Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

168288485 191731 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197201 191731 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471936 191495 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
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 - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.5 Fc1ccc2c(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168296886 192507 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5209180 192507 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
168272821 190594 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
CHEMBL5180543 190594 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
142471848 191267 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5190457 191267 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
86293506 118819 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL3421842 118819 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
86294248 118820 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
CHEMBL3421843 118820 1 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
168280914 190802 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5183772 190802 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471730 190385 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5177487 190385 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471832 190275 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
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 - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 471 8 3 4 5.1 Fc1ccc2c(Cc3nnc(Cc4c[nH]c5cc(F)ccc45)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168279197 190932 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5185547 190932 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168272497 190233 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5174969 190233 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168275406 190307 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5176083 190307 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471801 192299 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5206148 192299 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
86292350 118821 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
CHEMBL3421844 118821 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
142471891 190595 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5180551 190595 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168279055 191240 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5190056 191240 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471929 191167 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5188841 191167 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168271257 190514 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5179456 190514 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471719 190502 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5179321 190502 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
168271446 190605 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5180752 190605 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168286554 191403 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5192578 191403 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168283125 191077 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5187484 191077 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
142471692 192382 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5207543 192382 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471938 192008 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5201594 192008 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168295000 192472 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208764 192472 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471828 192072 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5202717 192072 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471846 191329 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5191532 191329 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471682 191514 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193951 191514 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471978 192443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208396 192443 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168275268 190158 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5173784 190158 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168274800 190092 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5172814 190092 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471665 191707 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5196971 191707 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471860 192505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5209165 192505 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471737 190304 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5176020 190304 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
142471923 191911 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200112 191911 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471893 190327 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
CHEMBL5176454 190327 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
9893924 4748 34 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 4748 34 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
142471814 192162 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5203972 192162 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
168296234 192288 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5205998 192288 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471924 190394 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5177573 190394 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471678 190042 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5171935 190042 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
139392666 190202 0 None -16 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST4Agonist activity at human SST4
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 -16 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human SST4Agonist activity at human SST4
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
117711399 118822 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL3421845 118822 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assayAgonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
142471772 191178 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5189042 191178 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168271928 190083 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5172730 190083 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471769 191785 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198142 191785 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471961 191421 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5192791 191421 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471655 190425 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5178013 190425 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471841 191585 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5195145 191585 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471677 191949 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200786 191949 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
139392804 191603 1 None -16 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST4Agonist activity at human SST4
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 -16 5 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human SST4Agonist activity at human SST4
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
142471716 191492 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193686 191492 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
56945132 171420 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL4462793 171420 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assayAgonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
168283525 191087 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5187631 191087 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471684 191452 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193172 191452 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471767 192282 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5205904 192282 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471768 192004 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5201540 192004 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471733 190565 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5180116 190565 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471896 191143 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5188361 191143 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168297256 192411 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208037 192411 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471703 191732 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197218 191732 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assayAgonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
43594 217702 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 542 9 4 12 -0.9 O[C@@H](C(=O)N[C@H]1[C@H]2SCC(CSC3=NN=NN3CS(O)(=O)=O)=C(N2C1=O)C(O)=O)C1=CC=CC=C1 None
38103 53792 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
40467109 53792 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
CHEMBL1604 53792 69 None 6309 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 349 4 3 5 0.3 CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1 None
6024 202709 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
CHEMBL1632 202709 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
CHEMBL617 202709 79 None 7244 2 Human 8.4 pIC50 = 8.4 Functional
NoneNone
Drug Central 396 6 2 7 0.6 CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1 None
30699 217704 0 None -1 14 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 423 7 2 8 0.5 CC(=O)OCC1=C(N2[C@H](SC1)[C@H](NC(=O)CSC1=CC=NC=C1)C2=O)C(O)=O None
7763 410 0 None -380 2 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18543899
2027 655 0 None -63 5 Human 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2004 642 0 None -19 2 Rat 8.1 pIC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
8487 3980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
9919857 3980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
DB12777 3980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11145612
2079 1914 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212
2080 1915 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212
2012 1375 0 None -1 4 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15658864
2013 2180 0 None -2 6 Human 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12450568
2026 654 0 None -10 5 Human 6.5 pIC50 None 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11897676
2019 3675 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
44386062 3675 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
CHEMBL440072 3675 0 None -79 4 Rat 8.2 pIC50 None 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9166718
2081 1916 0 None - 1 Human 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14667212




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

124168080 181834 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 507 6 2 7 4.4 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
CHEMBL4778342 181834 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at human SST4Agonist activity at human SST4
ChEMBL 507 6 2 7 4.4 Cc1cc(Cl)cc(-c2cnc3ncn(-c4cc(O)cc(F)c4)c(=O)c3c2CN(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127496
140762468 182683 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4789268 182683 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
134168328 193539 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5267842 193539 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 456 3 2 5 5.4 N#Cc1cccc(-c2ccc3ncc(-c4cc(F)cc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5273084 193747 0 None - 0 Human 6.0 pEC50 = 6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 438 3 2 5 5.2 N#Cc1cccc(-c2ccc3ncc(-c4cccc(F)c4)c(N4CCC(N)CC4)c3c2)c1O 10.1021/acsmedchemlett.2c00431
CHEMBL5283444 194209 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 431 3 2 4 5.5 NC1CCN(c2c(-c3cc(F)cc(F)c3)cnc3ccc(-c4cccc(O)c4)cc23)CC1 10.1021/acsmedchemlett.2c00431
124167759 181087 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4760001 181087 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
124167759 181087 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4760001 181087 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 429 6 2 7 3.2 Cc1cc(C)cc(-c2cnc3ncn(-c4cccc(O)c4)c(=O)c3c2CN(C)CCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279994 194046 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 449 3 2 4 5.6 NC1CCN(c2c(-c3cc(F)cc(F)c3)cnc3ccc(-c4cccc(F)c4O)cc23)CC1 10.1021/acsmedchemlett.2c00431
140762567 180277 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4750691 180277 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cc(O)cc(F)c4)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL5271468 193685 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 390 7 4 5 4.1 Cc1cc(C)cc(-c2cncc(C(=O)Nc3cccc(O)c3)c2NCCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5271468 193685 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 390 7 4 5 4.1 Cc1cc(C)cc(-c2cncc(C(=O)Nc3cccc(O)c3)c2NCCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279978 194045 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 411 5 3 4 4.6 Cc1cc(C)cc(-c2cncc(-c3ccc4c(O)cccc4c3)c2C(=O)NCCN)c1 10.1021/acsmedchemlett.2c00431
CHEMBL5279978 194045 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 411 5 3 4 4.6 Cc1cc(C)cc(-c2cncc(-c3ccc4c(O)cccc4c3)c2C(=O)NCCN)c1 10.1021/acsmedchemlett.2c00431
140762500 181733 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (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 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (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 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (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 6.2 pEC50 = 6.2 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (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
162648021 179973 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
CHEMBL4746816 179973 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at SST4 (unknown origin)Agonist activity at SST4 (unknown origin)
ChEMBL 520 5 2 5 5.9 Cc1cc(Cl)cc(N2C=Nc3cc(C)c(-c4cccc(F)c4O)cc3C2C(=O)N(C)C[C@@H]2CCCN2)c1 10.1016/j.bmcl.2020.127391
140762468 182683 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
CHEMBL4789268 182683 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assayAgonist activity at human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL 476 5 2 5 5.4 Cc1cc(C)cc(N2C=Nc3cc(Cl)c(-c4cccc(O)c4)cc3C2C(=O)N(C)C[C@H](C)N)c1 10.1021/acsmedchemlett.2c00431
16129706 209031 40 None -13 5 Human 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
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/jm960850i
CHEMBL1823872 209031 40 None -13 5 Human 10.1 pIC50 = 10.1 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
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/jm960850i
CHEMBL262379 210538 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
CHEMBL3350911 211529 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL415582 213190 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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 9.3 pIC50 = 9.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL216992 209348 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
CHEMBL406816 212623 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 9.2 pIC50 = 9.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 9.2 pIC50 = 9.2 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL1824055 209039 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
CHEMBL446380 213945 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL3350888 211511 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350886 211509 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350908 211527 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3122129 211107 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL504087 214173 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL3350896 211518 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
11468916 115463 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 9.0 pIC50 = 9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
25188220 12491 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL500326 214111 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL386784 212392 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
11457521 115459 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350884 211507 1 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350905 211524 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL2371085 210011 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL3350891 211514 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350893 211515 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350899 211521 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3122128 211106 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL263587 210578 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
CHEMBL3350898 211520 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350912 211530 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
25187400 12694 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL504457 214177 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL265912 210671 0 None - 0 Human 8.9 pIC50 = 8.9 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 4.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 4.
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+
CHEMBL2371060 210007 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL504248 214175 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL410047 212797 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
11389178 115460 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350900 115460 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL503036 214160 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL3350895 211517 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL442494 213913 0 None -17 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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
CHEMBL442494 213913 0 None -17 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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
16129706 209031 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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 -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL447989 213953 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
16129706 209031 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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 -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
16129706 209031 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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 -13 5 Human 8.8 pIC50 = 8.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
CHEMBL408338 212706 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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 8.8 pIC50 = 8.8 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 4.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 4.
