCCC1CCCN2C(=O)[C@@H](Cc3c[nH]c4ccccc34)SCCN(Cc3cccc4ccccc34)C(=O)C12 10.1016/s0960-894x(00)00552-7
CHEMBL93351 207308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)
ChEMBL 554 7 2 4 5.4 NCCCC1CCCN2C(=O)[C@@H](Cc3c[nH]c4ccccc34)SCCN(Cc3cccc4ccccc34)C(=O)C12 10.1016/s0960-894x(00)00552-7
86766069 129238 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 506 6 1 7 4.8 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(CC(C)(C)C)c2c1 nan
CHEMBL3670741 129238 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 506 6 1 7 4.8 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(CC(C)(C)C)c2c1 nan
90663869 106737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3144281 106737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1424 23 18 21 -2.3 C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CCS[C@@H]2O[C@@H](CO)[C@H](O)[C@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
86766073 129258 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 6 1 6 5.7 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(C5CC5)oc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
CHEMBL3670761 129258 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 6 1 6 5.7 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(C5CC5)oc4-c4ccc(F)c(Cl)c4)CC3)OC2=O)cc1 nan
49865345 15911 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL1223230 15911 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST5 receptor expressed in HEK293 cells by autoradiography
ChEMBL 1043 18 13 12 0.7 C[C@@H](O)[C@@H](CO)NC(=O)[C@@H]1C/C=C/C[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2cc3ccccc3[nH]2)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1 10.1021/jm1005868
CHEMBL3350885 211508 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H]([C@H](C)c2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL505704 214196 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(=O)NO)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL386784 212392 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
86766046 128391 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 500 5 1 6 4.2 Cn1cc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
CHEMBL3665784 128391 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 500 5 1 6 4.2 Cn1cc(-c2cc(F)c(F)cc2F)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)n1 nan
66764877 128381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 596 6 1 6 6.3 O=C(O)c1ccc(N2CC3(CCN(Cc4c(-c5cc(F)c(F)cc5F)nn(-c5ccccc5)c4Cl)CC3)OC2=O)cc1 nan
CHEMBL3665774 128381 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 596 6 1 6 6.3 O=C(O)c1ccc(N2CC3(CCN(Cc4c(-c5cc(F)c(F)cc5F)nn(-c5ccccc5)c4Cl)CC3)OC2=O)cc1 nan
44560866 188877 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL507148 188877 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
86766075 129266 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 550 5 1 6 5.4 Cc1cccn2c(-c3cc(F)c(F)cc3F)c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nc12 nan
CHEMBL3670769 129266 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 550 5 1 6 5.4 Cc1cccn2c(-c3cc(F)c(F)cc3F)c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nc12 nan
68093286 129227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 436 4 1 5 4.1 CC1(C)Cc2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
CHEMBL3670730 129227 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 436 4 1 5 4.1 CC1(C)Cc2cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)ccc2O1 nan
CHEMBL265912 210671 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm010037+
CHEMBL3350890 211513 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL425090 213329 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL452157 213976 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL452157 213976 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL452157 213976 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL525030 215631 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1SSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL452157 213976 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm801314f
CHEMBL452157 213976 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
118718854 115416 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 115416 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL509363 215434 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL415585 213193 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
118718507 115358 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
CHEMBL3349670 115358 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL 1050 14 11 12 3.4 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)NC(C)(C)C)NC1=O 10.1021/jm970730q
25187396 12684 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1187397 12684 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL501699 12684 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 475 9 4 4 2.4 CC(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)NCc2ccccc2)C1=O 10.1021/jm801205x
CHEMBL408338 212706 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm049520l
CHEMBL409100 212746 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.Tested for ability to bind to 20 uM thick cryostat sections of a membrane pellet of cells transfected with human cloned somatostatin (sst) receptor subtype 5.
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@H](C(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm010037+
CHEMBL219375 209413 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst5 receptor expressed in CHOK1 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm701445q
CHEMBL219375 209413 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm801314f
86766040 128380 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 6 1 6 6.1 CC(C)(C)Cn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(Cl)c2)n1 nan
CHEMBL3665773 128380 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 554 6 1 6 6.1 CC(C)(C)Cn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(-c2ccc(F)c(Cl)c2)n1 nan
56848173 128355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 552 8 1 7 5.6 CCOc1ccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3665748 128355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 552 8 1 7 5.6 CCOc1ccc(-c2nn(-c3ccccc3)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
86766032 128362 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 544 6 1 6 5.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccc(F)cc5)nc4-c4ccc(F)cc4)CC3)OC2=O)cc1 nan
CHEMBL3665755 128362 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 544 6 1 6 5.5 O=C(O)c1ccc(N2CC3(CCN(Cc4cn(-c5ccc(F)cc5)nc4-c4ccc(F)cc4)CC3)OC2=O)cc1 nan
145981179 166518 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
CHEMBL4278915 166518 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 514 5 1 6 4.8 Cn1cc(-c2ccc(C(F)(F)F)cc2CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cn1 10.1021/acsmedchemlett.8b00306
CHEMBL269532 210795 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
56848026 128405 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 534 9 1 6 5.6 CCOc1cc(CN2CCC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665798 128405 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 534 9 1 6 5.6 CCOc1cc(CN2CCC3(C2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3350889 211512 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None CNc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3122123 211102 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None CCCC[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
25188218 12564 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL1186753 12564 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL476240 12564 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 565 11 4 4 4.2 C[C@@H](NC(=O)[C@H](CCCCN)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O)c1ccccc1 10.1021/jm801205x
CHEMBL502511 214155 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1SSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL504395 214176 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1CSS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL504462 214179 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1SSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
11678313 17015 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254235 17015 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL2372604 210275 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 210275 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL3349678 211461 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
44346106 114114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 555 14 0 5 5.6 COc1ccc(CCCCN2C(=O)N(CCN3CCCC3)C(=O)[C@@H]2Cc2ccc(OCc3ccccc3)cc2)cc1 10.1016/s0960-894x(98)00647-7
CHEMBL332786 114114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Compound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cellsCompound was tested for inhibition of specific [125I]Tyr11-SRIF binding to human recombinant SST5 (somatostatin) receptor expressed in CHO-K1 cells
ChEMBL 555 14 0 5 5.6 COc1ccc(CCCCN2C(=O)N(CCN3CCCC3)C(=O)[C@@H]2Cc2ccc(OCc3ccccc3)cc2)cc1 10.1016/s0960-894x(98)00647-7
68092963 128378 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 456 6 1 7 3.7 CCOc1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3665771 128378 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 456 6 1 7 3.7 CCOc1nn(C(C)(C)C)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 nan
CHEMBL3350884 211507 1 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL503036 214160 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1CSS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
155550820 174289 0 None 5 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4549840 174289 0 None 5 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL2372606 210276 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC[C@H]2O[C@H](O)[C@H](O)[C@@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL2372608 210276 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC[C@H]2O[C@H](O)[C@H](O)[C@@H](O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL3349677 211460 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL3349669 211453 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL2011463 209111 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)N(C)C1=O 10.1021/ml200032v
CHEMBL446077 213943 0 None -9 3 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None CNCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm701618q
10114 2556 23 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 minsDisplacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
56927659 2556 23 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 minsDisplacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL2204935 2556 23 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 minsDisplacement of [125I]SS-28 from human SSTR-5 transfected in CHO cells after 90 to 120 mins
ChEMBL 494 4 3 7 4.3 Fc1ccc(cc1)c1cnc([nH]1)[C@H]1Cc2c3ccccc3[nH]c2[C@@](N1)(c1noc(n1)C)c1cnn(c1)C 10.1021/ml300063m
CHEMBL436892 213692 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](Cc3ccccc3)NC(N)=O)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm060363v
CHEMBL414316 213122 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)cc2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL441920 213900 13 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)O 10.1021/jm040794i
CHEMBL1824049 209033 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
11159133 115462 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350904 115462 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1152 15 15 15 0.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL511086 215592 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL447989 213953 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1SS[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL3122128 211106 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST5 receptor expressed in HEK293 cells after 2 hrs by autoradiographic analysis
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)COCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2013.12.003
66766101 128404 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 552 7 1 7 5.6 COc1ccc(-c2nn(-c3ccccc3)cc2CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
CHEMBL3665797 128404 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 552 7 1 7 5.6 COc1ccc(-c2nn(-c3ccccc3)cc2CN2CCCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1 nan
155553012 174086 0 None -1 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4544582 174086 0 None -1 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL1824056 209040 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm200307v
86766030 128354 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 5 1 6 6.2 Cc1cc(N2CC3(CCN(Cc4cn(C(C)(C)C)nc4-c4cc(F)c(Cl)cc4F)CC3)OC2=O)ccc1C(=O)O nan
CHEMBL3665747 128354 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 572 5 1 6 6.2 Cc1cc(N2CC3(CCN(Cc4cn(C(C)(C)C)nc4-c4cc(F)c(Cl)cc4F)CC3)OC2=O)ccc1C(=O)O nan
56847923 129246 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 449 5 1 6 3.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(C)c2c1 nan
CHEMBL3670749 129246 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 449 5 1 6 3.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(C)c2c1 nan
CHEMBL524870 215625 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1SS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
11642413 17100 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.9 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1254967 17100 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 544 11 3 7 3.9 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
86766072 129244 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 514 4 1 6 5.3 CC(C)(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(Cl)c(F)cc21 nan
CHEMBL3670747 129244 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 514 4 1 6 5.3 CC(C)(C)n1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(Cl)c(F)cc21 nan
CHEMBL501282 214136 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
155541897 173055 0 None 5 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL4519358 173055 0 None 5 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL3350883 211506 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]([C@@H](C)c2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
CHEMBL3350898 211520 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350888 211511 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030246p
CHEMBL3350888 211511 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
90663867 106735 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O)[C@@H]2O)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL3144279 106735 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1322 20 18 20 -3.1 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O)[C@@H]2O)CSSC[C@@H](C(=O)N[C@H](CO)[C@@H](C)O)NC1=O 10.1021/jm040794i
CHEMBL2372604 210275 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2372607 210275 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=5)
ChEMBL None None None C[C@H](O)[C@@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
86766065 128458 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 519 8 1 7 5.0 CCOc1cc(C)nc2c(OCC)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc12 nan
CHEMBL3665851 128458 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 519 8 1 7 5.0 CCOc1cc(C)nc2c(OCC)cc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc12 nan
CHEMBL510901 215590 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm701618q
CHEMBL3350894 211516 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
CHEMBL3350357 211475 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
CHEMBL2371108 210013 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm030246p
CHEMBL2304255 209487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to sst5 receptorBinding affinity to sst5 receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NCCNC(=O)CCCN([C@@H](Cc2ccccc2)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C1=O 10.1021/jm070886i
CHEMBL2304255 209487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccccc2)NCCNC(=O)CCCN([C@@H](Cc2ccccc2)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C1=O 10.1021/jm801205x
68092941 129233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 6 1 7 4.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(C(C)C)c2c1 nan
CHEMBL3670736 129233 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 478 6 1 7 4.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)nn(C(C)C)c2c1 nan
CHEMBL412473 212994 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)O)NC(=O)[C@H](CO)N(C)C(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL1824051 209035 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst5 receptor in HEK293 cells after 2 hrs by autoradiography
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm200307v
66765638 129259 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4sc(-c5ccccc5)nc4-c4ccccc4)CC3)OC2=O)cc1 nan
CHEMBL3670762 129259 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 525 6 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4sc(-c5ccccc5)nc4-c4ccccc4)CC3)OC2=O)cc1 nan
