Ligand source activities (1 row/activity)





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56841989 213420 6 None -3 6 Human 8.8 pEC50 = 8.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -3 6 Human 8.8 pEC50 = 8.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
56841989 213420 6 None -3 6 Human 8.8 pEC50 = 8.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -3 6 Human 8.8 pEC50 = 8.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4288294 213478 0 None -3 2 Human 7.0 pEC50 = 7 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3099727 211026 0 None -30 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)O[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
162676875 183572 0 None -1995 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assay
ChEMBL 4218 130 63 56 -15.0 CC(C)C[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c00740
CHEMBL4800389 183572 0 None -1995 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assay
ChEMBL 4218 130 63 56 -15.0 CC(C)C[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c00740
CHEMBL4277676 213375 0 None -31 3 Human 6.8 pEC50 = 6.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None -100 4 Human 6.8 pEC50 = 6.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277676 213375 0 None -31 3 Human 6.8 pEC50 = 6.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None -100 4 Human 6.8 pEC50 = 6.8 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3099723 211022 0 None -2 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL3099722 211021 0 None -85 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)O[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL4284905 213450 0 None -12 4 Human 8.6 pEC50 = 8.6 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4284905 213450 0 None -12 4 Human 8.6 pEC50 = 8.6 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL2110365 209213 4 None -213 3 Human 5.7 pEC50 = 5.7 Functional
Agonist potency for the inhibition of Forskolin stimulated cAMP synthesis in cells expressing cloned Y5 receptorsAgonist potency for the inhibition of Forskolin stimulated cAMP synthesis in cells expressing cloned Y5 receptors
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
CHEMBL4280392 213406 0 None -31 4 Human 6.6 pEC50 = 6.6 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 213406 0 None -31 4 Human 6.6 pEC50 = 6.6 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3099721 211020 0 None -95 4 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL4277590 213373 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
12607 3784 42 None -79 4 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
16033 3784 42 None -79 4 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
CHEMBL3559801 3784 42 None -79 4 Human 8.5 pEC50 = 8.5 Functional
Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)Positive allosteric modulation of human C-terminal eYFP-fused human NY5 receptor expressed in African green monkey COS7 cells co-expressing delta6Galphaqi4-myr assessed as potentiation of neuropeptide Y-mediated Ca2+ flux by measuring pancreatic polypeptide EC50 at 30 uM treated at 20 secs post baseline detection followed by addition of neuropeptide Y after 140 secs by Fluo2-AM fluorescent dye-based assay (Rvb = 8.5 +/- 0.1 No_unit)
ChEMBL 248 2 1 2 3.7 CC(C)(C)C1=CC=C(C=C1)OC2CCCCC2O 10.1021/acs.jmedchem.7b00976
CHEMBL4277590 213373 0 None -1 3 Human 8.5 pEC50 = 8.5 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279973 213401 0 None -19 4 Human 8.4 pEC50 = 8.4 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL3099724 211023 0 None -35 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL4294418 213531 0 None -199 2 Human 6.4 pEC50 = 6.4 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4279973 213401 0 None -19 4 Human 8.4 pEC50 = 8.4 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294418 213531 0 None -199 2 Human 6.4 pEC50 = 6.4 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL439904 213854 13 None -72 4 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assayAgonist activity at NPY5R (unknown origin) by CRE-luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.0c00740
CHEMBL3099724 211023 0 None -35 4 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
CHEMBL4276961 213368 0 None -50 4 Human 8.3 pEC50 = 8.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 213464 0 None -31 4 Human 8.3 pEC50 = 8.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4276961 213368 0 None -50 4 Human 8.3 pEC50 = 8.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 213464 0 None -31 4 Human 8.3 pEC50 = 8.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4285633 213457 0 None -6 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294277 213530 0 None -5 3 Human 7.3 pEC50 = 7.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4285633 213457 0 None -6 2 Human 7.3 pEC50 = 7.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294277 213530 0 None -5 3 Human 7.3 pEC50 = 7.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 213413 0 None -63 2 Human 6.3 pEC50 = 6.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 213413 0 None -63 2 Human 6.3 pEC50 = 6.3 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4278700 213390 0 None -31 4 Human 8.2 pEC50 = 8.2 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4278700 213390 0 None -31 4 Human 8.2 pEC50 = 8.2 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL429531 213537 15 None -29 2 Human 8.1 pEC50 = 8.1 Functional
Agonist potency for the inhibition of Forskolin stimulated cAMP synthesis in cells expressing cloned Y5 receptorsAgonist potency for the inhibition of Forskolin stimulated cAMP synthesis in cells expressing cloned Y5 receptors
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm010031k
CHEMBL4279794 213399 0 None -7 4 Human 8.1 pEC50 = 8.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 213513 0 None -7 4 Human 8.1 pEC50 = 8.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4279794 213399 0 None -7 4 Human 8.1 pEC50 = 8.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 213513 0 None -7 4 Human 8.1 pEC50 = 8.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282168 213429 0 None -158 2 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None -158 3 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282168 213429 0 None -158 2 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None -158 3 Human 6.1 pEC50 = 6.1 Functional
Activation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assayActivation of human Y5R expressed in HEK293 cells assessed as inhibition of isoproterenol-induced increase in intracellular cAMP levels by calcium 5 dye-based FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL439904 213854 13 None -72 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assayAgonist activity at human NPYY5 receptor expressed in HEK293 cells assessed as decrease in isoproterenol-induced cAMP level measured every 30 secs for 360 secs by FLIPR assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1021/ml400335g
22253974 65977 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 6 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836324 65977 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 6 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
44271559 98157 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 418 7 2 6 5.1 CCS(=O)(=O)Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL273811 98157 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 418 7 2 6 5.1 CCS(=O)(=O)Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
9908801 65972 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 5 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836319 65972 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 5 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
44271542 64587 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 433 7 2 6 4.5 CN(C)S(=O)(=O)Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL18163 64587 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 433 7 2 6 4.5 CN(C)S(=O)(=O)Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
22325336 188958 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL508271 188958 1 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
11491176 200043 38 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmcl.2010.09.064
CHEMBL595573 200043 38 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmcl.2010.09.064
9887852 65975 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 5 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836322 65975 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 5 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
44580050 184204 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL483251 184204 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
20587808 187856 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 377 2 1 6 3.0 COC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL496327 187856 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 377 2 1 6 3.0 COC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
12071667 188021 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497569 188021 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
22254068 65970 32 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836317 65970 32 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
20651581 65979 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 451 8 2 5 4.1 O=S(=O)(CC(F)(F)F)NCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836326 65979 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 451 8 2 5 4.1 O=S(=O)(CC(F)(F)F)NCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
22254003 65968 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 489 6 2 8 4.1 Cn1cnc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc4c(s3)CCSc3ccccc3-4)CC2)c1 10.1016/j.bmcl.2011.06.124
CHEMBL1836315 65968 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 489 6 2 8 4.1 Cn1cnc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc4c(s3)CCSc3ccccc3-4)CC2)c1 10.1016/j.bmcl.2011.06.124
57393057 71240 0 None - 1 Mouse 7.0 pIC50 = 7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 370 4 1 5 4.4 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956843 71240 0 None - 1 Mouse 7.0 pIC50 = 7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 370 4 1 5 4.4 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
44271459 59953 1 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 346 4 2 4 5.8 Clc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL17326 59953 1 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 346 4 2 4 5.8 Clc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
57391285 71267 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 371 4 1 6 3.8 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)cn3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956938 71267 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 371 4 1 6 3.8 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)cn3)nc2c1 10.1016/j.bmcl.2012.01.027
57399999 71265 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 316 5 1 5 3.2 CCS(=O)(=O)c1ccc2oc(NCc3ccccc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956935 71265 0 None - 1 Mouse 6.0 pIC50 = 6.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 316 5 1 5 3.2 CCS(=O)(=O)c1ccc2oc(NCc3ccccc3)nc2c1 10.1016/j.bmcl.2012.01.027
24950871 178529 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 446 1 1 4 6.9 O=C1CC2(CCCCC2)CC(O)=C1C1C2=C(CC3(CCCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL466756 178529 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 446 1 1 4 6.9 O=C1CC2(CCCCC2)CC(O)=C1C1C2=C(CC3(CCCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
10969955 110588 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
In vitro human Neuropeptide Y receptor Y5 functional antagonism (reporter gene assay)In vitro human Neuropeptide Y receptor Y5 functional antagonism (reporter gene assay)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL325475 110588 0 None 1 2 Human 8.0 pIC50 = 8.0 Functional
In vitro human Neuropeptide Y receptor Y5 functional antagonism (reporter gene assay)In vitro human Neuropeptide Y receptor Y5 functional antagonism (reporter gene assay)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
44271442 63248 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 7 2 6 4.9 CN(C[C@H]1CC[C@H](CNc2nc(N)c3ccccc3n2)CC1)S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL17911 63248 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 7 2 6 4.9 CN(C[C@H]1CC[C@H](CNc2nc(N)c3ccccc3n2)CC1)S(=O)(=O)c1cccc2ccccc12 10.1016/s0960-894x(00)00177-3
24950557 178822 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 380 1 1 4 5.3 Cc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL469256 178822 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 380 1 1 4 5.3 Cc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
9907999 164868 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL422012 164868 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
57398333 71263 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 308 4 1 5 3.4 CCS(=O)(=O)c1ccc2oc(NC3CCCCC3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956933 71263 0 None - 1 Mouse 5.9 pIC50 = 5.9 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 308 4 1 5 3.4 CCS(=O)(=O)c1ccc2oc(NC3CCCCC3)nc2c1 10.1016/j.bmcl.2012.01.027
57391273 71241 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 370 4 1 5 4.4 CCS(=O)(=O)c1ccc2oc(Nc3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956844 71241 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 370 4 1 5 4.4 CCS(=O)(=O)c1ccc2oc(Nc3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.01.027
2418871 71238 1 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 302 4 1 5 3.4 CCS(=O)(=O)c1ccc2oc(Nc3ccccc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956841 71238 1 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 302 4 1 5 3.4 CCS(=O)(=O)c1ccc2oc(Nc3ccccc3)nc2c1 10.1016/j.bmcl.2012.01.027
10046270 62796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increase
ChEMBL 396 4 1 6 2.3 COn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784131 62796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increase
ChEMBL 396 4 1 6 2.3 COn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
57391275 71246 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 433 5 1 7 4.1 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)c(F)c3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956850 71246 0 None - 1 Mouse 6.8 pIC50 = 6.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 433 5 1 7 4.1 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)c(F)c3)nc2c1 10.1016/j.bmcl.2012.01.027
44271493 98581 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 7 2 6 4.6 CN(C[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)c1nc(N)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL276768 98581 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 7 2 6 4.6 CN(C[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)c1nc(N)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
57401791 71258 0 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 361 7 2 6 3.7 CCOc1ccc(Nc2nc3cc(NS(=O)(=O)CC)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956928 71258 0 None - 1 Mouse 5.8 pIC50 = 5.8 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 361 7 2 6 3.7 CCOc1ccc(Nc2nc3cc(NS(=O)(=O)CC)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
42630820 187078 10 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as inhibition of NPY-induced increase in intracellular Ca2+ level by FLIPR assayAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as inhibition of NPY-induced increase in intracellular Ca2+ level by FLIPR assay
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL491288 187078 10 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as inhibition of NPY-induced increase in intracellular Ca2+ level by FLIPR assayAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as inhibition of NPY-induced increase in intracellular Ca2+ level by FLIPR assay
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
44271549 61049 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 425 7 3 6 3.9 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL17632 61049 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 425 7 3 6 3.9 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
57396549 71261 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 389 6 2 6 4.5 CCOc1ccc(Nc2nc3ccc(NS(=O)(=O)C(C)(C)C)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956931 71261 0 None - 1 Mouse 8.6 pIC50 = 8.6 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 389 6 2 6 4.5 CCOc1ccc(Nc2nc3ccc(NS(=O)(=O)C(C)(C)C)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
9923839 187040 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells assessed as inhibition of neuropeptide-induced increase in intracellular calcium levelAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells assessed as inhibition of neuropeptide-induced increase in intracellular calcium level
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL490937 187040 1 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells assessed as inhibition of neuropeptide-induced increase in intracellular calcium levelAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells assessed as inhibition of neuropeptide-induced increase in intracellular calcium level
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44271565 98131 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 461 6 3 6 4.3 Nc1nc(N[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL273597 98131 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 461 6 3 6 4.3 Nc1nc(N[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
44271531 98850 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 8 3 6 5.0 Nc1nc(NCC[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL278881 98850 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 489 8 3 6 5.0 Nc1nc(NCC[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
1562 899 13 None -1 7 Human 8.5 pIC50 = 8.5 Functional
Compound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cellsCompound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
5312114 899 13 None -1 7 Human 8.5 pIC50 = 8.5 Functional
Compound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cellsCompound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL17645 899 13 None -1 7 Human 8.5 pIC50 = 8.5 Functional
Compound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cellsCompound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL195380 899 13 None -1 7 Human 8.5 pIC50 = 8.5 Functional
Compound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cellsCompound was tested for its antagonistic activity against Neuropeptide Y receptor Y5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
2350190 51857 6 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.01.027
CHEMBL1585484 51857 6 None - 1 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.01.027
44271517 59036 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 394 5 2 4 7.2 c1ccc(Nc2nc(Nc3ccc(C4CCCCC4)cc3)nc3ccccc23)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL16936 59036 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 394 5 2 4 7.2 c1ccc(Nc2nc(Nc3ccc(C4CCCCC4)cc3)nc3ccccc23)cc1 10.1016/s0960-894x(00)00177-3
44271450 167134 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 326 4 2 4 5.4 Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL429053 167134 1 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 326 4 2 4 5.4 Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
57391274 71244 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 387 5 1 7 3.2 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4CCOCC4)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956848 71244 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 387 5 1 7 3.2 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4CCOCC4)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
57401790 71255 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 332 5 1 6 3.4 CCOc1ccc(Nc2nc3cc(S(C)(=O)=O)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956925 71255 0 None - 1 Mouse 6.7 pIC50 = 6.7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 332 5 1 6 3.4 CCOc1ccc(Nc2nc3cc(S(C)(=O)=O)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
44271541 60290 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 499 7 2 5 6.8 CN(C[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1)C(=O)c1ccccc1 10.1016/s0960-894x(00)00177-3
CHEMBL17427 60290 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 499 7 2 5 6.8 CN(C[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1)C(=O)c1ccccc1 10.1016/s0960-894x(00)00177-3
44271532 59743 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 380 4 2 4 6.4 Clc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1Cl 10.1016/s0960-894x(00)00177-3
CHEMBL17247 59743 1 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 380 4 2 4 6.4 Clc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1Cl 10.1016/s0960-894x(00)00177-3
9955360 98554 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 449 10 3 6 4.3 Nc1nc(NCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL276551 98554 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 449 10 3 6 4.3 Nc1nc(NCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
9907999 164868 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL422012 164868 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5Antagonistic activity of compound was determined by its ability to inhibit NPY induced [Ca2+]i increases in CHO cells which expressed the recombinant human Neuropeptide Y receptor type 5
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
44271484 98823 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 469 7 3 6 4.5 Nc1nc(NCc2ccc(CNS(=O)(=O)c3cccc4ccccc34)cc2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL278677 98823 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 469 7 3 6 4.5 Nc1nc(NCc2ccc(CNS(=O)(=O)c3cccc4ccccc34)cc2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
22254020 65969 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 491 6 2 7 5.5 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccs1 10.1016/j.bmcl.2011.06.124
CHEMBL1836316 65969 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 491 6 2 7 5.5 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccs1 10.1016/j.bmcl.2011.06.124
20651572 65985 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 407 5 2 6 3.3 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCOc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836332 65985 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 407 5 2 6 3.3 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCOc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
22254050 65971 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 6 4.4 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836318 65971 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 6 4.4 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
25346026 71242 3 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 386 5 1 6 4.3 CCS(=O)(=O)c1ccc2oc(Nc3ccc(OC(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956846 71242 3 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 386 5 1 6 4.3 CCS(=O)(=O)c1ccc2oc(Nc3ccc(OC(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
57399997 71254 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 416 5 1 8 3.4 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956923 71254 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 416 5 1 8 3.4 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
44271468 98891 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 485 7 3 5 6.4 O=C(NC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1)c1ccccc1 10.1016/s0960-894x(00)00177-3
CHEMBL279181 98891 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 485 7 3 5 6.4 O=C(NC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1)c1ccccc1 10.1016/s0960-894x(00)00177-3
57403501 71239 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 336 4 1 5 4.0 CCS(=O)(=O)c1ccc2oc(Nc3ccc(Cl)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956842 71239 0 None - 1 Mouse 6.5 pIC50 = 6.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 336 4 1 5 4.0 CCS(=O)(=O)c1ccc2oc(Nc3ccc(Cl)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
44271506 60014 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 342 5 2 5 5.1 COc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL17352 60014 1 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 342 5 2 5 5.1 COc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
44271550 61370 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 462 10 2 7 6.9 CCOP(=O)(Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1)OCC 10.1016/s0960-894x(00)00177-3
CHEMBL17686 61370 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 462 10 2 7 6.9 CCOP(=O)(Cc1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1)OCC 10.1016/s0960-894x(00)00177-3
1202745 189002 2 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL508770 189002 2 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
22254131 65952 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 529 7 2 7 5.7 COc1ccc(C)cc1S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836103 65952 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 529 7 2 7 5.7 COc1ccc(C)cc1S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
57403512 71260 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 361 7 2 6 3.7 CCOc1ccc(Nc2nc3ccc(NS(=O)(=O)CC)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956930 71260 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 361 7 2 6 3.7 CCOc1ccc(Nc2nc3ccc(NS(=O)(=O)CC)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
9884833 110552 41 None - 1 Human 7.4 pIC50 = 7.4 Functional
The compound was evaluated in vitro for: human Neuropeptide Y receptor Y5 functional antagonismThe compound was evaluated in vitro for: human Neuropeptide Y receptor Y5 functional antagonism
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL325226 110552 41 None - 1 Human 7.4 pIC50 = 7.4 Functional
The compound was evaluated in vitro for: human Neuropeptide Y receptor Y5 functional antagonismThe compound was evaluated in vitro for: human Neuropeptide Y receptor Y5 functional antagonism
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
44271486 163224 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCCC(CNS(=O)(=O)c3cccc4ccccc34)C2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL418359 163224 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCCC(CNS(=O)(=O)c3cccc4ccccc34)C2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
44271529 59090 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 469 7 3 6 4.5 Nc1nc(NCc2cccc(CNS(=O)(=O)c3cccc4ccccc34)c2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL16965 59090 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 469 7 3 6 4.5 Nc1nc(NCc2cccc(CNS(=O)(=O)c3cccc4ccccc34)c2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
44271525 60185 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 423 6 3 5 5.1 CC(=O)NC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL17398 60185 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 423 6 3 5 5.1 CC(=O)NC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
44271478 60438 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 501 8 3 6 5.6 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc(Nc4ccccc4)c4ccccc4n3)CC2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL17521 60438 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 501 8 3 6 5.6 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc(Nc4ccccc4)c4ccccc4n3)CC2)cc1 10.1016/s0960-894x(00)00177-3
44271487 98922 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 383 7 2 5 6.0 CCN(CC)c1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL279408 98922 3 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 383 7 2 5 6.0 CCN(CC)c1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
44271638 60402 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 438 6 2 6 6.0 O=C(O[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1)c1ccccc1 10.1016/s0960-894x(00)00177-3
CHEMBL17496 60402 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 438 6 2 6 6.0 O=C(O[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1)c1ccccc1 10.1016/s0960-894x(00)00177-3
22254119 65967 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 535 6 2 6 6.6 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2011.06.124
CHEMBL1836314 65967 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 535 6 2 6 6.6 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2011.06.124
44271637 59611 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 463 11 3 6 4.7 Nc1nc(NCCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL17196 59611 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 463 11 3 6 4.7 Nc1nc(NCCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
9886706 178642 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 390 1 1 4 5.3 O=C1CC2(CCC2)CC(O)=C1C1C2=C(CC3(CCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL467558 178642 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 390 1 1 4 5.3 O=C1CC2(CCC2)CC(O)=C1C1C2=C(CC3(CCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
44271592 61389 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 477 12 3 6 5.1 Nc1nc(NCCCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL17701 61389 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 477 12 3 6 5.1 Nc1nc(NCCCCCCCCNS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
57394791 71259 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 346 6 1 6 3.8 CCOc1ccc(Nc2nc3ccc(S(=O)(=O)CC)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956929 71259 0 None - 1 Mouse 6.3 pIC50 = 6.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 346 6 1 6 3.8 CCOc1ccc(Nc2nc3ccc(S(=O)(=O)CC)cc3o2)cc1 10.1016/j.bmcl.2012.01.027
44271562 98690 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 447 5 3 6 4.1 Nc1nc(N[C@H]2CCCC[C@H]2NS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL277551 98690 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 447 5 3 6 4.1 Nc1nc(N[C@H]2CCCC[C@H]2NS(=O)(=O)c2cccc3ccccc23)nc2ccccc12 10.1016/s0960-894x(00)00177-3
56683832 65976 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 6 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836323 65976 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 6 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
25067562 186971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
CHEMBL490427 186971 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
44271691 63259 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 318 4 2 4 5.1 c1ccc(Nc2nc(NC3CCCCC3)nc3ccccc23)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL17914 63259 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 318 4 2 4 5.1 c1ccc(Nc2nc(NC3CCCCC3)nc3ccccc23)cc1 10.1016/s0960-894x(00)00177-3
2387945 43719 6 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 346 6 1 6 3.8 CCOc1ccc(Nc2nc3cc(S(=O)(=O)CC)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1510429 43719 6 None - 1 Mouse 7.3 pIC50 = 7.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 346 6 1 6 3.8 CCOc1ccc(Nc2nc3cc(S(=O)(=O)CC)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
44271482 60269 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 461 6 2 6 4.3 Nc1nc(NCCC2CCN(S(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
CHEMBL17417 60269 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 461 6 2 6 4.3 Nc1nc(NCCC2CCN(S(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/s0960-894x(00)00177-3
44271467 60350 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 395 6 3 5 5.2 CNC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL17454 60350 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 395 6 3 5 5.2 CNC[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
57403513 71262 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 458 5 2 7 4.7 C[C@H]1CN(c2ccc(Nc3nc4ccc(NS(=O)(=O)C(C)(C)C)cc4o3)cc2)C[C@@H](C)O1 10.1016/j.bmcl.2012.01.027
CHEMBL1956932 71262 0 None - 1 Mouse 5.3 pIC50 = 5.3 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 458 5 2 7 4.7 C[C@H]1CN(c2ccc(Nc3nc4ccc(NS(=O)(=O)C(C)(C)C)cc4o3)cc2)C[C@@H](C)O1 10.1016/j.bmcl.2012.01.027
24950710 178815 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 418 1 1 4 6.1 O=C1CC2(CCCC2)CC(O)=C1C1C2=C(CC3(CCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL469173 178815 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 418 1 1 4 6.1 O=C1CC2(CCCC2)CC(O)=C1C1C2=C(CC3(CCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
44271533 60121 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 437 6 2 5 5.5 CC(=O)N(C)C[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL17395 60121 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 437 6 2 5 5.5 CC(=O)N(C)C[C@H]1CC[C@H](Nc2nc(Nc3ccc(Cl)cc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
22639804 98551 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 376 5 2 6 4.7 CC(=O)O[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL276530 98551 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 376 5 2 6 4.7 CC(=O)O[C@H]1CC[C@H](Nc2nc(Nc3ccccc3)c3ccccc3n2)CC1 10.1016/s0960-894x(00)00177-3