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+
16129706 209031 40 None -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 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 -13 5 Human 8.8 pIC50 = 8.8 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 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
CHEMBL406373 212606 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL425090 213329 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.7 pIC50 = 8.7 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3350881 211504 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350897 211519 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL452157 213976 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 8.7 pIC50 = 8.7 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
CHEMBL452157 213976 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL452157 213976 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 8.7 pIC50 = 8.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
CHEMBL3350894 211516 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL505128 214188 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
11563877 164720 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 7.0 pIC50 = 7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in CHO dhfr cell membranes after 60 mins by TopCount scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
44298251 194671 0 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL53204 194671 0 None - 1 Human 7.0 pIC50 = 7 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
56681776 63241 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)
ChEMBL 802 9 7 8 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)C2C(=O)[C@@H](Cc3c2[nH]c2ccccc32)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCC2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000316h
CHEMBL1790896 63241 0 None - 0 Human 7.0 pIC50 = 7 Binding
Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)Tested for binding affinity against human somatostatin receptor subtype 4 (hSSTR4)
ChEMBL 802 9 7 8 2.9 C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)C2C(=O)[C@@H](Cc3c2[nH]c2ccccc32)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]2CCCC2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm000316h
118718507 115358 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2079558 209194 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2079559 209195 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2079563 209196 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2079626 209197 2 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2311181 209507 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349505 211410 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349508 211413 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349597 211426 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349608 211436 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349610 211437 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349611 211438 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349612 211439 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349613 211440 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349614 211441 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349617 211443 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349618 211444 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349663 211447 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349665 211449 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349667 211451 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349671 211454 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349672 211455 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349673 211456 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349674 211457 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349675 211458 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349676 211459 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349677 211460 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349679 211462 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3349680 211463 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL3351090 211544 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
49865345 15911 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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 6.0 pIC50 = 6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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
155526536 171199 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 1405 26 16 21 -3.2 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](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 10.1016/j.ejmech.2018.11.030
CHEMBL4459308 171199 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 by radioligand binding assay
ChEMBL 1405 26 16 21 -3.2 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](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 10.1016/j.ejmech.2018.11.030
CHEMBL2372606 210276 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.0 pIC50 = 6.0 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
10577746 207252 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 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 6.0 pIC50 = 6.0 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 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
CHEMBL414544 213140 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
162646037 179514 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR4 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 5.0 pIC50 = 5.0 Binding
Displacement of [125I-Tyr11]-SS14 from human SSTR4 expressed in HEK293-A cells incubated for 30 mins by gamma counting based competition radioligand binding assayDisplacement of [125I-Tyr11]-SS14 from human SSTR4 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
CHEMBL387458 212410 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL455435 214003 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 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
44560867 189140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL3349598 211427 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL414446 213131 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL1824051 209035 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
CHEMBL1824052 209036 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
56651206 174631 0 None 1 2 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.9 pIC50 = 5.9 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
16737812 85506 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 508 10 3 3 4.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)CC(c2ccccc2)c2ccccc2)C1=O 10.1021/jm070246f
118718854 115416 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3350902 211523 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL509192 215334 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
44368019 10265 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 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](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
CHEMBL1161328 10265 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1136 12 12 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](Cc2ccccc2)NC(=O)N(C(=O)c2ccccc2)C(=O)N(C)[C@H](O)NC(=O)[C@@H](N)CSSCCNC(=O)[C@@H](Cc2ccccc2)NC1=O 10.1021/jm030243c
25187683 12451 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
25188218 12564 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
24777672 94912 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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 6.9 pIC50 = 6.9 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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
118718854 115416 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3350901 211522 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
44368398 10266 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 6.8 pIC50 = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL1824050 209034 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
25187681 12469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
25189327 12696 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL455760 214008 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 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
44368398 10266 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 7.8 pIC50 = 7.8 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
46919128 17086 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 552 12 4 7 2.5 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN=C(N)N 10.1021/jm1002777
CHEMBL1254882 17086 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 552 12 4 7 2.5 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN=C(N)N 10.1021/jm1002777
CHEMBL3350909 211528 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL442494 213913 0 None -17 5 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL504395 214176 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL2111200 209215 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL3350890 211513 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
25187953 12689 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL2111257 209216 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL442494 213913 0 None -17 5 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human sst4 by in vitro receptor autoradiography assayBinding affinity to human sst4 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
CHEMBL506892 214216 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL3350357 211475 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
118719101 115440 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL2371059 210006 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL1823873 209032 9 None -18 4 Human 8.6 pIC50 = 8.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
25187679 12671 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL3350880 211503 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350882 211505 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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](Cc2ccc(O)cc2)NC(N)=O)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
25189325 12446 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
25188496 12535 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL1907758 209068 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3350889 211512 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL501776 214144 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL524870 215625 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL442494 213913 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL442494 213913 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
CHEMBL505496 214193 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL442494 213913 0 None -17 5 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 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
CHEMBL2111200 209215 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3122127 211105 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL442494 213913 0 None -17 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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
CHEMBL407649 212674 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
155550820 174289 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
11535351 97052 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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 sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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
CHEMBL526550 215692 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiography
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@@H]1NC(=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](NC(=O)[C@H](N)Cc2ccccc2)SS1)C(N)=O 10.1021/jm701445q
70683416 73967 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 6.7 pIC50 = 6.7 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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
44388037 160979 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL411600 160979 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
155553012 174086 0 None 1 2 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.7 pIC50 = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
155541897 173055 0 None -5 2 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 4.7 pIC50 = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
CHEMBL425465 213335 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL367125 212158 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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](N)CSSC[C@@H](C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm049519m
44368398 10266 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 7.6 pIC50 = 7.6 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL414692 213147 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
49865344 15910 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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
CHEMBL1824049 209033 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
CHEMBL540408 215714 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL554624 215726 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](NC(=O)[C@H](N)Cc3ccccc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
42637563 195510 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 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(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553656 195510 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 989 12 9 12 2.4 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(N)=O)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL265846 210667 0 None - 0 Human 6.6 pIC50 = 6.6 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 4.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 4.
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+
42637503 195817 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL558161 195817 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1238 19 12 15 2.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
42637632 60275 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL174206 60275 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1334 20 11 14 5.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL3349506 211411 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL448431 213957 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL508585 214994 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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](Cc2ccc([N+](=O)[O-])cc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL452074 213974 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 cells by autoradiographyDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst4 receptor expressed in chinese hamster CCL39 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 - 3 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
11159133 115462 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL453936 213990 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL1907758 209068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
13690207 115382 0 None -2041 5 Human 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
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 -2041 5 Human 8.5 pIC50 = 8.5 Binding
Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4Tested for inhibition of radioligand binding to cloned somatostatin receptor hSSTR4
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
CHEMBL1907758 209068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL525030 215631 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL3350887 211510 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL505854 214198 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
16737814 85507 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 8.5 pIC50 = 8.5 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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
CHEMBL436962 213700 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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
16737814 85507 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 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 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 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 8.5 pIC50 = 8.5 Binding
Inhibition of human SSTR4 by radioligand binding assayInhibition of human SSTR4 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
118718854 115416 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL442494 213913 0 None -17 5 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in 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/jm701444y
CHEMBL3350357 211475 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3350913 211531 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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](C)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
CHEMBL3350725 211490 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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)c(I)c2)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
CHEMBL2369533 209632 0 None - 0 Human 8.5 pIC50 = 8.5 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 4.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 4.
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+
CHEMBL3122130 211108 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL1907758 209068 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL410184 212806 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL262135 210527 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL3349668 211452 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
118718854 115416 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 7.5 pIC50 = 7.5 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL2079558 209194 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
122179457 121454 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to somatostatin receptor type 4 (unknown origin)Binding affinity to somatostatin receptor type 4 (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 5.5 pIC50 = 5.5 Binding
Binding affinity to somatostatin receptor type 4 (unknown origin)Binding affinity to somatostatin receptor type 4 (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
CHEMBL1908984 209072 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563124 209072 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](N)CSSC[C@@H](C(=O)N[C@@H](Cc3ccc4ccccc4c3)C(N)=O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL2372604 210275 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.5 pIC50 = 6.5 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
49865343 15909 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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
CHEMBL2372603 210274 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 4 expressed in CCL39 cells; (n=2)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL447064 213947 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
25187955 12436 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL2372667 210280 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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
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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL5282589 194164 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
ChEMBL 633 14 7 7 0.1 CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H]1Cc2c([nH]c3ccccc23)CN([C@@H](CCCCN)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C1=O 10.1021/acs.jmedchem.6b01029
CHEMBL2011466 209114 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human sst4 by in vitro receptor autoradiography assayBinding affinity to human sst4 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
44368406 10267 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 7.4 pIC50 = 7.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
10114 2556 23 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 minsDisplacement of [125I]SS-28 from human SSTR-4 transfected in CHO cells after 60 to 90 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
CHEMBL436887 213691 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL3350885 211508 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
CHEMBL3122123 211102 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL2372713 210284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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
2082 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
5311374 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
CHEMBL1450103 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm0302445
2082 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
5311374 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
CHEMBL1450103 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030243c
2082 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
5311374 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
CHEMBL1450103 2259 14 None 7079 2 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1021/jm030245x
11343811 115461 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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 8.4 pIC50 = 8.4 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
25189052 12672 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL504462 214179 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL503596 214170 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
46902023 17038 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 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 5.4 pIC50 = 5.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 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
CHEMBL3349616 211442 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL2371051 210004 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL1824056 209040 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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
44325273 207308 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration required for somatostatin 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 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 4 receptor in radioligand binding assay ([125I]Tyr11-SRIF)Inhibitory concentration required for somatostatin 4 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
44444935 94642 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptorDisplacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 cells by autoradiographyDisplacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human CCL39 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
CHEMBL437905 213738 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)N(C)C(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL262790 210551 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
44368422 10268 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1123 10 13 14 -0.0 C[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](O)NC(=O)N1C 10.1021/jm030243c
CHEMBL1161333 10268 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand
ChEMBL 1123 10 13 14 -0.0 C[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(=O)O)CSSC[C@@H](N)C(=O)N[C@H](Cc2ccccc2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](O)NC(=O)N1C 10.1021/jm030243c
11642413 17100 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 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 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 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
44388123 169186 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL440618 169186 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1681 21 18 21 0.2 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
11548587 17115 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 560 11 3 7 4.4 CS[C@@H]1O[C@H](COCc2ccc3ccccc3c2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1255049 17115 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 560 11 3 7 4.4 CS[C@@H]1O[C@H](COCc2ccc3ccccc3c2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
45268875 195610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL555977 195610 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1363 19 12 15 2.6 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)CSSC[C@@H](C(=O)N[C@@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL499939 214104 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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)c(I)c2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc([N+](=O)[O-])cc2)NC(=O)CN2CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC2)CSSC[C@@H](C(=O)N[C@H](Cc2ccc(O)cc2)C(N)=O)NC1=O 10.1021/jm701618q
CHEMBL1908982 209071 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL552988 209071 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)c(I)c3)NC2=O)cc1 10.1021/jm801314f
CHEMBL502219 214151 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
90663869 106737 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.3 pIC50 = 6.3 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL413441 213071 0 None - 0 Human 6.3 pIC50 = 6.3 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 4.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 4.