CHEMBL3350909 211528 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm030245x
56847811 128413 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 602 10 1 9 5.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2OC)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665806 128413 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 602 10 1 9 5.5 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(-c4nnn[nH]4)cc2OC)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL505854 214198 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
11468916 115463 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1137 15 14 14 0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
CHEMBL3350910 115463 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1137 15 14 14 0.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm030245x
145989896 167016 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4288417 167016 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 517 9 1 4 7.2 CCOc1cc(CN2CCC(c3ncc(-c4ccc(F)cc4)[nH]3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL413735 213086 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNCCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
68093096 167253 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
CHEMBL4292738 167253 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 450 4 1 5 4.5 CC1(C)CCc2cccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c2O1 10.1021/acsmedchemlett.8b00306
52948576 16988 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 514 12 3 7 3.6 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCCN)C(OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1253954 16988 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 514 12 3 7 3.6 COC[C@H]1OC(OCc2ccc3ccccc3c2)[C@H](NCCCN)C(OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
52948630 17005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL1254140 17005 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST5 receptor expressed in CHO cells
ChEMBL 542 12 3 7 3.6 COC[C@H]1O[C@H](OCc2ccc3ccccc3c2)[C@H](NC(=O)CCCN)[C@H](OCc2ccc(Cl)cc2)[C@@H]1O 10.1021/jm1002777
CHEMBL387458 212410 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm0302445
44560867 189140 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510693 189140 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1204 18 12 14 1.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](N(C)C(=O)c2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
91936728 161727 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL413647 161727 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=6)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL436678 213685 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cellsInhibitory concentration against human somatostatin receptor type 5 in CHO-K1 cells
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(N)c(I)c2)CSSC[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)NC1=O 10.1021/jm050376t
CHEMBL2079558 209194 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
90663868 106736 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL3144280 106736 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL3144290 106736 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 5 expressed in CHO-K1 cells; (n=3)
ChEMBL 1484 23 21 25 -5.2 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC[C@]2(O)OC[C@H](O)[C@@H](O[C@@H]3O[C@@H](CO)[C@@H](O)[C@H](O)[C@@H]3O)[C@@H]2O)C(=O)N[C@@H](Cc2ccc(O)c(I)c2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm040794i
CHEMBL2011461 209109 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)N(C)C(=O)[C@H](Cc2ccccc2)N(C)C1=O 10.1021/ml200032v
162646037 179514 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
CHEMBL4741230 179514 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR5 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assay
ChEMBL 1387 27 17 19 -2.0 CC(C)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N1)C(N)=O 10.1021/acs.jmedchem.6b00164
118718854 115416 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350354 115416 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1152 13 13 16 0.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NN(C(=O)N(C)C(=O)c2ccccc2)[C@@H](O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL3350907 211526 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 5 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligand
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)N(C)[C@@H](C(=O)c2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030246p
CHEMBL3349676 211459 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 5 (hsst) receptorBinding affinity towards cloned human somatostatin 5 (hsst) receptor
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm970730q
CHEMBL219201 209409 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst5
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](Cc2ccccc2)NC(N)=O)C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm060363v
86766045 128389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4c(Cc5cc(F)c(F)cc5F)nn(-c5ccccc5)c4Cl)CC3)OC2=O)cc1 nan
CHEMBL3665782 128389 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.2 O=C(O)c1ccc(N2CC3(CCN(Cc4c(Cc5cc(F)c(F)cc5F)nn(-c5ccccc5)c4Cl)CC3)OC2=O)cc1 nan
25187953 12689 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL1187458 12689 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
CHEMBL503379 12689 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 725 10 4 6 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)N[C@@H]3Cc4c([nH]c5ccccc45)CN([C@@H](CCCCN)C(=O)NCc4ccccc4)C3=O)CC2)c2ccccc21 10.1021/jm801205x
16738359 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL374833 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL453938 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
16738359 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL374833 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
CHEMBL453938 137183 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST5 receptor
ChEMBL 641 13 4 4 5.6 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
89573310 166443 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
CHEMBL4277613 166443 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 437 6 1 6 3.7 COc1ncc(C2CC2)cc1CN1CCC2(CC1)CN(c1ccc(C(=O)O)cc1)C(=O)O2 10.1021/acsmedchemlett.8b00306
56848125 128382 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 9 1 6 5.4 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(Cc2cc(F)c(F)cc2F)n1 nan
CHEMBL3665775 128382 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 556 9 1 6 5.4 CCCCn1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c(Cc2cc(F)c(F)cc2F)n1 nan
56847842 128416 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 588 10 1 6 6.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C4(C(=O)O)CC4)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665809 128416 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 588 10 1 6 6.4 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C4(C(=O)O)CC4)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL436962 213700 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/jm049519m
56847925 129249 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 435 5 2 5 3.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c[nH]c2c1 nan
CHEMBL3670752 129249 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 435 5 2 5 3.9 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)c[nH]c2c1 nan
CHEMBL501776 214144 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
25187683 12451 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL1186082 12451 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL448713 12451 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 627 12 4 4 5.2 NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C1=O 10.1021/jm801205x
CHEMBL409653 212775 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
2051 3576 24 None -37 9 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
5311430 3576 24 None -37 9 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
CHEMBL311695 3576 24 None -37 9 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human sst5 by in vitro receptor autoradiography assayBinding affinity to human sst5 by in vitro receptor autoradiography assay
ChEMBL None None None None 10.1021/ml200032v
CHEMBL447177 213948 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)NCC(=O)O)NC1=O 10.1021/jm701618q
CHEMBL525397 215645 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1CSS[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
25122324 167100 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
CHEMBL4289922 167100 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assayDisplacement of (3-125I-Tyr11)-SRIF-28 from human SSTR5 expressed in CHO-K1 cell membranes by filtration binding assay
ChEMBL 441 7 2 5 3.5 CCOc1cc(CN2CCC3(CC2)NC(=O)NC3=O)cc(OCC)c1-c1ccc(F)cc1 10.1021/acsmedchemlett.8b00305
118719101 115440 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
CHEMBL3350724 115440 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 1356 21 16 16 2.5 CNc1ccc(C(C(C)C)[C@@H]2NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC2=O)cc1 10.1021/jm030245x
66765438 129261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 509 6 1 6 5.7 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4ccccc4)CC3)OC2=O)cc1 nan
CHEMBL3670764 129261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 509 6 1 6 5.7 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4ccccc4)CC3)OC2=O)cc1 nan
10577746 207252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1021/jm801205x
CHEMBL92914 207252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1021/jm801205x
10577746 207252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1016/s0960-894x(00)00552-7
CHEMBL92914 207252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)Inhibitory concentration required for somatostatin 5 receptor in radioligand binding assay ([125I]-Tyr11-SRIF)
ChEMBL 514 8 3 4 4.6 NCCCC[C@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)SCCN(Cc2cccc3ccccc23)C1=O 10.1016/s0960-894x(00)00552-7
86766047 128392 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4nn(Cc5ccc(Cl)cc5)cc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
CHEMBL3665785 128392 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 610 7 1 6 6.4 O=C(O)c1ccc(N2CC3(CCN(Cc4nn(Cc5ccc(Cl)cc5)cc4-c4ccc(F)c(F)c4F)CC3)OC2=O)cc1 nan
66765377 129257 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 563 6 1 6 6.1 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
CHEMBL3670760 129257 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 563 6 1 6 6.1 O=C(O)c1ccc(N2CC3(CCN(Cc4nc(-c5ccccc5)oc4-c4cc(F)c(F)cc4F)CC3)OC2=O)cc1 nan
44560873 189147 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1809 40 18 25 -1.0 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL510793 189147 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL 1809 40 18 25 -1.0 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)CCOCCOCCOCCNC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL2371085 210011 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2cccc3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm0302445
CHEMBL505128 214188 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1SSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
56847976 129250 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 511 6 1 6 5.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(-c3ccccc3)c2c1 nan
CHEMBL3670753 129250 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 511 6 1 6 5.3 COc1ccc2c(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cn(-c3ccccc3)c2c1 nan
CHEMBL446380 213945 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
56847772 128420 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2cccc(C(=O)O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665813 128420 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 548 9 1 6 6.0 CCOc1cc(CN2CCC3(CC2)CN(c2cccc(C(=O)O)c2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
86766064 124431 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 559 5 1 5 6.4 Cc1cc(-c2ccc(C(F)(F)F)nc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
CHEMBL3639647 124431 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 559 5 1 5 6.4 Cc1cc(-c2ccc(C(F)(F)F)nc2)c(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc1Cl nan
56847922 128412 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 10 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(C)(C)C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL3665805 128412 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 590 10 1 6 6.6 CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(C)(C)C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 nan
CHEMBL500326 214111 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL410047 212797 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](N)CSSC[C@@H](C(=O)O)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
45273131 194786 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1271 20 11 14 2.8 CN(C(=O)c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL538451 194786 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst5 receptor by autoradiography
ChEMBL 1271 20 11 14 2.8 CN(C(=O)c1ccc2ccccc2c1)[C@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(C(N)=O)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm801314f
CHEMBL504248 214175 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst5 receptor expressed in CHOK1 cells
ChEMBL None None None CC(=O)N[C@H]1CCSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm701444y
CHEMBL2372699 210281 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 5 (hsst5) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(C(=O)[C@@H](N)Cc2cccc3ccccc23)CCSSCCN(CC(N)=O)C(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm0100281
122179477 121474 5 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL3582336 121474 5 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assayDisplacement of [125I]SS-14 from human recombinant SSTR5 expressed in CHO cell membranes incubated for 60 to 90 mins by radioligand binding assay
ChEMBL 525 5 3 9 3.2 CCn1cc([C@@]2(c3nn(C)c(=O)o3)N[C@@H](c3nc(-c4ccc(F)cn4)c[nH]3)Cc3c2[nH]c2ccccc32)cn1 10.1021/ml500514w
CHEMBL448431 213957 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst5 receptor by autoradiography
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccc(F)cc23)NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
118963840 166926 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 518 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(OC(F)(F)F)c(Cl)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
CHEMBL4286833 166926 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranesDisplacement of [3-125I-Tyr11]-SRIF-14 or [3-125I-Tyr11]-SRIF-28 from human SSR5 expressed in CHOK1 cell membranes
ChEMBL 518 5 1 5 5.6 O=C(O)c1ccc(N2CC3(CCN(Cc4cc(Cl)c(OC(F)(F)F)c(Cl)c4)CC3)OC2=O)cc1 10.1021/acsmedchemlett.8b00306
66764933 129231 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 480 7 1 6 4.7 CCCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL3670734 129231 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).Binding Assay: SSTR5 binding assays can be performed by labeling somatostatin and determining the ability of a compound to inhibit somatostatin binding. (Poitout et al., J. Med. Chem. 44:29900-3000, (2001); Hocart et al., J. Med. Chem. 41:1146-1154, (1998); J. Med. Chem. 50, 6292-6295 (2007) and J. Med. Chem. 50, 6295-6298 (2007)). Binding assays were performed using (3-125I-Tyr11)-SRIF-14 or (3-125I-Tyr11)-SRIF-28 as the radioligand (used at 0.1 nM) and The Packard Unifilter assay plate. The assay buffer consisted of 50 mM TrisHCl (pH 7.8) with 1 mM EGTA, 5 in M MgCl2, leupeptin (10 μg/mL), pepstatin (10 μg/mL), bacitracin (200 μg/mL), and aprotinin (0.5 μg/mL).
ChEMBL 480 7 1 6 4.7 CCCCn1nc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)c2cc(F)ccc21 nan
CHEMBL3350726 211491 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(N)cc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm030245x
2019 3675 0 None -3 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44386062 3675 0 None -3 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL440072 3675 0 None -3 10 Human 9.5 pKd = 9.5 Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL407209 212647 1 None 17 4 Human 9.2 pKd = 9.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
46865535 5539 0 None -323 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 550 6 0 5 5.7 Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 10.1016/j.bmcl.2010.01.063
CHEMBL1076622 5539 0 None -323 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 550 6 0 5 5.7 Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 10.1016/j.bmcl.2010.01.063
9871544 14216 3 None -229 11 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076624 14216 3 None -229 11 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198948 14216 3 None -229 11 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL405561 212566 0 None -41 4 Human 6.9 pKd = 6.9 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL2370166 209805 0 None -7 5 Human 6.9 pKd = 6.9 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.