9884833 110552 41 None - 1 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for functional antagonism of Neuropeptide Y receptor Y5 activity in cellular Ca fluxCompound was evaluated for functional antagonism of Neuropeptide Y receptor Y5 activity in cellular Ca flux
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL325226 110552 41 None - 1 Human 8.2 pIC50 = 8.2 Functional
Compound was evaluated for functional antagonism of Neuropeptide Y receptor Y5 activity in cellular Ca fluxCompound was evaluated for functional antagonism of Neuropeptide Y receptor Y5 activity in cellular Ca flux
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
9887225 187148 3 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant NPY Y5 receptor expressed in mouse LMtk- cells assessed as inhibition of NPY-induced Ca2+ increaseAntagonist activity at human recombinant NPY Y5 receptor expressed in mouse LMtk- cells assessed as inhibition of NPY-induced Ca2+ increase
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL491930 187148 3 None -2 3 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant NPY Y5 receptor expressed in mouse LMtk- cells assessed as inhibition of NPY-induced Ca2+ increaseAntagonist activity at human recombinant NPY Y5 receptor expressed in mouse LMtk- cells assessed as inhibition of NPY-induced Ca2+ increase
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
1565 2207 15 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
624746 2207 15 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
CHEMBL491762 2207 15 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
24950556 189471 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(F)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL513701 189471 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(F)ccc32)=C(O)C1 10.1021/jm8003587
10110741 188000 3 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497359 188000 3 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ levelAntagonist activity at human NPY Y5 receptor transfected in mouse LMtk cells assessed as inhibition of neuropeptide Y-induced increase in intercellular Ca2+ level
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
57403511 71257 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 374 5 1 6 4.5 CCOc1ccc(Nc2nc3cc(S(=O)(=O)C(C)(C)C)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956927 71257 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 374 5 1 6 4.5 CCOc1ccc(Nc2nc3cc(S(=O)(=O)C(C)(C)C)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
57393069 71268 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 388 5 1 8 2.6 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4CCOCC4)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956939 71268 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 388 5 1 8 2.6 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4CCOCC4)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
44579887 193093 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 6 4.6 Cc1nc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)no1 10.1016/j.bmcl.2008.08.021
CHEMBL522589 193093 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 6 4.6 Cc1nc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)no1 10.1016/j.bmcl.2008.08.021
25211875 192649 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 7 3.5 Cn1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)n1 10.1016/j.bmcl.2008.08.021
CHEMBL521750 192649 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk cells assessed as inhibition of NPY-induced calcium increase
ChEMBL 400 2 1 7 3.5 Cn1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)n1 10.1016/j.bmcl.2008.08.021
57328464 71245 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 415 5 1 7 4.0 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956849 71245 0 None - 1 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 415 5 1 7 4.0 CCS(=O)(=O)c1ccc2oc(Nc3ccc(N4C[C@H](C)O[C@H](C)C4)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
44271437 98465 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 503 7 1 6 4.9 CN(C[C@H]1CC[C@H](CN(C)S(=O)(=O)c2cccc3ccccc23)CC1)c1nc(N)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL275845 98465 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 503 7 1 6 4.9 CN(C[C@H]1CC[C@H](CN(C)S(=O)(=O)c2cccc3ccccc23)CC1)c1nc(N)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
57396550 71264 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 364 4 1 5 4.6 CCS(=O)(=O)c1ccc2oc(NC3CCC(C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956934 71264 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 364 4 1 5 4.6 CCS(=O)(=O)c1ccc2oc(NC3CCC(C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2012.01.027
2418891 51012 5 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 358 4 1 5 4.7 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(C)(C)C)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1578465 51012 5 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 358 4 1 5 4.7 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(C)(C)C)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
24950714 178699 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(F)cccc32)=C(O)C1 10.1021/jm8003587
CHEMBL468225 178699 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(F)cccc32)=C(O)C1 10.1021/jm8003587
57398334 71266 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 371 4 1 6 3.8 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956937 71266 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 371 4 1 6 3.8 CCS(=O)(=O)c1ccc2oc(Nc3ccc(C(F)(F)F)nc3)nc2c1 10.1016/j.bmcl.2012.01.027
10047509 62795 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increase
ChEMBL 416 4 1 5 3.6 C[C@@H]1NC(c2ccc(=O)n(C(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1784130 62795 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increaseAntagonist activity at human recombinant NPYY5 receptor expressed in mouse LMtk- cells co-expressing Gqi5 assessed as inhibition of NPY-induced calcium increase
ChEMBL 416 4 1 5 3.6 C[C@@H]1NC(c2ccc(=O)n(C(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
9801629 65978 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 409 4 2 5 3.7 CS(=O)(=O)N[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836325 65978 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 409 4 2 5 3.7 CS(=O)(=O)N[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
213847 60384 7 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 312 4 2 4 5.1 c1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
CHEMBL17483 60384 7 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cellsAntagonistic activity against neuropeptide Y receptor type 5 subtype stably expressed in LM(tk-)cells
ChEMBL 312 4 2 4 5.1 c1ccc(Nc2nc(Nc3ccccc3)c3ccccc3n2)cc1 10.1016/s0960-894x(00)00177-3
9803547 178640 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 444 1 1 4 5.8 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Br)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL467550 178640 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 444 1 1 4 5.8 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Br)ccc32)=C(O)C1 10.1021/jm8003587
24950712 189367 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Cl)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL512787 189367 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Cl)ccc32)=C(O)C1 10.1021/jm8003587
57393058 71243 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 360 6 1 6 4.2 CCS(=O)(=O)c1ccc2oc(Nc3ccc(OC(C)C)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
CHEMBL1956847 71243 0 None - 1 Mouse 8.0 pIC50 = 8.0 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 360 6 1 6 4.2 CCS(=O)(=O)c1ccc2oc(Nc3ccc(OC(C)C)cc3)nc2c1 10.1016/j.bmcl.2012.01.027
9847327 65974 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 465 9 2 5 4.5 O=S(=O)(CC(F)(F)F)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836321 65974 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 465 9 2 5 4.5 O=S(=O)(CC(F)(F)F)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
44577739 189391 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 422 5 1 4 6.6 CCC1(CC)CC(=O)C(C2C3=C(CC(CC)(CC)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL512996 189391 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentrationAntagonist activity at human recombinant neuropeptide Y5 receptor expressed in CHO cells coexpressing Gqi5 assessed as inhibition of neuropeptide Y-induced increase in intracellular calcium concentration
ChEMBL 422 5 1 4 6.6 CCC1(CC)CC(=O)C(C2C3=C(CC(CC)(CC)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
20651605 65973 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 425 9 2 5 4.3 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836320 65973 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 425 9 2 5 4.3 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
57399998 71256 0 None - 1 Mouse 7.0 pIC50 = 7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 360 6 1 6 4.2 CCOc1ccc(Nc2nc3cc(S(=O)(=O)C(C)C)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
CHEMBL1956926 71256 0 None - 1 Mouse 7.0 pIC50 = 7 Functional
Antagonist activity at mouse neuropeptide Y5 receptorAntagonist activity at mouse neuropeptide Y5 receptor
ChEMBL 360 6 1 6 4.2 CCOc1ccc(Nc2nc3cc(S(=O)(=O)C(C)C)ccc3o2)cc1 10.1016/j.bmcl.2012.01.027
44158542 17545 0 None - 0 Human 10.6 pKi = 10.6 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3cnc(-c4ccccc4F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257993 17545 0 None - 0 Human 10.6 pKi = 10.6 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3cnc(-c4ccccc4F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
24994659 17580 0 None - 0 Human 10.5 pKi = 10.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3ccn(-c4ccccc4F)n3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258111 17580 0 None - 0 Human 10.5 pKi = 10.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3ccn(-c4ccccc4F)n3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
52944983 17611 0 None - 0 Human 10.4 pKi = 10.4 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cncnc1 10.1016/j.bmcl.2010.08.041
CHEMBL1258225 17611 0 None - 0 Human 10.4 pKi = 10.4 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cncnc1 10.1016/j.bmcl.2010.08.041
44158762 17544 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257992 17544 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
52941430 17642 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cnccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258341 17642 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cnccn1 10.1016/j.bmcl.2010.08.041
44158764 17789 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 430 5 1 7 4.2 Cc1ccccc1-c1ccc(NC[C@H]2CC[C@]3(CC2)CN(c2cccnn2)C(=O)O3)nn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258787 17789 0 None - 0 Human 10.2 pKi = 10.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 430 5 1 7 4.2 Cc1ccccc1-c1ccc(NC[C@H]2CC[C@]3(CC2)CN(c2cccnn2)C(=O)O3)nn1 10.1016/j.bmcl.2010.08.041
24996879 17579 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 7 4.6 O=C1O[C@]2(CC[C@H](CNc3nc(-c4ccccn4)cs3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258110 17579 0 None - 0 Human 10.1 pKi = 10.1 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 7 4.6 O=C1O[C@]2(CC[C@H](CNc3nc(-c4ccccn4)cs3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
52942650 17441 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnc1 10.1016/j.bmcl.2010.08.041
CHEMBL1257636 17441 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnc1 10.1016/j.bmcl.2010.08.041
52942663 17641 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 439 5 1 6 4.5 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnc1F 10.1016/j.bmcl.2010.08.041
CHEMBL1258340 17641 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 439 5 1 6 4.5 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnc1F 10.1016/j.bmcl.2010.08.041
52942671 17679 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258453 17679 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
44158763 17752 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 452 5 1 7 4.2 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4cc(F)cc(F)c4)nn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258674 17752 0 None - 0 Human 10.0 pKi = 10 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 452 5 1 7 4.2 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4cc(F)cc(F)c4)nn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
44159473 17442 0 None - 0 Human 9.9 pKi = 9.9 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 7 4.6 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4nccs4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257637 17442 0 None - 0 Human 9.9 pKi = 9.9 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 421 5 1 7 4.6 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4nccs4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
44159236 17479 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 416 5 1 7 3.9 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccn4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257760 17479 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 416 5 1 7 3.9 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccn4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
44159353 17480 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 408 6 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3ccc(OC4CCC4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257761 17480 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 408 6 1 6 4.4 O=C1O[C@]2(CC[C@H](CNc3ccc(OC4CCC4)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
52950004 17751 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 434 5 1 7 4.1 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258673 17751 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 434 5 1 7 4.1 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
25071621 19100 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.5 O=C1OC2(CCN(c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289154 19100 0 None - 0 Human 9.8 pKi = 9.8 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.5 O=C1OC2(CCN(c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
52948742 17680 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1ccnnc1 10.1016/j.bmcl.2010.08.041
CHEMBL1258454 17680 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 422 5 1 7 3.8 O=C1O[C@]2(CC[C@H](CNc3cnn(-c4ccccc4F)c3)CC2)CN1c1ccnnc1 10.1016/j.bmcl.2010.08.041
52948986 17716 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 442 5 1 8 4.2 Cc1nnc(N2C[C@]3(CC[C@@H](CNc4cnn(-c5ccccc5F)c4)CC3)OC2=O)s1 10.1016/j.bmcl.2010.08.041
CHEMBL1258562 17716 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 442 5 1 8 4.2 Cc1nnc(N2C[C@]3(CC[C@@H](CNc4cnn(-c5ccccc5F)c4)CC3)OC2=O)s1 10.1016/j.bmcl.2010.08.041
25071620 19099 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 442 3 1 4 5.4 O=C1OC2(CCN(c3nc4cc(-c5ccc(F)cc5)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289153 19099 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 442 3 1 4 5.4 O=C1OC2(CCN(c3nc4cc(-c5ccc(F)cc5)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
44160200 17790 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 430 5 1 7 4.2 Cc1cccc(-c2ccc(NC[C@H]3CC[C@]4(CC3)CN(c3cccnn3)C(=O)O4)nc2)n1 10.1016/j.bmcl.2010.08.041
CHEMBL1258788 17790 0 None - 0 Human 9.6 pKi = 9.6 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 430 5 1 7 4.2 Cc1cccc(-c2ccc(NC[C@H]3CC[C@]4(CC3)CN(c3cccnn3)C(=O)O4)nc2)n1 10.1016/j.bmcl.2010.08.041
44158545 17610 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3ncc(-c4ccccc4F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258224 17610 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 433 5 1 6 4.7 O=C1O[C@]2(CC[C@H](CNc3ncc(-c4ccccc4F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
44160199 17822 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 434 5 1 7 4.1 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccc4F)cn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258907 17822 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 434 5 1 7 4.1 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccc4F)cn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
25071310 19114 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 431 3 1 4 5.5 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289267 19114 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 431 3 1 4 5.5 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25072880 19134 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccc(F)cc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289386 19134 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccc(F)cc1 10.1016/j.bmcl.2010.09.064
25073190 19227 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 372 2 1 4 4.5 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccccc3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
CHEMBL1290037 19227 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 372 2 1 4 4.5 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccccc3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
49862239 15009 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 6 1 5 4.1 CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)c1ccccc1 10.1016/j.bmcl.2010.06.140
CHEMBL1209159 15009 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 6 1 5 4.1 CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)c1ccccc1 10.1016/j.bmcl.2010.06.140
25072875 19167 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1cccc(N2C[C@]3(CC[C@@H](c4nc5cc(OC(F)(F)F)ccc5[nH]4)CC3)OC2=O)n1 10.1016/j.bmcl.2010.09.064
CHEMBL1289609 19167 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1cccc(N2C[C@]3(CC[C@@H](c4nc5cc(OC(F)(F)F)ccc5[nH]4)CC3)OC2=O)n1 10.1016/j.bmcl.2010.09.064
52943793 17404 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 435 5 1 6 4.7 Cc1ncccc1N1C[C@]2(CC[C@@H](CNc3cnn(-c4ccccc4F)c3)CC2)OC1=O 10.1016/j.bmcl.2010.08.041
CHEMBL1257520 17404 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 435 5 1 6 4.7 Cc1ncccc1N1C[C@]2(CC[C@@H](CNc3cnn(-c4ccccc4F)c3)CC2)OC1=O 10.1016/j.bmcl.2010.08.041
49862241 15012 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 7 1 5 4.0 O=C(CCc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209162 15012 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 7 1 5 4.0 O=C(CCc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862400 15053 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 398 6 1 5 4.3 Fc1cc(F)cc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)c1 10.1016/j.bmcl.2010.06.140
CHEMBL1209345 15053 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 398 6 1 5 4.3 Fc1cc(F)cc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)c1 10.1016/j.bmcl.2010.06.140
25073189 19115 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1F 10.1016/j.bmcl.2010.09.064
CHEMBL1289268 19115 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 449 3 1 4 5.7 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1F 10.1016/j.bmcl.2010.09.064
25071931 19201 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 415 2 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289820 19201 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 415 2 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25072877 19228 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 2 1 4 4.6 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccc(F)cc3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
CHEMBL1290038 19228 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 2 1 4 4.6 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccc(F)cc3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
49862240 15010 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 6 1 5 4.1 O=C(N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C1(c2ccccc2)CC1 10.1016/j.bmcl.2010.06.140
CHEMBL1209160 15010 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 6 1 5 4.1 O=C(N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C1(c2ccccc2)CC1 10.1016/j.bmcl.2010.06.140
49862289 15023 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 6 1 5 4.1 O=C([C@H]1C[C@@H]1c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209216 15023 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 6 1 5 4.1 O=C([C@H]1C[C@@H]1c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
22253974 65977 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 6 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836324 65977 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 6 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
9887852 65975 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 5 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836322 65975 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 411 9 2 5 4.0 CCS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
44159235 17514 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 406 4 1 5 4.5 O=C1O[C@]2(CC[C@H](CNc3ccc(C(F)(F)F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257881 17514 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 406 4 1 5 4.5 O=C1O[C@]2(CC[C@H](CNc3ccc(C(F)(F)F)cn3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
49862157 14991 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 394 5 1 5 3.8 O=C(c1cccc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209052 14991 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 394 5 1 5 3.8 O=C(c1cccc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862200 14998 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 3.6 O=C(Cc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209101 14998 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 3.6 O=C(Cc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862200 14999 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 3.6 O=C(Cc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209102 14999 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 3.6 O=C(Cc1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
9845943 65982 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 7 3.3 COc1cccc2c1OCCc1sc(N[C@H]3CC[C@H](CNS(C)(=O)=O)CC3)nc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836329 65982 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 7 3.3 COc1cccc2c1OCCc1sc(N[C@H]3CC[C@H](CNS(C)(=O)=O)CC3)nc1-2 10.1016/j.bmcl.2011.06.124
9888553 65984 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 5 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836331 65984 0 None - 0 Human 9.0 pKi = 9.0 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 5 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
49862401 15054 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 6 1 5 4.6 CC(c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209346 15054 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 6 1 5 4.6 CC(c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
25071929 19079 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 426 2 1 4 4.3 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289038 19079 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 426 2 1 4 4.3 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25073191 19151 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
CHEMBL1289503 19151 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
25073801 19184 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
CHEMBL1289714 19184 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
9908801 65972 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 5 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836319 65972 0 None - 1 Human 8.9 pKi = 8.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 5 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
22254068 65970 32 None - 1 Rat 8.9 pKi = 8.9 Functional
Antagonist activity at rat NPY5 receptorAntagonist activity at rat NPY5 receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836317 65970 32 None - 1 Rat 8.9 pKi = 8.9 Functional
Antagonist activity at rat NPY5 receptorAntagonist activity at rat NPY5 receptor
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
22254068 65970 32 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836317 65970 32 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 423 5 2 6 4.0 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
44159706 17717 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 417 5 1 8 3.3 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccn4)cn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
CHEMBL1258563 17717 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 417 5 1 8 3.3 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ncccn4)cn3)CC2)CN1c1cccnn1 10.1016/j.bmcl.2010.08.041
49862158 14992 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 412 5 1 5 3.9 O=C(c1cc(F)cc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209053 14992 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 412 5 1 5 3.9 O=C(c1cc(F)cc(F)c1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862339 15036 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 362 6 1 5 4.0 c1ccc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)cc1 10.1016/j.bmcl.2010.06.140
CHEMBL1209280 15036 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 362 6 1 5 4.0 c1ccc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)cc1 10.1016/j.bmcl.2010.06.140
25072242 19338 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 4.6 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1290706 19338 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 4.6 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
22254110 65983 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 415 8 2 6 3.7 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836330 65983 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 415 8 2 6 3.7 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
22254020 65969 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 491 6 2 7 5.5 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccs1 10.1016/j.bmcl.2011.06.124
CHEMBL1836316 65969 0 None - 1 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 491 6 2 7 5.5 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccs1 10.1016/j.bmcl.2011.06.124
24987242 17296 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 435 3 1 6 4.2 O=C(Nc1nc(-c2ccccn2)cs1)N1CCC2(CC1)CN(c1ccccc1)C(=O)O2 10.1016/j.bmcl.2010.08.041
CHEMBL1257173 17296 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 435 3 1 6 4.2 O=C(Nc1nc(-c2ccccn2)cs1)N1CCC2(CC1)CN(c1ccccc1)C(=O)O2 10.1016/j.bmcl.2010.08.041
24987242 17296 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 435 3 1 6 4.2 O=C(Nc1nc(-c2ccccn2)cs1)N1CCC2(CC1)CN(c1ccccc1)C(=O)O2 10.1016/j.bmcl.2010.09.064
CHEMBL1257173 17296 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 435 3 1 6 4.2 O=C(Nc1nc(-c2ccccn2)cs1)N1CCC2(CC1)CN(c1ccccc1)C(=O)O2 10.1016/j.bmcl.2010.09.064
49862337 15034 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 272 4 2 5 2.1 c1ccc(-c2csc(NC[C@@H]3[C@H]4CNC[C@H]43)n2)nc1 10.1016/j.bmcl.2010.06.140
CHEMBL1209278 15034 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 272 4 2 5 2.1 c1ccc(-c2csc(NC[C@@H]3[C@H]4CNC[C@H]43)n2)nc1 10.1016/j.bmcl.2010.06.140
10872843 102938 0 None - 1 Human 7.0 pKi = 7 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 390 7 2 3 4.9 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(OCc2ccccc2)cc1 10.1021/jm0004547
CHEMBL306277 102938 0 None - 1 Human 7.0 pKi = 7 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 390 7 2 3 4.9 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(OCc2ccccc2)cc1 10.1021/jm0004547
49862156 14989 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 5 1 5 3.6 O=C(c1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209050 14989 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 5 1 5 3.6 O=C(c1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
22254119 65967 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 535 6 2 6 6.6 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2011.06.124
CHEMBL1836314 65967 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 535 6 2 6 6.6 O=S(=O)(NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2011.06.124
4527770 15055 5 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 321 3 1 4 5.0 FC(F)(F)c1ccc(Nc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2010.08.041
CHEMBL1209347 15055 5 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 321 3 1 4 5.0 FC(F)(F)c1ccc(Nc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2010.08.041
4527770 15055 5 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 321 3 1 4 5.0 FC(F)(F)c1ccc(Nc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2010.06.140
CHEMBL1209347 15055 5 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 321 3 1 4 5.0 FC(F)(F)c1ccc(Nc2nc(-c3ccccn3)cs2)cc1 10.1016/j.bmcl.2010.06.140
20651572 65985 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 407 5 2 6 3.3 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCOc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836332 65985 0 None - 1 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 407 5 2 6 3.3 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCOc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
9982218 101764 6 None - 1 Rat 7.8 pKi = 7.8 Functional
Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL1435188 101764 6 None - 1 Rat 7.8 pKi = 7.8 Functional
Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL299879 101764 6 None - 1 Rat 7.8 pKi = 7.8 Functional
Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5Functional response of NPY to inhibit forskolin-stimulated cAMP in cells stably transfected with rat Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
25071930 19080 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 366 2 1 4 3.7 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289039 19080 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 366 2 1 4 3.7 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
25072244 19200 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccnc1F 10.1016/j.bmcl.2010.09.064
CHEMBL1289819 19200 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 450 3 1 5 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccnc1F 10.1016/j.bmcl.2010.09.064
20651606 65980 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 427 9 2 6 3.2 CC(C)S(=O)(=O)NCCOCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836327 65980 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 427 9 2 6 3.2 CC(C)S(=O)(=O)NCCOCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
49862155 14988 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 342 5 1 5 3.0 CC(C)C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209049 14988 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 342 5 1 5 3.0 CC(C)C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862156 14990 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 5 1 5 3.6 O=C(c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209051 14990 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 376 5 1 5 3.6 O=C(c1ccccc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
25072245 19150 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 465 3 1 4 6.2 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1Cl 10.1016/j.bmcl.2010.09.064
CHEMBL1289502 19150 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 465 3 1 4 6.2 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccc1Cl 10.1016/j.bmcl.2010.09.064
22254050 65971 1 None - 1 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 6 4.4 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836318 65971 1 None - 1 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 6 4.4 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
22254003 65968 0 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 489 6 2 8 4.1 Cn1cnc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc4c(s3)CCSc3ccccc3-4)CC2)c1 10.1016/j.bmcl.2011.06.124
CHEMBL1836315 65968 0 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 489 6 2 8 4.1 Cn1cnc(S(=O)(=O)NC[C@H]2CC[C@H](Nc3nc4c(s3)CCSc3ccccc3-4)CC2)c1 10.1016/j.bmcl.2011.06.124
9885994 205098 0 None - 1 Human 7.6 pKi = 7.6 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77639 205098 0 None - 1 Human 7.6 pKi = 7.6 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
25072246 19185 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccnc1 10.1016/j.bmcl.2010.09.064
CHEMBL1289715 19185 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 3 1 5 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)CN1c1cccnc1 10.1016/j.bmcl.2010.09.064
46927904 14982 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 314 4 1 5 2.3 CC(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1208996 14982 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 314 4 1 5 2.3 CC(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
9801629 65978 0 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 409 4 2 5 3.7 CS(=O)(=O)N[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836325 65978 0 None - 1 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 409 4 2 5 3.7 CS(=O)(=O)N[C@H]1CC[C@H](Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2011.06.124
20651581 65979 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 451 8 2 5 4.1 O=S(=O)(CC(F)(F)F)NCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836326 65979 0 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 451 8 2 5 4.1 O=S(=O)(CC(F)(F)F)NCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