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](NC(=O)[C@H](Cc3ccc(O)cc3)NC(N)=O)CSSC[C@@H](C(=O)O)NC(=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/jm010037+
CHEMBL413735 213086 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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
CHEMBL219201 209409 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4
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
CHEMBL502511 214155 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
118718854 115416 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
118719275 115481 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3351044 115481 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL2371070 210008 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL3122124 211103 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 cells after 2 hrs by autoradiographic analysisDisplacement of [125I]-[LTT]-SS28 from human SST4 receptor expressed in Chinese hamster CCL-39 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
CHEMBL3350883 211506 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
91936729 167578 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
CHEMBL430066 167578 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 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)
ChEMBL None None None None 10.1021/jm040794i
42637136 196504 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 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](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL563462 196504 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 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](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
11828523 195005 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human SSTR4Inhibition of human SSTR4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1016/j.bmcl.2010.03.045
CHEMBL54832 195005 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human SSTR4Inhibition of human SSTR4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1016/j.bmcl.2010.03.045
11828523 195005 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL54832 195005 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL511086 215592 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
44368398 10266 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 7.3 pIC50 = 7.3 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
25188776 12482 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
16151826 195856 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL558600 195856 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
44388121 166722 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL428295 166722 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1555 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)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)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
25189054 12704 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL1824058 209042 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 cells after 2 hrs by autoradiographyDisplacement of 125I-[LTT]-SRIF-28 from human sst4 receptor in CCL39 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](Cc2cn(Cc3ccccc3)cn2)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
56651207 175897 0 None 1 2 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 6.2 pIC50 = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
CHEMBL525397 215645 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
44368406 10267 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL262975 210556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
70689221 77856 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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 8.2 pIC50 = 8.2 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
25187685 12470 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL3349507 211412 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL261895 210520 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL2372699 210281 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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
44388029 96454 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
CHEMBL262258 96454 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1659 18 18 20 0.0 CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]3CCCCCCNC(=O)CC[C@@H](NC(=O)[C@@H](Cc4ccccc4)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC3=O)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049519m
70689723 73968 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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
CHEMBL3349664 211448 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
52943613 16970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 510 11 3 7 3.2 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
CHEMBL1253788 16970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 510 11 3 7 3.2 CS[C@@H]1O[C@H](COCc2ccccc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCN 10.1021/jm1002777
44388124 159370 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 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
CHEMBL410048 159370 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 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1680 21 18 21 -0.4 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@@H](CCCCN)NC(=O)[C@H](N)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccc(O)cc3I)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049520l
155528330 171340 0 None 1 2 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.2 pIC50 = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
44290734 155835 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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 8.2 pIC50 = 8.2 Binding
Binding affinity of human Somatostatin receptor type 4 (hsst4) by the displacement of [125I]- Tyr11 somatostatin-14 in CHO-K1 cellsBinding affinity of human Somatostatin receptor type 4 (hsst4) 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
25188780 12431 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
25187396 12684 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL384855 212338 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 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3I)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
45273131 194786 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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 7.2 pIC50 = 7.2 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 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
CHEMBL446077 213943 0 None - 3 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
52947330 16979 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 600 13 4 7 3.6 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCCN=C(N)N 10.1021/jm1002777
CHEMBL1253871 16979 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cellsDisplacement of [125I]iodotyrosyl from human SST4 receptor expressed in CHO cells
ChEMBL 600 13 4 7 3.6 CS[C@@H]1O[C@H](COCc2ccc(Cl)cc2)[C@@H](O)[C@@H](OCc2ccc3ccccc3c2)[C@H]1NC(=O)CCCN=C(N)N 10.1021/jm1002777
44560873 189147 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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 sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL2372604 210275 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=5)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
16738359 137183 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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
155529288 171397 0 None 1 2 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.1 pIC50 = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
16737813 142081 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 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 7.1 pIC50 = 7.1 Binding
Displacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptorDisplacement of [125I][Leu8-D-Trp22, Tyr25]-SRIF28 from human SST4 receptor
ChEMBL 418 8 3 3 2.9 NCCCCCN1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O 10.1021/jm070246f
CHEMBL3349669 211453 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL415144 213172 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 4Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None CC(C)NCc1ccc(C[C@H]2C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)CSSC[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3I)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc3ccccc3)C(=O)N[C@@H](Cc3ccccc3)C(=O)N[C@@H](Cc3c[nH]c4ccccc34)C(=O)N2C)cc1 10.1021/jm049520l
CHEMBL438285 213764 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL None None None NCCCC[C@@H]1NC(=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
90663873 106739 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
25187398 12448 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 receptor expressed in chinese hamster CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombinant sst4 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
CHEMBL502777 214157 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 cellsDisplacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF-28 from human cloned sst4 receptor expressed in CCL39 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
CHEMBL263306 210566 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL3350726 211491 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.Binding affinity towards human somatostatin receptor type 4 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
44368489 10269 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL1161334 10269 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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
CHEMBL524327 215602 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
44298204 101524 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 683 21 3 9 5.5 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCCc1cccnc1 10.1021/jm0205088
CHEMBL298149 101524 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration required against human Somatostatin receptor type 4Inhibitory concentration required against human Somatostatin receptor type 4
ChEMBL 683 21 3 9 5.5 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCCc1cccnc1 10.1021/jm0205088
CHEMBL505704 214196 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
90663874 106740 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL498985 214089 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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(=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
90663867 106735 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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 6.1 pIC50 = 6.1 Binding
In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 cells; (n=3)In vitro inhibition of [125I][Leu8,D-Trp22,Tyr25] somatostatin 28 binding to human somatostatin receptor type 4 expressed in CCL39 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
CHEMBL412029 212972 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4Inhibition of [125I](Leu8,DTrp22,Tyr25)-SRIF28 binding to human sst4
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
CHEMBL499760 214101 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL415585 213193 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL3350906 211525 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu8,DTrp22,Tyr25]SRIF-28 as radioligandBinding affinity towards human Somatostatin receptor type 4 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](C)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
CHEMBL415359 213185 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.Binding affinity at human Somatostatin receptor type 4 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
CHEMBL501282 214136 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL510901 215590 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I][LTT]SRIF28 from human cloned sst4 receptor by autoradiographyDisplacement of [125I][LTT]SRIF28 from human cloned sst4 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
CHEMBL2079559 209195 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
CHEMBL559150 215744 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
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)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm801314f
CHEMBL265836 210666 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
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)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H]([C@@H](C)O)NC2=O)cc1 10.1021/jm049519m
CHEMBL3349678 211461 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards cloned human somatostatin 4 (hsst) receptorBinding affinity towards cloned human somatostatin 4 (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
42637069 195509 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 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](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
CHEMBL553655 195509 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiographyDisplacement of [125I]LTT-SRIF-28 from human sst4 receptor by autoradiography
ChEMBL 1074 15 10 13 1.6 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](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 10.1021/jm801314f
44388109 161757 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
CHEMBL413924 161757 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4Inhibition of 125I-[Leu8,D-Trp22,Tyr25]SRIF-28 binding to human somatostatin receptor type 4
ChEMBL 1653 22 20 21 -0.0 CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H]3CCC(=O)NCCCCC[C@@H](NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@@H]([C@@H](C)O)NC2=O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)O)CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)N[C@H](CCCCN)C(=O)N[C@H](Cc2ccccc2)C(=O)N3)cc1 10.1021/jm049519m
2019 3675 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
44386062 3675 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL440072 3675 0 None -4 10 Human 9.7 pKd = 9.7 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 mins
ChEMBL None None None None 10.1021/acs.jmedchem.8b02036
CHEMBL437093 213705 0 None -16 5 Human 6.0 pKd = 6 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
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
46865536 11919 0 None -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -131 7 Human 6.0 pKd = 6.0 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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
44565112 12759 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1187847 12759 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL523814 12759 0 None -1548 6 Human 5.9 pKd = 5.9 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 481 7 0 6 4.4 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
44565159 194891 0 None -4466 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL540705 194891 0 None -4466 5 Human 5.8 pKd = 5.8 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 497 7 0 7 4.5 CN(CCC(=O)N1CCN(c2ccc3nonc3c2)CC1)CCC1c2ccccc2Oc2ccccc21 10.1016/j.bmcl.2009.01.072
9871544 14216 3 None -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -30 11 Human 6.8 pKd = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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
2030 3672 10 None -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -21379 10 Human 4.8 pKd = 4.8 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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
CHEMBL265636 210658 0 None -12 4 Human 6.7 pKd = 6.7 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
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
10162564 12540 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL1186652 12540 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL473763 12540 0 None -4168 8 Human 5.6 pKd = 5.6 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 475 7 0 3 5.1 CN(CCC(=O)N1CCN(c2ccc(F)c(F)c2)CC1)CCC1c2ccccc2-c2ccccc21 10.1016/j.bmcl.2009.01.072
CHEMBL2370166 209805 0 None -120 5 Human 5.6 pKd = 5.6 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO 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
CHEMBL384836 212337 0 None -19 5 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
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
17955460 176775 0 None -4365 9 Human 5.5 pKd = 5.5 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 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 -4365 9 Human 5.5 pKd = 5.5 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 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
CHEMBL413830 213089 0 None -13 5 Human 6.5 pKd = 6.5 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
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
44447073 94550 0 None -9772 10 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -9772 10 Human 5.4 pKd = 5.4 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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
46865535 5539 0 None -123 7 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -123 7 Human 6.4 pKd = 6.4 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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
CHEMBL2370167 209806 0 None -1905 5 Human 5.4 pKd = 5.4 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO 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
CHEMBL2370168 209807 0 None -1023 5 Human 5.3 pKd = 5.3 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO 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
9849682 94952 0 None -23988 10 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -23988 10 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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
155544425 173382 0 None -251188 5 Human 5.3 pKd = 5.3 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 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 -251188 5 Human 5.3 pKd = 5.3 Binding
Displacement of [125I]somatostatin from human SSTR4 expressed in CHO-K1 cell membranes after 120 minsDisplacement of [125I]somatostatin from human SSTR4 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
44447078 94617 0 None -30 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -30 7 Human 5.3 pKd = 5.3 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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
CHEMBL409019 212742 0 None -20 5 Human 6.2 pKd = 6.2 Binding
Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)Binding affinity was determined on cloned human somatostatin receptor-1 (hsst4)
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
46880588 14217 0 None -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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 -8 7 Human 5.2 pKd = 5.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 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
44447077 94616 0 None -19 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -19 7 Human 5.1 pKd = 5.1 Binding
Binding affinity to human recombinant sst4 receptorBinding affinity to human recombinant sst4 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 -6606 5 Human 5.1 pKd = 5.1 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in 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](Cc2ccccc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](Cc2ccccc2)NC1=O 10.1021/jm970393l
168272497 190233 0 None 3467 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5174969 190233 0 None 3467 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 448 8 2 4 5.1 Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168280914 190802 0 None 18197 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5183772 190802 0 None 18197 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168288485 191731 0 None 2454 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197201 191731 0 None 2454 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 209031 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