ChEMBL None None None C[C@@H](c1ccccc1)N1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C1=O 10.1021/jm970393l
17955460 176775 0 None -18620 9 Human 4.8 pKd = 4.8 Binding
Binding affinity to human sst5 receptorBinding affinity to human sst5 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL460542 176775 0 None -18620 9 Human 4.8 pKd = 4.8 Binding
Binding affinity to human sst5 receptorBinding affinity to human sst5 receptor
ChEMBL 491 7 0 4 5.3 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL384836 212337 0 None -1 5 Human 7.8 pKd = 7.8 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1C)C(N)=O 10.1021/jm000361p
46865536 11919 0 None -213 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1076623 11919 0 None -213 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
CHEMBL1182658 11919 0 None -213 7 Human 5.8 pKd = 5.8 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 553 6 0 6 5.2 C[C@@H](Cc1ccc2nsnc2c1)CN1C[C@@H](C(=O)N2CCN(c3ccc(F)c(F)c3)CC2)[C@H]2CCCC[C@H]2C1 10.1016/j.bmcl.2010.01.063
2030 3672 10 None -2511 10 Human 5.8 pKd = 5.8 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
5311377 3672 10 None -2511 10 Human 5.8 pKd = 5.8 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL251541 3672 10 None -2511 10 Human 5.8 pKd = 5.8 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 464 4 0 6 3.0 COc1cccc2c1C[C@H]1C[C@H](CN([C@@H]1C2)C)C(=O)N1CCN(CC1)c1ccc(cc1)[N+](=O)[O-] 10.1016/j.bmcl.2007.04.086
CHEMBL405421 212560 0 None -22 4 Human 7.6 pKd = 7.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
44447078 94617 0 None -128 7 Human 4.6 pKd = 4.6 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252232 94617 0 None -128 7 Human 4.6 pKd = 4.6 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL413373 213062 0 None -8 4 Human 7.6 pKd = 7.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None CN[C@H](Cc1ccc(O)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000361p
CHEMBL409019 212742 0 None 1 5 Human 7.6 pKd = 7.6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1C)C(N)=O 10.1021/jm000361p
CHEMBL2370167 209806 0 None -45 5 Human 6.5 pKd = 6.5 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN([C@H](C)c2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
CHEMBL265636 210658 0 None -21 4 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccccc2)CSSC[C@@H](C(=O)N(C)[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm000361p
CHEMBL385409 212349 0 None -3 4 Human 7.5 pKd = 7.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL407571 212669 0 None -4 4 Human 8.3 pKd = 8.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None CN[C@H](Cc1ccccc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000361p
CHEMBL438471 213773 0 None -6 4 Human 7.3 pKd = 7.3 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N(C)[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
9849682 94952 0 None -275422 10 Human 4.3 pKd = 4.3 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL254500 94952 0 None -275422 10 Human 4.3 pKd = 4.3 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL411017 212858 0 None -44 4 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
44447073 94550 0 None -17378 10 Human 5.2 pKd = 5.2 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL251835 94550 0 None -17378 10 Human 5.2 pKd = 5.2 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 534 2 1 6 3.8 CN1C[C@H](C(=O)N2CCN(c3ccc4nonc4c3)CC2)C[C@@H]2c3cccc4[nH]c(Br)c(c34)C[C@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL2370168 209807 0 None -18 5 Human 7.2 pKd = 7.2 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
44447077 94616 0 None -165 7 Human 4.2 pKd = 4.2 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL252231 94616 0 None -165 7 Human 4.2 pKd = 4.2 Binding
Binding affinity to human recombinant sst5 receptorBinding affinity to human recombinant sst5 receptor
ChEMBL 523 2 1 5 2.9 CN1C[C@@H](C(=O)N2CCN(c3cccc(=O)n3C)CC2)C[C@H]2c3cccc4[nH]c(Br)c(c34)C[C@@H]21 10.1016/j.bmcl.2007.12.030
CHEMBL421362 213274 0 None -14 5 Human 8.1 pKd = 8.1 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CCL-39 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
CHEMBL413830 213089 0 None -2 5 Human 7.1 pKd = 7.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)CSSC[C@@H](C(=O)N(C)[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm000361p
CHEMBL408752 212730 0 None -54 4 Human 8.1 pKd = 8.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL412466 212992 0 None -4 4 Human 8.1 pKd = 8.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N(C)[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL384164 212318 0 None -6 3 Human 7.1 pKd = 7.1 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
155544425 173382 0 None -436 5 Human 8.0 pKd = 8.0 Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
CHEMBL4527856 173382 0 None -436 5 Human 8.0 pKd = 8.0 Binding
Displacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR5 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL 1785 27 15 26 3.3 COc1cc2cc(c1Cl)N(C)C(=O)C[C@H](OC(=O)[C@H](C)N(C)C(=O)CCSSC[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc3ccccc3)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O)[C@@]1(C)O[C@H]1[C@H](C)[C@@H]1C[C@@](O)(NC(=O)O1)[C@H](OC)/C=C/C=C(\C)C2 10.1021/acs.jmedchem.8b02036
46880588 14217 0 None -125 7 Human 4.0 pKd = 4.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1076625 14217 0 None -125 7 Human 4.0 pKd = 4.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL1198974 14217 0 None -125 7 Human 4.0 pKd = 4.0 Binding
Binding affinity to human SST5 receptorBinding affinity to human SST5 receptor
ChEMBL 526 7 0 5 4.6 COc1ccc(C[C@@H](C)CN2C[C@H]3CCCC[C@H]3[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)C2)cn1 10.1016/j.bmcl.2010.01.063
CHEMBL437093 213705 0 None -1 5 Human 7.0 pKd = 7.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N(C)[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
CHEMBL386676 212386 0 None -2 4 Human 7.0 pKd = 7.0 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst5)
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@H](N)Cc2ccc(O)cc2)C(=O)N(C)[C@@H](Cc2ccccc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(N)=O 10.1021/jm000361p
91809292 125767 0 None -3 4 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1619 27 18 17 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647691 125767 0 None -3 4 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1619 27 18 17 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809287 160258 0 None -1 6 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL4110066 160258 0 None -1 6 Human 10.1 pKi = 10.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3349606 211435 0 None 3 4 Human 10.0 pKi = 10 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None CN(C)CCNC(=O)O[C@@H]1C[C@H]2C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(OCc4ccccc4)cc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N2C1 10.1021/jm021093t
2018 3007 28 None 6 4 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
9941444 3007 28 None 6 4 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349607 3007 28 None 6 4 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
DB06663 3007 28 None 6 4 Human 9.9 pKi = 9.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
16129706 209031 40 None -9 5 Human 9.9 pKi = 9.9 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00107-x
CHEMBL1823872 209031 40 None -9 5 Human 9.9 pKi = 9.9 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00107-x
16129706 209031 40 None -9 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 209031 40 None -9 5 Human 9.8 pKi = 9.8 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL3349521 211421 0 None -1 4 Human 9.8 pKi = 9.8 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
91809286 125763 0 None 1 6 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1489 23 16 15 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647687 125763 0 None 1 6 Human 9.8 pKi = 9.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1489 23 16 15 2.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3098601 211018 0 None 1 5 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1C/C=C\C[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
16129706 209031 40 None -9 5 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
CHEMBL1823872 209031 40 None -9 5 Human 9.6 pKi = 9.6 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
91809290 125765 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1636 27 18 16 3.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647689 125765 0 None -5 4 Human 9.6 pKi = 9.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1636 27 18 16 3.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3349605 211434 0 None 2 4 Human 9.6 pKi = 9.6 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
16129706 209031 40 None -9 5 Human 9.6 pKi = 9.6 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 209031 40 None -9 5 Human 9.6 pKi = 9.6 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL3349599 211428 0 None 2 5 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
91809296 125771 0 None -16 4 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1488 23 17 17 1.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647695 125771 0 None -16 4 Human 9.5 pKi = 9.5 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1488 23 17 17 1.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCS(=O)(=O)C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809291 125766 0 None -7 4 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1473 23 16 14 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647690 125766 0 None -7 4 Human 9.4 pKi = 9.4 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1473 23 16 14 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
11705763 168315 0 None 5 5 Human 9.4 pKi = 9.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL434159 168315 0 None 5 5 Human 9.4 pKi = 9.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 484 10 2 7 5.4 Cc1cccc2c(C(=O)CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
16129706 209031 40 None -9 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL1823872 209031 40 None -9 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL3349517 211418 0 None 1 4 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL3349602 211431 0 None 1 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
CHEMBL3349604 211433 0 None 15 5 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
CHEMBL442494 213913 0 None -1 5 Human 9.4 pKi = 9.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm0005048
16129706 209031 40 None -9 5 Human 9.4 pKi = 9.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 209031 40 None -9 5 Human 9.4 pKi = 9.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823873 209032 9 None -1 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2013.11.065
91809283 125760 0 None -6 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1456 23 17 16 2.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647684 125760 0 None -6 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1456 23 17 16 2.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809277 125754 0 None -1 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1457 23 16 14 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647678 125754 0 None -1 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1457 23 16 14 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
91809303 125778 0 None -1 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1659 28 18 16 3.8 CC(=O)N(CCC(=O)N[C@@H](CN[C@@H]1CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)Cc1ccc(O)cc1)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3647702 125778 0 None -1 6 Human 9.3 pKi = 9.3 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1659 28 18 16 3.8 CC(=O)N(CCC(=O)N[C@@H](CN[C@@H]1CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC1=O)Cc1ccc(O)cc1)C[C@@H]1C[C@@H]2c3cccc4[nH]cc(c34)C[C@H]2N(C)C1 nan
CHEMBL3349524 211423 0 None 1 4 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL3349603 211432 0 None 3 5 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCCCNC(=O)O[C@@H]1C[C@H]2C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H](Cc3c[nH]c4ccccc34)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc3ccc(OCc4ccccc4)cc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N2C1 10.1021/jm021093t
16129706 209031 40 None -9 5 Human 9.2 pKi = 9.2 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
CHEMBL1823872 209031 40 None -9 5 Human 9.2 pKi = 9.2 Binding
Binding affinity against human sst5 receptor at a dose of 10 uMBinding affinity against human sst5 receptor at a dose of 10 uM
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/j.bmcl.2005.05.061
91809288 125764 0 None -4 6 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647688 125764 0 None -4 6 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1472 23 17 16 1.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NCC[S@@+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3349516 211417 0 None -10 4 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
91809310 125785 0 None -3 4 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1618 27 19 17 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647709 125785 0 None -3 4 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1618 27 19 17 3.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809294 125769 0 None -10 4 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1912 34 19 19 3.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647693 125769 0 None -10 4 Human 9.1 pKi = 9.1 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1912 34 19 19 3.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)C[S+]([O-])C[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809275 125752 0 None -7 6 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1603 27 18 17 3.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647676 125752 0 None -7 6 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1603 27 18 17 3.6 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809301 125776 0 None -19 4 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1470 22 17 16 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647700 125776 0 None -19 4 Human 9.0 pKi = 9.0 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1470 22 17 16 2.4 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3349513 211414 0 None -1 4 Human 9.0 pKi = 9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC1=O 10.1021/jm021093t
CHEMBL3349522 211422 0 None -7 4 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)N[C@@H](C)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
91809319 126377 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1453 22 16 14 3.3 C[C@@H](O)C1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3650455 126377 0 None -1 3 Human 8.9 pKi = 8.9 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1453 22 16 14 3.3 C[C@@H](O)C1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL1794035 208937 0 None -5 5 Human 8.9 pKi = 8.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm0005048
16129706 209031 40 None -9 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards somatostatin receptor type 5Binding affinity towards somatostatin receptor type 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
CHEMBL1823872 209031 40 None -9 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards somatostatin receptor type 5Binding affinity towards somatostatin receptor type 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm050376t
91809284 125761 0 None -7 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1896 34 20 20 5.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
CHEMBL3647685 125761 0 None -7 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1896 34 20 20 5.5 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(O)cc2)NC1=O nan
91809285 125762 0 None -12 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1880 34 19 19 5.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647686 125762 0 None -12 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1880 34 19 19 5.8 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](CCCCNC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809308 125783 0 None -4 4 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1602 27 18 16 4.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647707 125783 0 None -4 4 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1602 27 18 16 4.2 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809276 125753 0 None -4 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1620 27 18 16 4.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
CHEMBL3647677 125753 0 None -4 6 Human 8.8 pKi = 8.8 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1620 27 18 16 4.3 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC[C@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccc(F)cc2)NC1=O nan
44397389 124044 0 None 1 5 Human 8.8 pKi = 8.8 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL363092 124044 0 None 1 5 Human 8.8 pKi = 8.8 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
44397620 67874 0 None 1 2 Human 8.0 pKi = 8 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 442 9 2 6 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL191025 67874 0 None 1 2 Human 8.0 pKi = 8 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 442 9 2 6 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL3349514 211415 0 None -5 4 Human 7.0 pKi = 7 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL3349525 211424 0 None 10 4 Human 7.0 pKi = 7 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL2370168 209807 0 None -18 5 Human 7.0 pKi = 7 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN(Cc2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
CHEMBL2369733 209661 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N(C)[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369756 209674 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)N(C)C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369759 209677 0 None -1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)C(N)CNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369760 209678 0 None -42 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@@H](N)CCNC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
155529288 171397 0 None -1 2 Human 5.0 pKi = 5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4462329 171397 0 None -1 2 Human 5.0 pKi = 5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1072 19 12 13 0.7 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL2369735 209663 0 None -18 5 Human 7.0 pKi = 7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2369751 209669 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H]1CSSC[C@H](N(C)C(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@H](C)O)C(=O)N1 10.1021/jm0005048