49862338 15035 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 328 6 1 5 3.5 CC(C)CN1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209279 15035 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 328 6 1 5 3.5 CC(C)CN1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862340 15037 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 4.6 Cc1cc(C)cc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)c1 10.1016/j.bmcl.2010.06.140
CHEMBL1209281 15037 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 390 6 1 5 4.6 Cc1cc(C)cc(CN2C[C@H]3[C@@H](CNc4nc(-c5ccccn5)cs4)[C@H]3C2)c1 10.1016/j.bmcl.2010.06.140
25074110 19213 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 434 2 1 4 5.2 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
CHEMBL1289937 19213 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 434 2 1 4 5.2 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1cccc(F)n1 10.1016/j.bmcl.2010.09.064
49862336 15033 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 384 5 1 6 2.7 O=C(C1CCOCC1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209277 15033 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 384 5 1 6 2.7 O=C(C1CCOCC1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
25022356 19339 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 348 2 1 4 3.6 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
CHEMBL1290707 19339 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 348 2 1 4 3.6 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)CN1c1ccccc1 10.1016/j.bmcl.2010.09.064
22254131 65952 0 None - 1 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 529 7 2 7 5.7 COc1ccc(C)cc1S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
CHEMBL1836103 65952 0 None - 1 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 529 7 2 7 5.7 COc1ccc(C)cc1S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccccc2-3)CC1 10.1016/j.bmcl.2011.06.124
20651605 65973 0 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 425 9 2 5 4.3 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836320 65973 0 None - 1 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 425 9 2 5 4.3 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
10429613 163339 0 None 60 2 Human 6.3 pKi = 6.3 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL419086 163339 0 None 60 2 Human 6.3 pKi = 6.3 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
44158441 17515 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 432 5 1 5 5.3 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nc3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
CHEMBL1257882 17515 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptorAntagonist activity at human NPY Y5 receptor
ChEMBL 432 5 1 5 5.3 O=C1O[C@]2(CC[C@H](CNc3ccc(-c4ccccc4F)nc3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.08.041
49862198 14997 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 377 5 1 6 3.0 O=C(c1cccnc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209100 14997 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 377 5 1 6 3.0 O=C(c1cccnc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
49862288 15022 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 7 1 5 4.8 CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C(C)c1ccccc1 10.1016/j.bmcl.2010.06.140
CHEMBL1209215 15022 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 432 7 1 5 4.8 CC(C(=O)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1)C(C)c1ccccc1 10.1016/j.bmcl.2010.06.140
49862290 15025 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 370 5 1 6 2.5 O=C(C1CCCO1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209218 15025 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 370 5 1 6 2.5 O=C(C1CCCO1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
25072243 19135 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 445 3 1 4 5.8 Cc1ccccc1N1C[C@]2(CC[C@@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)OC1=O 10.1016/j.bmcl.2010.09.064
CHEMBL1289387 19135 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 445 3 1 4 5.8 Cc1ccccc1N1C[C@]2(CC[C@@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)OC1=O 10.1016/j.bmcl.2010.09.064
25072876 19212 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
CHEMBL1289936 19212 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 416 2 1 4 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)CN1c1ccccn1 10.1016/j.bmcl.2010.09.064
54752621 67819 0 None - 0 Rat 8.3 pKi = 8.3 Functional
Antagonist activity at rat NPY Y5 receptorAntagonist activity at rat NPY Y5 receptor
ChEMBL 369 10 2 6 2.2 CN(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909725 67819 0 None - 0 Rat 8.3 pKi = 8.3 Functional
Antagonist activity at rat NPY Y5 receptorAntagonist activity at rat NPY Y5 receptor
ChEMBL 369 10 2 6 2.2 CN(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
49862199 14968 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 377 5 1 6 3.0 O=C(c1ccncc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1208795 14968 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 377 5 1 6 3.0 O=C(c1ccncc1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
11824961 205170 0 None - 1 Human 6.3 pKi = 6.3 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL78265 205170 0 None - 1 Human 6.3 pKi = 6.3 Functional
Tested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptorTested in a cellular assay measuring forskolin-induced cyclic AMP accumulation in 293 cells transfected with the human NPY5 receptor
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
49862241 15011 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 7 1 5 4.0 O=C(CCc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209161 15011 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 404 7 1 5 4.0 O=C(CCc1ccccc1)N1C[C@H]2[C@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
20651616 65981 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 7 3.3 COc1ccc2c(c1)OCCc1sc(NC[C@H]3CC[C@H](NS(C)(=O)=O)CC3)nc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836328 65981 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 437 6 2 7 3.3 COc1ccc2c(c1)OCCc1sc(NC[C@H]3CC[C@H](NS(C)(=O)=O)CC3)nc1-2 10.1016/j.bmcl.2011.06.124
9847327 65974 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 465 9 2 5 4.5 O=S(=O)(CC(F)(F)F)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836321 65974 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 465 9 2 5 4.5 O=S(=O)(CC(F)(F)F)NCCCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2011.06.124
46927903 15024 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 370 5 1 6 2.4 O=C(C1CCOC1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
CHEMBL1209217 15024 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonist activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 370 5 1 6 2.4 O=C(C1CCOC1)N1C[C@H]2[C@@H](CNc3nc(-c4ccccn4)cs3)[C@H]2C1 10.1016/j.bmcl.2010.06.140
25073188 19243 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 373 2 1 5 3.9 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccccn3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
CHEMBL1290147 19243 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 373 2 1 5 3.9 N#Cc1ccc2[nH]c([C@H]3CC[C@]4(CC3)CN(c3ccccn3)C(=O)O4)nc2c1 10.1016/j.bmcl.2010.09.064
25072568 19168 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1ncccc1N1C[C@]2(CC[C@@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)OC1=O 10.1016/j.bmcl.2010.09.064
CHEMBL1289610 19168 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assayAntagonistic activity at human NPY Y5 receptor expressed in HEK293 cells assessed as inhibition of calcium level by FLIPR assay
ChEMBL 446 3 1 5 5.2 Cc1ncccc1N1C[C@]2(CC[C@@H](c3nc4cc(OC(F)(F)F)ccc4[nH]3)CC2)OC1=O 10.1016/j.bmcl.2010.09.064
56683832 65976 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 6 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
CHEMBL1836323 65976 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assayAntagonist activity at human NPY5 receptor assessed as calcium mobilization by FLIPR assay
ChEMBL 397 8 2 6 3.6 CS(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.06.124
1522 336 0 None 1 5 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12069595
1522 336 0 None -1 5 Rat 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12069595
11589975 1674 0 None - 1 Human 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 5 1 3 5.2 O=C(N(CCc1ccncc1)C)Nc1ccc2c(c1)c1CCCCc1n2C(C)C 16436501
1563 1674 0 None - 1 Human 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 390 5 1 3 5.2 O=C(N(CCc1ccncc1)C)Nc1ccc2c(c1)c1CCCCc1n2C(C)C 16436501




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56841989 213420 6 None -17 7 Mouse 9.3 pEC50 = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -17 7 Mouse 9.3 pEC50 = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
56841989 213420 6 None -17 7 Mouse 9.3 pEC50 = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -17 7 Mouse 9.3 pEC50 = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 213406 0 None - 4 Mouse 6.7 pEC50 = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None - 4 Mouse 5.7 pEC50 = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4276961 213368 0 None - 4 Mouse 8.6 pEC50 = 8.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4276961 213368 0 None - 4 Mouse 8.6 pEC50 = 8.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4280392 213406 0 None - 4 Mouse 6.7 pEC50 = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None - 4 Mouse 5.7 pEC50 = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 213513 0 None - 4 Mouse 7.6 pEC50 = 7.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 213513 0 None - 4 Mouse 7.6 pEC50 = 7.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 213467 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 213467 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None - 4 Mouse 6.2 pEC50 = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from mouse Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
70675708 128482 0 None - 0 Mouse 9.9 pIC50 = 9.9 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 378 7 2 6 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccccc3)no2)CC1 nan
CHEMBL3666784 128482 0 None - 0 Mouse 9.9 pIC50 = 9.9 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 378 7 2 6 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccccc3)no2)CC1 nan
70682528 76902 0 None - 0 Mouse 9.8 pIC50 = 9.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(F)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070148 76902 0 None - 0 Mouse 9.8 pIC50 = 9.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(F)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
70695120 76905 0 None - 0 Mouse 9.8 pIC50 = 9.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(Cl)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070151 76905 0 None - 0 Mouse 9.8 pIC50 = 9.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(Cl)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
70675728 128485 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3F)no2)CC1 nan
CHEMBL3666787 128485 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3F)no2)CC1 nan
10758227 118978 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 286 5 1 3 3.9 CCCCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
CHEMBL342438 118978 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 286 5 1 3 3.9 CCCCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
70675706 128480 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 396 7 2 6 3.2 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
CHEMBL3666782 128480 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 396 7 2 6 3.2 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
18004956 187204 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 453 2 1 3 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492370 187204 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 453 2 1 3 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
70688847 76801 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(C)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2069316 76801 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3ccc(C)c(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
71453237 81348 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 425 4 1 5 3.5 O=S(=O)(CC(F)(F)F)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159167 81348 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 425 4 1 5 3.5 O=S(=O)(CC(F)(F)F)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70675705 128479 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
CHEMBL3666781 128479 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
70675727 128484 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)c(F)c3)no2)CC1 nan
CHEMBL3666786 128484 0 None - 0 Mouse 9.7 pIC50 = 9.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)c(F)c3)no2)CC1 nan
70675729 128486 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cc(F)cc(F)c3)no2)CC1 nan
CHEMBL3666788 128486 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cc(F)cc(F)c3)no2)CC1 nan
10255890 98463 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 513 4 1 5 5.4 O=C(Nc1ccc(Cl)c2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL275841 98463 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 513 4 1 5 5.4 O=C(Nc1ccc(Cl)c2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
68613905 125442 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 404 4 2 4 4.8 O=C(N[C@H]1CC[C@@H](c2nc(-c3ccc(Cl)c(Cl)c3)c[nH]2)CC1)c1ccon1 nan
CHEMBL3646136 125442 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 404 4 2 4 4.8 O=C(N[C@H]1CC[C@@H](c2nc(-c3ccc(Cl)c(Cl)c3)c[nH]2)CC1)c1ccon1 nan
71454971 81346 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 399 5 1 5 3.6 CC(C)CS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159165 81346 0 None - 0 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 399 5 1 5 3.6 CC(C)CS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70688848 76915 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 433 4 1 5 3.7 O=c1ccc(-c2nc3cc(S(=O)(=O)CC(F)(F)F)ccc3[nH]2)cn1-c1ccccc1 10.1016/j.bmcl.2012.07.020
CHEMBL2070161 76915 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 433 4 1 5 3.7 O=c1ccc(-c2nc3cc(S(=O)(=O)CC(F)(F)F)ccc3[nH]2)cn1-c1ccccc1 10.1016/j.bmcl.2012.07.020
71458601 81339 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 383 5 1 4 4.1 CCCS(=O)(=O)c1ccc2[nH]c(N3CCCC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159158 81339 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 383 5 1 4 4.1 CCCS(=O)(=O)c1ccc2[nH]c(N3CCCC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
10471957 25589 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 332 2 1 4 4.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc4ccccc4o3)cc2n1 10.1021/jm000269t
CHEMBL135143 25589 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 332 2 1 4 4.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc4ccccc4o3)cc2n1 10.1021/jm000269t
10712643 29386 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(F)cc3)cc2n1 10.1021/jm000269t
CHEMBL138379 29386 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(F)cc3)cc2n1 10.1021/jm000269t
10783815 119282 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3cccc(F)c3)cc2n1 10.1021/jm000269t
CHEMBL343817 119282 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3cccc(F)c3)cc2n1 10.1021/jm000269t
70697155 76911 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3ccnc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070157 76911 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3ccnc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
70675703 128477 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)no2)CC1 nan
CHEMBL3666779 128477 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)no2)CC1 nan
70675704 128478 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 364 7 2 6 2.6 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccccc3)no2)CC1 nan
CHEMBL3666780 128478 0 None - 0 Mouse 9.5 pIC50 = 9.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 364 7 2 6 2.6 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccccc3)no2)CC1 nan
11793187 28218 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc(F)cc(F)c3)cc2n1 10.1021/jm000269t
CHEMBL137378 28218 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc(F)cc(F)c3)cc2n1 10.1021/jm000269t
10266238 170805 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 290 2 1 3 3.7 Cc1nc(N2CC=CCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL445328 170805 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 290 2 1 3 3.7 Cc1nc(N2CC=CCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
68059511 125452 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 463 5 1 6 5.2 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccn4)CC3)ccc21 nan
CHEMBL3646146 125452 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 463 5 1 6 5.2 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccn4)CC3)ccc21 nan
66575661 76894 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070140 76894 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
56835982 81343 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 371 4 1 5 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159162 81343 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 371 4 1 5 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
56835982 81343 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 371 4 1 5 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2159162 81343 0 None - 0 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 371 4 1 5 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.11.005
56649677 76891 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 362 4 1 3 4.7 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070137 76891 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 362 4 1 3 4.7 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
9868487 202787 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human Neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity against human Neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 452 4 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1016/s0960-894x(01)00448-6
CHEMBL62166 202787 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity against human Neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity against human Neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 452 4 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1016/s0960-894x(01)00448-6
9868487 202787 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 452 4 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm980521l
CHEMBL62166 202787 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 452 4 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm980521l
10736124 28311 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.2 Cc1ccc(-c2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL137449 28311 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.2 Cc1ccc(-c2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
10040233 119213 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 296 2 1 4 3.8 Cc1nc(N2CCCCC2)c2nc(-c3ccc(C)o3)cc-2[nH]1 10.1021/jm000269t
CHEMBL343318 119213 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 296 2 1 4 3.8 Cc1nc(N2CCCCC2)c2nc(-c3ccc(C)o3)cc-2[nH]1 10.1021/jm000269t
89986727 128493 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 374 7 2 6 2.7 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(F)CCCC3)no2)CC1 nan
CHEMBL3666794 128493 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 374 7 2 6 2.7 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(F)CCCC3)no2)CC1 nan
10915401 205147 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 361 6 1 3 5.0 CC(Cc1ccncc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL78089 205147 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 361 6 1 3 5.0 CC(Cc1ccncc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
70697153 76901 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3F)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070147 76901 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3F)nc2c1 10.1016/j.bmcl.2012.07.020
10030142 58154 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 537 10 3 6 3.7 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL167991 58154 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 537 10 3 6 3.7 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
70684603 76909 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccn3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070155 76909 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccn3)nc2c1 10.1016/j.bmcl.2012.07.020
68601225 124402 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 453 5 1 6 5.3 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccc4C#N)CC3)ccc21 nan
CHEMBL3639450 124402 0 None - 0 Mouse 9.3 pIC50 = 9.3 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 453 5 1 6 5.3 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccc4C#N)CC3)ccc21 nan
18004895 187680 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL495169 187680 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004895 187680 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL495169 187680 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
68598300 125454 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 456 4 1 6 3.7 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](N2c3ccccc3OS2(=O)=O)CC1 nan
CHEMBL3646148 125454 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 456 4 1 6 3.7 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](N2c3ccccc3OS2(=O)=O)CC1 nan
44271202 59133 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 515 4 1 5 4.8 O=C(Nc1ccc(F)c(C(F)(F)F)c1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL16986 59133 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 515 4 1 5 4.8 O=C(Nc1ccc(F)c(C(F)(F)F)c1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
44271276 59955 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 471 5 1 6 3.8 CC(=O)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
CHEMBL17327 59955 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 471 5 1 6 3.8 CC(=O)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
71454968 81337 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 5 1 5 3.3 CCCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159156 81337 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 5 1 5 3.3 CCCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
91755094 128497 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 406 7 2 6 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(C)CC(F)(F)C3)no2)CC1 nan
CHEMBL3666798 128497 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 406 7 2 6 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(C)CC(F)(F)C3)no2)CC1 nan
9930807 197600 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.07.103
CHEMBL570633 197600 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.07.103
89986736 128501 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 420 7 2 6 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
CHEMBL3666801 128501 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 420 7 2 6 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
68606925 125441 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 389 5 2 4 4.3 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3ccccc3)cc2)CC1)c1ccon1 nan
CHEMBL3646135 125441 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 389 5 2 4 4.3 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3ccccc3)cc2)CC1)c1ccon1 nan
9908945 193062 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL522388 193062 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
68059308 125451 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 487 5 1 6 5.6 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccc4C#N)CC3)ccc21 nan
CHEMBL3646145 125451 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 487 5 1 6 5.6 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccc4C#N)CC3)ccc21 nan
9957190 198212 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 489 4 1 4 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(C(=O)c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL575214 198212 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 489 4 1 4 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(C(=O)c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
68594586 125453 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 414 5 1 5 4.6 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](Oc2cc(Cl)ccn2)CC1 nan
CHEMBL3646147 125453 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 414 5 1 5 4.6 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](Oc2cc(Cl)ccn2)CC1 nan
44583541 193301 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccc(Cl)cc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL524085 193301 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccc(Cl)cc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
10786956 27797 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 360 2 1 3 4.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(C(F)(F)F)cc3)cc2n1 10.1021/jm000269t
CHEMBL137086 27797 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 360 2 1 3 4.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(C(F)(F)F)cc3)cc2n1 10.1021/jm000269t
9882119 118564 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 278 2 1 3 3.5 Cc1nc(N2CCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL341563 118564 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 278 2 1 3 3.5 Cc1nc(N2CCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
89986726 128491 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 434 7 2 6 4.1 CC(C)(c1ccccc1)c1noc(N[C@H]2CC[C@H](CNS(=O)(=O)C(C)(C)C)CC2)n1 nan
CHEMBL3666792 128491 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 434 7 2 6 4.1 CC(C)(c1ccccc1)c1noc(N[C@H]2CC[C@H](CNS(=O)(=O)C(C)(C)C)CC2)n1 nan
10052173 57573 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 513 6 1 6 4.5 COc1ccc2c(c1)CC(NCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL166606 57573 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 513 6 1 6 4.5 COc1ccc2c(c1)CC(NCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44271202 59133 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 515 4 1 5 4.8 O=C(Nc1ccc(F)c(C(F)(F)F)c1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL16986 59133 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 515 4 1 5 4.8 O=C(Nc1ccc(F)c(C(F)(F)F)c1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
68601090 125439 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 407 5 2 4 4.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3ccccc3F)cc2)CC1)c1ccon1 nan
CHEMBL3646133 125439 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 407 5 2 4 4.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3ccccc3F)cc2)CC1)c1ccon1 nan
23442592 169337 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 459 10 2 7 3.8 COc1ccc(C)cc1S(=O)(=O)NCCCNc1ncc(C(=O)c2ccccc2C)s1 10.1016/j.bmcl.2005.05.009
CHEMBL441850 169337 0 None - 0 Mouse 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 459 10 2 7 3.8 COc1ccc(C)cc1S(=O)(=O)NCCCNc1ncc(C(=O)c2ccccc2C)s1 10.1016/j.bmcl.2005.05.009
44271382 98527 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 479 4 1 5 4.7 O=C(Nc1cccc2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL276283 98527 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 479 4 1 5 4.7 O=C(Nc1cccc2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
71458603 81347 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 411 3 1 5 3.4 O=S(=O)(c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1)C(F)(F)F 10.1016/j.bmcl.2012.09.025
CHEMBL2159166 81347 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 411 3 1 5 3.4 O=S(=O)(c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1)C(F)(F)F 10.1016/j.bmcl.2012.09.025
70675731 128489 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 397 7 2 7 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cn3)no2)CC1 nan
CHEMBL3666790 128489 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 397 7 2 7 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cn3)no2)CC1 nan
89986749 128494 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 420 6 2 6 3.4 CC1(c2noc(N[C@H]3CC[C@H](CNS(=O)(=O)C(C)(C)C)CC3)n2)CC(F)(F)C1 nan
CHEMBL3666795 128494 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 420 6 2 6 3.4 CC1(c2noc(N[C@H]3CC[C@H](CNS(=O)(=O)C(C)(C)C)CC3)n2)CC(F)(F)C1 nan
71458605 81352 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 4 1 5 3.2 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(C)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159171 81352 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 4 1 5 3.2 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(C)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70675705 128479 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
CHEMBL3666781 128479 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 382 7 2 6 2.8 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
18004997 193087 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL522540 193087 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004997 193087 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL522540 193087 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44583539 193424 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4Cl)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL526084 193424 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4Cl)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9908374 187747 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 389 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL495580 187747 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 389 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9869232 188043 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(C(F)(F)F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL497641 188043 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(C(F)(F)F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
18004896 187234 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492568 187234 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
71462130 81351 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 405 4 1 5 3.6 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(Cl)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159170 81351 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 405 4 1 5 3.6 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(Cl)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
23442647 67155 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 517 9 2 6 5.1 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)s1 10.1016/j.bmcl.2005.05.009
CHEMBL187607 67155 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 517 9 2 6 5.1 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)s1 10.1016/j.bmcl.2005.05.009
44271207 98908 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 521 6 1 6 5.4 O=C(Nc1ccc(Oc2ccccc2)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL279309 98908 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 521 6 1 6 5.4 O=C(Nc1ccc(Oc2ccccc2)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
70675727 128484 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)c(F)c3)no2)CC1 nan
CHEMBL3666786 128484 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a human NPY Y5 receptor (WO96/16542) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Inbitrogen) according to the instruction manual. The cells that stably express human NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing human NPY Y5 receptor, the compound of this invention and 30,000 cpm [1251] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 400 7 2 6 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)c(F)c3)no2)CC1 nan
70675709 128483 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 368 6 2 6 2.4 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
CHEMBL3666785 128483 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 368 6 2 6 2.4 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(F)c3)no2)CC1 nan
18004939 193240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL523715 193240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004939 193240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL523715 193240 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
11349780 199726 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 7 2.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL593465 199726 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 7 2.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
44271385 60552 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 533 6 1 6 4.8 O=C(c1ccccc1)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
CHEMBL17590 60552 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 533 6 1 6 4.8 O=C(c1ccccc1)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
70675730 128487 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 384 6 2 6 2.9 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(Cl)c3)no2)CC1 nan