168279197 190932 0 None 1621 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5185547 190932 0 None 1621 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 209031 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
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/jm0108449
CHEMBL1823872 209031 40 None -13 5 Human 9.2 pKi = 9.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
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/jm0108449
2082 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
5311374 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
CHEMBL1450103 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting methodDisplacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
ChEMBL 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 10.1039/C8MD00388B
168274800 190092 0 None 630 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5172814 190092 0 None 630 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471832 190275 0 None 138 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor 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 138 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor 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
168271257 190514 0 None 8912 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5179456 190514 0 None 8912 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471936 191495 0 None 776 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor 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 776 5 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor 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
16129706 209031 40 None -13 5 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 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 -13 5 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 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
142471730 190385 0 None 741 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5177487 190385 0 None 741 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.3 FC(F)(F)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168272821 190594 0 None 4677 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
CHEMBL5180543 190594 0 None 4677 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/D1MD00044F
142471924 190394 0 None 524 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5177573 190394 0 None 524 3 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 432 8 2 4 4.6 Fc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
168296886 192507 0 None 5754 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5209180 192507 0 None 5754 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccccc1Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471678 190042 0 None 660 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5171935 190042 0 None 660 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
142471848 191267 0 None 263 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5190457 191267 0 None 263 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 8 2 4 5.2 Fc1ccc2c(Cc3nnc(Cc4cccc(Br)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
168275406 190307 0 None 794 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5176083 190307 0 None 794 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4ccc(Cl)c(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
10115 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
11442741 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
CHEMBL4451852 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting methodDisplacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
ChEMBL 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 10.1039/C8MD00388B
168279055 191240 0 None 4265 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5190056 191240 0 None 4265 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 464 8 2 4 5.6 Clc1cc(Cl)cc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
16129706 209031 40 None -13 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined 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 10.1021/jm021093t
CHEMBL1823872 209031 40 None -13 5 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined 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 10.1021/jm021093t
CHEMBL4299281 213558 0 None -44 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
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](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=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]([C@@H](C)O)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.2016.02.046
142471891 190595 0 None 436 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5180551 190595 0 None 436 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
16129706 209031 40 None -13 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
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/jm980118e
CHEMBL1823872 209031 40 None -13 5 Human 8.9 pKi = 8.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
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/jm980118e
16129706 209031 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards somatostatin receptor type 4Binding affinity towards somatostatin receptor type 4
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 -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards somatostatin receptor type 4Binding affinity towards somatostatin receptor type 4
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
168275268 190158 0 None 2884 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5173784 190158 0 None 2884 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 482 8 2 4 5.7 Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471929 191167 0 None 676 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5188841 191167 0 None 676 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471978 192443 0 None 891 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208396 192443 0 None 891 2 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 396 8 2 4 4.3 c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
16129706 209031 40 None -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
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 -13 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
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 -44 5 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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
CHEMBL3098601 211018 0 None -8 5 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 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
142471801 192299 0 None 199 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5206148 192299 0 None 199 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 9 2 5 5.3 COc1ccc2[nH]cc(Cc3nnc(Cc4cccc(C(F)(F)F)c4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
91809283 125760 0 None -134 6 Human 8.0 pKi = 8.0 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 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 -134 6 Human 8.0 pKi = 8.0 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 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
10009650 99795 0 None 3 4 Human 7.0 pKi = 7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
CHEMBL285333 99795 0 None 3 4 Human 7.0 pKi = 7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)[C@H](OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm9800346
44298251 194671 0 None - 1 Human 7.0 pKi = 7 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL53204 194671 0 None - 1 Human 7.0 pKi = 7 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@@H]1O[C@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2c[nH]cn2)C(OCc2ccccc2)[C@H]1OCc1ccccc1 10.1021/jm0205088
CHEMBL2311098 209505 0 None -83 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369733 209661 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369735 209663 0 None -181 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369749 209667 0 None -83 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369750 209668 0 None -27 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369751 209669 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369752 209670 0 None -19 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369753 209671 0 None -11 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369754 209672 0 None -107 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369755 209673 0 None -165 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369756 209674 0 None -5 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369757 209675 0 None -40 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369758 209676 0 None -36 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369759 209677 0 None -1 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
CHEMBL2369761 209679 0 None -8 5 Human 6.0 pKi = 6 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
10625762 37384 0 None -1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 11 3 4 5.2 NCCCC/N=C(\S)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL145472 37384 0 None -1 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 11 3 4 5.2 NCCCC/N=C(\S)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10554709 119314 0 None 3 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 549 7 3 5 5.4 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc2[nH]nnc2c1 10.1021/jm980118e
CHEMBL344074 119314 0 None 3 2 Human 6.0 pKi = 6 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 549 7 3 5 5.4 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc2[nH]nnc2c1 10.1021/jm980118e
90665461 109261 0 None -5 5 Human 5.0 pKi = 5 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 -5 5 Human 5.0 pKi = 5 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
10876118 196253 0 None - 1 Human 6.0 pKi = 6.0 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1c[nH]cn1 10.1021/jm0205088
CHEMBL56181 196253 0 None - 1 Human 6.0 pKi = 6.0 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 668 20 3 8 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1c[nH]cn1 10.1021/jm0205088
CHEMBL275806 210823 0 None -6 4 Human 6.0 pKi = 6.0 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
90644981 111813 0 None -660 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 111813 0 None -660 4 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS28 from human SST5 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
142471719 190502 0 None 204 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5179321 190502 0 None 204 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.5 Cn1cc(CCc2nnc(Cc3cccc(C(F)(F)F)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
9852911 99383 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 -8 6 Human 6.0 pKi = 6.0 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
9852911 99383 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
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 10.1016/j.ejmech.2018.11.030
CHEMBL282618 99383 0 None -8 6 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
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 10.1016/j.ejmech.2018.11.030
10815650 164932 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 512 12 3 5 4.6 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL422475 164932 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 512 12 3 5 4.6 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
127029955 138886 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
CHEMBL3780791 138886 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
CHEMBL3782073 138886 0 None 2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 391 6 1 3 5.3 NCCCc1cc(Cl)cc2c(=O)cc(CCc3cccc4ccccc34)oc12 10.1016/j.ejmech.2016.02.046
9872511 122019 0 None 21 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 3 4 4.1 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL359453 122019 0 None 21 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 3 4 4.1 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
142471938 192008 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5201594 192008 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 410 9 2 4 4.5 c1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471860 192505 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5209165 192505 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 428 9 2 4 4.6 Fc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10603005 119138 0 None - 1 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 562 8 3 4 5.7 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCc1nc2ccccc2[nH]1 10.1021/jm980118e
CHEMBL342781 119138 0 None - 1 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 562 8 3 4 5.7 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCc1nc2ccccc2[nH]1 10.1021/jm980118e
10974575 100794 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 713 20 2 8 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(Cl)nc1 10.1021/jm0205088
CHEMBL293114 100794 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 713 20 2 8 7.4 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(Cl)nc1 10.1021/jm0205088
90665463 109262 0 None -4 5 Human 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 4.9 pKi = 4.9 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
CHEMBL1791312 208925 0 None -123 2 Human 6.9 pKi = 6.9 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
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](Cc2cnccn2)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/jm058184l
CHEMBL2371893 210147 0 None -112 5 Human 5.9 pKi = 5.9 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
10865371 101074 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 693 20 2 8 7.1 Cc1ccc(CO[C@H]2[C@H](OCc3ccccc3)[C@@H](OCc3ccccc3)[C@H](OCCc3c[nH]c4ccccc34)O[C@@H]2COCCCCCN)cn1 10.1021/jm0205088
CHEMBL294830 101074 0 None - 1 Human 5.9 pKi = 5.9 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 693 20 2 8 7.1 Cc1ccc(CO[C@H]2[C@H](OCc3ccccc3)[C@@H](OCc3ccccc3)[C@H](OCCc3c[nH]c4ccccc34)O[C@@H]2COCCCCCN)cn1 10.1021/jm0205088
44397648 66764 0 None -32 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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 -32 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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
10650940 121984 0 None 5 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 582 13 3 4 6.1 S=C(NCCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL359215 121984 0 None 5 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 582 13 3 4 6.1 S=C(NCCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
10436888 119311 0 None 295 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 524 10 3 4 4.8 O=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL344059 119311 0 None 295 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 524 10 3 4 4.8 O=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
142471961 191421 0 None 275 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5192791 191421 0 None 275 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 494 10 2 5 5.4 FC(F)(F)Oc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44397706 67191 0 None -77 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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 -77 5 Human 6.9 pKi = 6.9 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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
10745635 119347 0 None 1 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 2 5 5.7 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL344285 119347 0 None 1 2 Human 5.9 pKi = 5.9 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 2 5 5.7 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
10053855 168554 0 None -263 2 Human 5.9 pKi = 5.9 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 574 8 2 6 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
CHEMBL435631 168554 0 None -263 2 Human 5.9 pKi = 5.9 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 574 8 2 6 3.2 C[C@@H](c1c[nH]c2ccccc12)[C@H](C(=O)N(C)C[C@H]1OC[C@H](N)CO1)N1CCN(C2CCCN(c3ccccc3)C2)C1=O 10.1016/s0960-894x(99)00016-5
155519582 170386 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL4447896 170386 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL2372960 210326 0 None -4 4 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
9893924 4748 34 None 52 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 4748 34 None 52 2 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
10698706 33808 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 591 8 2 4 7.1 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL142293 33808 0 None - 1 Human 4.8 pKi = 4.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 591 8 2 4 7.1 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL408987 212740 0 None -9 5 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
2054 3974 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
71306 3974 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL264186 3974 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL3349523 3974 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
DB04894 3974 15 None -446 11 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
ChEMBL None None None None 10.1021/jm021093t
CHEMBL437220 213711 0 None -63 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
10369961 34639 0 None 48 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 536 11 3 4 5.2 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142986 34639 0 None 48 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 536 11 3 4 5.2 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
142471896 191143 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5188361 191143 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 446 9 2 4 4.8 Fc1cc(F)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
44820545 52494 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 519 11 3 3 5.3 S=C(NCCCc1cnc[nH]1)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cc1 10.1039/c1md00200g
CHEMBL1591395 52494 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 519 11 3 3 5.3 S=C(NCCCc1cnc[nH]1)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cc1 10.1039/c1md00200g
CHEMBL2372957 210323 0 None -85 4 Human 5.8 pKi = 5.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
9852911 99383 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to sst4 receptor (unknown origin)Binding affinity to sst4 receptor (unknown origin)
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 10.1016/j.ejmech.2016.02.046
CHEMBL282618 99383 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Binding affinity to sst4 receptor (unknown origin)Binding affinity to sst4 receptor (unknown origin)
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 10.1016/j.ejmech.2016.02.046
9852911 99383 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
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/jm0205088
CHEMBL282618 99383 0 None -8 6 Human 5.8 pKi = 5.8 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
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/jm0205088
9893924 4748 34 None 52 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/c1md00200g
CHEMBL103769 4748 34 None 52 2 Human 7.8 pKi = 7.8 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/c1md00200g
9985523 99161 0 None 1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 1 5 Human 5.8 pKi = 5.8 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