49862889 15163 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 497 7 1 4 5.9 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210031 15163 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 497 7 1 4 5.9 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2010.06.026
49862904 15165 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 463 9 1 7 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-n1ccnc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210083 15165 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 463 9 1 7 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-n1ccnc1 10.1016/j.bmcl.2010.06.026
13690207 115382 0 None -29 5 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1016/j.bmcl.2013.11.065
CHEMBL3350037 115382 0 None -29 5 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR5 expressed in CHO-K1 cells
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1016/j.bmcl.2013.11.065
CHEMBL429166 213509 0 None 1 4 Human 7.0 pKi = 7.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
44435539 166564 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 403 4 0 5 4.5 COc1cc(CN2CCC3(CC2)OC(=O)c2ccccc23)c(OC)c2ccccc12 10.1021/jm701144e
CHEMBL427975 166564 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 403 4 0 5 4.5 COc1cc(CN2CCC3(CC2)OC(=O)c2ccccc23)c(OC)c2ccccc12 10.1021/jm701144e
56651207 175897 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4586779 175897 0 None -1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 655 10 5 9 3.6 NC/C=C/CO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2/C=C/COC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
90665463 109262 0 None -4 5 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 882 28 3 9 4.5 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CCN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3218124 109262 0 None -4 5 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 882 28 3 9 4.5 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CCN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL2369754 209672 0 None -12 5 Human 7.0 pKi = 7.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
24740863 89158 0 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL236610 89158 0 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
24740863 89158 0 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1021/jm701143p
CHEMBL236610 89158 0 None -1 6 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl 10.1021/jm701143p
44385504 61048 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 489 7 4 3 6.4 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL176313 61048 0 None -2 5 Human 6.0 pKi = 6.0 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 489 7 4 3 6.4 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
44385712 60344 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL174490 60344 0 None -1 4 Human 5.9 pKi = 5.9 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 343 5 4 2 4.4 CC(=N)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
2051 3576 24 None -37 9 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
5311430 3576 24 None -37 9 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
CHEMBL311695 3576 24 None -37 9 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
44435540 97164 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 404 6 1 4 4.3 COc1cc(CN2CCC(NC(=O)c3ccccc3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
CHEMBL268075 97164 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 404 6 1 4 4.3 COc1cc(CN2CCC(NC(=O)c3ccccc3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
16129706 209031 40 None -9 5 Human 6.9 pKi = 6.9 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00051-8
CHEMBL1823872 209031 40 None -9 5 Human 6.9 pKi = 6.9 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1016/s0960-894x(01)00051-8
71458043 78903 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 494 10 3 5 4.3 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(Cc3ccccc3)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL2112934 78903 0 None -1 5 Human 5.9 pKi = 5.9 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 494 10 3 5 4.3 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(Cc3ccccc3)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
155528330 171340 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4461404 171340 0 None -1 2 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 513 11 5 7 2.5 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OCCCCN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
11848624 89146 0 None -2 6 Human 6.9 pKi = 6.9 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL236587 89146 0 None -2 6 Human 6.9 pKi = 6.9 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
11848624 89146 0 None -2 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL236587 89146 0 None -2 6 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
24740636 148097 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 524 8 1 6 6.5 COc1cc(CN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
CHEMBL393515 148097 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 524 8 1 6 6.5 COc1cc(CN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
11848679 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
CHEMBL236788 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
11848679 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1021/jm801205x
CHEMBL236788 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst5 receptor expressed in chinese hamster CCL39 cells
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1021/jm801205x
11848679 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1021/jm701143p
CHEMBL236788 89244 0 None 134 6 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N 10.1021/jm701143p
CHEMBL262017 210526 0 None -7 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards somatostatin receptor type 5Binding affinity towards somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CSSC[C@H](C(=O)N[C@H](C=O)[C@@H](C)O)NC1=O 10.1021/jm050376t
10580397 99315 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 677 20 3 7 6.9 NCCCCCNC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282129 99315 0 None -2 5 Human 5.9 pKi = 5.9 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 677 20 3 7 6.9 NCCCCCNC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
155546680 173565 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL4532486 173565 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
44397815 67757 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 469 10 1 5 6.3 CN(C)CCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL190786 67757 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 469 10 1 5 6.3 CN(C)CCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
90665462 109230 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL3217760 109230 0 None -4 4 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 867 27 3 9 4.1 COC(=O)CCN(Cc1ccccc1)C(=O)CCN(C[C@@H](C)O)C(=O)CCN(CCCCN)C(=O)CN(CCc1c[nH]c2ccccc12)C(=O)CCN(Cc1ccccc1)C(C)=O 10.1039/C2MD20265D
CHEMBL438726 213789 0 None -40 4 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2c(F)c(F)c(F)c(F)c2F)CSSC[C@H](C(=O)N[C@@H](Cc2c(F)c(F)c(F)c(F)c2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL439136 213827 0 None -4 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369749 209667 0 None -11 5 Human 6.9 pKi = 6.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL2372957 210323 0 None -7 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
CHEMBL408347 212707 0 None -11 4 Human 6.9 pKi = 6.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2372958 210324 0 None -3 3 Human 5.9 pKi = 5.9 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CS2=CCc3ccccc32)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
24740635 89889 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 467 6 2 4 6.1 Cc1cccc2c(CN3CCC(Nc4nc5ccccc5n4Cc4ccc(F)cc4)CC3)c[nH]c12 10.1021/jm701143p
CHEMBL237864 89889 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 467 6 2 4 6.1 Cc1cccc2c(CN3CCC(Nc4nc5ccccc5n4Cc4ccc(F)cc4)CC3)c[nH]c12 10.1021/jm701143p
24740640 89951 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 383 6 2 6 4.5 CCOc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1O 10.1021/jm701143p
CHEMBL238056 89951 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 383 6 2 6 4.5 CCOc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1O 10.1021/jm701143p
11963995 91865 0 None 15 3 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
CHEMBL241329 91865 0 None 15 3 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
CHEMBL2372956 210322 0 None -2 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(Cl)cc2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
46882832 5746 0 None 64 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC 10.1016/j.bmcl.2009.09.024
CHEMBL1078450 5746 0 None 64 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC 10.1016/j.bmcl.2009.09.024
CHEMBL438281 213763 0 None -8 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2F)CSSC[C@H](C(=O)N[C@@H](Cc2ccccc2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369734 209662 0 None -2 5 Human 6.8 pKi = 6.8 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)N(C)C1=O 10.1021/jm0005048
10094509 130686 0 None -44 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 435 7 4 3 5.5 COc1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL368334 130686 0 None -44 5 Human 5.8 pKi = 5.8 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 435 7 4 3 5.5 COc1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
15965425 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human somatostatin receptor type 5Binding affinity to human somatostatin receptor type 5
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
2046 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human somatostatin receptor type 5Binding affinity to human somatostatin receptor type 5
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
CHEMBL99895 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity to human somatostatin receptor type 5Binding affinity to human somatostatin receptor type 5
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/acs.jmedchem.6b01029
15965425 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Somatostatin receptor type 5 (hsst5)Binding affinity towards Somatostatin receptor type 5 (hsst5)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
2046 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Somatostatin receptor type 5 (hsst5)Binding affinity towards Somatostatin receptor type 5 (hsst5)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
CHEMBL99895 2206 7 None -16218 5 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Somatostatin receptor type 5 (hsst5)Binding affinity towards Somatostatin receptor type 5 (hsst5)
ChEMBL 645 11 5 7 4.3 NCCCC[C@@H](C(=O)OC(C)(C)C)NC(=O)[C@@H]([C@H](c1c[nH]c2c1cccc2)C)NC(=O)N1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1021/jm020424z
24740520 89242 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 456 6 1 5 5.2 Fc1ccc(Cn2c(NC3CCN(Cc4ccc5c(c4)CCO5)CC3)nc3ccccc32)cc1 10.1021/jm701143p
CHEMBL236786 89242 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 456 6 1 5 5.2 Fc1ccc(Cn2c(NC3CCN(Cc4ccc5c(c4)CCO5)CC3)nc3ccccc32)cc1 10.1021/jm701143p
24740295 145721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 464 7 2 7 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1Cl 10.1021/jm701143p
CHEMBL391637 145721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 464 7 2 7 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1Cl 10.1021/jm701143p
90665461 109261 0 None 2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 807 13 3 7 4.3 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218123 109261 0 None 2 5 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 807 13 3 7 4.3 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL407496 212665 0 None -5 5 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(F)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
46882227 6176 0 None 57 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1081133 6176 0 None 57 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL2369758 209676 0 None -6 5 Human 6.8 pKi = 6.8 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
11848626 5747 0 None 56 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
CHEMBL1078451 5747 0 None 56 4 Human 6.8 pKi = 6.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
24740639 146116 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 383 6 1 6 4.4 COc1ccc(CN2CCC(Nc3nc4ccccc4s3)CC2)cc1OC 10.1021/jm701143p
CHEMBL391950 146116 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 383 6 1 6 4.4 COc1ccc(CN2CCC(Nc3nc4ccccc4s3)CC2)cc1OC 10.1021/jm701143p
16062555 5956 0 None 562 4 Human 7.8 pKi = 7.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
CHEMBL1079874 5956 0 None 562 4 Human 7.8 pKi = 7.8 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
49862994 15188 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 430 9 2 6 3.5 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL1210268 15188 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 430 9 2 6 3.5 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
46911065 15189 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 401 6 1 4 4.2 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
CHEMBL1210269 15189 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 401 6 1 4 4.2 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
46882133 5808 0 None 5 7 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078896 5808 0 None 5 7 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
11848677 148352 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL393718 148352 0 None 1 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL414116 213111 0 None -9 4 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
44385757 61336 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 461 6 4 2 6.8 CC(C)(C)c1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL176730 61336 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 461 6 4 2 6.8 CC(C)(C)c1ccc(C(=N)N[C@H](Cc2c[nH]c3ccccc23)c2nc(-c3ccccc3)c[nH]2)cc1 10.1016/s0960-894x(01)00107-x
49862887 15161 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 368 6 2 5 2.8 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
CHEMBL1210029 15161 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 368 6 2 5 2.8 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
46882577 5857 1 None 51 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1079312 5857 1 None 51 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
24740862 148008 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
CHEMBL393436 148008 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
24740862 148008 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1021/jm701143p
CHEMBL393436 148008 0 None 4 5 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F 10.1021/jm701143p
46882578 5858 0 None 51 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1079313 5858 0 None 51 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
11848625 5792 0 None -2 6 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1078745 5792 0 None -2 6 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
44397706 67191 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL187768 67191 0 None -1 5 Human 8.7 pKi = 8.7 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 456 9 2 6 5.4 Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
44397835 67519 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL189554 67519 0 None 2 2 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
16129706 209031 40 None -9 5 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Somatostatin receptor type 5 (hsst5)Binding affinity towards Somatostatin receptor type 5 (hsst5)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL1823872 209031 40 None -9 5 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Somatostatin receptor type 5 (hsst5)Binding affinity towards Somatostatin receptor type 5 (hsst5)
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm020424z
CHEMBL408362 212710 0 None -58 5 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O 10.1021/jm980194h
91809306 125781 0 None -16 4 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1738 28 16 17 6.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647705 125781 0 None -16 4 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1738 28 16 17 6.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](N(CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
91809300 125775 0 None -30 4 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1454 22 16 15 2.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647699 125775 0 None -30 4 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1454 22 16 15 2.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccncc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
49862928 15169 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 557 10 1 6 6.1 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210141 15169 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 557 10 1 6 6.1 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.06.026
91809313 125788 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1616 26 18 16 3.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
CHEMBL3647712 125788 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.Radioligand Binding Assay: Membranes for in vitro receptor binding assays were obtained by the following procedures. CHO-K1 cells expressing one of the somatostatin receptors were homogenized in ice-cold buffer with 10 mM Tris-HCl, 5 mM EDTA, 3 mM EGTA, 1 mM phenylmethylsuphonyl fluoride, pH 7.6, using Polytron PT10-35GT (Kinematica) at 18,000 rpm for 30 seconds and centrifuged at 500xg for 10 minutes. The supernatant containing the plasma membranes was centrifuged at 100,000xg for 30 minutes and the pellet was resuspended in buffer containing 20 mM glycine-glycine, 1 mM MgCl2, 250 mM sucrose, pH 7.2, for storage at -80 C.For the SSTR1, 2 and 5 assays, membranes and various concentrations of test compounds were incubated in 96-well plates for 60 minutes at 25 C. with 0.05 nM [125I-Tyr11]-SRIF-14 (for hSSTR1; PerkinElmer Life Science), 0.05 nM [125I-Tyr]-seglitide (for hSSTR2; PerkinElmer Life Science) or 0.05 nM [125I-Tyr]-[DPhe-cyclo(Cys-Tyr-DTrp-Lys-Val-Cys)-Thr-NH2] (for hSSTR5.