CHEMBL3666789 128487 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 384 6 2 6 2.9 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3cccc(Cl)c3)no2)CC1 nan
70675732 128490 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 411 6 2 7 3.0 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cn3)no2)CC1 nan
CHEMBL3666791 128490 0 None - 0 Mouse 9.1 pIC50 = 9.1 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 411 6 2 7 3.0 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cn3)no2)CC1 nan
10927348 169385 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 394 6 1 2 6.2 CC(Cc1ccc(Cl)cc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL442182 169385 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 394 6 1 2 6.2 CC(Cc1ccc(Cl)cc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
9889156 192607 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(Cl)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL521545 192607 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(Cl)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
11407098 200070 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccc(F)cc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595790 200070 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccc(F)cc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
18004955 187569 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL494593 187569 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004955 187569 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL494593 187569 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
12108781 187690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL495201 187690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
12108781 187690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL495201 187690 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44583438 192605 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL521537 192605 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
135543802 204043 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 467 6 3 5 4.0 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4cc(O)ccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
CHEMBL69881 204043 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 467 6 3 5 4.0 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4cc(O)ccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
10926406 14043 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 5 1 3 5.3 CC(C)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL119743 14043 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 5 1 3 5.3 CC(C)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
11111992 110589 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 393 5 1 5 3.6 CS(=O)(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL325486 110589 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 393 5 1 5 3.6 CS(=O)(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
44583540 188038 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4cccc(Cl)c4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL497621 188038 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4cccc(Cl)c4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44461023 205659 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.1 O=C(C1CCOC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81994 205659 0 None - 0 Human 9.0 pIC50 = 9 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.1 O=C(C1CCOC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44379101 119927 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 543 6 2 7 3.3 COc1ccc2c(c1)C(O)(CNC(=O)C1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL349486 119927 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 543 6 2 7 3.3 COc1ccc2c(c1)C(O)(CNC(=O)C1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44344243 113315 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 526 12 4 6 3.6 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)CNC1CCc2cc(O)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL331551 113315 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 526 12 4 6 3.6 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)CNC1CCc2cc(O)ccc2C1Cc1cccnc1 10.1021/jm990468g
20616896 125046 0 None - 0 Mouse 9.0 pIC50 = 9 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 421 9 2 7 3.5 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cccs2)s1 10.1016/j.bmcl.2005.05.009
CHEMBL364386 125046 0 None - 0 Mouse 9.0 pIC50 = 9 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 421 9 2 7 3.5 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cccs2)s1 10.1016/j.bmcl.2005.05.009
71454972 81354 0 None - 0 Mouse 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 369 5 1 4 3.7 CCCS(=O)(=O)c1ccc2[nH]c(N3CCC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159174 81354 0 None - 0 Mouse 9.0 pIC50 = 9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 369 5 1 4 3.7 CCCS(=O)(=O)c1ccc2[nH]c(N3CCC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70675757 128498 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 434 6 2 6 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
CHEMBL3666799 128498 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 434 6 2 6 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
71451430 81350 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 389 4 1 5 3.1 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(F)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159169 81350 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 389 4 1 5 3.1 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(F)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
9796081 115421 2 None - 0 Human 9.0 pIC50 = 9.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 292 2 1 3 3.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL335039 115421 2 None - 0 Human 9.0 pIC50 = 9.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 292 2 1 3 3.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
68606301 125450 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 467 5 1 5 5.4 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccc4C#N)CC3)cc2)C[C@@H](C)O1 nan
CHEMBL3646144 125450 0 None - 0 Mouse 9.0 pIC50 = 9.0 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 467 5 1 5 5.4 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccc4C#N)CC3)cc2)C[C@@H](C)O1 nan
9953800 187755 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL495630 187755 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44583394 187842 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4Cl)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL496196 187842 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4Cl)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44583435 193159 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1ccccc1-c1cnc(NC(=O)N2CCC3(CC2)OC(=O)c2ccccc23)nc1 10.1016/j.bmcl.2009.05.013
CHEMBL523060 193159 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1ccccc1-c1cnc(NC(=O)N2CCC3(CC2)OC(=O)c2ccccc23)nc1 10.1016/j.bmcl.2009.05.013
44271223 98533 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 2 6 2.8 O=C(NCC(O)c1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL276322 98533 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 2 6 2.8 O=C(NCC(O)c1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
10685135 26324 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 2 4 3.2 Nc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL135883 26324 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 2 4 3.2 Nc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
9953150 187908 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 406 2 1 6 3.9 O=C1OC2(CCN(C(=O)Nc3nsc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL496621 187908 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 406 2 1 6 3.9 O=C1OC2(CCN(C(=O)Nc3nsc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
46226641 201829 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 405 3 1 6 4.4 O=C1O[C@]2(CC[C@H](C(=O)Nc3csc(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL607037 201829 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 405 3 1 6 4.4 O=C1O[C@]2(CC[C@H](C(=O)Nc3csc(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
44573574 193193 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 441 5 1 3 4.4 CCCCc1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmcl.2009.02.035
CHEMBL523330 193193 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 441 5 1 3 4.4 CCCCc1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmcl.2009.02.035
44379095 58126 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 541 6 1 6 4.3 COc1ccc2c(c1)CC(CNC(=O)C1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL167709 58126 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 541 6 1 6 4.3 COc1ccc2c(c1)CC(CNC(=O)C1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44271223 98533 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 2 6 2.8 O=C(NCC(O)c1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL276322 98533 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 2 6 2.8 O=C(NCC(O)c1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
18004944 198382 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 452 3 1 5 3.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cc(-c4ccccc4)no3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL576727 198382 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 452 3 1 5 3.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cc(-c4ccccc4)no3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44583463 193481 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4C(F)(F)F)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL526645 193481 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4C(F)(F)F)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9952232 199969 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL595120 199969 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
11491176 200043 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595573 200043 38 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
12108783 193294 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccccc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL524051 193294 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccccc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44583541 193301 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccc(Cl)cc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL524085 193301 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 423 2 1 5 4.7 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccc(Cl)cc4)no3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
1562 899 13 None - 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
5312114 899 13 None - 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL17645 899 13 None - 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
CHEMBL195380 899 13 None - 2 Human 8.9 pIC50 = 8.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2005.03.052
44271289 169189 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 493 12 1 5 5.2 CCCCCCCCCCNC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL440647 169189 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 493 12 1 5 5.2 CCCCCCCCCCNC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
71453236 81344 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 4 1 5 3.3 CC(C)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159163 81344 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 4 1 5 3.3 CC(C)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70675707 128481 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 368 6 2 6 2.4 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)no2)CC1 nan
CHEMBL3666783 128481 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 368 6 2 6 2.4 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)no2)CC1 nan
45481798 198053 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 2 4 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cc(-c4ccccc4)n[nH]3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL574084 198053 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 2 4 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cc(-c4ccccc4)n[nH]3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
1562 899 13 None 2 2 Rat 8.9 pIC50 = 8.9 Binding
Compound was tested for rat Neuropeptide Y receptor type 5Compound was tested for rat Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
5312114 899 13 None 2 2 Rat 8.9 pIC50 = 8.9 Binding
Compound was tested for rat Neuropeptide Y receptor type 5Compound was tested for rat Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL17645 899 13 None 2 2 Rat 8.9 pIC50 = 8.9 Binding
Compound was tested for rat Neuropeptide Y receptor type 5Compound was tested for rat Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL195380 899 13 None 2 2 Rat 8.9 pIC50 = 8.9 Binding
Compound was tested for rat Neuropeptide Y receptor type 5Compound was tested for rat Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
9908945 193062 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL522388 193062 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44573541 193315 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 474 5 3 5 3.5 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)CC1 10.1016/j.bmcl.2009.02.035
CHEMBL524192 193315 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 474 5 3 5 3.5 CS(=O)(=O)Nc1ccccc1N1CCN(C(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)CC1 10.1016/j.bmcl.2009.02.035
44271284 58089 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 459 4 2 6 3.6 Cc1cc(O)ccc1NC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL16740 58089 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 459 4 2 6 3.6 Cc1cc(O)ccc1NC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
44271317 60411 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 1 6 3.3 COc1ccc(CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
CHEMBL17502 60411 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 1 6 3.3 COc1ccc(CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
44271385 60552 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 533 6 1 6 4.8 O=C(c1ccccc1)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
CHEMBL17590 60552 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 533 6 1 6 4.8 O=C(c1ccccc1)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
71458604 81349 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 453 4 1 5 4.3 CC(C)(C(F)(F)F)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159168 81349 0 None - 0 Mouse 8.9 pIC50 = 8.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 453 4 1 5 4.3 CC(C)(C(F)(F)F)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
70675779 128492 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 384 5 2 6 2.8 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)no2)CC1 nan
CHEMBL3666793 128492 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 384 5 2 6 2.8 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)no2)CC1 nan
68605769 125446 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 412 5 2 6 4.3 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Nc4cccc(F)n4)CC3)ccc21 nan
CHEMBL3646140 125446 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 412 5 2 6 4.3 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](Nc4cccc(F)n4)CC3)ccc21 nan
68606747 125447 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 443 5 1 5 4.9 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccn4)CC3)cc2)C[C@@H](C)O1 nan
CHEMBL3646141 125447 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 443 5 1 5 4.9 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(Cl)ccn4)CC3)cc2)C[C@@H](C)O1 nan
9802119 197081 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL567495 197081 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
9802118 198913 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL584526 198913 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
9908890 199785 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.08.019
CHEMBL593934 199785 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.08.019
18004985 193055 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 1 3 5.2 CS(=O)(=O)N1C[C@]2(CC[C@H](C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL522321 193055 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 1 3 5.2 CS(=O)(=O)N1C[C@]2(CC[C@H](C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44271207 98908 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 521 6 1 6 5.4 O=C(Nc1ccc(Oc2ccccc2)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL279309 98908 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 521 6 1 6 5.4 O=C(Nc1ccc(Oc2ccccc2)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
46912808 125433 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 425 5 2 5 3.5 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1)c1cccc(F)n1 nan
CHEMBL3646127 125433 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 425 5 2 5 3.5 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1)c1cccc(F)n1 nan
44580050 184204 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL483251 184204 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44401591 68897 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL192266 68897 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 8 3 7 5.1 Nc1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
23442776 125798 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 475 11 2 8 3.5 COc1ccc(OC)c(S(=O)(=O)NCCCNc2ncc(C(=O)c3ccccc3C)s2)c1 10.1016/j.bmcl.2005.05.009
CHEMBL364796 125798 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 475 11 2 8 3.5 COc1ccc(OC)c(S(=O)(=O)NCCCNc2ncc(C(=O)c3ccccc3C)s2)c1 10.1016/j.bmcl.2005.05.009
89986718 128502 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 406 7 2 6 2.6 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
CHEMBL3666802 128502 0 None - 0 Mouse 8.8 pIC50 = 8.8 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 406 7 2 6 2.6 CCS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)C(F)(F)F)no2)CC1 nan
10565529 116730 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 4.5 Cc1cc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL337427 116730 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 4.5 Cc1cc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
9796164 96956 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 294 1 1 1 4.9 Clc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL266241 96956 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 294 1 1 1 4.9 Clc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
9823032 187871 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 413 2 2 4 3.3 O=C1Cc2ccccc2C2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)N1 10.1016/j.bmcl.2009.05.013
CHEMBL496392 187871 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 413 2 2 4 3.3 O=C1Cc2ccccc2C2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)N1 10.1016/j.bmcl.2009.05.013
9979057 187069 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 412 2 1 3 6.1 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccc(F)cc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL491229 187069 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 412 2 1 3 6.1 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccc(F)cc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
9887225 187148 3 None - 1 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL491930 187148 3 None - 1 Mouse 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9887225 187148 3 None - 1 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL491930 187148 3 None - 1 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]PYY from rat NPY Y5 receptorDisplacement of [125I]PYY from rat NPY Y5 receptor
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9952231 199820 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL594163 199820 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
44271267 98786 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 2 6 3.1 O=C(Nc1ccc(CCO)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL278280 98786 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 2 6 3.1 O=C(Nc1ccc(CCO)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
9926566 28027 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.3 Cc1nc(N2CCCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137259 28027 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.3 Cc1nc(N2CCCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
68616467 125444 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 404 4 2 4 4.5 O=C(N[C@H]1CC[C@@H](c2nc(-c3cccc(C(F)(F)F)c3)c[nH]2)CC1)c1ccon1 nan
CHEMBL3646138 125444 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 404 4 2 4 4.5 O=C(N[C@H]1CC[C@@H](c2nc(-c3cccc(C(F)(F)F)c3)c[nH]2)CC1)c1ccon1 nan
68607021 125449 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 501 5 1 5 5.8 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccc4C#N)CC3)cc2)C[C@@H](C)O1 nan
CHEMBL3646143 125449 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 501 5 1 5 5.8 C[C@H]1CN(c2ccc(NC(=O)[C@H]3CC[C@@H](Oc4cc(C(F)(F)F)ccc4C#N)CC3)cc2)C[C@@H](C)O1 nan
44580708 187855 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 375 3 1 4 4.4 CC(C)Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL496326 187855 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 375 3 1 4 4.4 CC(C)Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
45481809 198023 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL573860 198023 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
9933356 197059 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL567310 197059 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
9952815 197088 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL567527 197088 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
9953802 197641 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL570864 197641 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
11224238 198968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(CF)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL585107 198968 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(CF)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
11633103 198979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL585203 198979 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
44583436 187754 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1cccc(-c2cnc(NC(=O)N3CCC4(CC3)OC(=O)c3ccccc34)nc2)c1 10.1016/j.bmcl.2009.05.013
CHEMBL495625 187754 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1cccc(-c2cnc(NC(=O)N3CCC4(CC3)OC(=O)c3ccccc34)nc2)c1 10.1016/j.bmcl.2009.05.013
44583559 187873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 405 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL496399 187873 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 405 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
9952815 197088 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL567527 197088 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
70682529 76910 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cncc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070156 76910 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cncc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
70675752 128503 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 424 6 2 6 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(F)CC(F)(F)C3)no2)CC1 nan
CHEMBL3666803 128503 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 424 6 2 6 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C3(F)CC(F)(F)C3)no2)CC1 nan
9955287 197060 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL567318 197060 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
9886573 187980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 2 4 3.8 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4)n[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL497211 187980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 2 4 3.8 O=C1OC2(CCN(C(=O)Nc3cc(-c4ccccc4)n[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
70688845 76897 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 1 4 4.3 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(OC(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070143 76897 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 1 4 4.3 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(OC(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.07.020
70684604 76912 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 393 5 1 5 3.6 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccc(=O)n(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070158 76912 0 None - 0 Mouse 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 393 5 1 5 3.6 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccc(=O)n(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
10757242 28552 0 None - 0 Human 8.0 pIC50 = 8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 272 4 1 3 3.6 CCCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
CHEMBL137638 28552 0 None - 0 Human 8.0 pIC50 = 8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 272 4 1 3 3.6 CCCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
44580667 187967 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 364 2 1 6 3.1 O=C1OC2(CCN(c3nc4cc([N+](=O)[O-])ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497152 187967 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 364 2 1 6 3.1 O=C1OC2(CCN(c3nc4cc([N+](=O)[O-])ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44580666 188022 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 397 1 1 4 4.0 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497570 188022 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 397 1 1 4 4.0 O=C1OC2(CCN(c3nc4cc(Br)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
10186456 103413 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 523 7 2 7 4.6 Nc1cc(C2CCC(CNS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL3084802 103413 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 523 7 2 7 4.6 Nc1cc(C2CCC(CNS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44312780 103412 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 523 7 2 7 4.6 Nc1cc(C2CCC(CNS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)nn1-c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL3084801 103412 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 523 7 2 7 4.6 Nc1cc(C2CCC(CNS(=O)(=O)c3ccccc3[N+](=O)[O-])CC2)nn1-c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00448-6
9924627 193075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 352 3 1 2 4.4 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(F)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL522489 193075 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 352 3 1 2 4.4 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(F)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
9850107 11012 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 536 8 2 5 3.4 O=C(CN1CCC(NS(=O)(=O)c2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL117400 11012 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 536 8 2 5 3.4 O=C(CN1CCC(NS(=O)(=O)c2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
44344497 103443 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 533 10 2 5 5.1 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3)CC1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL3084895 103443 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 533 10 2 5 5.1 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3)CC1)C2Cc1cccnc1 10.1021/jm990468g
44271355 59652 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 500 4 1 7 4.5 Cc1ccc2nc(NC(=O)C3CCN(C(=O)Cn4c(=O)sc5ccc(Cl)cc54)CC3)sc2c1 10.1016/s0960-894x(02)00113-0
CHEMBL17214 59652 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 500 4 1 7 4.5 Cc1ccc2nc(NC(=O)C3CCN(C(=O)Cn4c(=O)sc5ccc(Cl)cc54)CC3)sc2c1 10.1016/s0960-894x(02)00113-0
3087469 28247 4 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 294 2 1 4 2.8 Cc1nc(N2CCOCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137404 28247 4 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 294 2 1 4 2.8 Cc1nc(N2CCOCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10664487 30676 0 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 298 2 1 4 4.0 Cc1nc(N2CCCCC2)c2[nH]c(-c3cccs3)cc2n1 10.1021/jm000269t
CHEMBL139483 30676 0 None - 0 Human 7.0 pIC50 = 7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 298 2 1 4 4.0 Cc1nc(N2CCCCC2)c2[nH]c(-c3cccs3)cc2n1 10.1021/jm000269t
44313331 204860 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 420 6 2 6 3.9 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccccc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL75662 204860 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 420 6 2 6 3.9 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccccc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
10295464 205701 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82374 205701 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10257065 12887 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cc(Cl)ccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL1188887 12887 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cc(Cl)ccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL537634 12887 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cc(Cl)ccc54)CC3)ccc21 10.1021/jm049599u
44271556 98436 0 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 444 6 1 3 5.2 O=S(=O)(c1cccc2ccccc12)N1CCC(CNCc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(00)00177-3
CHEMBL275610 98436 0 None - 0 Human 6.0 pIC50 = 6 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 444 6 1 3 5.2 O=S(=O)(c1cccc2ccccc12)N1CCC(CNCc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(00)00177-3
44377690 58148 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CCCC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)C2 10.1016/s0960-894x(02)00002-1
CHEMBL167926 58148 0 None - 0 Human 6.0 pIC50 = 6 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CCCC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)C2 10.1016/s0960-894x(02)00002-1
25067562 184198 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
CHEMBL483239 184198 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
44579862 186873 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1cc2[nH]c([C@H]3CC[C@]4(CC3)OC(=O)c3ccccc34)nc2cc1Cl 10.1016/j.bmcl.2008.08.021
CHEMBL489609 186873 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1cc2[nH]c([C@H]3CC[C@]4(CC3)OC(=O)c3ccccc34)nc2cc1Cl 10.1016/j.bmcl.2008.08.021
44390110 161692 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 328 5 1 5 4.3 COc1cccc(Nc2ncc(C(=O)c3ccccc3F)s2)c1 10.1016/j.bmcl.2005.01.063
CHEMBL413359 161692 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 328 5 1 5 4.3 COc1cccc(Nc2ncc(C(=O)c3ccccc3F)s2)c1 10.1016/j.bmcl.2005.01.063
44580502 192908 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 336 1 0 5 4.0 O=C1OC2(CCN(c3nc4ccccc4s3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL522213 192908 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 336 1 0 5 4.0 O=C1OC2(CCN(c3nc4ccccc4s3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
10481364 12989 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 471 6 1 5 5.3 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc(Oc3ccccc3)cc2)CC1 10.1021/jm049599u
CHEMBL1189619 12989 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 471 6 1 5 5.3 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc(Oc3ccccc3)cc2)CC1 10.1021/jm049599u
CHEMBL539084 12989 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 471 6 1 5 5.3 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc(Oc3ccccc3)cc2)CC1 10.1021/jm049599u
10616756 26283 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 298 2 1 3 4.3 Cc1nc(N2CCCCC2)c2nc(C3CCCCC3)cc-2[nH]1 10.1021/jm000269t
CHEMBL135831 26283 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 298 2 1 3 4.3 Cc1nc(N2CCCCC2)c2nc(C3CCCCC3)cc-2[nH]1 10.1021/jm000269t
45481639 198452 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 420 2 1 4 3.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL577358 198452 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 420 2 1 4 3.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)nc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44379410 58109 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 10 3 6 3.5 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc(Cl)c3C)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL167558 58109 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 10 3 6 3.5 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc(Cl)c3C)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44344312 103423 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 565 9 2 5 4.8 COc1ccc2c(c1)CCC(NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3F)CC1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL3084871 103423 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 565 9 2 5 4.8 COc1ccc2c(c1)CCC(NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3F)CC1)C2Cc1cccnc1 10.1021/jm990468g