10816544 33810 0 None 43 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 551 10 2 4 5.6 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1ccccn1 10.1021/jm980118e
CHEMBL142295 33810 0 None 43 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 551 10 2 4 5.6 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1ccccn1 10.1021/jm980118e
10650427 34435 0 None 1 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 2 5 5.3 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142823 34435 0 None 1 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 2 5 5.3 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCn1ccnc1 10.1021/jm980118e
10625454 119364 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 507 11 3 6 4.5 O=[N+]([O-])c1ccc(N(CC/N=C(\S)NCCCc2c[nH]cn2)Cc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm980118e
CHEMBL344404 119364 0 None 2 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 507 11 3 6 4.5 O=[N+]([O-])c1ccc(N(CC/N=C(\S)NCCCc2c[nH]cn2)Cc2ccc(Cl)c(Cl)c2)nc1 10.1021/jm980118e
CHEMBL413171 213051 0 None -1 5 Human 6.8 pKi = 6.8 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
10698494 34945 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 580 12 3 5 5.9 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143245 34945 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 580 12 3 5 5.9 S=C(NCCCNc1ccccn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
44820569 52478 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1)C(=S)NCCCc1cnc[nH]1 10.1039/c1md00200g
CHEMBL1591268 52478 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1)C(=S)NCCCc1cnc[nH]1 10.1039/c1md00200g
56945132 171420 0 None 251 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
CHEMBL4462793 171420 0 None 251 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 478 9 2 4 5.8 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl 10.1039/C8MD00388B
10770814 100792 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
155546680 173565 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
56651206 174631 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
122181227 121846 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
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 SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 628 16 1 5 8.3 NCCCCC[C@@H]1[C@@H](OCc2ccccc2)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)CN1Cc1ccc2ccccc2c1 10.1039/C4MD00074A
13690207 115382 0 None -2041 5 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
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/jm980118e
CHEMBL3350037 115382 0 None -2041 5 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
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/jm980118e
CHEMBL1794035 208937 0 None -7 5 Human 8.7 pKi = 8.7 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
91809287 160258 0 None -41 6 Human 8.7 pKi = 8.7 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 -41 6 Human 8.7 pKi = 8.7 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
142471684 191452 0 None 1174 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193172 191452 0 None 1174 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
155541853 173043 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 1636 26 21 23 -3.8 CC(=O)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)CSSC[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)NC1=O 10.1039/C8MD00388B
CHEMBL4519096 173043 0 None -3 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 1636 26 21 23 -3.8 CC(=O)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)N)CSSC[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)NC1=O 10.1039/C8MD00388B
168296234 192288 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5205998 192288 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 430 8 2 4 5.0 Clc1ccccc1Cc1nnc(Cc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
142471841 191585 0 None 363 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5195145 191585 0 None 363 3 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc2[nH]cc(Cc3nnc(Cc4ccc(F)cc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
91809286 125763 0 None -128 6 Human 7.7 pKi = 7.7 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 -128 6 Human 7.7 pKi = 7.7 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
10699714 99417 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
10325243 100495 0 None 1 5 Human 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 5.7 pKi = 5.7 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
44308969 204364 0 None -1258 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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 -1258 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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
10601454 35309 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 499 11 3 4 5.0 NCCCC/N=C(\S)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143668 35309 0 None -1 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 499 11 3 4 5.0 NCCCC/N=C(\S)NCCCN(Cc1cccc2ccccc12)c1ccc(Br)cn1 10.1021/jm980118e
90665458 109258 0 None -2 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 -2 3 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
155550820 174289 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
127032867 138870 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
CHEMBL3781875 138870 0 None 2 2 Human 5.7 pKi = 5.7 Binding
Binding affinity to human sst4 receptorBinding affinity to human sst4 receptor
ChEMBL 338 10 2 3 4.3 NCCCCCOc1ccccc1OCCc1c[nH]c2ccccc12 10.1016/j.ejmech.2016.02.046
155558366 174738 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 410 9 2 4 4.3 c1ccc(CCn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
CHEMBL4560435 174738 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 410 9 2 4 4.3 c1ccc(CCn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
127033186 138878 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-SRIF14 from human sst4 receptorDisplacement of [125I]-SRIF14 from human sst4 receptor
ChEMBL 779 17 5 9 6.1 CC(C)CC[C@]1(Cc2ccccc2)NC=C([C@@]2(Cc3ccccc3)NC=C([C@]3(CCCN)NC=C([C@@]4(CC(C)C)NC=C(Cc5ccccc5)C4=O)C3=O)C2=O)C1=O 10.1016/j.ejmech.2016.02.046
CHEMBL3782021 138878 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-SRIF14 from human sst4 receptorDisplacement of [125I]-SRIF14 from human sst4 receptor
ChEMBL 779 17 5 9 6.1 CC(C)CC[C@]1(Cc2ccccc2)NC=C([C@@]2(Cc3ccccc3)NC=C([C@]3(CCCN)NC=C([C@@]4(CC(C)C)NC=C(Cc5ccccc5)C4=O)C3=O)C2=O)C1=O 10.1016/j.ejmech.2016.02.046
142471846 191329 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5191532 191329 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
155553012 174086 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.7 pKi = 5.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
90665462 109230 0 None -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 -6 4 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
155541897 173055 0 None -5 2 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 4.7 pKi = 4.7 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
44309052 203947 0 None -109 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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 -109 5 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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
155557409 174663 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 427 8 2 4 4.8 NCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/C8MD00388B
CHEMBL4558708 174663 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 427 8 2 4 4.8 NCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/C8MD00388B
91809285 125762 0 None -186 6 Human 7.6 pKi = 7.6 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 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 -186 6 Human 7.6 pKi = 7.6 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 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
44308836 102791 0 None -616 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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 -616 5 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 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
91809276 125753 0 None -74 6 Human 7.6 pKi = 7.6 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 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 -74 6 Human 7.6 pKi = 7.6 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 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
44820563 26035 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCc1cnc[nH]1)C(=S)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1 10.1039/c1md00200g
CHEMBL1355048 26035 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 534 11 2 4 5.1 CN(CCCc1cnc[nH]1)C(=S)NCCCN(Cc1ccc(Cl)cc1)c1ccc(Br)cn1 10.1039/c1md00200g
10974426 96927 0 None - 1 Human 6.6 pKi = 6.6 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 680 20 2 9 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cnccn1 10.1021/jm0205088
CHEMBL266004 96927 0 None - 1 Human 6.6 pKi = 6.6 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 680 20 2 9 6.1 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cnccn1 10.1021/jm0205088
142471840 191843 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198961 191843 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL2372956 210322 0 None -51 4 Human 5.5 pKi = 5.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
142471665 191707 0 None 602 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5196971 191707 0 None 602 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 414 8 2 4 4.4 Fc1ccc2c(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
142471655 190425 0 None 562 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
CHEMBL5178013 190425 0 None 562 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 426 9 2 5 4.3 COc1ccc2[nH]cc(Cc3nnc(Cc4ccccc4)n3CCCc3c[nH]cn3)c2c1 10.1039/D1MD00044F
142471677 191949 0 None 1621 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200786 191949 0 None 1621 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.5 FC(F)(F)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
91809288 125764 0 None -18 6 Human 8.5 pKi = 8.5 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 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 -18 6 Human 8.5 pKi = 8.5 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 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
142471769 191785 0 None 301 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5198142 191785 0 None 301 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 456 10 2 6 4.3 COc1ccc(Cc2nnc(Cc3c[nH]c4ccc(OC)cc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
86293506 118819 0 None 229 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL3421842 118819 0 None 229 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 309 3 2 3 2.4 Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1 10.1021/ml500538a
CHEMBL1791306 208923 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
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/jm058184l
142471768 192004 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5201540 192004 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 435 9 2 5 4.4 N#Cc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10554930 100192 0 None 1 5 Human 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 5.5 pKi = 5.5 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
CHEMBL439136 213827 0 None -9 4 Human 6.5 pKi = 6.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
CHEMBL3349599 211428 0 None -1000 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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
CHEMBL3349604 211433 0 None -794 5 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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
24936235 121842 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
CHEMBL3589939 121842 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting method
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1016/j.ejmech.2018.11.030
2051 3576 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
5311430 3576 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
CHEMBL311695 3576 24 None -16595 9 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL None None None None 10.1021/jm980118e
24936235 121842 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
CHEMBL3589939 121842 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
ChEMBL 391 10 5 6 0.6 NCCCCCOC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)CN1CCc1c[nH]c2ccccc12 10.1039/C4MD00074A
168280615 190880 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 4 5.6 NCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5184884 190880 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 4 5.6 NCCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL437448 213719 0 None -208 5 Human 5.5 pKi = 5.5 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
142471703 191732 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5197218 191732 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 455 10 2 6 4.4 O=[N+]([O-])c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
11125276 100557 0 None - 1 Human 6.4 pKi = 6.4 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL291474 100557 0 None - 1 Human 6.4 pKi = 6.4 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
142471682 191514 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193951 191514 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
10166743 123946 0 None -47 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -47 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
142471893 190327 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
CHEMBL5176454 190327 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 516 12 2 5 6.1 c1ccc(COc2cccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)c2)cc1 10.1039/D1MD00044F
142471814 192162 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5203972 192162 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1ccccc1Cc1nnc(CCc2c[nH]c3ccccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
44385504 61048 0 None -9 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -9 5 Human 5.4 pKi = 5.4 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
13690207 115382 0 None -2041 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 -2041 5 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
86294248 118820 1 None 1023 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
CHEMBL3421843 118820 1 None 1023 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 298 3 2 4 1.4 Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21 10.1021/ml500538a
142471737 190304 0 None 77 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
CHEMBL5176020 190304 0 None 77 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 1 5 5.8 Cn1cc(CCc2nnc(Cc3ccc(Cl)c(Cl)c3)n2CCCc2c[nH]cn2)c2ccccc21 10.1039/D1MD00044F
10553122 34052 0 None 1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 490 12 2 5 4.9 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142492 34052 0 None 1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 490 12 2 5 4.9 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
9959684 33947 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 566 7 2 4 5.6 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm980118e
CHEMBL142402 33947 0 None 2 2 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 566 7 2 4 5.6 S=C(NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)N1CCC(c2c[nH]cn2)CC1 10.1021/jm980118e
10505242 33842 0 None -1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 489 9 3 4 4.4 NCCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142321 33842 0 None -1 2 Human 5.4 pKi = 5.4 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 489 9 3 4 4.4 NCCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL264028 210603 0 None -24 5 Human 6.4 pKi = 6.4 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
51003591 56755 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to human SSTR4Binding affinity to human SSTR4
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 5.4 pKi = 5.4 Binding
Binding affinity to human SSTR4Binding affinity to human SSTR4
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
51003591 56755 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.4 pKi = 5.4 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.4 pKi = 5.4 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
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 5.4 pKi = 5.4 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
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
155546826 173649 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 396 8 2 4 4.1 c1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
CHEMBL4534401 173649 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 396 8 2 4 4.1 c1ccc(Cn2c(CCc3c[nH]cn3)nnc2CCc2c[nH]c3ccccc23)cc1 10.1039/C8MD00388B
86292350 118821 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
CHEMBL3421844 118821 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 303 3 2 4 1.8 CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12 10.1021/ml500538a
10602230 33967 0 None 1 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 526 9 3 4 4.6 S=C(NCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142422 33967 0 None 1 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 526 9 3 4 4.6 S=C(NCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10578474 34187 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 543 10 2 4 5.1 S=C(NCCCN1CCCC1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142613 34187 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 543 10 2 4 5.1 S=C(NCCCN1CCCC1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
155555535 174441 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cc2nnc(CCc3c[nH]cn3)n2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
CHEMBL4553349 174441 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method
ChEMBL 464 8 2 4 5.4 Clc1ccc(Cc2nnc(CCc3c[nH]cn3)n2CCc2c[nH]c3ccccc23)cc1Cl 10.1039/C8MD00388B
90665459 109259 0 None 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 4 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
142471716 191492 0 None 208 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5193686 191492 0 None 208 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 5 4.4 COc1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
142471767 192282 0 None 1348 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5205904 192282 0 None 1348 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 444 9 2 4 5.1 Clc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL442494 213913 0 None -17 5 Human 8.3 pKi = 8.3 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
142471772 191178 0 None 870 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5189042 191178 0 None 870 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 9 2 4 5.3 Brc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL1823873 209032 9 None -18 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human SSTR4 expressed in CHO-K1 cellsDisplacement of [125I]-somatostatin from human SSTR4 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
100930865 34791 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
44362068 34791 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
CHEMBL143100 34791 0 None 91 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 488 12 2 4 4.5 C/S(=N/CCCc1c[nH]cn1)NCCCN(Cc1ccc(Br)cc1)c1ccccn1 10.1021/jm980118e
10580397 99315 0 None 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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 1 5 Human 6.3 pKi = 6.3 Binding
Binding affinity for human receptor subtype hSSTR4.Binding affinity for human receptor subtype hSSTR4.