ChEMBL 1616 26 18 16 3.7 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)CCCCNC(=O)[C@H](Cc2ccccc2)NC1=O nan
49862961 15181 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 506 10 2 6 5.1 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210209 15181 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 506 10 2 6 5.1 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
11963995 91865 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
CHEMBL241329 91865 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 387 6 1 4 3.8 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1021/jm701144e
44435541 154746 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 460 6 1 4 5.5 COc1cc(CN2CCC(NC(=O)c3ccc(C(C)(C)C)cc3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
CHEMBL400021 154746 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 460 6 1 4 5.5 COc1cc(CN2CCC(NC(=O)c3ccc(C(C)(C)C)cc3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
122181227 121846 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
CHEMBL3589942 121846 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
CHEMBL385745 212363 0 None -1 4 Human 6.7 pKi = 6.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
46882181 5681 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1077908 5681 0 None -1 5 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
49862886 15160 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 367 6 1 4 3.5 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
CHEMBL1210028 15160 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 367 6 1 4 3.5 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
90665460 109260 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 793 13 3 7 3.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218122 109260 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 793 13 3 7 3.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
44386389 130083 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 473 6 4 2 6.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL367699 130083 0 None -4 5 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 473 6 4 2 6.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00107-x
49862996 15191 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 429 8 1 5 4.1 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL1210271 15191 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 429 8 1 5 4.1 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
49863043 15196 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 381 6 1 4 3.9 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
CHEMBL1210374 15196 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 381 6 1 4 3.9 CCOc1cc(CN2CCC[C@@H](NC(=O)c3cncc(C)c3)CC2)ccc1C 10.1016/j.bmcl.2010.06.026
2070 697 5 None -3467 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
9802572 697 5 None -3467 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
CHEMBL2069499 697 5 None -3467 4 Human 5.7 pKi = 5.7 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
10210016 60435 0 None -11 3 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 441 6 4 2 5.7 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(F)cc1F 10.1016/s0960-894x(01)00107-x
CHEMBL175197 60435 0 None -11 3 Human 5.7 pKi = 5.7 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 441 6 4 2 5.7 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(F)cc1F 10.1016/s0960-894x(01)00107-x
CHEMBL2372962 210328 0 None -26 3 Human 5.7 pKi = 5.7 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2c[nH]c3ccccc23)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)CS1=CCCC1 10.1021/jm9806289
46882622 5762 0 None 44 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078528 5762 0 None 44 4 Human 6.7 pKi = 6.7 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
16062553 6065 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL1080586 6065 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
24740752 89147 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C 10.1016/j.bmcl.2009.09.024
CHEMBL236588 89147 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C 10.1016/j.bmcl.2009.09.024
24740752 89147 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C 10.1021/jm701143p
CHEMBL236588 89147 0 None 436 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C 10.1021/jm701143p
44377591 55633 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 536 9 3 6 5.6 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL162140 55633 0 None 1 4 Human 5.6 pKi = 5.6 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 536 9 3 6 5.6 CC(C)(C(=O)NCCc1c[nH]c2ccccc12)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
155549889 173907 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 358 7 4 5 1.6 NCCCCC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL4540289 173907 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 358 7 4 5 1.6 NCCCCC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1Cc1cccc2ccccc12 10.1016/j.ejmech.2018.11.030
44385652 60392 0 None -9 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 405 6 4 2 5.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccccc1 10.1016/s0960-894x(01)00107-x
CHEMBL174872 60392 0 None -9 5 Human 5.6 pKi = 5.6 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 405 6 4 2 5.5 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccccc1 10.1016/s0960-894x(01)00107-x
46882226 6148 0 None 41 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL1080951 6148 0 None 41 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL437220 213711 0 None -9 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
49863042 15195 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 415 8 1 5 3.7 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL1210373 15195 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 415 8 1 5 3.7 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL421362 213274 0 None -14 5 Human 7.6 pKi = 7.6 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
46882180 5841 0 None 5 6 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
CHEMBL1079180 5841 0 None 5 6 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F 10.1016/j.bmcl.2009.09.024
46882579 5859 0 None 39 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1079314 5859 0 None 39 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46882225 6147 0 None 39 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
CHEMBL1080950 6147 0 None 39 4 Human 6.6 pKi = 6.6 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
44397875 127061 0 None 16 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 419 10 2 5 5.1 CCc1ccc(-c2nnc(SCCc3c[nH]c4ccccc34)n2CCCCN)cc1 10.1016/j.bmcl.2005.05.061
CHEMBL365627 127061 0 None 16 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 419 10 2 5 5.1 CCc1ccc(-c2nnc(SCCc3c[nH]c4ccccc34)n2CCCCN)cc1 10.1016/j.bmcl.2005.05.061
CHEMBL2372964 210330 0 None -1 4 Human 6.6 pKi = 6.6 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(F)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
44397628 67388 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL188767 67388 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
90665459 109259 0 None -5 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218121 109259 0 None -5 3 Human 4.6 pKi = 4.6 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 646 11 3 6 2.9 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CCC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
44363816 39675 0 None -77 5 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)
ChEMBL 589 14 3 5 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL147499 39675 0 None -77 5 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)In vitro binding affinity was evaluated against human Somatostatin receptor type 5 (hSSTR-5)
ChEMBL 589 14 3 5 5.0 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N[C@H](CCCCN)C(=O)OC(C)(C)C)N1CCN(CCCc2ccccc2)C1=O 10.1016/s0960-894x(99)00016-5
44354398 115502 0 None -190 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 583 12 4 6 3.6 CC(C)C(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
CHEMBL335223 115502 0 None -190 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 583 12 4 6 3.6 CC(C)C(=O)N1CCC(C(=O)NC(C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C)[C@@H](C)c2c[nH]c3ccccc23)CC1 10.1016/s0960-894x(00)00687-9
CHEMBL415201 213180 0 None -8 4 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
24740753 146117 0 None 33 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL391951 146117 0 None 33 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
24740753 146117 0 None 33 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL391951 146117 0 None 33 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1021/jm701143p
16062816 6064 0 None 1479 5 Human 8.5 pKi = 8.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL1080585 6064 0 None 1479 5 Human 8.5 pKi = 8.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2009.09.024
CHEMBL3349601 211430 0 None -3 4 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O 10.1021/jm021093t
CHEMBL1201185 208601 28 None -7 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC1=O 10.1021/jm021093t
10325243 100495 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 549 17 1 7 5.3 CO[C@@H]1O[C@H](COCCCCCN)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29102 100495 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 549 17 1 7 5.3 CO[C@@H]1O[C@H](COCCCCCN)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL384607 212333 0 None -3 3 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(C#N)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(C#N)cc2)C(N)=O)NC1=O 10.1021/jm9806289
46882517 6215 0 None 32 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1081317 6215 0 None 32 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
11848833 5807 0 None 323 4 Human 7.5 pKi = 7.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1078895 5807 0 None 323 4 Human 7.5 pKi = 7.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 10.1016/j.bmcl.2009.09.024
CHEMBL2369757 209675 0 None -12 5 Human 6.5 pKi = 6.5 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2cccnc2)CSSC[C@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)NC1=O 10.1021/jm0005048
56651206 174631 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
CHEMBL4557933 174631 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 659 11 5 9 3.8 NCCCCO[C@@H]1[C@@H](NC(=O)Cc2c[nH]c3ccccc23)COC(=O)c2c(O)cccc2CCCOC[C@@H](OCc2ccccc2)[C@H]1O 10.1016/j.ejmech.2018.11.030
24740748 89952 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 397 7 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC 10.1021/jm701143p
CHEMBL238057 89952 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 397 7 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC 10.1021/jm701143p
46882831 5744 0 None 301 4 Human 7.5 pKi = 7.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
CHEMBL1078449 5744 0 None 301 4 Human 7.5 pKi = 7.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N 10.1016/j.bmcl.2009.09.024
CHEMBL2370167 209806 0 None -45 5 Human 7.5 pKi = 7.5 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)CN([C@H](C)c2ccccc2)C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
46882445 5811 0 None 30 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078903 5811 0 None 30 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
44309052 203947 0 None -165 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@H]1CCC[C@@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL69303 203947 0 None -165 5 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@H]1CCC[C@@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
44354415 116620 0 None -131 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL336819 116620 0 None -131 2 Human 6.5 pKi = 6.5 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 603 13 4 6 4.6 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(Cc2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
10699714 99417 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282803 99417 0 None -1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
155550820 174289 0 None 5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
CHEMBL4549840 174289 0 None 5 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 1275 22 16 18 -2.3 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@H](CO)C(C)C)NC(=O)[C@H](CC(=O)N[C@@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2NC(C)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1016/j.ejmech.2018.11.030
101884861 121844 0 None - 1 Human 4.5 pKi = 4.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 358 7 4 5 1.6 NCCCCC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
CHEMBL3589940 121844 0 None - 1 Human 4.5 pKi = 4.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 358 7 4 5 1.6 NCCCCC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
46882664 5717 0 None 2 5 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078240 5717 0 None 2 5 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46882620 5715 0 None 28 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078215 5715 0 None 28 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