44344356 103429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 547 9 2 5 4.6 COc1ccc2c(c1)CCC(NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3)CC1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL3084877 103429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 547 9 2 5 4.6 COc1ccc2c(c1)CCC(NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3)CC1)C2Cc1cccnc1 10.1021/jm990468g
9810707 169415 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CCC(NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL442399 169415 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CCC(NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
20616889 66932 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 421 9 2 7 3.5 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cccs2)n1 10.1016/j.bmcl.2005.05.009
CHEMBL186620 66932 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 421 9 2 7 3.5 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cccs2)n1 10.1016/j.bmcl.2005.05.009
23442542 67134 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 445 10 2 7 3.5 COc1cccc(S(=O)(=O)NCCCNc2ncc(C(=O)c3ccccc3C)s2)c1 10.1016/j.bmcl.2005.05.009
CHEMBL187507 67134 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 445 10 2 7 3.5 COc1cccc(S(=O)(=O)NCCCNc2ncc(C(=O)c3ccccc3C)s2)c1 10.1016/j.bmcl.2005.05.009
10325002 13139 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 6 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm049599u
CHEMBL1190573 13139 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 6 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm049599u
CHEMBL541121 13139 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 6 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm049599u
10457755 48427 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 477 6 3 6 3.5 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccs2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
CHEMBL155553 48427 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 477 6 3 6 3.5 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccs2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
70688846 76898 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 375 5 1 2 5.7 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)cc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070144 76898 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 375 5 1 2 5.7 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3)cc2c1 10.1016/j.bmcl.2012.07.020
44580710 188159 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 362 2 2 5 2.3 NC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL498594 188159 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 362 2 2 5 2.3 NC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
22934120 97258 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1ccc(-c2nc3c([nH]2)-c2ccccc2CCC3)nc1 10.1016/s0960-894x(02)00090-2
CHEMBL268810 97258 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1ccc(-c2nc3c([nH]2)-c2ccccc2CCC3)nc1 10.1016/s0960-894x(02)00090-2
22934115 203540 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL6646 203540 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
10519637 28528 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 282 2 1 4 3.5 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccco3)cc2n1 10.1021/jm000269t
CHEMBL137619 28528 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 282 2 1 4 3.5 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccco3)cc2n1 10.1021/jm000269t
22257113 102914 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 499 5 2 4 4.4 O=C(NC1=NC2CCc3cc(Cl)ccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
CHEMBL306099 102914 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 499 5 2 4 4.4 O=C(NC1=NC2CCc3cc(Cl)ccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
71519169 86175 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 376 5 1 3 4.6 CCS(=O)(=O)c1ccc2[nH]c(Cc3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312078 86175 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 376 5 1 3 4.6 CCS(=O)(=O)c1ccc2[nH]c(Cc3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
10256047 12818 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 5 1 4 5.9 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C2CCCCC2)cc1 10.1021/jm049599u
CHEMBL1188309 12818 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 5 1 4 5.9 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C2CCCCC2)cc1 10.1021/jm049599u
CHEMBL536045 12818 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 5 1 4 5.9 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(C2CCCCC2)cc1 10.1021/jm049599u
44312965 103490 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 472 6 2 5 4.6 Nc1cc(-c2ccc(CNS(=O)(=O)c3ccccc3)cc2)nn1-c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL308508 103490 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 472 6 2 5 4.6 Nc1cc(-c2ccc(CNS(=O)(=O)c3ccccc3)cc2)nn1-c1ccc(C(F)(F)F)cc1 10.1016/s0960-894x(01)00448-6
44289816 164096 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 513 8 2 3 5.1 O=C(Cc1ccccc1)NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
CHEMBL42096 164096 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 513 8 2 3 5.1 O=C(Cc1ccccc1)NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
44288395 162572 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
CHEMBL41686 162572 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 517 10 5 3 4.0 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)N[C@H]1CCc2ccccc21 10.1016/s0960-894x(00)00292-4
11783658 110612 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 373 2 1 3 4.5 CC(C)n1c2ccccc2c2c(F)c(NC(=O)N3CCOCC3)c(F)cc21 10.1021/jm011125x
CHEMBL325639 110612 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 373 2 1 3 4.5 CC(C)n1c2ccccc2c2c(F)c(NC(=O)N3CCOCC3)c(F)cc21 10.1021/jm011125x
44344608 103450 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 553 8 2 4 4.9 O=C(NC1CCc2cc(F)ccc2C1Cc1cccnc1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2F)CC1 10.1021/jm990468g
CHEMBL3084904 103450 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 553 8 2 4 4.9 O=C(NC1CCc2cc(F)ccc2C1Cc1cccnc1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2F)CC1 10.1021/jm990468g
71518852 86160 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 366 5 1 4 4.3 CCS(=O)(=O)c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312063 86160 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 366 5 1 4 4.3 CCS(=O)(=O)c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1 10.1016/j.bmcl.2012.11.005
10071200 50267 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 427 6 3 6 2.4 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccs2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
CHEMBL157157 50267 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 427 6 3 6 2.4 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccs2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
10547234 118797 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 335 5 2 4 4.4 CCCNc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL342153 118797 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 335 5 2 4 4.4 CCCNc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44401626 71354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195810 71354 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 558 7 2 6 5.2 O=S(=O)(NCC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
11284878 64343 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181217 64343 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(N[C@H]2CC[C@@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10779946 116676 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 4.5 Cc1cc2cc(-c3ccccc3)[nH]c2c(N2CCCCC2)n1 10.1021/jm000269t
CHEMBL337105 116676 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 4.5 Cc1cc2cc(-c3ccccc3)[nH]c2c(N2CCCCC2)n1 10.1021/jm000269t
44308516 167807 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 513 6 2 5 3.9 COc1ccc2c(c1)CCC1N=C(NC(=O)[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4F)CC3)CC21 10.1016/s0960-894x(99)00676-9
CHEMBL430604 167807 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 513 6 2 5 3.9 COc1ccc2c(c1)CCC1N=C(NC(=O)[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4F)CC3)CC21 10.1016/s0960-894x(99)00676-9
10916153 204986 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 390 7 2 3 5.5 CCN(C(=O)Nc1ccc(Oc2ccccc2)cc1)[C@H](C)[C@@H](O)c1ccccc1 10.1021/jm0004547
CHEMBL76627 204986 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 390 7 2 3 5.5 CCN(C(=O)Nc1ccc(Oc2ccccc2)cc1)[C@H](C)[C@@H](O)c1ccccc1 10.1021/jm0004547
11824961 205170 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL78265 205170 0 None - 1 Human 6.9 pIC50 = 6.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
9857217 97065 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL267193 97065 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
22934114 97364 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL269561 97364 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
44461107 169235 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 437 4 1 5 4.8 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL441059 169235 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 437 4 1 5 4.8 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44379089 58141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 501 10 3 6 2.8 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc(C)c3)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL167860 58141 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 501 10 3 6 2.8 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc(C)c3)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44580747 188060 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 376 2 2 5 3.2 CC(=O)Nc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL497786 188060 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 376 2 2 5 3.2 CC(=O)Nc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44573448 187269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccc(Cl)cc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL492779 187269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccc(Cl)cc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
10614625 116645 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 0 4 3.9 Cc1nc(N2CCCCC2)c2c(cc(-c3ccccc3)n2C)n1 10.1021/jm000269t
CHEMBL336985 116645 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 0 4 3.9 Cc1nc(N2CCCCC2)c2c(cc(-c3ccccc3)n2C)n1 10.1021/jm000269t
10959714 204962 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 6 1 2 6.0 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C(C)(C)Cc1ccccc1 10.1021/jm0004547
CHEMBL76478 204962 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 6 1 2 6.0 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C(C)(C)Cc1ccccc1 10.1021/jm0004547
10455186 13926 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 390 4 1 5 3.1 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
CHEMBL1196451 13926 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 390 4 1 5 3.1 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
CHEMBL556999 13926 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 390 4 1 5 3.1 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
44390156 63500 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 416 4 1 4 6.2 O=C(c1cnc(Nc2cccc(C(F)(F)F)c2)s1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.01.063
CHEMBL179979 63500 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 416 4 1 4 6.2 O=C(c1cnc(Nc2cccc(C(F)(F)F)c2)s1)c1ccccc1C(F)(F)F 10.1016/j.bmcl.2005.01.063
10481215 12826 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1cccc2c1-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL1188388 12826 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1cccc2c1-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL536275 12826 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1cccc2c1-c1ccccc1C2=O 10.1021/jm049599u
44583437 187785 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1ccc(-c2cnc(NC(=O)N3CCC4(CC3)OC(=O)c3ccccc34)nc2)cc1 10.1016/j.bmcl.2009.05.013
CHEMBL495828 187785 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 430 3 1 6 3.8 COc1ccc(-c2cnc(NC(=O)N3CCC4(CC3)OC(=O)c3ccccc34)nc2)cc1 10.1016/j.bmcl.2009.05.013
44390067 63471 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 339 4 1 6 4.7 Cc1cc(C(=O)c2cnc(Nc3cccc(C#N)c3)s2)c(C)s1 10.1016/j.bmcl.2005.01.063
CHEMBL179848 63471 0 None - 0 Mouse 7.9 pIC50 = 7.9 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 339 4 1 6 4.7 Cc1cc(C(=O)c2cnc(Nc3cccc(C#N)c3)s2)c(C)s1 10.1016/j.bmcl.2005.01.063
10738836 28030 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 348 2 1 4 5.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc4ccccc4s3)cc2n1 10.1021/jm000269t
CHEMBL137260 28030 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 348 2 1 4 5.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc4ccccc4s3)cc2n1 10.1021/jm000269t
22325344 193140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.2 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL522913 193140 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.2 O=C1OC2(CCN(c3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44377916 57164 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 523 10 2 6 3.6 COc1ccc2c(c1OC)CC(NCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL164748 57164 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 523 10 2 6 3.6 COc1ccc2c(c1OC)CC(NCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
44289833 166129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 3 4 3.5 CC(C)(C)NC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
CHEMBL42611 166129 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 3 4 3.5 CC(C)(C)NC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
10573317 119249 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 368 3 1 3 5.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(-c4ccccc4)cc3)cc2n1 10.1021/jm000269t
CHEMBL343564 119249 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 368 3 1 3 5.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccc(-c4ccccc4)cc3)cc2n1 10.1021/jm000269t
10520484 165363 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 294 2 1 5 2.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3cnccn3)cc2n1 10.1021/jm000269t
CHEMBL423720 165363 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 294 2 1 5 2.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3cnccn3)cc2n1 10.1021/jm000269t
44580505 188103 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.7 O=C1O[C@]2(CC[C@@H](c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL498197 188103 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.7 O=C1O[C@]2(CC[C@@H](c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
20556258 63765 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 419 4 1 7 2.9 COc1cc2nc(N3CCC(N4Cc5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
CHEMBL18016 63765 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 419 4 1 7 2.9 COc1cc2nc(N3CCC(N4Cc5ccccc5C4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
44370270 48044 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 597 9 3 5 6.8 CC(C)c1cc(C(C)C)c(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cc4ccccc4s3)CC2)c(C(C)C)c1 10.1016/j.bmcl.2003.11.070
CHEMBL155048 48044 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 597 9 3 5 6.8 CC(C)c1cc(C(C)C)c(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cc4ccccc4s3)CC2)c(C(C)C)c1 10.1016/j.bmcl.2003.11.070
44313078 204826 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 447 6 2 6 4.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4cccc(N(C)C)c4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL75369 204826 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 447 6 2 6 4.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4cccc(N(C)C)c4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44370250 51086 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 472 6 3 6 2.8 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3cccnc23)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
CHEMBL157905 51086 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 472 6 3 6 2.8 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3cccnc23)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
10253263 69491 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 450 4 1 5 4.4 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2ncccc2c1 10.1021/jm049599u
CHEMBL193382 69491 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 450 4 1 5 4.4 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2ncccc2c1 10.1021/jm049599u
10883239 169711 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 373 2 1 5 2.5 CS(=O)(=O)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL443809 169711 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 373 2 1 5 2.5 CS(=O)(=O)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
9824246 167779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(C)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00449-8
CHEMBL430414 167779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line by using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(C)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00449-8
9824246 167779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(C)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL430414 167779 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(C)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
44579864 193096 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 2 1 6 4.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5nnco5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL522609 193096 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 2 1 6 4.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5nnco5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
44460811 163342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 500 6 2 6 5.3 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)-c2ccccc2Sc2ccccc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL419104 163342 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 500 6 2 6 5.3 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)-c2ccccc2Sc2ccccc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461003 205611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 476 5 1 4 6.5 CC(=O)C1(c2ccccc2)CCC(CC(=O)Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81621 205611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 476 5 1 4 6.5 CC(=O)C1(c2ccccc2)CCC(CC(=O)Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460943 205612 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 455 5 2 5 5.9 O=C(N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)c1cccs1 10.1016/j.bmcl.2004.03.014
CHEMBL81636 205612 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 455 5 2 5 5.9 O=C(N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)c1cccs1 10.1016/j.bmcl.2004.03.014
44461201 205862 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 460 9 2 6 3.7 COCCCNCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL83748 205862 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 460 9 2 6 3.7 COCCCNCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
71451429 81341 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 5 1 5 3.3 CCCS(=O)(=O)c1ccc2[nH]c(C3CN(c4ccccc4)CCO3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159160 81341 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 385 5 1 5 3.3 CCCS(=O)(=O)c1ccc2[nH]c(C3CN(c4ccccc4)CCO3)nc2c1 10.1016/j.bmcl.2012.09.025
10830247 28246 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 1 4 3.3 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccn3)cc2n1 10.1021/jm000269t
CHEMBL137403 28246 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 1 4 3.3 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccn3)cc2n1 10.1021/jm000269t
10810223 118779 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 5 1 4 4.0 COc1ccc(CCc2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL341993 118779 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 5 1 4 4.0 COc1ccc(CCc2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
10047390 204970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 413 3 1 3 5.8 Cc1cc(C(=O)Nc2cc(Cl)cc(Cl)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL76512 204970 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 413 3 1 3 5.8 Cc1cc(C(=O)Nc2cc(Cl)cc(Cl)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44460881 205365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 484 7 2 5 5.4 O=C(CCN1CCCCC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79815 205365 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 484 7 2 5 5.4 O=C(CCN1CCCCC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
11284878 70441 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194602 70441 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
10736625 119181 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 314 4 2 3 4.5 Cc1nc(NCc2ccccc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL343102 119181 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 314 4 2 3 4.5 Cc1nc(NCc2ccccc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10007341 120065 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL350620 120065 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
10007341 120065 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL350620 120065 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
44289698 173081 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 2 4 5.3 CC(C)(C)OC(=O)NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
CHEMBL45199 173081 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 2 4 5.3 CC(C)(C)OC(=O)NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
70695681 78355 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 383 7 3 3 3.9 O=C(O)CCc1cccc(CC(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)c1 10.1021/jm025513q
CHEMBL2110162 78355 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 383 7 3 3 3.9 O=C(O)CCc1cccc(CC(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)c1 10.1021/jm025513q
10849420 119222 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 230 1 1 3 2.5 Cc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
CHEMBL343394 119222 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 230 1 1 3 2.5 Cc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
12822578 60354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 481 5 1 8 3.5 COc1cc2nc(N3CCC(N4C(=O)CC(C5CCCCC5)CC4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
CHEMBL17456 60354 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 481 5 1 8 3.5 COc1cc2nc(N3CCC(N4C(=O)CC(C5CCCCC5)CC4=O)CC3)nc(N)c2cc1OC 10.1016/s0960-894x(00)00177-3
44573567 187469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL494018 187469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44573606 192665 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccncc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL521862 192665 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccncc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44573449 193133 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 402 3 1 2 5.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccc(C(F)(F)F)cc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL522866 193133 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 402 3 1 2 5.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccc(C(F)(F)F)cc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
10617610 28628 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(F)c2n1 10.1021/jm000269t
CHEMBL137711 28628 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(F)c2n1 10.1021/jm000269t
44580503 187768 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 320 1 1 5 2.6 O=C1OC2(CCN(c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL495725 187768 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 320 1 1 5 2.6 O=C1OC2(CCN(c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
1284592 105822 43 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 270 3 1 3 4.7 Fc1ccc(-c2csc(Nc3ccccc3)n2)cc1 10.1016/j.bmcl.2004.03.014
CHEMBL312711 105822 43 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 270 3 1 3 4.7 Fc1ccc(-c2csc(Nc3ccccc3)n2)cc1 10.1016/j.bmcl.2004.03.014
44313092 168052 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 447 6 2 6 4.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(N(C)C)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL432352 168052 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 447 6 2 6 4.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(N(C)C)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
10959285 205060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 358 4 1 2 5.1 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C1Cc2ccccc2C1 10.1021/jm0004547
CHEMBL77208 205060 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 358 4 1 2 5.1 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C1Cc2ccccc2C1 10.1021/jm0004547
11068453 103156 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 362 6 3 3 4.7 C[C@@H](NC(=O)Nc1ccc(Oc2ccccc2)cc1)[C@@H](O)c1ccccc1 10.1021/jm0004547
CHEMBL308046 103156 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 362 6 3 3 4.7 C[C@@H](NC(=O)Nc1ccc(Oc2ccccc2)cc1)[C@@H](O)c1ccccc1 10.1021/jm0004547
44390111 62786 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 332 4 1 4 4.9 O=C(c1cnc(Nc2ccc(Cl)cc2)s1)c1ccccc1F 10.1016/j.bmcl.2005.01.063
CHEMBL178412 62786 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 332 4 1 4 4.9 O=C(c1cnc(Nc2ccc(Cl)cc2)s1)c1ccccc1F 10.1016/j.bmcl.2005.01.063
17965215 28450 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 2 1 3 4.7 Cc1nc2cc(-c3ccccc3)nc-2c(N2C(C)CCCC2C)[nH]1 10.1021/jm000269t
CHEMBL137538 28450 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 2 1 3 4.7 Cc1nc2cc(-c3ccccc3)nc-2c(N2C(C)CCCC2C)[nH]1 10.1021/jm000269t
44580665 193361 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4c(-c5ccccc5)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL524988 193361 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4c(-c5ccccc5)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44573647 193196 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cncc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL523339 193196 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cncc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
44460473 205586 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL81427 205586 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44461159 205678 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 7 1 6 4.6 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(OC)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82196 205678 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 7 1 6 4.6 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(OC)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44289834 168686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)N[C@H]1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
CHEMBL43659 168686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)N[C@H]1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
23442779 126296 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 475 11 2 8 3.5 COc1ccc(OC)c(S(=O)(=O)NCCCNc2nc(C(=O)c3ccccc3C)cs2)c1 10.1016/j.bmcl.2005.05.009
CHEMBL365021 126296 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 475 11 2 8 3.5 COc1ccc(OC)c(S(=O)(=O)NCCCNc2nc(C(=O)c3ccccc3C)cs2)c1 10.1016/j.bmcl.2005.05.009
44271382 98527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 479 4 1 5 4.7 O=C(Nc1cccc2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL276283 98527 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 479 4 1 5 4.7 O=C(Nc1cccc2ccccc12)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
71454970 81340 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 1 4 4.4 CCCS(=O)(=O)c1ccc2[nH]c(C3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159159 81340 0 None - 0 Mouse 7.8 pIC50 = 7.8 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 1 4 4.4 CCCS(=O)(=O)c1ccc2[nH]c(C3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
10094963 12876 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 407 5 1 5 3.4 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
CHEMBL1188798 12876 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 407 5 1 5 3.4 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
CHEMBL537412 12876 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 407 5 1 5 3.4 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4ccccc43)CC2)cc1 10.1021/jm049599u
10645275 119297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 374 3 1 3 4.8 Cc1nc(N2CCCCC2)c2nc(Cc3cccc(C(F)(F)F)c3)cc-2[nH]1 10.1021/jm000269t
CHEMBL343924 119297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 374 3 1 3 4.8 Cc1nc(N2CCCCC2)c2nc(Cc3cccc(C(F)(F)F)c3)cc-2[nH]1 10.1021/jm000269t
44289857 101307 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 514 7 3 3 5.6 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)Nc1ccccc1 10.1016/s0960-894x(00)00311-5
CHEMBL296557 101307 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 514 7 3 3 5.6 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)Nc1ccccc1 10.1016/s0960-894x(00)00311-5
44370180 47297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 471 6 3 5 3.4 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
CHEMBL154412 47297 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 471 6 3 5 3.4 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
44313061 103143 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 449 6 2 7 4.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4[N+](=O)[O-])cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL307901 103143 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 449 6 2 7 4.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4[N+](=O)[O-])cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
10498644 26569 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 4 1 4 3.8 Cc1nc(N2CCCCC2)c2nc(COc3ccccc3)cc-2[nH]1 10.1021/jm000269t
CHEMBL136093 26569 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 4 1 4 3.8 Cc1nc(N2CCCCC2)c2nc(COc3ccccc3)cc-2[nH]1 10.1021/jm000269t
44460788 205306 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 7 1 6 3.9 CN(CC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1)CC1CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79301 205306 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 7 1 6 3.9 CN(CC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1)CC1CC1 10.1016/j.bmcl.2004.03.014
44460922 205939 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 415 6 1 6 3.7 CCOCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(C)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL84269 205939 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 415 6 1 6 3.7 CCOCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(C)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44573656 187213 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 0 3 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492393 187213 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 0 3 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
13152287 205656 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 282 0 1 4 4.5 Nc1nc2c(s1)-c1ccccc1Sc1ccccc1-2 10.1016/j.bmcl.2004.03.014
CHEMBL81979 205656 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 282 0 1 4 4.5 Nc1nc2c(s1)-c1ccccc1Sc1ccccc1-2 10.1016/j.bmcl.2004.03.014
10303307 64476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181393 64476 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 565 7 2 6 5.8 CN(C)c1nc(NC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9924211 192643 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 344 1 1 5 3.1 N#Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL521720 192643 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 344 1 1 5 3.1 N#Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44460707 105821 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 431 4 1 6 3.7 O=C([C@@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL312710 105821 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 431 4 1 6 3.7 O=C([C@@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44344454 103436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 539 9 2 4 5.4 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1F 10.1021/jm990468g
CHEMBL3084885 103436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 539 9 2 4 5.4 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1F 10.1021/jm990468g
10403909 64544 1 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 323 4 1 5 4.1 N#Cc1cccc(Nc2ncc(C(=O)c3ccccc3F)s2)c1 10.1016/j.bmcl.2005.01.063
CHEMBL181458 64544 1 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 323 4 1 5 4.1 N#Cc1cccc(Nc2ncc(C(=O)c3ccccc3F)s2)c1 10.1016/j.bmcl.2005.01.063
2350190 51857 6 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.07.020
CHEMBL1585484 51857 6 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.07.020
2350190 51857 6 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.11.005
CHEMBL1585484 51857 6 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 423 5 1 5 3.5 O=S(=O)(c1ccc2[nH]c(SCc3cccc(Cl)c3)nc2c1)N1CCOCC1 10.1016/j.bmcl.2012.11.005
10805667 28187 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 2 1 3 4.4 Cc1nc2cc(-c3ccccc3)nc-2c(N2CC(C)CC(C)C2)[nH]1 10.1021/jm000269t