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
CHEMBL3349602 211431 0 None -1258 5 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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
10094509 130686 0 None -138 5 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -138 5 Human 5.3 pKi = 5.3 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
142471828 192072 0 None 134 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5202717 192072 0 None 134 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 478 9 2 4 5.8 Clc1cc(Cl)cc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10769191 33792 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 557 11 2 4 5.5 S=C(NCCCN1CCCC1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL142283 33792 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 557 11 2 4 5.5 S=C(NCCCN1CCCC1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
10841338 34107 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 602 10 3 4 7.3 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1cccc(-c2c[nH]cn2)c1 10.1021/jm980118e
CHEMBL142549 34107 0 None 3 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 602 10 3 4 7.3 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1cccc(-c2c[nH]cn2)c1 10.1021/jm980118e
10531093 168264 0 None 10 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 3 4 5.8 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL433872 168264 0 None 10 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 568 12 3 4 5.8 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1021/jm980118e
11828523 195005 0 None - 1 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
CHEMBL54832 195005 0 None - 1 Human 7.3 pKi = 7.3 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 669 20 3 9 5.5 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2cnc[nH]2)[C@@H](OCc2ccccc2)[C@@H]1OCc1cccnc1 10.1021/jm0205088
155565048 175501 0 None -1 2 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
122181226 121845 0 None 1 2 Human 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
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 5.3 pKi = 5.3 Binding
Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4Inhibition of radiolabeled somatostatin-14 binding to human recombinant SSTR4
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
142471733 190565 0 None 75 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
CHEMBL5180116 190565 0 None 75 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 394 7 2 4 4.4 CC(C)(C)Cc1nnc(Cc2c[nH]c3cc(F)ccc23)n1CCCc1c[nH]cn1 10.1039/D1MD00044F
11050695 195484 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccncc1 10.1021/jm0205088
CHEMBL55298 195484 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccncc1 10.1021/jm0205088
CHEMBL2369734 209662 0 None -8 5 Human 6.2 pKi = 6.2 Binding
Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 receptor expressed on CHO cellsAbility to displace [125 I]labelled Tyr11-somatostatin from human hsst-4 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
168295000 192472 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208764 192472 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 474 9 2 6 3.7 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
56651207 175897 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 6.2 pKi = 6.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
44385712 60344 0 None -8 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -8 4 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
90644981 111813 0 None -660 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
CHEMBL3287613 111813 0 None -660 4 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation countingDisplacement of [125I]SS14 from human SST4 expressed in CHO membrane after 60 to 90 mins by scintillation counting
ChEMBL 365 5 3 2 4.1 O=C(N[C@@H]1CCCC[C@@H]1NCc1c[nH]c2ccccc12)c1ccc(F)cc1 10.1021/ml500079u
9893924 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
CHEMBL103769 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting methodDisplacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting method
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1039/C8MD00388B
9893924 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL103769 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
9893924 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm0108449
CHEMBL103769 4748 34 None 52 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm0108449
168283525 191087 0 None 851 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5187631 191087 0 None 851 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 439 8 2 5 4.3 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL1791304 208921 0 None -25 2 Human 7.2 pKi = 7.2 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
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](Cc2cnccn2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
91809284 125761 0 None -288 6 Human 7.2 pKi = 7.2 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 -288 6 Human 7.2 pKi = 7.2 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
91809277 125754 0 None -204 6 Human 7.2 pKi = 7.2 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 -204 6 Human 7.2 pKi = 7.2 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
CHEMBL3349603 211432 0 None -999 5 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cellsBinding affinity towards human Somatostatin receptor type 4 (sst4) using Tyr11-[125I]-SRIF as radioligand was determined in CHO cells
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
168283125 191077 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
CHEMBL5187484 191077 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 441 9 2 4 5.2 NCCCCn1c(CCc2c[nH]c3ccccc23)nnc1Cc1ccc(Cl)c(Cl)c1 10.1039/D1MD00044F
2055 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
383414 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
90488715 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL1680 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
CHEMBL262746 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
DB00104 2907 48 None -501 14 Human 7.2 pKi = 7.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL None None None None 10.1039/C8MD00388B
44386389 130083 0 None -13 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -13 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
CHEMBL406738 212618 0 None -8 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
10887003 194713 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 697 20 2 8 6.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(F)nc1 10.1021/jm0205088
CHEMBL53440 194713 0 None - 1 Human 6.2 pKi = 6.2 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 697 20 2 8 6.9 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccc(F)nc1 10.1021/jm0205088
155528330 171340 0 None 1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.2 pKi = 5.2 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
CHEMBL2372959 210325 0 None -2 5 Human 6.2 pKi = 6.2 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
9827283 78588 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 499 9 4 3 4.1 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
CHEMBL2112223 78588 0 None -147 4 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human sst4 receptor expressed in CHO-K1 cellsBinding affinity towards human sst4 receptor expressed in CHO-K1 cells
ChEMBL 499 9 4 3 4.1 NCCCCCNC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/jm980194h
44820544 52404 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 396 9 4 4 2.5 S=C(NCCCNc1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1039/c1md00200g
CHEMBL1590268 52404 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human SST4 receptorBinding affinity to human SST4 receptor
ChEMBL 396 9 4 4 2.5 S=C(NCCCNc1ccc(Br)cn1)NCCCc1c[nH]cn1 10.1039/c1md00200g
142471923 191911 0 None 512 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5200112 191911 0 None 512 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 488 10 2 6 3.9 CS(=O)(=O)c1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
168271446 190605 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5180752 190605 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 421 8 2 5 4.2 N#Cc1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
91809303 125778 0 None -22 6 Human 8.1 pKi = 8.1 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 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 -22 6 Human 8.1 pKi = 8.1 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 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
142471692 192382 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
CHEMBL5207543 192382 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 440 10 2 5 4.5 COc1cccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1 10.1039/D1MD00044F
10554498 31289 0 None 4 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 540 10 3 4 5.0 S=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL140151 31289 0 None 4 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 540 10 3 4 5.0 S=C(NCCCc1c[nH]cn1)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
117711399 118822 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL3421845 118822 0 None 104 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 minsDisplacement of [3-125l-Tyr]-somatostatin-(1 -14) from human recombinant somatostatin 4 receptor expressed in CHO cell membranes incubated for 180 mins
ChEMBL 310 3 2 4 1.8 Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1 10.1021/ml500538a
CHEMBL1791305 208922 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
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](Cc2cnccn2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
10528970 34432 0 None 4 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 2 5 4.0 S=C(NCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL142822 34432 0 None 4 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 486 11 2 5 4.0 S=C(NCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
10720221 35089 0 None 1 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 500 12 2 5 4.4 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
CHEMBL143367 35089 0 None 1 2 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 500 12 2 5 4.4 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCn1ccnc1 10.1021/jm980118e
127032865 138761 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 393 6 1 3 5.4 NCCCc1cc(Cl)cc2c1OC(CCc1cccc3ccccc13)CC2=O 10.1016/j.ejmech.2016.02.046
CHEMBL3780496 138761 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting methodDisplacement of [125I]tyr11-SRIF from human sst4 receptor after 60 mins by liquid scintillation counting method
ChEMBL 393 6 1 3 5.4 NCCCc1cc(Cl)cc2c1OC(CCc1cccc3ccccc13)CC2=O 10.1016/j.ejmech.2016.02.046
44385652 60392 0 None -28 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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 -28 5 Human 5.2 pKi = 5.2 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
2070 697 5 None -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) 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 -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) 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 -11220 4 Human 5.2 pKi = 5.2 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](Cc2c1[nH]c1c2cccc1)c1ncc([nH]1)c1ccccc1 10.1021/jm0108449
44361984 34419 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 510 12 2 3 5.7 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCc1ccccc1 10.1021/jm980118e
CHEMBL142811 34419 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 510 12 2 3 5.7 S=C(NCCCCN(Cc1ccc(Br)cc1)c1ccccn1)NCCCc1ccccc1 10.1021/jm980118e
10793795 35219 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 605 9 2 4 7.5 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
CHEMBL143539 35219 0 None - 1 Human 4.2 pKi = 4.2 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 605 9 2 4 7.5 S=C(NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)Nc1ccc(N2CCCCC2)cc1 10.1021/jm980118e
168286554 191403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5192578 191403 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 324 6 2 4 2.8 Fc1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
90665460 109260 0 None -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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 -3 5 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 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
155529288 171397 0 None 1 2 Human 5.1 pKi = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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 5.1 pKi = 5.1 Binding
Displacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 expressed in African green monkey COS1 cell membranes after 2 hrs by scintillation counting methodDisplacement of [125I]somatostatin-14 (Tyr11) from human SSTR4 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
44377555 57531 0 None -12 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
CHEMBL166247 57531 0 None -12 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
ChEMBL 384 5 1 5 5.2 NCCCc1nc(-c2csc3ccccc23)cn2cc(-c3ccccc3)nc12 10.1016/s0960-894x(01)00051-8
71458043 78903 0 None -6 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
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 -6 5 Human 5.1 pKi = 5.1 Binding
Inhibitory constant on human somatostatin receptor 4Inhibitory constant on human somatostatin receptor 4
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
CHEMBL410181 212805 0 None -2 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
44397389 124044 0 None -43 5 Human 7.1 pKi = 7.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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 -43 5 Human 7.1 pKi = 7.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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
CHEMBL1791304 208921 0 None -25 2 Human 7.1 pKi = 7.1 Binding
Inhibition of human somatostatin receptor type 4 (n=5)Inhibition of human somatostatin receptor type 4 (n=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](Cc2cnccn2)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O 10.1021/jm058184l
CHEMBL2369719 209657 0 None -3 2 Human 7.1 pKi = 7.1 Binding
Inhibition of human somatostatin receptor type 4Inhibition of human somatostatin receptor type 4
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/jm058184l
168297256 192411 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
CHEMBL5208037 192411 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 492 9 2 6 3.8 CS(=O)(=O)c1ccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)cc1 10.1039/D1MD00044F