46882621 5723 0 None 28 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078283 5723 0 None 28 4 Human 6.5 pKi = 6.5 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
10096510 57428 0 None 10 4 Human 6.4 pKi = 6.4 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL165402 57428 0 None 10 4 Human 6.4 pKi = 6.4 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 475 7 2 6 5.2 CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
46882516 6349 0 None 27 4 Human 6.4 pKi = 6.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1082040 6349 0 None 27 4 Human 6.4 pKi = 6.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
10411795 130619 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 457 6 4 2 5.9 O=C(Nc1ccc(F)cc1F)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL368176 130619 0 None -21 3 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 457 6 4 2 5.9 O=C(Nc1ccc(F)cc1F)N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1 10.1016/s0960-894x(01)00107-x
CHEMBL407195 212646 0 None -18 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
24740864 89159 0 None 269 4 Human 7.4 pKi = 7.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C 10.1016/j.bmcl.2009.09.024
CHEMBL236611 89159 0 None 269 4 Human 7.4 pKi = 7.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C 10.1016/j.bmcl.2009.09.024
24740864 89159 0 None 269 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C 10.1021/jm701143p
CHEMBL236611 89159 0 None 269 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C 10.1021/jm701143p
9852911 99383 0 None -24 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL282618 99383 0 None -24 6 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccc1 10.1021/jm9800346
11112736 16529 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1237140 16529 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL1788167 16529 0 None -3090 3 Human 5.4 pKi = 5.4 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-5) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
46882708 5803 0 None 26 4 Human 6.4 pKi = 6.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1078841 5803 0 None 26 4 Human 6.4 pKi = 6.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL385689 212359 0 None -5 4 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL408987 212740 0 None -2 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)CNC1=O 10.1021/jm9806289
CHEMBL421362 213274 0 None -14 5 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm021093t
10770814 100792 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL29311 100792 0 None -2 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 678 20 2 7 7.4 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
155553012 174086 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
CHEMBL4544582 174086 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 511 10 5 7 2.3 Cc1ccc(S[C@H]2O[C@H](CO)[C@@H](O)[C@H](OC/C=C/CN)[C@@H]2NC(=O)Cc2c[nH]c3ccccc23)cc1 10.1016/j.ejmech.2018.11.030
24740521 89243 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 453 6 2 4 5.8 Fc1ccc(Cn2c(NC3CCN(Cc4ccc5[nH]ccc5c4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
CHEMBL236787 89243 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 453 6 2 4 5.8 Fc1ccc(Cn2c(NC3CCN(Cc4ccc5[nH]ccc5c4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
24740519 154609 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 444 7 1 5 5.3 COc1ccc(CN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1021/jm701143p
CHEMBL399218 154609 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 444 7 1 5 5.3 COc1ccc(CN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 10.1021/jm701143p
49862905 15166 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 411 8 1 5 3.9 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1C 10.1016/j.bmcl.2010.06.026
CHEMBL1210084 15166 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 411 8 1 5 3.9 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1C 10.1016/j.bmcl.2010.06.026
49862906 15167 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 431 8 1 5 4.2 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2010.06.026
CHEMBL1210085 15167 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 431 8 1 5 4.2 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1Cl 10.1016/j.bmcl.2010.06.026
46911015 15179 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210207 15179 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 491 9 1 5 5.4 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
49862888 15162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.0 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210030 15162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 447 7 1 4 5.0 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)ccc1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
44435542 91864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 419 6 1 5 4.0 COc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
CHEMBL241328 91864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 419 6 1 5 4.0 COc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)c(OC)c2ccccc12 10.1021/jm701144e
CHEMBL2369750 209668 0 None -1 5 Human 7.4 pKi = 7.4 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None CN[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@@H]([C@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm0005048
10554930 100192 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 562 17 3 7 4.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL28824 100192 0 None -1 5 Human 5.4 pKi = 5.4 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 562 17 3 7 4.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
2247 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2009.09.024
249 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2009.09.024
2603 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2009.09.024
CHEMBL296419 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2009.09.024
DB00637 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1016/j.bmcl.2009.09.024
2247 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm701143p
249 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm701143p
2603 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm701143p
CHEMBL296419 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm701143p
DB00637 505 81 None -85 42 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1021/jm701143p
44397990 68014 0 None -2 2 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2ccccc12 10.1016/j.bmcl.2005.05.061
CHEMBL191255 68014 0 None -2 2 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 441 9 2 5 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2ccccc12 10.1016/j.bmcl.2005.05.061
155541897 173055 0 None 5 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
CHEMBL4519358 173055 0 None 5 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 583 7 3 9 3.7 CC(C)CCO[C@@H]1[C@@H](O)[C@@H](O)[C@H]2Cn3cc(nn3)COCCCCCCN(CCc3c[nH]c4ccccc34)CC[C@H]1O2 10.1016/j.ejmech.2018.11.030
9851998 24585 0 None -831 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(C(=O)c2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
CHEMBL134280 24585 0 None -831 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to hsst5 was determinedBinding affinity to hsst5 was determined
ChEMBL 617 12 4 6 4.3 C[C@@H](c1c[nH]c2ccccc12)C(NC(=O)C1CCN(C(=O)c2ccccc2)CC1)C(=O)N[C@@H](CCCCN)C(=O)OC(C)(C)C 10.1016/s0960-894x(00)00687-9
10248767 57192 0 None 5 4 Human 6.4 pKi = 6.4 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL164964 57192 0 None 5 4 Human 6.4 pKi = 6.4 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 373 6 1 6 3.9 NCCCc1nc(-c2cccc([N+](=O)[O-])c2)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
49862903 15164 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 404 6 2 5 3.1 CCOc1cc(CN2CCCC(NC(=O)c3ccc(N)nc3)CC2)cc(F)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL1210082 15164 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 404 6 2 5 3.1 CCOc1cc(CN2CCCC(NC(=O)c3ccc(N)nc3)CC2)cc(F)c1F 10.1016/j.bmcl.2010.06.026
44308969 204364 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@@H]1CCC[C@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL71723 204364 0 None -2818 5 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NC[C@@H]1CCC[C@H](CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL2371893 210147 0 None -4 5 Human 7.3 pKi = 7.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(C(F)(F)F)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL408787 212732 0 None -28 3 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)C(c2ccccc2)c2ccccc2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)C(c2ccccc2)c2ccccc2)NC1=O 10.1021/jm9806289
CHEMBL413709 213083 0 None -2 3 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)c(I)c2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2372959 210325 0 None -1 5 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H](N)C2Cc3ccccc3C2)CSSC[C@@H](C(=O)N[C@H](C(N)=O)C2Cc3ccccc3C2)NC1=O 10.1021/jm9806289
46882746 5637 0 None 21 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1077742 5637 0 None 21 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL510755 215588 0 None -1 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned sst5 receptorBinding affinity to human cloned sst5 receptor
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL2311098 209505 0 None -4 5 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL264028 210603 0 None -2 5 Human 7.3 pKi = 7.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(I)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(I)cc2)C(N)=O)NC1=O 10.1021/jm9806289
24740861 5678 0 None 20 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF 10.1016/j.bmcl.2009.09.024
CHEMBL1077877 5678 0 None 20 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF 10.1016/j.bmcl.2009.09.024
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None None 10.1021/jm021093t
13690207 115382 0 None -29 5 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm021093t
CHEMBL3350037 115382 0 None -29 5 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm021093t
49862960 15180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 473 9 1 5 5.2 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccccc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210208 15180 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 473 9 1 5 5.2 CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccccc1 10.1016/j.bmcl.2010.06.026
CHEMBL2369755 209673 0 None 2 5 Human 8.2 pKi = 8.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)N(C)C(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
CHEMBL446077 213943 0 None -9 3 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned sst5 receptorBinding affinity to human cloned sst5 receptor
ChEMBL None None None CNCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC(=O)[C@H]([C@@H](C)O)NC1=O 10.1021/jm701618q
51003591 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human SSTR5Binding affinity to human SSTR5
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2010.11.088
CHEMBL1643110 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to human SSTR5Binding affinity to human SSTR5
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.bmcl.2010.11.088
12891521 198685 1 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 428 7 1 4 5.3 Fc1ccc(Cn2c(NC3CCN(CCc4ccccc4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
CHEMBL58025 198685 1 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 428 7 1 4 5.3 Fc1ccc(Cn2c(NC3CCN(CCc4ccccc4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
51003591 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL1643110 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
51003591 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
CHEMBL1643110 56755 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 661 19 2 6 7.3 NCCCCCOC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
44308836 102791 0 None -1258 5 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NCC1CCCC(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
CHEMBL305279 102791 0 None -1258 5 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human sst5 receptor expressed in CHO-K1 cellsBinding affinity towards human sst5 receptor expressed in CHO-K1 cells
ChEMBL 539 7 4 3 4.7 NCC1CCCC(CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)N2CCC3(C=Cc4ccccc43)CC2)C1 10.1021/jm980194h
44397747 67131 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 469 9 2 5 5.3 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc(Br)c1 10.1016/j.bmcl.2005.05.061
CHEMBL187498 67131 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 469 9 2 5 5.3 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc(Br)c1 10.1016/j.bmcl.2005.05.061
9985523 99161 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL281200 99161 0 None -3 5 Human 5.3 pKi = 5.3 Binding
Binding affinity for human receptor subtype hSSTR5.Binding affinity for human receptor subtype hSSTR5.