CHEMBL137360 28187 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 2 1 3 4.4 Cc1nc2cc(-c3ccccc3)nc-2c(N2CC(C)CC(C)C2)[nH]1 10.1021/jm000269t
44377476 120036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 477 8 2 4 3.9 Cc1ccc2c(c1)CC(NCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL350379 120036 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 477 8 2 4 3.9 Cc1ccc2c(c1)CC(NCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
71458602 81342 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 397 5 1 4 3.7 CCCS(=O)(=O)c1ccc2[nH]c(C3CCC(=O)N(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159161 81342 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 397 5 1 4 3.7 CCCS(=O)(=O)c1ccc2[nH]c(C3CCC(=O)N(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
44313576 105486 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 399 3 1 3 5.3 Cc1cc(C(=O)Nc2cccc3c2CCCC3)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL312086 105486 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 399 3 1 3 5.3 Cc1cc(C(=O)Nc2cccc3c2CCCC3)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
9981738 13946 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 424 4 1 5 3.8 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL1196600 13946 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 424 4 1 5 3.8 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL557583 13946 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 424 4 1 5 3.8 N#Cc1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
44580709 193339 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 391 3 1 6 3.4 CCOC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL524644 193339 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 391 3 1 6 3.4 CCOC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
18005004 197846 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(OC)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572431 197846 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(OC)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
10970192 11032 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 351 2 1 3 4.5 Cc1cccc2c3cc(NC(=O)N4CCOCC4)ccc3n(C(C)C)c12 10.1021/jm011125x
CHEMBL117563 11032 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 351 2 1 3 4.5 Cc1cccc2c3cc(NC(=O)N4CCOCC4)ccc3n(C(C)C)c12 10.1021/jm011125x
10969955 110588 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL325475 110588 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
9862646 163460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 337 2 1 3 4.2 CC(C)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL419951 163460 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 337 2 1 3 4.2 CC(C)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
9908946 197245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL568370 197245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
45487538 198942 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4CF)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL584815 198942 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4CF)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
9908946 197245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
CHEMBL568370 197245 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
46226607 199821 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4cccc(F)c4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL594164 199821 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4cccc(F)c4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
18004891 193288 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 428 3 2 4 2.5 CC(=O)c1ccc(NC(=O)N2CCC3(CC2)CN(S(N)(=O)=O)c2ccccc23)cc1 10.1016/j.bmcl.2009.02.035
CHEMBL524029 193288 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 428 3 2 4 2.5 CC(=O)c1ccc(NC(=O)N2CCC3(CC2)CN(S(N)(=O)=O)c2ccccc23)cc1 10.1016/j.bmcl.2009.02.035
9946965 193072 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL522456 193072 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
44461200 104282 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 446 8 2 6 3.3 COCCNCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL309967 104282 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 446 8 2 6 3.3 COCCNCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460988 105627 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.3 O=C([C@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL312362 105627 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.3 O=C([C@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10111792 105982 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 5 1 5 3.7 COCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL313087 105982 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 5 1 5 3.7 COCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461051 106128 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.1 COCCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL313454 106128 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.1 COCCC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461022 168024 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.3 O=C([C@@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL432169 168024 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 4 1 5 4.3 O=C([C@@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10272418 205592 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 401 4 1 4 4.7 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81484 205592 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 401 4 1 4 4.7 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10226374 205604 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 5 1 6 3.4 O=C(CN1CCOCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81586 205604 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 5 1 6 3.4 O=C(CN1CCOCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460919 205674 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 4 2 5 4.8 COC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82158 205674 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 4 2 5 4.8 COC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461180 205959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 399 4 1 4 4.5 O=C(C1CC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL84453 205959 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 399 4 1 4 4.5 O=C(C1CC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44271276 59955 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 471 5 1 6 3.8 CC(=O)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
CHEMBL17327 59955 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 471 5 1 6 3.8 CC(=O)c1cccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)c1 10.1016/s0960-894x(02)00113-0
44573705 187568 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cccnc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL494592 187568 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cccnc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
9930851 197197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL568144 197197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44579888 186872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 454 2 1 6 5.4 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5noc(C(F)(F)F)n5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL489608 186872 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 454 2 1 6 5.4 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5noc(C(F)(F)F)n5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
9930851 197197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL568144 197197 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
22660756 200131 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL596264 200131 1 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
46226628 201367 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL604480 201367 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
44573705 187568 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cccnc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL494592 187568 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cccnc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
11491176 200043 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595573 200043 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
11407098 200070 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccc(F)cc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595790 200070 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccc(F)cc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
10662967 25741 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 276 2 1 3 3.3 Cc1nc(N2CC=CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL135262 25741 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 276 2 1 3 3.3 Cc1nc(N2CC=CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44580223 184201 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 399 1 1 6 3.6 O=C1OC2(CCN(c3nc4cc5c(cc4[nH]3)OC(F)(F)O5)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL483244 184201 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 399 1 1 6 3.6 O=C1OC2(CCN(c3nc4cc5c(cc4[nH]3)OC(F)(F)O5)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
45481804 197850 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572451 197850 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ncc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45487589 196805 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL565624 196805 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
45487576 198753 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
CHEMBL583007 198753 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2ccncc21 10.1016/j.bmcl.2009.07.103
45487628 198944 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL584902 198944 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(F)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44583506 193373 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL525173 193373 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)nc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44579846 187022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 428 2 1 3 6.6 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(-c5ccccc5)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL490824 187022 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 428 2 1 3 6.6 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(-c5ccccc5)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
44579862 187073 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1cc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2cc1Cl 10.1016/j.bmcl.2008.08.021
CHEMBL491239 187073 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1cc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2cc1Cl 10.1016/j.bmcl.2008.08.021
46226653 200101 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL596025 200101 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
46226580 201855 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL607144 201855 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
15940921 200040 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595560 200040 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
68605776 125448 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 386 6 1 4 4.7 N#Cc1ccccc1O[C@H]1CC[C@@H](C(=O)Nc2ccc(OC(F)F)cc2)CC1 nan
CHEMBL3646142 125448 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 386 6 1 4 4.7 N#Cc1ccccc1O[C@H]1CC[C@@H](C(=O)Nc2ccc(OC(F)F)cc2)CC1 nan
22934132 204622 9 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL7342 204622 9 None - 0 Human 8.6 pIC50 = 8.6 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
45487530 198933 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(CF)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL584732 198933 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 432 4 1 6 4.2 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(CF)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44583557 187749 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL495594 187749 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44579810 186866 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 394 2 1 3 6.0 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL489587 186866 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 394 2 1 3 6.0 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
15940921 200040 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL595560 200040 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
44271373 59539 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 460 5 1 7 3.0 COc1ccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cn1 10.1016/s0960-894x(02)00113-0
CHEMBL17165 59539 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 460 5 1 7 3.0 COc1ccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cn1 10.1016/s0960-894x(02)00113-0
44271317 60411 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 1 6 3.3 COc1ccc(CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
CHEMBL17502 60411 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 473 6 1 6 3.3 COc1ccc(CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
44303643 201143 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 431 6 2 4 5.0 COc1ccc(-c2cc(NC(=O)CC34CCCC3Cc3ccccc3C4)[nH]n2)cc1OC 10.1021/jm980521l
CHEMBL60319 201143 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 431 6 2 4 5.0 COc1ccc(-c2cc(NC(=O)CC34CCCC3Cc3ccccc3C4)[nH]n2)cc1OC 10.1021/jm980521l
12071667 188021 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497569 188021 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 395 2 1 4 4.9 O=C1OC2(CCN(c3nc4cc(-c5ccccc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
9825886 198055 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4nccs4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL574088 198055 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4nccs4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45481807 198456 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 5 3.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL577372 198456 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 5 3.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
9887225 187148 3 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL491930 187148 3 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44583462 193179 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL523228 193179 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 418 2 1 5 4.0 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44579825 187070 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 422 3 1 4 5.5 O=C(c1ccccc1)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
CHEMBL491230 187070 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 422 3 1 4 5.5 O=C(c1ccccc1)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
44579826 187098 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 395 2 1 4 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccccn5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL491427 187098 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 395 2 1 4 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5ccccn5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
46226636 199937 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
CHEMBL594888 199937 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
46226627 199970 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
CHEMBL595121 199970 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
45481800 198508 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc4ncccc4c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL577794 198508 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc4ncccc4c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
70693071 76914 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 419 3 1 5 3.7 O=c1ccc(-c2nc3cc(S(=O)(=O)C(F)(F)F)ccc3[nH]2)cn1-c1ccccc1 10.1016/j.bmcl.2012.07.020
CHEMBL2070160 76914 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 419 3 1 5 3.7 O=c1ccc(-c2nc3cc(S(=O)(=O)C(F)(F)F)ccc3[nH]2)cn1-c1ccccc1 10.1016/j.bmcl.2012.07.020
9908890 199818 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1OC2(CCC(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.08.019
CHEMBL594156 199818 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 399 3 1 5 4.3 O=C1OC2(CCC(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.08.019
44401616 70033 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193970 70033 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 601 8 2 7 5.3 CN(C)c1nc(NCC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
45481641 197848 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 477 4 1 4 4.8 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Oc4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572442 197848 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 477 4 1 4 4.8 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Oc4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45487632 196839 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL565826 196839 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
10477251 174641 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 420 1 1 3 6.0 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(C(F)(F)F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL455815 174641 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 420 1 1 3 6.0 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(C(F)(F)F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
44271373 59539 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 460 5 1 7 3.0 COc1ccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cn1 10.1016/s0960-894x(02)00113-0
CHEMBL17165 59539 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 460 5 1 7 3.0 COc1ccc(NC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cn1 10.1016/s0960-894x(02)00113-0
44271289 169189 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 493 12 1 5 5.2 CCCCCCCCCCNC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL440647 169189 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 493 12 1 5 5.2 CCCCCCCCCCNC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
71519170 86176 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 390 5 1 4 4.3 CCS(=O)(=O)c1ccc2[nH]c(C(=O)c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312079 86176 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 390 5 1 4 4.3 CCS(=O)(=O)c1ccc2[nH]c(C(=O)c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
20587808 187856 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 377 2 1 6 3.0 COC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL496327 187856 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 377 2 1 6 3.0 COC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
18004934 198183 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 427 3 1 4 3.2 CC(=O)c1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmc.2009.05.064
CHEMBL574996 198183 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 427 3 1 4 3.2 CC(=O)c1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmc.2009.05.064
45487631 196807 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
CHEMBL565626 196807 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2cnccc21 10.1016/j.bmcl.2009.07.103
46226612 201748 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
CHEMBL606631 201748 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2cnccc21 10.1016/j.bmc.2009.08.019
10133076 193256 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 359 3 1 3 4.1 N#Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL523819 193256 3 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 359 3 1 3 4.1 N#Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
70695118 76900 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3F)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070146 76900 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 380 4 1 3 4.8 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3F)nc2c1 10.1016/j.bmcl.2012.07.020
9895868 69582 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193438 69582 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NCC2CCC(CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
9895868 12899 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL1188966 12899 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL537846 12899 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 615 9 2 7 5.6 CN(C)c1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
45481811 198149 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cscn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL574771 198149 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 468 3 1 5 4.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4cscn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
46226575 201861 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL607192 201861 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 389 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)on3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
10314778 63972 1 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 333 5 1 5 4.6 CCc1ccccc1C(=O)c1cnc(Nc2cccc(C#N)c2)s1 10.1016/j.bmcl.2005.01.063
CHEMBL180692 63972 1 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 333 5 1 5 4.6 CCc1ccccc1C(=O)c1cnc(Nc2cccc(C#N)c2)s1 10.1016/j.bmcl.2005.01.063
44271355 59652 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 500 4 1 7 4.5 Cc1ccc2nc(NC(=O)C3CCN(C(=O)Cn4c(=O)sc5ccc(Cl)cc54)CC3)sc2c1 10.1016/s0960-894x(02)00113-0
CHEMBL17214 59652 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 500 4 1 7 4.5 Cc1ccc2nc(NC(=O)C3CCN(C(=O)Cn4c(=O)sc5ccc(Cl)cc54)CC3)sc2c1 10.1016/s0960-894x(02)00113-0
71519165 86170 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 378 5 1 4 4.8 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312073 86170 0 None - 0 Mouse 8.6 pIC50 = 8.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 378 5 1 4 4.8 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
68615948 125437 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 431 5 2 5 3.8 N#Cc1ccccc1C(=O)N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1 nan
CHEMBL3646131 125437 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 431 5 2 5 3.8 N#Cc1ccccc1C(=O)N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1 nan
68605737 125445 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 397 5 2 5 4.2 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](Nc2cccc(F)n2)CC1 nan
CHEMBL3646139 125445 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 397 5 2 5 4.2 O=C(Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@H](Nc2cccc(F)n2)CC1 nan
1562 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Compound was tested for human Neuropeptide Y receptor type 5Compound was tested for human Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
5312114 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Compound was tested for human Neuropeptide Y receptor type 5Compound was tested for human Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL17645 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Compound was tested for human Neuropeptide Y receptor type 5Compound was tested for human Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
CHEMBL195380 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Compound was tested for human Neuropeptide Y receptor type 5Compound was tested for human Neuropeptide Y receptor type 5
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/s0960-894x(00)00177-3
45487565 199023 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmcl.2009.07.103
CHEMBL585851 199023 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmcl.2009.07.103
44583556 187748 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL495593 187748 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
45487565 199023 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
CHEMBL585851 199023 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
46226635 200132 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
CHEMBL596266 200132 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2ccncc21 10.1016/j.bmc.2009.08.019
1562 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2003.11.070
5312114 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2003.11.070
CHEMBL17645 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2003.11.070
CHEMBL195380 899 13 None - 2 Human 8.5 pIC50 = 8.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 10.1016/j.bmcl.2003.11.070
9867212 104895 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against rat neuropeptide Y5 receptorIn vitro binding affinity against rat neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL311229 104895 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against rat neuropeptide Y5 receptorIn vitro binding affinity against rat neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44271267 98786 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 2 6 3.1 O=C(Nc1ccc(CCO)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL278280 98786 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 473 6 2 6 3.1 O=C(Nc1ccc(CCO)cc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
60197259 86172 1 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)nc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312075 86172 1 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)nc3)nc2c1 10.1016/j.bmcl.2012.11.005
10831203 119453 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 3 1 3 4.2 CCc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL345082 119453 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 3 1 3 4.2 CCc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44580745 193409 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 376 2 2 5 2.6 CNC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL525908 193409 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 376 2 2 5 2.6 CNC(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44312754 103411 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 493 6 3 6 4.3 Nc1ccccc1S(=O)(=O)NCC1CCC(c2cc(N)n(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/s0960-894x(01)00448-6
CHEMBL3084800 103411 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 493 6 3 6 4.3 Nc1ccccc1S(=O)(=O)NCC1CCC(c2cc(N)n(-c3ccc(C(F)(F)F)cc3)n2)CC1 10.1016/s0960-894x(01)00448-6
22934129 204086 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1ccc2c(c1)CCCc1nc(-c3ccncc3)[nH]c1-2 10.1016/s0960-894x(02)00090-2
CHEMBL7017 204086 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1ccc2c(c1)CCCc1nc(-c3ccncc3)[nH]c1-2 10.1016/s0960-894x(02)00090-2
44583505 188044 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(C(F)(F)F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL497644 188044 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 468 2 1 5 4.9 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(C(F)(F)F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44579806 186988 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 343 1 1 4 4.2 N#Cc1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
CHEMBL490608 186988 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 343 1 1 4 4.2 N#Cc1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
44460681 205399 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 453 4 1 4 5.5 O=C(c1ccccc1F)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL80041 205399 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 453 4 1 4 5.5 O=C(c1ccccc1F)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461118 205942 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 451 6 1 5 5.4 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL84285 205942 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 451 6 1 5 5.4 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10368454 12819 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 457 6 1 5 5.0 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
CHEMBL1188311 12819 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 457 6 1 5 5.0 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
CHEMBL536048 12819 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 457 6 1 5 5.0 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
10872843 102938 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 390 7 2 3 4.9 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(OCc2ccccc2)cc1 10.1021/jm0004547
CHEMBL306277 102938 0 None - 1 Human 7.7 pIC50 = 7.7 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 390 7 2 3 4.9 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(OCc2ccccc2)cc1 10.1021/jm0004547
10044852 132486 1 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 373 4 1 5 5.0 N#Cc1cccc(Nc2ncc(C(=O)c3ccccc3C(F)(F)F)s2)c1 10.1016/j.bmcl.2005.01.063
CHEMBL369763 132486 1 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 373 4 1 5 5.0 N#Cc1cccc(Nc2ncc(C(=O)c3ccccc3C(F)(F)F)s2)c1 10.1016/j.bmcl.2005.01.063
44370240 47851 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 435 6 3 5 2.6 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cccs3)CC2)cc1 10.1016/j.bmcl.2003.11.070
CHEMBL154889 47851 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 435 6 3 5 2.6 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cccs3)CC2)cc1 10.1016/j.bmcl.2003.11.070
18004985 187238 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 1 3 5.2 CS(=O)(=O)N1C[C@]2(CC[C@@H](C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492582 187238 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 460 4 1 3 5.2 CS(=O)(=O)N1C[C@]2(CC[C@@H](C(=O)Nc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44271463 60331 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 307 6 3 5 3.0 NCCCCNc1nc(N)c2cc(-c3ccccc3)ccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL17441 60331 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 307 6 3 5 3.0 NCCCCNc1nc(N)c2cc(-c3ccccc3)ccc2n1 10.1016/s0960-894x(00)00177-3
71450852 78583 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 490 8 3 5 2.8 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)C(=O)NC1=NC2CCc3cc(F)ccc3C2C1 10.1016/s0960-894x(99)00676-9
CHEMBL2112218 78583 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 490 8 3 5 2.8 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)C(=O)NC1=NC2CCc3cc(F)ccc3C2C1 10.1016/s0960-894x(99)00676-9
44460704 205748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 6 1 6 4.1 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)COC(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL82710 205748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 6 1 6 4.1 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)COC(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
9934437 103440 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 470 9 2 3 5.2 C=CCC1c2ccc(F)cc2CCC1NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
CHEMBL3084890 103440 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 470 9 2 3 5.2 C=CCC1c2ccc(F)cc2CCC1NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
11754800 12867 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 441 5 1 5 4.1 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL1188721 12867 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 441 5 1 5 4.1 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL537191 12867 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 441 5 1 5 4.1 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(Cl)ccc43)CC2)cc1 10.1021/jm049599u
70697154 76906 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3C)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070152 76906 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3C)nc2c1 10.1016/j.bmcl.2012.07.020
44271460 60345 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 473 13 2 5 7.1 CCCCN(CCCC)CCCNc1nc(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
CHEMBL17450 60345 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 473 13 2 5 7.1 CCCCN(CCCC)CCCNc1nc(Nc2cccc(C(F)(F)F)c2)c2ccccc2n1 10.1016/s0960-894x(00)00177-3
44377734 119864 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 491 8 2 4 4.4 O=S(=O)(NCCN1CCC(CNC2CCCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL348806 119864 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 491 8 2 4 4.4 O=S(=O)(NCCN1CCC(CNC2CCCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
44460868 168123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 513 7 2 6 4.6 CC(C)N1CCN(CC(=O)N[C@H]2CC[C@H](CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL432931 168123 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 513 7 2 6 4.6 CC(C)N1CCN(CC(=O)N[C@H]2CC[C@H](CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)CC1 10.1016/j.bmcl.2004.03.014
10451123 105619 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 5.0 Cc1cccc(-n2nc(C(=O)Nc3cc(Cl)cc(Cl)c3)cc2C)c1 10.1016/s0960-894x(01)00449-8
CHEMBL312308 105619 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 5.0 Cc1cccc(-n2nc(C(=O)Nc3cc(Cl)cc(Cl)c3)cc2C)c1 10.1016/s0960-894x(01)00449-8