11705763 168315 0 None -2089 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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 -2089 5 Human 6.1 pKi = 6.1 Binding
Binding affinity against human sst4 receptor at a dose of 10 uMBinding affinity against human sst4 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
10768264 34853 0 None 2 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 10 2 4 5.0 CN(C)CCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
CHEMBL143164 34853 0 None 2 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 517 10 2 4 5.0 CN(C)CCC/N=C(\S)NCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.1021/jm980118e
15965425 2206 7 None -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
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 -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
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 -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity to human somatostatin receptor type 4Binding affinity to human somatostatin receptor type 4
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 -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
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 -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
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 -8128 5 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Somatostatin receptor type 4 (hsst4)Binding affinity towards Somatostatin receptor type 4 (hsst4)
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
168274078 190288 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 320 7 2 4 2.9 c1ccc2c(CCc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5175762 190288 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 320 7 2 4 2.9 c1ccc2c(CCc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
44363816 39675 0 None -22 5 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)
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 -22 5 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)In vitro binding affinity was evaluated against human Somatostatin receptor type 4 (hSSTR-4)
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
CHEMBL407496 212665 0 None -27 5 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
CHEMBL2372964 210330 0 None -6 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
10963480 100767 0 None - 1 Human 6.1 pKi = 6.1 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccn1 10.1021/jm0205088
CHEMBL292906 100767 0 None - 1 Human 6.1 pKi = 6.1 Binding
Tested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligandTested for binding affinity at human Somatostatin receptor type 4 using ([3-125I-Tyr11)]-SRIF-14 as the radioligand
ChEMBL 679 20 2 8 6.7 NCCCCCOC[C@H]1O[C@@H](OCCc2c[nH]c3ccccc23)[C@H](OCc2ccccc2)[C@@H](OCc2ccccc2)[C@@H]1OCc1ccccn1 10.1021/jm0205088
CHEMBL2372961 210327 0 None -74 4 Human 6.1 pKi = 6.1 Binding
The compound was tested for binding affinity against human Somatostatin receptor type 4The compound was tested for binding affinity against human Somatostatin receptor type 4
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
91809275 125752 0 None -776 6 Human 7.0 pKi = 7.0 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 -776 6 Human 7.0 pKi = 7.0 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
142471746 190714 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 486 10 2 4 6.2 c1ccc(-c2ccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)cc2)cc1 10.1039/D1MD00044F
CHEMBL5182380 190714 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 486 10 2 4 6.2 c1ccc(-c2ccc(Cc3nnc(CCc4c[nH]c5ccccc45)n3CCCc3c[nH]cn3)cc2)cc1 10.1039/D1MD00044F
11800917 35113 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1c[nH]cn1 10.1021/jm980118e
CHEMBL143409 35113 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligandIn vitro binding affinity at somatostatin receptor 4 in transfected BHK cells using [125 I]Tyr11-SRIF-14 as radioligand
ChEMBL 554 11 3 4 5.4 S=C(NCCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1)NCCc1c[nH]cn1 10.1021/jm980118e
11112736 16529 0 None -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) 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 -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) 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 -8128 3 Human 5.0 pKi = 5.0 Binding
Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtypeInhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype
ChEMBL 426 8 3 2 7.0 CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 10.1021/jm0108449
CHEMBL2370166 209805 0 None -120 5 Human 6.0 pKi = 6.0 Binding
In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) expressed in CHO-K1 cells.In vitro inhibition of radioligand binding to human somatostatin receptor (hsst4) 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
168271928 190083 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
CHEMBL5172730 190083 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysisDisplacement of [125I]-Tyr-SRIF 14 from human SST4 receptor expressed in membrane measured after 90 mins by gamma counting analysis
ChEMBL 306 6 2 4 2.7 c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1 10.1039/D1MD00044F
2078 621 0 None -1 2 Mouse 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
73755026 621 0 None -1 2 Mouse 7.4 pKd = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
2078 621 0 None 1 2 Human 7.6 pKd = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
73755026 621 0 None 1 2 Human 7.6 pKd = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12595949
2055 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF 1 14 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -501 14 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-somatostatin-14 -9 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
None 216349 0 Functional 537 5 Human 9.7 pKi = 9.7 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
16161315 216096 0 UNDEFINED -9 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-SST-28 -9 12 Human 9.3 pKi = 9.3 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 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 1 14 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-SRIF-14 -9 12 Human 9.2 pKi = 9.2 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 216349 0 125I-LTT-SST-28 537 5 Human 9.2 pKi = 9.2 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 537 5 Human 9.2 pKi = 9.2 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
16161315 216096 0 125I-CGP23996 -18 12 Rat 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-Tyr11-somatostatin -18 12 Rat 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 -9 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-Tyr11-SRIF -9 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
16161315 216096 0 125I-Tyr11-SRIF -9 12 Mouse 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
16161315 216096 0 125I-LTT-SRIF28 -9 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
16161315 216096 0 125I-SRIF-28 -9 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
16161315 216096 0 125I-SOMATOSTATIN 14 -9 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
16161315 216096 0 125I-SRIF -9 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
16161315 216096 0 125I-CGP23996 -9 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
2055 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -501 14 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-SRIF -9 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
16161315 216096 0 125I-LTT-SST-28 -9 12 Human 8.8 pKi = 8.8 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-LTT-SST-28 -9 12 Human 8.8 pKi = 8.8 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-SOMATOSTATIN -9 12 Human 8.8 pKi = 8.8 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 -9 12 Human 8.8 pKi = 8.8 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
2055 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SOMATOSTATIN 14 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-SRIF-28 -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 UNDEFINED -501 14 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -3090 14 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-SOMATOSTATIN -1288 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 216097 0 125I-SRIF -1288 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 216097 0 125I-SRIF-28 -1288 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 216097 0 125I-Tyr11-SRIF -6025 11 Mouse 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
2247 505 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 81 UNDEFINED -5754 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
46882665 5632 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
CHEMBL1077721 5632 0 UNDEFINED -15 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cccnc4o3)CC2)ccc1OC None
46882666 5633 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
CHEMBL1077722 5633 0 UNDEFINED -13 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOc1cc(CN2CCC(Nc3nc4ccncc4o3)CC2)ccc1OC None
46882746 5637 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
CHEMBL1077742 5637 0 UNDEFINED -21 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 1 6 3.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC None
24740861 5678 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
CHEMBL1077877 5678 0 UNDEFINED -20 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 399 8 1 6 4.3 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCCF None
46882789 5679 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
CHEMBL1077887 5679 0 UNDEFINED -19 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C(F)(F)F None
46882181 5681 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
CHEMBL1077908 5681 0 UNDEFINED -50 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 536 10 2 8 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5ccccc5)ccc4o3)CC2)ccc1OC None
46882790 5702 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
CHEMBL1078081 5702 0 UNDEFINED -18 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 407 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC1CC1 None
46882620 5715 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
CHEMBL1078215 5715 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 465 8 1 7 5.2 CCOc1cc(CN2CCC(Nc3nc4cc(OC(F)(F)F)ccc4o3)CC2)ccc1OC None
46882664 5717 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
CHEMBL1078240 5717 0 UNDEFINED -28 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 494 8 2 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1OC None
46882621 5723 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
CHEMBL1078283 5723 0 UNDEFINED -28 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 438 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4cc(NC(C)=O)ccc4o3)CC2)ccc1OC None
46882831 5744 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
CHEMBL1078449 5744 0 UNDEFINED -301 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 410 8 2 7 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1N None
46882832 5746 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
CHEMBL1078450 5746 0 UNDEFINED -64 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 467 10 1 8 4.9 CCOC(=O)c1c(OCC)cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC None
11848626 5747 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
CHEMBL1078451 5747 0 UNDEFINED -56 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OCC)c1F None
46882622 5762 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
CHEMBL1078528 5762 0 UNDEFINED -44 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 488 9 1 8 3.6 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)ccc1OC None
11848625 5792 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1078745 5792 0 UNDEFINED -107 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 451 8 1 7 4.9 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882708 5803 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL1078841 5803 0 UNDEFINED -26 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 6 4.3 CCNc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
11848833 5807 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
CHEMBL1078895 5807 0 UNDEFINED -323 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 423 8 1 6 5.5 CC(C)Oc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc(OC(C)C)c1 None
46882133 5808 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
CHEMBL1078896 5808 0 UNDEFINED -54 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 478 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(NC(=O)C5CCC5)ccc4o3)CC2)ccc1OC None
46882445 5811 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
CHEMBL1078903 5811 0 UNDEFINED -30 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOc1cc(N2CCC(Nc3nc4ccccc4s3)CC2)ccc1OC None
46882180 5841 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
CHEMBL1079180 5841 0 UNDEFINED -39 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 482 7 2 7 3.7 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)ccc1F None
46882577 5857 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
CHEMBL1079312 5857 1 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 415 7 1 6 5.0 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)ccc4o3)CC2)ccc1OC None
46882578 5858 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
CHEMBL1079313 5858 0 UNDEFINED -51 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 1 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)ccc1OC None
46882579 5859 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
CHEMBL1079314 5859 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 426 8 1 8 4.2 CCOc1cc(CN2CCC(Nc3nc4cc([N+](=O)[O-])ccc4o3)CC2)ccc1OC None
46882182 5921 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
CHEMBL1079686 5921 0 UNDEFINED -190 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 567 11 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)N(C)C)ccc4o3)CC2)cc(OCC)c1-n1cccc1 None
16062555 5956 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1079874 5956 0 UNDEFINED -562 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 457 9 2 7 4.5 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F None
11848835 6063 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
CHEMBL1080584 6063 0 UNDEFINED -1258 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 456 9 2 7 3.9 CCOc1cc(CN2CCC(Nc3nc4cc(C(N)=O)ccc4o3)CC2)cc(OCC)c1F None
16062816 6064 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
CHEMBL1080585 6064 0 UNDEFINED -3311 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 473 9 2 7 5.1 CCOc1cc(CN2CCC(Nc3nc4cc(C(=O)O)ccc4o3)CC2)cc(OCC)c1Cl None
16062553 6065 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