ChEMBL 572 17 2 6 6.2 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)C[C@@H]1OCc1ccccc1 10.1021/jm9800346
155565048 175501 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2cccc3ccccc23)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1016/j.ejmech.2018.11.030
CHEMBL4577766 175501 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR5 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2cccc3ccccc23)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1016/j.ejmech.2018.11.030
24740638 89891 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 369 5 2 6 4.1 COc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1O 10.1021/jm701143p
CHEMBL237866 89891 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 369 5 2 6 4.1 COc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)ccc1O 10.1021/jm701143p
46882182 5921 0 None 95 5 Human 7.3 pKi = 7.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 10.1016/j.bmcl.2009.09.024
CHEMBL1079686 5921 0 None 95 5 Human 7.3 pKi = 7.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 10.1016/j.bmcl.2009.09.024
CHEMBL2372961 210327 0 None -43 4 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
46882789 5679 0 None 19 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F 10.1016/j.bmcl.2009.09.024
CHEMBL1077887 5679 0 None 19 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F 10.1016/j.bmcl.2009.09.024
24740865 89160 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 435 7 1 6 5.2 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC(F)(F)F 10.1021/jm701143p
CHEMBL236612 89160 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 435 7 1 6 5.2 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC(F)(F)F 10.1021/jm701143p
CHEMBL414386 213129 0 None -6 4 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
11848677 148352 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL393718 148352 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL2372963 210329 0 None -20 3 Human 6.3 pKi = 6.3 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(F)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
46882790 5702 0 None 18 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 10.1016/j.bmcl.2009.09.024
CHEMBL1078081 5702 0 None 18 4 Human 6.3 pKi = 6.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 10.1016/j.bmcl.2009.09.024
44377623 119916 0 None 16 2 Human 6.3 pKi = 6.3 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 449 9 2 6 4.7 CCCCNC(=O)C(C)(C)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
CHEMBL349355 119916 0 None 16 2 Human 6.3 pKi = 6.3 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 449 9 2 6 4.7 CCCCNC(=O)C(C)(C)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 10.1016/s0960-894x(01)00051-8
46882224 6348 0 None 181 5 Human 7.3 pKi = 7.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
CHEMBL1082036 6348 0 None 181 5 Human 7.3 pKi = 7.3 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 10.1016/j.bmcl.2009.09.024
44397385 67313 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 443 9 2 7 4.4 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cnc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL188402 67313 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 443 9 2 7 4.4 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cnc2ccccc2n1 10.1016/j.bmcl.2005.05.061
44397907 67964 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 447 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cc2ccccc2s1 10.1016/j.bmcl.2005.05.061
CHEMBL191171 67964 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 447 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cc2ccccc2s1 10.1016/j.bmcl.2005.05.061
49862930 15171 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 458 10 2 6 4.2 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC(C)C)nc3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL1210143 15171 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 458 10 2 6 4.2 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC(C)C)nc3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2010.06.026
CHEMBL3349518 211419 0 None -10 4 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](C)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
49862962 15183 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 554 10 2 6 5.8 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)cc(OCc2ccccc2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210210 15183 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 554 10 2 6 5.8 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)cc(OCc2ccccc2)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
13690207 115382 0 None -29 5 Human 8.2 pKi = 8.2 Binding
Binding affinity towards somatostatin receptor type 5Binding affinity towards somatostatin receptor type 5
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm050376t
CHEMBL3350037 115382 0 None -29 5 Human 8.2 pKi = 8.2 Binding
Binding affinity towards somatostatin receptor type 5Binding affinity towards somatostatin receptor type 5
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1021/jm050376t
49862931 15172 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 488 10 2 6 5.0 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1-c1ccccc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210144 15172 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 488 10 2 6 5.0 CCOc1cc(CN2CCC(NC(=O)c3ccc(NC)nc3)CC2)cc(OCC)c1-c1ccccc1 10.1016/j.bmcl.2010.06.026
15952316 91866 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 450 7 1 5 3.5 CCOc1cc(CN2CCC(NC(=O)c3cccc(S(C)(=O)=O)c3)CC2)ccc1Cl 10.1021/jm701144e
CHEMBL241330 91866 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST5RBinding affinity to human SST5R
ChEMBL 450 7 1 5 3.5 CCOc1cc(CN2CCC(NC(=O)c3cccc(S(C)(=O)=O)c3)CC2)ccc1Cl 10.1021/jm701144e
44377555 57531 0 None 2 5 Human 6.2 pKi = 6.2 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 57531 0 None 2 5 Human 6.2 pKi = 6.2 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
24740518 89241 1 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 414 6 1 4 5.3 Fc1ccc(Cn2c(NC3CCN(Cc4ccccc4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
CHEMBL236785 89241 1 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 414 6 1 4 5.3 Fc1ccc(Cn2c(NC3CCN(Cc4ccccc4)CC3)nc3ccccc32)cc1 10.1021/jm701143p
CHEMBL2372960 210326 0 None -18 4 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O)C1CCCS1 10.1021/jm9806289
46882665 5632 0 None 15 4 Human 6.2 pKi = 6.2 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1077721 5632 0 None 15 4 Human 6.2 pKi = 6.2 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
49862995 15190 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 401 6 1 4 4.2 CCOc1cc(CN2CCC[C@H](NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
CHEMBL1210270 15190 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 401 6 1 4 4.2 CCOc1cc(CN2CCC[C@H](NC(=O)c3cncc(C)c3)CC2)ccc1Cl 10.1016/j.bmcl.2010.06.026
44397788 67390 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 430 9 3 5 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2cc[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL188777 67390 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 430 9 3 5 5.0 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1cccc2cc[nH]c12 10.1016/j.bmcl.2005.05.061
142471936 191495 0 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5193727 191495 0 None -9332 5 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
24740750 89707 0 None 151 4 Human 7.2 pKi = 7.2 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O 10.1016/j.bmcl.2009.09.024
CHEMBL237660 89707 0 None 151 4 Human 7.2 pKi = 7.2 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O 10.1016/j.bmcl.2009.09.024
24740750 89707 0 None 151 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O 10.1021/jm701143p
CHEMBL237660 89707 0 None 151 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O 10.1021/jm701143p
44397834 166124 0 None 9 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 427 8 2 5 5.3 NCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL426072 166124 0 None 9 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 427 8 2 5 5.3 NCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL437448 213719 0 None -4 5 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Br)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc(Br)cc2)C(N)=O)NC1=O 10.1021/jm9806289
13690207 115382 0 None -29 5 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1039/C2MD20265D
CHEMBL3350037 115382 0 None -29 5 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 1018 17 13 14 -0.8 C[C@@H](O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](N)Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1 10.1039/C2MD20265D
24740637 89890 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 433 6 1 6 5.5 COc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
CHEMBL237865 89890 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 433 6 1 6 5.5 COc1cc(CN2CCC(Nc3nc4ccccc4s3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
CHEMBL264539 210628 0 None 1 3 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC[C@H](C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(-c3ccccc3)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc(-c3ccccc3)cc2)C(N)=O)NC1=O 10.1021/jm9806289
10166743 123946 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 439 6 4 2 6.1 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL362859 123946 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
ChEMBL 439 6 4 2 6.1 N=C(N[C@H](Cc1c[nH]c2ccccc12)c1nc(-c2ccccc2)c[nH]1)c1ccc(Cl)cc1 10.1016/s0960-894x(01)00107-x
CHEMBL412561 213004 0 None -6 3 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@H](N)Cc2ccc(F)cc2)CSSC[C@H](C(=O)N[C@H](Cc2ccc(F)cc2)C(N)=O)NC1=O 10.1021/jm9806289
49862929 15170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 492 9 2 6 4.7 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210142 15170 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 492 9 2 6 4.7 CCOc1cc(CN2CCC(NC(=O)c3ccc(N)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
44397472 125054 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2cc(F)ccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL364418 125054 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 460 9 2 6 5.2 NCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2cc(F)ccc2n1 10.1016/j.bmcl.2005.05.061
49862959 15178 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 511 9 1 5 5.7 CCOc1cc(CN2CCC(NC(=O)c3ccc(Cl)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210206 15178 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 511 9 1 5 5.7 CCOc1cc(CN2CCC(NC(=O)c3ccc(Cl)nc3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
44397725 124354 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 455 10 2 5 6.0 NCCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL363712 124354 0 None 8 2 Human 7.2 pKi = 7.2 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 455 10 2 5 6.0 NCCCCCn1c(SCCc2c[nH]c3ccccc23)nnc1-c1ccc2ccccc2c1 10.1016/j.bmcl.2005.05.061
CHEMBL385746 212364 0 None -4 4 Human 7.2 pKi = 7.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2311098 209505 0 None -4 5 Human 7.2 pKi = 7.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
46882666 5633 0 None 13 4 Human 6.1 pKi = 6.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL1077722 5633 0 None 13 4 Human 6.1 pKi = 6.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC 10.1016/j.bmcl.2009.09.024
CHEMBL412859 213032 0 None -19 3 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@H](C(N)=O)C(c2ccccc2)c2ccccc2)NC1=O 10.1021/jm9806289
CHEMBL411556 212886 0 None -12 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2cccc(F)c2)CSSC[C@@H](C(=O)N[C@@H](Cc2cccc(F)c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL406152 212596 0 None -9 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2cccc(F)c2)CSSC[C@H](C(=O)N[C@@H](Cc2cccc(F)c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369761 209679 0 None -6 5 Human 6.1 pKi = 6.1 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None CNC(=O)[C@@H](NC(=O)[C@@H]1CSSC[C@@H](N(C)C(=O)C(N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]([C@H](C)O)C(=O)N1)C(c1ccccc1)c1ccccc1 10.1021/jm0005048
122181226 121845 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2ccc3ccccc3c2)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1039/C4MD00074A
CHEMBL3589941 121845 0 None -1 2 Human 5.1 pKi = 5.1 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR5
ChEMBL 484 10 1 8 3.3 CC(=O)O[C@H]1CN(Cc2ccc3ccccc3c2)[C@H](CCCCCN)[C@@H](OC(C)=O)[C@@H]1OC(C)=O 10.1039/C4MD00074A
CHEMBL3349515 211416 0 None 12 4 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
CHEMBL3349520 211420 0 None -3 4 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cellBinding affinity towards human Somatostatin receptor type 5 (sst5) using Tyr11-[125I]-SRIF as radioligand was determined in COS cell
ChEMBL None None None C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm021093t
71461645 78904 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL2112935 78904 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Inhibitory constant on human somatostatin receptor 5Inhibitory constant on human somatostatin receptor 5
ChEMBL 367 5 2 4 4.4 NCCCc1nc(-c2c[nH]c3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
24740749 89953 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 417 6 1 6 5.1 COc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
CHEMBL238058 89953 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 417 6 1 6 5.1 COc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)c(OC)c2ccccc12 10.1021/jm701143p
11848835 6063 0 None 1258 4 Human 8.1 pKi = 8.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
CHEMBL1080584 6063 0 None 1258 4 Human 8.1 pKi = 8.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F 10.1016/j.bmcl.2009.09.024
44397648 66764 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL185861 66764 0 None -2 5 Human 8.1 pKi = 8.1 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 476 9 2 6 5.7 NCCCCn1c(SCCc2c[nH]c3c(Cl)cccc23)nnc1-c1ccc2ccccc2n1 10.1016/j.bmcl.2005.05.061
CHEMBL406738 212618 0 None -10 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)CC[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
24740751 147881 0 None 120 4 Human 7.1 pKi = 7.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 10.1016/j.bmcl.2009.09.024
CHEMBL393333 147881 0 None 120 4 Human 7.1 pKi = 7.1 Binding
Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayDisplacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay
ChEMBL 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 10.1016/j.bmcl.2009.09.024
24740751 147881 0 None 120 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 10.1021/jm701143p
CHEMBL393333 147881 0 None 120 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
ChEMBL 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 10.1021/jm701143p
CHEMBL275806 210823 0 None -5 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(=O)O)NC1=O 10.1021/jm9806289
CHEMBL2370166 209805 0 None -7 5 Human 7.1 pKi = 7.1 Binding
In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human Somatostatin receptor type 5 expressed in CHO-K1 cells.