44460712 105511 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 419 6 1 6 3.6 COCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL312169 105511 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 419 6 1 6 3.6 COCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44344259 113093 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 542 11 3 5 3.6 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)C(=O)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL331319 113093 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 542 11 3 5 3.6 N[C@@H](CCCCNS(=O)(=O)c1ccccc1F)C(=O)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
9891987 101514 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2ccccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL298037 101514 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 495 6 2 6 4.2 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2ccccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
71519004 86168 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 386 5 1 5 4.0 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(OC(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312071 86168 0 None - 0 Mouse 7.7 pIC50 = 7.7 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 386 5 1 5 4.0 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(OC(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
9949840 28733 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 340 2 1 3 4.5 Cc1nc(N2CCc3ccccc3C2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137808 28733 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 340 2 1 3 4.5 Cc1nc(N2CCc3ccccc3C2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10638643 116711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 309 2 0 4 4.7 Cc1nc(N2CCCCC2)c2sc(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL337305 116711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 309 2 0 4 4.7 Cc1nc(N2CCCCC2)c2sc(-c3ccccc3)cc2n1 10.1021/jm000269t
10970360 168514 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 5 0 3 4.8 CCn1c2ccccc2c2cc(N(C)C(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL435384 168514 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 5 0 3 4.8 CCn1c2ccccc2c2cc(N(C)C(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
44390066 63832 1 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 335 5 1 6 4.0 COc1ccc(C(=O)c2cnc(Nc3cccc(C#N)c3)s2)cc1 10.1016/j.bmcl.2005.01.063
CHEMBL180251 63832 1 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 335 5 1 6 4.0 COc1ccc(C(=O)c2cnc(Nc3cccc(C#N)c3)s2)cc1 10.1016/j.bmcl.2005.01.063
11110676 10164 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.1 CCn1c2ccccc2c2cc(CC(=O)NCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL115911 10164 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.1 CCn1c2ccccc2c2cc(CC(=O)NCc3ccncc3)ccc21 10.1021/jm011125x
44313057 103144 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4N)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL307902 103144 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4N)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44573614 187208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccncc4)c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL492375 187208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccncc4)c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44573614 187208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccncc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492375 187208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cccc(-c4ccncc4)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44460842 205541 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 383 6 2 5 3.5 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)cs2)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81000 205541 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 383 6 2 5 3.5 CS(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(-c3ccc(F)cc3)cs2)CC1 10.1016/j.bmcl.2004.03.014
11757324 103418 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 551 10 2 5 5.2 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3F)CC1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL3084865 103418 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 551 10 2 5 5.2 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccccc3F)CC1)C2Cc1cccnc1 10.1021/jm990468g
10051835 14009 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL1197071 14009 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL559210 14009 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 467 4 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
10860014 110619 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 315 4 2 2 4.3 O=C(CCc1ccncc1)Nc1ccc2[nH]c3ccccc3c2c1 10.1021/jm011125x
CHEMBL325666 110619 1 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 315 4 2 2 4.3 O=C(CCc1ccncc1)Nc1ccc2[nH]c3ccccc3c2c1 10.1021/jm011125x
10519375 29391 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 278 2 1 3 3.6 c1ccc(-c2cc3nc[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL138383 29391 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 278 2 1 3 3.6 c1ccc(-c2cc3nc[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
10430847 204714 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 396 3 1 4 5.0 Cc1cc(C(=O)Nc2cccc3ncccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL74161 204714 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 396 3 1 4 5.0 Cc1cc(C(=O)Nc2cccc3ncccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44313570 169138 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 381 3 1 3 4.7 Cc1cc(C(=O)Nc2c(F)cccc2F)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL440310 169138 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 381 3 1 3 4.7 Cc1cc(C(=O)Nc2c(F)cccc2F)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
9806557 169507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 515 7 3 4 4.3 O=C(CN1CCC(NC(=O)Nc2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL44338 169507 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 515 7 3 4 4.3 O=C(CN1CCC(NC(=O)Nc2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
10298981 205357 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 471 5 1 6 3.3 CN1CCN(CC(=O)N2CCC(CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79714 205357 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 471 5 1 6 3.3 CN1CCN(CC(=O)N2CCC(CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)CC1 10.1016/j.bmcl.2004.03.014
44379363 57550 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 551 11 3 6 4.0 COc1ccc2c(c1)C(O)(CNCCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL166399 57550 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 551 11 3 6 4.0 COc1ccc2c(c1)C(O)(CNCCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
10935409 205075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 298 5 1 2 4.7 CC[C@@H](C)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77355 205075 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 298 5 1 2 4.7 CC[C@@H](C)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
12078328 118783 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 336 4 1 4 3.8 COc1ccc(Cc2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL342042 118783 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 336 4 1 4 3.8 COc1ccc(Cc2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
9807658 64546 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181466 64546 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 551 8 2 6 6.1 CN(C)c1nc(NC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44460812 205609 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 484 7 1 7 4.3 COc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)CCN4CCCCC4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL81611 205609 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 484 7 1 7 4.3 COc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)CCN4CCCCC4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
10111849 204879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 404 5 2 5 4.2 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL75823 204879 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 404 5 2 5 4.2 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccccc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
22934130 203962 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 290 2 1 2 4.2 COc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL6938 203962 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 290 2 1 2 4.2 COc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
71518998 86162 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 330 6 1 4 3.0 CCS(=O)(=O)c1ccc2[nH]c(OCCc3ccccc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312065 86162 0 None - 0 Mouse 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 330 6 1 4 3.0 CCS(=O)(=O)c1ccc2[nH]c(OCCc3ccccc3)nc2c1 10.1016/j.bmcl.2012.11.005
44460798 104140 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 434 4 1 6 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)c4ccccn4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL309449 104140 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 434 4 1 6 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)c4ccccn4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44460830 104392 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 361 6 1 4 4.1 CN(C)C(=O)CCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2004.03.014
CHEMBL310292 104392 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 361 6 1 4 4.1 CN(C)C(=O)CCCCNc1nc2c(s1)CCCc1ccc(F)cc1-2 10.1016/j.bmcl.2004.03.014
10414854 13179 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL1190951 13179 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
CHEMBL541891 13179 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2=O 10.1021/jm049599u
9936263 101228 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 513 6 2 6 4.4 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL296022 101228 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 513 6 2 6 4.4 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
10831332 27991 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 308 2 2 4 2.9 Cc1nc(N2CCC(O)CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137236 27991 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 308 2 2 4 2.9 Cc1nc(N2CCC(O)CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44580593 187860 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 349 2 1 5 3.2 COc1cccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc12 10.1016/j.bmcl.2008.08.018
CHEMBL496345 187860 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 349 2 1 5 3.2 COc1cccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc12 10.1016/j.bmcl.2008.08.018
10810784 27587 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 360 2 1 3 4.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3C(F)(F)F)cc2n1 10.1021/jm000269t
CHEMBL136944 27587 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 360 2 1 3 4.9 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3C(F)(F)F)cc2n1 10.1021/jm000269t
44288067 166361 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
CHEMBL42747 166361 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 513 9 5 4 3.2 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N1CCCc2cc(O)ccc2C1 10.1016/s0960-894x(00)00292-4
9799669 205810 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 373 3 1 4 4.1 CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL83255 205810 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 373 3 1 4 4.1 CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
46226642 199786 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
CHEMBL593935 199786 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
11753885 12866 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 421 5 1 5 3.8 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(C)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL1188718 12866 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 421 5 1 5 3.8 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(C)ccc43)CC2)cc1 10.1021/jm049599u
CHEMBL537187 12866 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 421 5 1 5 3.8 CC(=O)c1ccc(NC(=O)CN2CCC(N3C(=O)OCc4cc(C)ccc43)CC2)cc1 10.1021/jm049599u
44289890 166208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 486 7 2 4 3.5 O=C(CN1CC[C@H](NC(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL42658 166208 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 486 7 2 4 3.5 O=C(CN1CC[C@H](NC(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
11792487 28708 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 4 2 4 4.4 Cc1nc2cc(-c3ccccc3)nc-2c(NCc2ccc(C)o2)[nH]1 10.1021/jm000269t
CHEMBL137786 28708 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 4 2 4 4.4 Cc1nc2cc(-c3ccccc3)nc-2c(NCc2ccc(C)o2)[nH]1 10.1021/jm000269t
44288390 161834 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41457 161834 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 491 11 5 3 3.5 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccc(Cl)cc1)C(=O)NCc1ccccc1 10.1016/s0960-894x(00)00292-4
44313241 204948 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 436 5 2 4 6.2 Cc1cc(C(=O)Nc2ccccc2Nc2ccccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL76413 204948 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 436 5 2 4 6.2 Cc1cc(C(=O)Nc2ccccc2Nc2ccccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44344208 13507 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CC[C@@H](NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL119355 13507 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CC[C@@H](NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
44344455 103437 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 521 9 2 4 5.2 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1 10.1021/jm990468g
CHEMBL3084886 103437 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 521 9 2 4 5.2 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1 10.1021/jm990468g
11143423 11643 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 381 4 1 4 4.6 CCOc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL118098 11643 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 381 4 1 4 4.6 CCOc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
44573532 187462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 392 4 1 4 4.0 COC(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL493997 187462 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 392 4 1 4 4.0 COC(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
1305 511 14 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
9934033 511 14 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
CHEMBL182150 511 14 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 425 5 2 5 4.1 O=C(c1ccc(c(c1)F)F)N[C@@H]1CC[C@@H](CC1)Nc1nc2ccccc2c(n1)N(C)C 10.1016/j.bmcl.2005.05.121
44370177 169202 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 505 6 3 5 4.1 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Cl)cc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
CHEMBL440735 169202 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 505 6 3 5 4.1 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Cl)cc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
10498512 28672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 4 1 3 4.6 CCCc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137758 28672 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 4 1 3 4.6 CCCc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
22325323 193410 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 337 1 1 4 3.4 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL525918 193410 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 337 1 1 4 3.4 O=C1OC2(CCN(c3nc4cc(F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
10159053 205368 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 419 6 1 6 3.6 CCOCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79849 205368 1 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 419 6 1 6 3.6 CCOCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44379102 158785 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 529 7 2 7 3.8 COc1ccc2c(c1)C(O)(CNCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL409418 158785 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 529 7 2 7 3.8 COc1ccc2c(c1)C(O)(CNCC1CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC1)CCC2 10.1016/s0960-894x(02)00018-5
9892202 172582 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 500 7 2 4 3.9 O=C(CN1CCC(NC(=O)c2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL44886 172582 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 500 7 2 4 3.9 O=C(CN1CCC(NC(=O)c2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
44370266 46262 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 549 6 3 5 4.2 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Br)cc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
CHEMBL153522 46262 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 549 6 3 5 4.2 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Br)cc2)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
10666064 29274 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 321 3 1 4 3.7 CN(C)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL138278 29274 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 321 3 1 4 3.7 CN(C)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
11811424 204975 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 398 6 2 3 4.4 C[C@H]([C@@H](O)c1ccccc1)N(C)/C(=N/c1ccc(Cc2ccccc2)cc1)NC#N 10.1021/jm0004547
CHEMBL76549 204975 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 398 6 2 3 4.4 C[C@H]([C@@H](O)c1ccccc1)N(C)/C(=N/c1ccc(Cc2ccccc2)cc1)NC#N 10.1021/jm0004547
10617383 27221 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 307 3 2 4 3.7 CNc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL136650 27221 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 307 3 2 4 3.7 CNc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44312955 204497 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 422 5 2 5 4.4 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL72547 204497 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 422 5 2 5 4.4 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44460883 105626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 470 6 2 5 5.0 O=C(CN1CCCCC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL312361 105626 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 470 6 2 5 5.0 O=C(CN1CCCCC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460964 163639 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 8 2 5 4.9 CN(C)CCCC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL420399 163639 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 8 2 5 4.9 CN(C)CCCC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10903122 204927 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 314 5 2 3 3.3 COc1ccc(NC(=O)N(C)[C@H](C)[C@@H](O)c2ccccc2)cc1 10.1021/jm0004547
CHEMBL76265 204927 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 314 5 2 3 3.3 COc1ccc(NC(=O)N(C)[C@H](C)[C@@H](O)c2ccccc2)cc1 10.1021/jm0004547
44313494 104748 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 435 5 1 3 6.0 Cc1cc(C(=O)Nc2ccccc2Cc2ccccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL310694 104748 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 435 5 1 3 6.0 Cc1cc(C(=O)Nc2ccccc2Cc2ccccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
10807285 27755 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.3 Cc1nc2cc(-c3ccccc3)nc-2c(N2CCCCC2C)[nH]1 10.1021/jm000269t
CHEMBL137058 27755 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.3 Cc1nc2cc(-c3ccccc3)nc-2c(N2CCCCC2C)[nH]1 10.1021/jm000269t
68595241 125443 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 370 4 2 4 4.2 O=C(N[C@H]1CC[C@@H](c2nc(-c3cccc(Cl)c3)c[nH]2)CC1)c1ccon1 nan
CHEMBL3646137 125443 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 370 4 2 4 4.2 O=C(N[C@H]1CC[C@@H](c2nc(-c3cccc(Cl)c3)c[nH]2)CC1)c1ccon1 nan
44573743 187689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL495200 187689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44573704 193292 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL524044 193292 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004938 198459 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL577398 198459 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4cccc(F)c4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
11824465 10332 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 4 1 4 4.4 CC(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL116210 10332 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 357 4 1 4 4.4 CC(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
9884833 110552 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL325226 110552 41 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 351 2 1 3 4.5 Cc1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
11002751 168090 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 355 2 1 3 4.4 CC(C)n1c2ccc(F)cc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL432628 168090 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 355 2 1 3 4.4 CC(C)n1c2ccc(F)cc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
45487608 196846 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL565848 196846 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4F)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
18004920 187314 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 478 4 2 4 4.1 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Oc4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492999 187314 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 478 4 2 4 4.1 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Oc4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44573743 187689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL495200 187689 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44573704 193292 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccn4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL524044 193292 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccccn4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44271565 98131 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 461 6 3 6 4.3 Nc1nc(N[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/j.bmcl.2004.03.014
CHEMBL273597 98131 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 461 6 3 6 4.3 Nc1nc(N[C@H]2CC[C@H](CNS(=O)(=O)c3cccc4ccccc34)CC2)nc2ccccc12 10.1016/j.bmcl.2004.03.014
44461196 104743 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 456 7 1 5 4.4 CN(CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)CC1CC1 10.1016/j.bmcl.2004.03.014
CHEMBL310670 104743 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 456 7 1 5 4.4 CN(CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)CC1CC1 10.1016/j.bmcl.2004.03.014
44461199 205553 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 486 7 1 6 4.2 COC[C@@H]1CCCN1CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81103 205553 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 486 7 1 6 4.2 COC[C@@H]1CCCN1CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461018 205880 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 470 6 2 6 4.0 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL83830 205880 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 470 6 2 6 4.0 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc3c(s2)CCSc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
1504 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
1518 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
1521 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
24868177 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
44288922 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
77068007 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
90479759 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
CHEMBL438945 2807 8 None -9 10 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL None None None None 10.1021/jm990468g
71458606 81353 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 401 5 1 6 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(OC)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159172 81353 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 401 5 1 6 2.9 CCS(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccc(OC)cc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
91755093 128495 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 370 6 2 6 2.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)no2)CC1 nan
CHEMBL3666796 128495 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 370 6 2 6 2.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)no2)CC1 nan
45487630 196806 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL565625 196806 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4cccc(OCF)c4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44579827 192705 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 395 2 1 4 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5cccnc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL521959 192705 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 395 2 1 4 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(-c5cccnc5)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
11013840 205068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 360 6 1 2 5.6 C[C@H](Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77273 205068 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 360 6 1 2 5.6 C[C@H](Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
45481642 197851 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 5 3.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572456 197851 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 5 3.2 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45481801 198339 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccc(OC)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL576333 198339 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccc(OC)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
68597664 125440 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 412 5 2 7 3.1 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4ccon4)CC3)ccc21 nan
CHEMBL3646134 125440 0 None - 0 Mouse 8.5 pIC50 = 8.5 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 412 5 2 7 3.1 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4ccon4)CC3)ccc21 nan
18004996 198022 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL573858 198022 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
25067562 186971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
CHEMBL490427 186971 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)o1 10.1016/j.bmcl.2008.08.021
44271208 163253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor at a concentration of 10e-6 MTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor at a concentration of 10e-6 M
ChEMBL 488 6 2 7 2.5 Cc1cccc(C(O)CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)n1 10.1016/s0960-894x(02)00113-0
CHEMBL418546 163253 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor at a concentration of 10e-6 MTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor at a concentration of 10e-6 M
ChEMBL 488 6 2 7 2.5 Cc1cccc(C(O)CNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)n1 10.1016/s0960-894x(02)00113-0
18004890 197885 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 465 4 1 5 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572688 197885 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 465 4 1 5 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45481805 198381 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 6 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nnc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL576726 198381 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 6 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nnc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44583588 192941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 406 2 1 6 3.9 O=C1OC2(CCN(C(=O)Nc3nnc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL522237 192941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 406 2 1 6 3.9 O=C1OC2(CCN(C(=O)Nc3nnc(-c4ccccc4)s3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
10110741 188000 3 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497359 188000 3 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44583558 193059 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL522378 193059 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 2 1 5 3.6 O=C1OC2(CCN(C(=O)Nc3cn(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
91755095 128500 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 369 6 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)co2)CC1 nan
CHEMBL3666800 128500 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 369 6 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)co2)CC1 nan
9822252 184115 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 399 2 2 4 3.4 O=C1NC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL482667 184115 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 399 2 2 4 3.4 O=C1NC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44379085 57180 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 8 2 5 3.9 COc1ccc2c(c1)CC(NCC1CCN(C(=O)CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL164873 57180 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 535 8 2 5 3.9 COc1ccc2c(c1)CC(NCC1CCN(C(=O)CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
71519168 86174 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 384 5 1 4 4.5 CCS(=O)(=O)c1ccc2[nH]c(O[C@H]3CC[C@H](c4ccccc4)CC3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312077 86174 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 384 5 1 4 4.5 CCS(=O)(=O)c1ccc2[nH]c(O[C@H]3CC[C@H](c4ccccc4)CC3)nc2c1 10.1016/j.bmcl.2012.11.005
46912713 125434 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 441 5 2 5 4.0 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1)c1cccc(Cl)n1 nan
CHEMBL3646128 125434 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 441 5 2 5 4.0 O=C(N[C@H]1CC[C@@H](C(=O)Nc2ccn(-c3ccccc3F)n2)CC1)c1cccc(Cl)n1 nan
44271318 98440 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 504 4 1 7 4.4 O=C(Nc1nc2cc(Cl)ccc2o1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL275642 98440 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 504 4 1 7 4.4 O=C(Nc1nc2cc(Cl)ccc2o1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
45481803 197849 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572450 197849 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 469 3 1 5 3.4 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4F)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44583395 187843 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(Cl)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL496197 187843 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 434 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3ncc(-c4ccc(Cl)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
11509561 199727 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
CHEMBL593466 199727 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ncccc21 10.1016/j.bmc.2009.08.019
10613667 23055 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 0 4 4.2 Cc1nc(N2CCCCC2)c2oc(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL133032 23055 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 0 4 4.2 Cc1nc(N2CCCCC2)c2oc(-c3ccccc3)cc2n1 10.1021/jm000269t
10161870 204654 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 463 7 2 7 4.0 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc(N(C)C)c4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL73643 204654 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 463 7 2 7 4.0 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc(N(C)C)c4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
10154767 188272 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 348 3 1 2 4.6 Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL499973 188272 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 348 3 1 2 4.6 Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
10414311 12812 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 4 2 5 4.6 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4O)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL1188255 12812 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 4 2 5 4.6 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4O)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL535824 12812 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 4 2 5 4.6 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4O)CC1)C(=O)OC2 10.1021/jm049599u
44289909 163562 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)N[C@@H]1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
CHEMBL42031 163562 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)N[C@@H]1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
44344633 111387 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 330 6 1 3 3.9 O=C(CCc1ccncc1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm011125x
CHEMBL327151 111387 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 330 6 1 3 3.9 O=C(CCc1ccncc1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm011125x