CHEMBL1080586 6065 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 7 2 6 4.7 CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl None
46882225 6147 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
CHEMBL1080950 6147 0 UNDEFINED -39 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 526 9 2 8 4.1 CCOc1cc(CN2CCC(Nc3nc4cc(Cl)c(S(N)(=O)=O)cc4o3)CC2)cc(OCC)c1F None
46882226 6148 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
CHEMBL1080951 6148 0 UNDEFINED -41 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 419 6 1 5 5.6 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4o3)CC2)ccc1Cl None
46882227 6176 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
CHEMBL1081133 6176 0 UNDEFINED -57 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 540 10 2 10 3.8 CCOc1cc(CN2CCC(Nc3nc4cc(NS(=O)(=O)c5cn(C)cn5)ccc4o3)CC2)ccc1OC None
46882517 6215 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
CHEMBL1081317 6215 0 UNDEFINED -32 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 398 7 1 7 4.2 CCOc1cc(CN2CCC(Nc3nc4cccnc4s3)CC2)ccc1OC None
46882224 6348 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
CHEMBL1082036 6348 0 UNDEFINED -181 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 543 10 1 9 4.7 CCOc1cc(CN2CCC(Nc3nc4cc(S(=O)(=O)CC)ccc4o3)CC2)cc(OC2CCOCC2)c1 None
46882516 6349 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
CHEMBL1082040 6349 0 UNDEFINED -27 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 431 7 1 6 5.4 CCOc1cc(CN2CCC(Nc3nc4ccc(Cl)cc4s3)CC2)ccc1OC None
11848624 89146 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL236587 89146 0 UNDEFINED -245 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 7 1 6 4.3 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740752 89147 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
CHEMBL236588 89147 0 UNDEFINED -436 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 4.9 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OCC(C)C None
24740863 89158 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
CHEMBL236610 89158 0 UNDEFINED -134 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 1 5 5.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1Cl None
24740864 89159 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
CHEMBL236611 89159 0 UNDEFINED -269 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 365 6 1 5 4.6 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1C None
11848679 89244 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
CHEMBL236788 89244 0 UNDEFINED -776 6 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 489 9 3 9 2.9 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)cc(OCC)c1N None
24740750 89707 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
CHEMBL237660 89707 0 UNDEFINED -151 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 6 4.0 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1O None
24740753 146117 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
CHEMBL391951 146117 0 UNDEFINED -33 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 8 1 6 4.7 CCCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC None
24740751 147881 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
CHEMBL393333 147881 0 UNDEFINED -120 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 421 7 1 6 5.2 COc1ccc(CN2CCC(Nc3nc4ccccc4o3)CC2)cc1OC1CCCC1 None
24740862 148008 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
CHEMBL393436 148008 0 UNDEFINED -51 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 6 1 5 4.4 CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1F None
11848677 148352 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
CHEMBL393718 148352 0 UNDEFINED -32 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 460 8 2 8 3.0 CCOc1cc(CN2CCC(Nc3nc4cc(S(N)(=O)=O)ccc4o3)CC2)ccc1OC None
None 216348 0 125I-LTT-SST-28 -245 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 216495 0 125I-LTT-SST-28 -19952 5 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase None None None None None
None 217624 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 383 6 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)C3=NC4=CC=CC=C4S3)OC None
None 217625 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 1 6 4.8 CCOC1=C(C=CC(=C1)NC2CCN(CC2)CC3=NC4=CC=CC=C4S3)OC None
None 217626 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 425 7 1 6 4.6 CCOC1=C(C=CC(=C1)CN2CCC(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 217627 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 397 7 2 6 5.5 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NC3=NC4=CC=CC=C4S3)OC None
None 217628 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 411 8 2 6 5.2 CCOC1=C(C=CC(=C1)NC2CCC(CC2)NCC3=NC4=CC=CC=C4S3)OC None
None 217629 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 412 5 1 6 4.1 CCOC1=C(C=CC(=C1)N2CCN(CC2)C(=O)NC3=NC4=CC=CC=C4S3)OC None
None 217630 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 405 8 2 6 6.1 CCOC1=C(C=CC(=C1)NCC2=CC(=CC=C2)NC3=NC4=CC=CC=C4S3)OC None
None 217631 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=C(O3)C=CC=N4)OC None
None 217632 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 380 7 2 5 4.0 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4N3)OC None
None 217633 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 382 7 1 7 3.7 CCOC1=C(N=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC None
None 217634 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 409 8 1 6 5.1 CCOC1=C(C=CC(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)OC(C)C None
None 217635 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 413 8 1 6 4.8 CCOC1=CC(=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCC None
None 217636 0 UNDEFINED -1 3 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 429 9 2 7 3.8 CCOC1=C(C=C(C(=C1)CN2CCC(CC2)NC3=NC4=CC=CC=C4O3)F)OCCO None
2054 3974 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-CGP23996 -446 11 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-LTT-SST-28 -1288 11 Human 6.9 pKi = 6.9 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
13105142 216098 0 UNDEFINED -23442 5 Human 6.9 pKi = 6.9 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-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF-28 -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SRIF -446 11 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216346 0 125I-Tyr11-somatostatin-14 -57 8 Human 7.8 pKi = 7.8 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 -57 8 Human 7.8 pKi = 7.8 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
2054 3974 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr11-SRIF -575 11 Mouse 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr10-CST14 -501 14 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216346 0 125I-SOMATOSTATIN -57 8 Human 6.8 pKi = 6.8 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
2055 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-SRIF -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr11-SRIF -18 12 Rat 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-Tyr11-SRIF -9 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
2055 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SST-28 -501 14 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-Tyr10-CST14 -446 11 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216347 0 125I-LTT-SST-28 -6165 5 Human 6.5 pKi = 6.5 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 -6165 5 Human 6.5 pKi = 6.5 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 216097 0 125I-Tyr11-SRIF -1288 11 Human 5.5 pKi = 5.5 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-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-SOMATOSTATIN -446 11 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-LTT-SRIF28 -501 14 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase None None None None None
16161315 216096 0 125I-Tyr10-CST14 -9 12 Human 8.4 pKi = 8.4 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
13105142 216098 0 125I-LTT-SRIF28 -23442 5 Human 5.4 pKi = 5.4 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-LTT-SRIF28 -23442 5 Human 5.4 pKi = 5.4 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-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
2054 3974 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SST-28 -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 UNDEFINED -446 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-LTT-SST-28 -1288 11 Human 5.3 pKi = 5.3 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
None 216097 0 125I-CGP23996 -38 11 Rat 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
2054 3974 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
71306 3974 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL264186 3974 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL3349523 3974 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
DB04894 3974 15 125I-LTT-SRIF28 -446 11 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase None None None None None
2055 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
383414 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
90488715 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL1680 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
CHEMBL262746 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
DB00104 2907 48 None -501 14 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysisDisplacement of [125I]-somatostatin from human sst4 receptor after 2 hrs by beta scintillation counting analysis
Drug Central None None None None None
None 216097 0 125I-LTT-SST-28 -1288 11 Human 8.2 pKi = 8.2 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
16161315 216096 0 125I-Tyr11-SRIF -18 12 Rat 8.2 pKi = 8.2 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
2031 2273 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
71349 2273 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB06791 2273 0 UNDEFINED -112 9 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216097 0 125I-Tyr11-SRIF -1288 11 Human 8.1 pKi = 8.1 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 -38 11 Rat 8.1 pKi = 8.1 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
2055 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-Tyr11-somatostatin-14 -501 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase None None None None None
13105142 216098 0 125I-Tyr10-CST14 -23442 5 Human 5.1 pKi = 5.1 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
None 216350 0 125I-LTT-SST-28 -112 5 Human 7.1 pKi = 7.1 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 -112 5 Human 7.1 pKi = 7.1 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 216348 0 125I-LTT-SST-28 -245 5 Human 5.1 pKi = 5.1 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 -245 5 Human 5.1 pKi = 5.1 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
16161315 216096 0 None -9 12 Human 8.0 pKi = 8.0 Binding
Inhibition of human sst4 receptor expressed in CHO cellsInhibition of human sst4 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
13105142 216098 0 125I-CGP23996 -23442 5 Human 5.0 pKi = 5.0 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 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
383414 2907 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
90488715 2907 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL1680 2907 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
CHEMBL262746 2907 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
DB00104 2907 48 125I-CGP23996 -501 14 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase None None None None None
2028 1506 0 None -398 6 Human 5.9 pKi = 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
2014 2214 0 None -35 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2014 2214 0 None -35 9 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2040 648 0 None -6 4 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
3513 2845 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
5311371 2845 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
CHEMBL1474351 2845 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 538 11 3 4 5.2 O=C(NCCCc1cnc[nH]1)NCCCN(c1ccc(cn1)Br)Cc1ccc(c(c1)Cl)Cl 9822540
2004 642 0 None -4 7 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2069 652 0 None 1 2 Human 8.5 pKi = 8.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16130961 891 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16130961 891 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2005 891 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2005 891 0 None -2 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2007 1170 0 None -6 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2007 1170 0 None -6 6 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
10115 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
11442741 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
CHEMBL4451852 2110 14 None - 1 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 468 10 4 5 1.4 NCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NS(=O)(=O)c1ccc(c2c1cccc2)C 15333679
2082 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
5311374 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
CHEMBL1450103 2259 14 None 7079 2 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 485 11 4 4 3.1 COC(=O)[C@@H](NC(=O)CCCc1c([nH]c2c1cc(F)cc2F)c1ccccc1)CCCN=C(N)N 9784130
154734381 217714 0 None -1 8 Human 8.1 pKi None 8.1 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
2066 3166 0 None -79 4 Human 6.0 pKi None 6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10354394
2029 2375 0 None -79 6 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12616335
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
16133849 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2020 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
91935900 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL501796 3676 12 None -15 9 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
2019 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
44386062 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11520208
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15333679
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7988476
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8769372
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9600011
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9724791
CHEMBL440072 3675 0 None -4 10 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9784130
2008 1211 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10598788
2008 1211 0 None -1 6 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9650799