ChEMBL None None None C[C@@H](c1ccccc1)N1CC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C1=O 10.1021/jm970393l
CHEMBL439005 213817 0 None -1 4 Human 7.1 pKi = 7.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369753 209671 0 None 3 5 Human 7.1 pKi = 7.1 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@@H]1C(=O)N[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)C(=O)N[C@@H](Cc2cccnc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCCN)C(=O)N1C 10.1021/jm0005048
49863044 15197 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 505 9 1 5 5.8 CCOc1cc(CN2CCCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
CHEMBL1210375 15197 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cellsDisplacement of radio labeled 11 Tyr SST14 from human SST5 receptor expressed in CHO cells
ChEMBL 505 9 1 5 5.8 CCOc1cc(CN2CCCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 10.1016/j.bmcl.2010.06.026
44397924 67586 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 512 10 2 7 6.0 Cc1cccc2c(C(=O)C(C)(C)CSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL190070 67586 0 None 2 2 Human 8.0 pKi = 8.0 Binding
Inhibitory constant against human sst5 receptor at a dose of 10 uMInhibitory constant against human sst5 receptor at a dose of 10 uM
ChEMBL 512 10 2 7 6.0 Cc1cccc2c(C(=O)C(C)(C)CSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 10.1016/j.bmcl.2005.05.061
CHEMBL437057 213703 0 None -5 3 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2c(F)c(F)c(F)c(F)c2F)CSSC[C@H](C(=O)N[C@@H](Cc2c(F)c(F)c(F)c(F)c2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL414598 213146 0 None -13 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2c(F)c(F)c(F)c(F)c2F)CSSC[C@@H](C(=O)N[C@@H](Cc2c(F)c(F)c(F)c(F)c2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL2369752 209670 0 None -1 5 Human 7.0 pKi = 7.0 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 receptor expressed on CHO cells
ChEMBL None None None C[C@H](O)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)N(C)C(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(Cl)cc2)CSSC[C@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm0005048
142471832 190275 0 None -13182 5 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175637 190275 0 None -13182 5 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from SST5 receptor (unknown origin) expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
90665458 109258 0 None 1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL3218120 109258 0 None 1 3 Human 5.0 pKi = 5.0 Binding
Displacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst5 receptor after 2 hrs by beta scintillation counting analysis
ChEMBL 632 11 3 6 2.5 C[C@@H](O)CN1CCC(=O)N(Cc2ccccc2)CCC(=O)N(CCc2c[nH]c3ccccc23)CC(=O)N(CCCCN)CCC1=O 10.1039/C2MD20265D
CHEMBL413171 213051 0 None -8 5 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2c(F)c(F)c(F)c(F)c2F)CSSC[C@H](C(=O)N[C@@H](Cc2c(F)c(F)c(F)c(F)c2F)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL410181 212805 0 None -3 5 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(=O)N[C@@H](Cc2ccc3ccccc3c2)C(N)=O)NC1=O 10.1021/jm9806289
CHEMBL406491 212611 0 None -26 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 5The compound was tested for binding affinity against human Somatostatin receptor type 5
ChEMBL None None None CC(C)[C@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2F)CSSC[C@@H](C(=O)N[C@@H](Cc2ccccc2F)C(N)=O)NC1=O 10.1021/jm9806289
2047 2215 0 None -5 4 Rat 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2036 643 0 None 1 5 Mouse 7.7 pKd = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
13105142 216098 0 125I-CGP23996 -4 5 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
13105142 216098 0 125I-Tyr3-octreotide -4 5 Human 10.2 pKi = 10.2 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
16161315 216096 0 125I-Tyr11-SRIF-14 -4 12 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr3-octreotide -4 12 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-CGP23996 -4 12 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr11-somatostatin-14 -4 12 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 UNDEFINED -4 12 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SRIF28 -4 12 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr11-SRIF -4 12 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SRIF28 -4 12 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr11-SRIF -4 12 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr3-octreotide -32 14 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216346 0 125I-Tyr11-somatostatin-14 4 8 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
None 216346 0 UNDEFINED 4 8 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
16161315 216096 0 125I-SRIF-28 -4 12 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-SOMATOSTATIN 14 -4 12 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-SRIF -4 12 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
None 216350 0 125I-LTT-SST-28 4 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
None 216350 0 UNDEFINED 4 5 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
2031 2273 0 UNDEFINED -2 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 2273 0 UNDEFINED -2 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 2273 0 UNDEFINED -2 9 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-LTT-SST-28 -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 UNDEFINED -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SST-28 -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 UNDEFINED -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SST-28 -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 UNDEFINED -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SST-28 -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 UNDEFINED -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SST-28 -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 UNDEFINED -15 11 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 216098 0 125I-Tyr10-CST14 -4 5 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2054 3974 15 125I-Tyr3-octreotide -15 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr3-octreotide -15 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr3-octreotide -15 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr3-octreotide -15 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr3-octreotide -15 11 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-somatostatin-14 -4 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SST-28 -4 12 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr10-CST14 -4 12 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-Tyr10-CST14 -4 12 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 -32 14 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -32 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-CGP23996 -4 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
None 216350 0 Functional 4 5 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 536 11 4 5 5.2 CC(COC(=O)C(CCCCN)NC(=O)CC1=C(NC2=C1C=CC3=CC=CC=C32)C4=CC5=CC=CC=C5C=C4)N None
16161315 216096 0 125I-SOMATOSTATIN -4 12 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2054 3974 15 125I-LTT-SST-28 -15 11 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SST-28 -15 11 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SST-28 -15 11 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SST-28 -15 11 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SST-28 -15 11 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-CGP23996 -15 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-CGP23996 -15 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-CGP23996 -15 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-CGP23996 -15 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-CGP23996 -15 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 216098 0 125I-LTT-SRIF28 -4 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
2055 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 -32 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-CGP23996 -123 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216348 0 125I-LTT-SST-28 -91 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
None 216097 0 125I-SRIF-28 -123 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-SRIF -123 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216348 0 125I-LTT-SST-28 -91 5 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
None 216348 0 UNDEFINED -91 5 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 584 17 5 8 2.8 CCCCC(C(=O)NC(CCCCN)C(=O)OC)NC(=O)NC(CC1=CC=CC=C1)C(=O)NC2=CC=C(C=C2)[N+](=O)[O-] None
2055 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -32 14 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -32 14 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-SOMATOSTATIN -123 11 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-LTT-SST-28 -123 11 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
13105142 216098 0 125I-LTT-SRIF28 -4 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
13105142 216098 0 UNDEFINED -4 5 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 808 11 8 8 2.0 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O None
None 216346 0 125I-SOMATOSTATIN 4 8 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1077 14 12 13 0.6 CC(C1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)N)C(=O)N)CC6=CC=CC=C6)O None
16161315 216096 0 125I-LTT-SST-28 -4 12 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SST-28 -4 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
16161315 216096 0 125I-LTT-SST-28 -4 12 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
None 216495 0 125I-LTT-SST-28 -3981 5 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-LTT-SST-28 -123 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
None 216097 0 125I-Tyr11-SRIF -123 11 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
2054 3974 15 125I-LTT-SRIF28 -15 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SRIF28 -15 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SRIF28 -15 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SRIF28 -15 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SRIF28 -15 11 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216349 0 125I-LTT-SST-28 -10471 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
None 216349 0 UNDEFINED -10471 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 485 11 4 4 3.1 COC(=O)C(CCCN=C(N)N)NC(=O)CCCC1=C(NC2=C(C=C(C=C12)F)F)C3=CC=CC=C3 None
None 216347 0 125I-LTT-SST-28 -85113 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 585 8 5 5 4.2 CC(C1=CNC2=CC=CC=C21)C(C(=O)NCC3CCCC(C3)CN)NC(=O)N4CCC(CC4)N5C6=CC=CC=C6NC5=O None
None 216347 0 UNDEFINED -85113 5 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 585 8 5 5 4.2 CC(C1=CNC2=CC=CC=C21)C(C(=O)NCC3CCCC(C3)CN)NC(=O)N4CCC(CC4)N5C6=CC=CC=C6NC5=O None
2055 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr10-CST14 -32 14 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN 14 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-SRIF -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-SRIF-28 -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF-28 -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF-28 -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF-28 -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF-28 -15 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-LTT-SST-28 -123 11 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 868 11 9 9 2.1 CC1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1C)CC2=CC=CC=C2)C(C)C)CCCCN)CC3=CNC4=CC=CC=C43)CC5=CC=C(C=C5)O.CC(=O)O None
1599 2341 50 None -6 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
3955 2341 50 None -6 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
7215 2341 50 None -6 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
CHEMBL841 2341 50 None -6 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
DB00836 2341 50 None -6 16 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 None
2247 505 81 None -85 42 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 None -85 42 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 None -85 42 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 None -85 42 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 None -85 42 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsDisplacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2055 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 UNDEFINED -32 14 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-Tyr10-CST14 -15 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr10-CST14 -15 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr10-CST14 -15 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr10-CST14 -15 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr10-CST14 -15 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SRIF28 -32 14 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-somatostatin-14 -32 14 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-SOMATOSTATIN -15 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SOMATOSTATIN -15 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SOMATOSTATIN -15 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SOMATOSTATIN -15 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SOMATOSTATIN -15 11 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase None None None None None
154734381 217714 0 None -1 8 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 1095 17 13 14 0.8 CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)NC(=O)[C@@H](N)CC1=CC=C2C=CC=CC2=C1 None
16161315 216096 0 None -4 12 Human 8.0 pKi = 8.0 Binding
Inhibition of human sst5 receptor expressed in CHO cellsInhibition of human sst5 receptor expressed in CHO cells
Drug Central 1637 26 22 23 -4.9 C[C@@H](C(=O)NCC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)CCCCN)CC(=O)N)CC2=CC=CC=C2)CC3=CC=CC=C3)CC4=CNC5=CC=CC=C54)CCCCN)C(C)O)CC6=CC=CC=C6)C(C)O)CO)C(=O)O)N None
2055 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
383414 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
90488715 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
CHEMBL1680 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
CHEMBL262746 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
DB00104 2907 48 None -12 14 Mouse 8.0 pKi = 8 Binding
NoneNone
Drug Central None None None None None
2036 643 0 None -25 5 Rat 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2066 3166 0 None -39 4 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10354394
2034 639 0 None -19 4 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2065 234 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9804621
2029 2375 0 None -35 6 Mouse 6.7 pKi = 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2028 1506 0 None -28 6 Mouse 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2051 3576 24 None -416 9 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311430 3576 24 None -416 9 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL311695 3576 24 None -416 9 Rat 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2028 1506 0 None -19 6 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2014 2214 0 None -19 9 Rat 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2067 3167 0 None -1 3 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10354394
2034 639 0 None -1 4 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2051 3576 24 None -131 9 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
5311430 3576 24 None -131 9 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
CHEMBL311695 3576 24 None -131 9 Mouse 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2031 2273 0 None -42 9 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71349 2273 0 None -42 9 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB06791 2273 0 None -42 9 Rat 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16130961 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16130961 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2005 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 891 0 None -25 6 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2032 637 0 None -39 7 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2055 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
383414 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
90488715 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL1680 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL262746 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB00104 2907 48 None -48 14 Rat 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2036 643 0 None -1 5 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
2084 653 0 None -39 2 Rat 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2029 2375 0 None -1 6 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2014 2214 0 None -2 9 Mouse 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2054 3974 15 None -21 11 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71306 3974 15 None -21 11 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL264186 3974 15 None -21 11 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL3349523 3974 15 None -21 11 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB04894 3974 15 None -21 11 Rat 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2054 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
71306 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL264186 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL3349523 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB04894 3974 15 None -15 11 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2047 2215 0 None -1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2047 2215 0 None -1 4 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2031 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
71349 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB06791 2273 0 None -2 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2051 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
5311430 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL311695 3576 24 None -37 9 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3675 0 None -33 10 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
44386062 3675 0 None -33 10 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
CHEMBL440072 3675 0 None -33 10 Mouse 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2019 3675 0 None -33 10 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3675 0 None -33 10 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3675 0 None -33 10 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16130961 891 0 None -3 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2005 891 0 None -3 6 Mouse 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2004 642 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2004 642 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2004 642 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2004 642 0 None -3 7 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2083 651 0 None -1 2 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311026 651 0 None -1 2 Rat 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2004 642 0 None -2 7 Rat 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2038 646 0 None -3 2 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2083 651 0 None 1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
5311026 651 0 None 1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2055 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
383414 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
90488715 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
CHEMBL1680 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
CHEMBL262746 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
DB00104 2907 48 None -12 14 Mouse 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2003 641 0 None 10 2 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2032 637 0 None -3 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2032 637 0 None -3 7 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3676 12 None -7 9 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3676 12 None -7 9 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3676 12 None -7 9 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3676 12 None -7 9 Rat 9.0 pKi = 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2007 1170 0 None -2 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 1170 0 None -2 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 1170 0 None -2 6 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2007 1170 0 None -2 6 Mouse 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
10116 3451 0 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 4 4.5 CCOc1cc(CN2CCC3(CC2)NC(=O)N(C3)c2ccc(cc2)C(=O)O)c(cc1C)C1CC1 28938487
124138271 3451 0 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 463 7 2 4 4.5 CCOc1cc(CN2CCC3(CC2)NC(=O)N(C3)c2ccc(cc2)C(=O)O)c(cc1C)C1CC1 28938487
2008 1211 0 None -1 6 Mouse 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2016 2260 4 None 7 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
5311375 2260 4 None 7 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
CHEMBL252764 2260 4 None 7 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 536 11 4 5 5.2 NCCCC[C@@H](C(=O)OC[C@@H](N)C)NC(=O)Cc1c([nH]c2c1ccc1c2cccc1)c1ccc2c(c1)cccc2 9784130
2037 645 0 None 1 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2084 653 0 None 39 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3676 12 None 1 9 Mouse 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2020 3676 12 None 1 9 Mouse 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
91935900 3676 12 None 1 9 Mouse 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
CHEMBL501796 3676 12 None 1 9 Mouse 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10818261
2036 643 0 None -1 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2036 643 0 None -1 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2036 643 0 None -1 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2036 643 0 None -1 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2036 643 0 None -1 5 Human 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2014 2214 0 None -2 9 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 2214 0 None -2 9 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2014 2214 0 None -2 9 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2014 2214 0 None -2 9 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2055 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
383414 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
90488715 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL1680 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL262746 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
DB00104 2907 48 None -32 14 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 3675 0 None -3 10 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
2008 1211 0 None -1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 1211 0 None -1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2008 1211 0 None -1 6 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
16133849 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 3676 12 None -1 9 Human 9.8 pKi None 9.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9652348