44573565 187492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 349 3 2 3 3.8 Nc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL494174 187492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 349 3 2 3 3.8 Nc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
10433145 13976 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 399 4 1 4 3.9 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Cl)cc1 10.1021/jm049599u
CHEMBL1196846 13976 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 399 4 1 4 3.9 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Cl)cc1 10.1021/jm049599u
CHEMBL558393 13976 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 399 4 1 4 3.9 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(Cl)cc1 10.1021/jm049599u
44401671 70266 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL194173 70266 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 7 1 7 4.9 CN(C)c1nc(NCC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
44313039 103154 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4cccc(N)c4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL308034 103154 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4cccc(N)c4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44289818 169145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 515 7 2 4 5.6 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)Oc1ccccc1 10.1016/s0960-894x(00)00311-5
CHEMBL44036 169145 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 515 7 2 4 5.6 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)Oc1ccccc1 10.1016/s0960-894x(00)00311-5
11204090 69836 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL193771 69836 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(NC2CCC(NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
70693068 76904 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3Cl)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070150 76904 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3Cl)nc2c1 10.1016/j.bmcl.2012.07.020
44377915 57173 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 497 8 2 4 4.2 O=S(=O)(NCCN1CC(CNC2CCCc3ccc(Cl)cc3C2)C1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL164805 57173 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 497 8 2 4 4.2 O=S(=O)(NCCN1CC(CNC2CCCc3ccc(Cl)cc3C2)C1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
10848957 28488 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 224 1 2 3 2.5 Cc1nc(N)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137572 28488 14 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 224 1 2 3 2.5 Cc1nc(N)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10872140 54013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 4 2 2 5.1 O=C(Cc1cccc2ccccc12)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
CHEMBL160595 54013 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 4 2 2 5.1 O=C(Cc1cccc2ccccc12)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
71519000 86164 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccccc3C(F)(F)F)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312067 86164 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccccc3C(F)(F)F)nc2c1 10.1016/j.bmcl.2012.11.005
10522130 28432 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 3 1 3 4.4 c1ccc(-c2cc3nc(C4CC4)[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL137530 28432 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 3 1 3 4.4 c1ccc(-c2cc3nc(C4CC4)[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
22934144 97234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL268654 97234 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
44573407 187455 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 334 3 1 2 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL493971 187455 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 334 3 1 2 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44390147 122145 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 376 5 1 4 5.7 CCc1ccccc1C(=O)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
CHEMBL359685 122145 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 376 5 1 4 5.7 CCc1ccccc1C(=O)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
44370179 164890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 421 6 3 5 2.3 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
CHEMBL422150 164890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 421 6 3 5 2.3 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
10892838 13006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 329 4 1 3 4.3 Cn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL118973 13006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 329 4 1 3 4.3 Cn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
10522285 116246 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.5 CCc1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
CHEMBL335861 116246 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.5 CCc1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
23283651 103427 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 583 10 2 5 6.3 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL3084875 103427 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 583 10 2 5 6.3 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC1)C2Cc1cccnc1 10.1021/jm990468g
11014171 104103 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 372 4 1 2 5.5 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C1CCc2ccccc2C1 10.1021/jm0004547
CHEMBL309370 104103 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 372 4 1 2 5.5 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C1CCc2ccccc2C1 10.1021/jm0004547
11067876 11041 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.1 CCn1c2ccccc2c2cc(CNC(=O)Cc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL117626 11041 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.1 CCn1c2ccccc2c2cc(CNC(=O)Cc3ccncc3)ccc21 10.1021/jm011125x
136058111 203521 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 499 7 2 5 4.4 COc1ccc2c(c1)CCC1N=C(NC[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4F)CC3)CC21 10.1016/s0960-894x(99)00676-9
CHEMBL66371 203521 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 499 7 2 5 4.4 COc1ccc2c(c1)CCC1N=C(NC[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4F)CC3)CC21 10.1016/s0960-894x(99)00676-9
11078514 204991 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 346 6 1 2 5.2 CN(CCc1ccccc1)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL76661 204991 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 346 6 1 2 5.2 CN(CCc1ccccc1)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
11003942 110398 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 402 3 1 5 2.3 CN(C)S(=O)(=O)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL324366 110398 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 402 3 1 5 2.3 CN(C)S(=O)(=O)n1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
44344734 112899 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 348 6 1 4 4.0 O=C(CSc1ccncc1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm011125x
CHEMBL331019 112899 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 348 6 1 4 4.0 O=C(CSc1ccncc1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm011125x
44573607 192872 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ncccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL522192 192872 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ncccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44313274 204725 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 395 3 1 3 5.6 Cc1cc(C(=O)Nc2cccc3ccccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL74252 204725 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 395 3 1 3 5.6 Cc1cc(C(=O)Nc2cccc3ccccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44313223 102892 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 423 3 1 3 5.2 Cc1cc(C(=O)Nc2cccc(Br)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL305922 102892 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 423 3 1 3 5.2 Cc1cc(C(=O)Nc2cccc(Br)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
9903829 116681 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 280 4 1 3 3.7 CCN(CC)c1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
CHEMBL337152 116681 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 280 4 1 3 3.7 CCN(CC)c1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
22325346 173067 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 1 1 4 3.5 Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL451955 173067 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 1 1 4 3.5 Cc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
9806525 100254 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 514 8 2 4 3.8 O=C(Cc1ccccc1)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
CHEMBL288763 100254 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 514 8 2 4 3.8 O=C(Cc1ccccc1)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
22325338 193392 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 349 2 1 5 3.2 COc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL525543 193392 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 349 2 1 5 3.2 COc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44313042 170070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc(C)c4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL444319 170070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 434 6 2 6 4.2 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc(C)c4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
44312926 204620 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 438 6 2 6 4.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(F)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL73401 204620 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 438 6 2 6 4.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccc(F)cc4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
44460713 205602 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 405 5 1 6 3.2 COCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81551 205602 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 405 5 1 6 3.2 COCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
9805850 166145 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 496 6 2 5 4.0 CC(C)(C)OC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
CHEMBL42620 166145 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 496 6 2 5 4.0 CC(C)(C)OC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1 10.1016/s0960-894x(00)00311-5
21336511 57183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL164897 57183 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
44461145 205393 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 435 6 1 5 4.9 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL80006 205393 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 435 6 1 5 4.9 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
70684602 76908 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)n3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070154 76908 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 363 4 1 4 4.1 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)n3)nc2c1 10.1016/j.bmcl.2012.07.020
10832634 28172 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3c(F)cccc3F)cc2n1 10.1021/jm000269t
CHEMBL137350 28172 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3c(F)cccc3F)cc2n1 10.1021/jm000269t
11825270 204955 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 388 7 1 2 6.2 CC(C)C(Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL76439 204955 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 388 7 1 2 6.2 CC(C)C(Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
25881665 179845 5 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Allosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiologyAllosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiology
ChEMBL 397 3 1 7 1.8 CS(=O)(=O)N1CCCC[C@H]1C(=O)Nc1nc2cc3c(cc2s1)OCCO3 10.1021/acs.jmedchem.0c02000
CHEMBL4745232 179845 5 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Allosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiologyAllosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiology
ChEMBL 397 3 1 7 1.8 CS(=O)(=O)N1CCCC[C@H]1C(=O)Nc1nc2cc3c(cc2s1)OCCO3 10.1021/acs.jmedchem.0c02000
25881665 179845 5 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Allosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiologyAllosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiology
ChEMBL 397 3 1 7 1.8 CS(=O)(=O)N1CCCC[C@H]1C(=O)Nc1nc2cc3c(cc2s1)OCCO3 10.1021/acs.jmedchem.0c02000
CHEMBL4745232 179845 5 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Allosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiologyAllosteric antagonist activity at NPY5R in mouse descending colon mucosa assessed as reduction in rPP-induced ion transport by electrophysiology
ChEMBL 397 3 1 7 1.8 CS(=O)(=O)N1CCCC[C@H]1C(=O)Nc1nc2cc3c(cc2s1)OCCO3 10.1021/acs.jmedchem.0c02000
70693069 76907 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3C)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070153 76907 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 4 1 3 5.0 CCS(=O)(=O)c1ccc2[nH]c(-c3cc(-c4ccccc4)ccc3C)nc2c1 10.1016/j.bmcl.2012.07.020
135430853 102077 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 451 6 2 4 4.3 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4ccccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
CHEMBL1744020 102077 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 451 6 2 4 4.3 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4ccccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
CHEMBL302126 102077 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 451 6 2 4 4.3 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4ccccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
44377452 120159 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(CNC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL351508 120159 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(CNC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44579807 193278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 352 1 1 3 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL523964 193278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 352 1 1 3 4.9 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
44573646 187267 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)n1 10.1016/j.bmcl.2009.01.101
CHEMBL492766 187267 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)n1 10.1016/j.bmcl.2009.01.101
44289827 165635 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 499 7 2 3 5.2 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00311-5
CHEMBL42437 165635 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 499 7 2 3 5.2 O=C(NC[C@H]1CC[C@H](C(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)CC1)c1ccccc1 10.1016/s0960-894x(00)00311-5
10052377 12827 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 6 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc(C(=O)c4ccccc4)cc3)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL1188389 12827 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 6 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc(C(=O)c4ccccc4)cc3)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL536276 12827 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 483 6 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc(C(=O)c4ccccc4)cc3)CC1)C(=O)OC2 10.1021/jm049599u
11035908 14027 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.9 Cc1cc2c(c(C)c1NC(=O)N1CCOCC1)c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL119726 14027 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.9 Cc1cc2c(c(C)c1NC(=O)N1CCOCC1)c1ccccc1n2C(C)C 10.1021/jm011125x
44390162 64351 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 382 4 1 5 5.8 Cc1cc(C(=O)c2cnc(Nc3cccc(C(F)(F)F)c3)s2)c(C)s1 10.1016/j.bmcl.2005.01.063
CHEMBL181250 64351 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 382 4 1 5 5.8 Cc1cc(C(=O)c2cnc(Nc3cccc(C(F)(F)F)c3)s2)c(C)s1 10.1016/j.bmcl.2005.01.063
18004995 187306 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 454 2 2 3 3.6 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492986 187306 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 454 2 2 3 3.6 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)c(Cl)c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44461006 104158 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 443 4 1 6 3.8 O=C1CC[C@H](C(=O)N2CCC(CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)O1 10.1016/j.bmcl.2004.03.014
CHEMBL309550 104158 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 443 4 1 6 3.8 O=C1CC[C@H](C(=O)N2CCC(CNc3nc4c(s3)CCCc3ccc(F)cc3-4)CC2)O1 10.1016/j.bmcl.2004.03.014
44460920 164693 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 416 5 1 5 3.7 CN(C)CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL421714 164693 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 416 5 1 5 3.7 CN(C)CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10139215 205668 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 456 5 1 5 4.6 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82080 205668 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 456 5 1 5 4.6 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10111791 205884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 4 1 5 4.7 CCOC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL83860 205884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 403 4 1 5 4.7 CCOC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
101138140 104884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 421 7 2 5 5.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm0004547
10982716 104884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 421 7 2 5 5.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm0004547
CHEMBL311159 104884 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 421 7 2 5 5.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2cccc([N+](=O)[O-])c2)cc1 10.1021/jm0004547
10959710 205073 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 4 2 3 5.2 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc2oc3ccccc3c2c1 10.1021/jm0004547
CHEMBL77333 205073 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 4 2 3 5.2 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc2oc3ccccc3c2c1 10.1021/jm0004547
71519166 86171 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccn4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312074 86171 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccn4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
46912902 125435 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 416 5 2 2 5.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2cccc(-c3ccccc3F)c2)CC1)c1ccccc1 nan
CHEMBL3646129 125435 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 416 5 2 2 5.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2cccc(-c3ccccc3F)c2)CC1)c1ccccc1 nan
68604357 125438 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 407 5 2 4 4.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2cccc(-c3ccccc3F)c2)CC1)c1ccon1 nan
CHEMBL3646132 125438 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 407 5 2 4 4.4 O=C(N[C@H]1CC[C@@H](C(=O)Nc2cccc(-c3ccccc3F)c2)CC1)c1ccon1 nan
9890550 193176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccncc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL523205 193176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccncc4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45481795 198284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccc(F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL575858 198284 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 483 4 1 5 3.7 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccc(F)cc4)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
9890550 193176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccncc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL523205 193176 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 462 3 1 4 4.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccncc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
9840567 202674 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 332 3 0 2 5.2 Cc1cc(N2CCCC2)cc(/C=C/c2cccc(C(F)(F)F)c2)n1 10.1021/jm980521l
CHEMBL61488 202674 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 332 3 0 2 5.2 Cc1cc(N2CCCC2)cc(/C=C/c2cccc(C(F)(F)F)c2)n1 10.1021/jm980521l
45481808 198326 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 4 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccco4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL576159 198326 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 451 3 1 4 4.3 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-c4ccco4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
9887226 200104 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL596031 200104 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 400 3 1 6 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
10018851 63870 1 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 319 4 1 5 4.3 Cc1ccccc1C(=O)c1cnc(Nc2cccc(C#N)c2)s1 10.1016/j.bmcl.2005.01.063
CHEMBL180359 63870 1 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 319 4 1 5 4.3 Cc1ccccc1C(=O)c1cnc(Nc2cccc(C#N)c2)s1 10.1016/j.bmcl.2005.01.063
89973939 128496 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 383 5 2 5 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)co2)CC1 nan
CHEMBL3666797 128496 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.Binding Assay: cDNA sequence encoding a mouse NPY Y5 receptor (Biochim. Biophys. Acta 1328:83-89, 1997) was cloned in a vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 8957). The obtained expression vector was transfected into CHO cells as a host by using Lipofect AMINE reagent (Trademark, Gico BRL Co., Ltd.) according to the instruction manual. The cells that stably express NPY Y5 receptor were obtained.The membranes prepared from the CHO cells expressing NPY Y5 receptor, the compound of this invention and 30,000 cpm [125I] peptide YY (60 pM of final concentration: Healthcare) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours, and then the membrane was filtered from the mixture through a glass filter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was quantified with a gamma counter.
ChEMBL 383 5 2 5 3.4 CC(C)(C)S(=O)(=O)NC[C@H]1CC[C@H](Nc2nc(C(F)(F)F)co2)CC1 nan
56836045 81345 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 399 3 1 5 3.7 CC(C)(C)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159164 81345 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 399 3 1 5 3.7 CC(C)(C)S(=O)(=O)c1ccc2[nH]c(N3CCOC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
9923839 187040 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL490937 187040 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
10293081 187241 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 379 4 1 4 4.2 O=[N+]([O-])c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL492594 187241 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 379 4 1 4 4.2 O=[N+]([O-])c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
71518999 86163 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 366 6 1 4 3.5 CCS(=O)(=O)c1ccc2[nH]c(OCC(F)(F)c3ccccc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312066 86163 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 366 6 1 4 3.5 CCS(=O)(=O)c1ccc2[nH]c(OCC(F)(F)c3ccccc3)nc2c1 10.1016/j.bmcl.2012.11.005
9952231 199820 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL594163 199820 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4)n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
44271377 59257 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 429 4 1 5 3.6 O=C(Nc1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL17037 59257 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 429 4 1 5 3.6 O=C(Nc1ccccc1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
46912987 125436 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 421 5 2 5 4.1 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4ccccc4)CC3)ccc21 nan
CHEMBL3646130 125436 0 None - 0 Mouse 8.4 pIC50 = 8.4 Binding
Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.Binding Assay: cDNA sequence encoding mouse NPY Y5 receptor (Biochem. Biophys. Acta 1328: 83-89, 1997) was cloned in the expression vector (pME18S, Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into CHO cells as a host according to the instruction manual using Lipofectamine reagent (Trademark, Gibco BRL Co., Ltd.). The cells that stably express NPY Y5 receptor were obtained.The membrane samples prepared from the CHO cells expressing NPY Y5 receptor, the compound of the invention and 30,000 cpm 125I peptide YY (60 pM of final concentration: Amersham) were incubated in the assay buffer (20 mM HEPES-Hanks buffer containing 0.1% bovine serum albumin, pH 7.4) at 25° C. for 2 hours. The membrane samples were then filtered from the mixture through a glassfilter (GF/C) presoaked with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer (pH 7.4), radioactivity retained on the filters was determined using gamma counter.
ChEMBL 421 5 2 5 4.1 CC(C)n1c(=O)oc2cc(NC(=O)[C@H]3CC[C@@H](NC(=O)c4ccccc4)CC3)ccc21 nan
45487629 199025 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL585854 199025 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 448 5 1 7 4.0 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccccc4OCF)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44579863 187100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1Cl 10.1016/j.bmcl.2008.08.021
CHEMBL491436 187100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 410 2 1 5 4.7 COC(=O)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1Cl 10.1016/j.bmcl.2008.08.021
20629114 73448 47 None - 1 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.09.025
CHEMBL2016681 73448 47 None - 1 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.09.025
20629114 73448 47 None - 1 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.11.005
CHEMBL2016681 73448 47 None - 1 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.11.005
9952232 199969 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL595120 199969 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of rat Y5 receptorInhibition of rat Y5 receptor
ChEMBL 388 3 1 6 3.5 O=C1O[C@]2(CC[C@H](C(=O)Nc3cnn(-c4ccccc4)c3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
44271284 58089 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 459 4 2 6 3.6 Cc1cc(O)ccc1NC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL16740 58089 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 459 4 2 6 3.6 Cc1cc(O)ccc1NC(=O)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
44271318 98440 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 504 4 1 7 4.4 O=C(Nc1nc2cc(Cl)ccc2o1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL275642 98440 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 504 4 1 7 4.4 O=C(Nc1nc2cc(Cl)ccc2o1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
22325320 184205 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 355 1 1 4 3.5 O=C1OC2(CCN(c3nc4cc(F)c(F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL483252 184205 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 355 1 1 4 3.5 O=C1OC2(CCN(c3nc4cc(F)c(F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44573648 172762 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)ccn1 10.1016/j.bmcl.2009.01.101
CHEMBL451113 172762 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 360 3 1 4 3.5 N#Cc1cc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)ccn1 10.1016/j.bmcl.2009.01.101
10273149 187522 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 412 3 1 2 5.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(Br)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL494398 187522 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 412 3 1 2 5.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(Br)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
45481797 198325 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4OC)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL576158 198325 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 495 5 1 6 3.6 CCS(=O)(=O)N1CC2(CCN(C(=O)Nc3cn(-c4ccccc4OC)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44401508 69821 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
CHEMBL193666 69821 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 433 10 2 6 3.6 CCCCS(=O)(=O)NCC1CCC(CNc2nc(N(C)C)c3ccccc3n2)CC1 10.1016/j.bmcl.2005.03.052
56835976 81158 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 398 5 1 5 3.2 CCCS(=O)(=O)c1ccc2[nH]c(N3CCN(C)C(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2158014 81158 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 398 5 1 5 3.2 CCCS(=O)(=O)c1ccc2[nH]c(N3CCN(C)C(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
44344629 110341 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 4 3.6 O=C(Nc1ccc2c(c1)c1ccccc1n2C1CCOC1)N1CCOCC1 10.1021/jm011125x
CHEMBL324028 110341 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 4 3.6 O=C(Nc1ccc2c(c1)c1ccccc1n2C1CCOC1)N1CCOCC1 10.1021/jm011125x
44312981 204427 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 418 5 2 5 4.5 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(C)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL72133 204427 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 418 5 2 5 4.5 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(C)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44461040 205324 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 421 4 1 5 4.3 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79500 205324 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 421 4 1 5 4.3 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(F)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
9867212 104895 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL311229 104895 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44344352 103428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 535 8 2 4 4.8 O=C(NC1CCc2cc(F)ccc2C1Cc1cccnc1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
CHEMBL3084876 103428 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 535 8 2 4 4.8 O=C(NC1CCc2cc(F)ccc2C1Cc1cccnc1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
70695119 76903 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3Cl)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070149 76903 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 396 4 1 3 5.3 CCS(=O)(=O)c1ccc2[nH]c(-c3cccc(-c4ccccc4)c3Cl)nc2c1 10.1016/j.bmcl.2012.07.020
10715854 28285 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 361 3 1 4 4.6 c1ccc(-c2cc3nc(N4CCCCC4)nc(N4CCCCC4)c3[nH]2)cc1 10.1021/jm000269t
CHEMBL137428 28285 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 361 3 1 4 4.6 c1ccc(-c2cc3nc(N4CCCCC4)nc(N4CCCCC4)c3[nH]2)cc1 10.1021/jm000269t
10667094 116797 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 337 5 2 5 2.7 Cc1nc(NCCN2CCOCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL337815 116797 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 337 5 2 5 2.7 Cc1nc(NCCN2CCOCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
70695117 76893 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccccc3-c3ccccc3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070139 76893 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccccc3-c3ccccc3)nc2c1 10.1016/j.bmcl.2012.07.020
10642181 165162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 3 1 4 3.9 COc1ccc(-c2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL422816 165162 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 3 1 4 3.9 COc1ccc(-c2cc3[nH]c(C)nc(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
45481643 198056 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 452 3 1 6 2.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-n4nccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL574089 198056 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 452 3 1 6 2.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(-n4nccn4)cc3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44460789 205307 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 460 5 1 7 2.9 O=C(CN1CCOCC1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79302 205307 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 460 5 1 7 2.9 O=C(CN1CCOCC1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44401460 70907 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 391 7 2 6 2.5 CN(C)c1nc(NCC2CCC(CNS(C)(=O)=O)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL195123 70907 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 391 7 2 6 2.5 CN(C)c1nc(NCC2CCC(CNS(C)(=O)=O)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
71519001 86165 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312068 86165 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.11.005
44370176 51592 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 485 6 3 5 3.8 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cc4ccccc4s3)CC2)cc1 10.1016/j.bmcl.2003.11.070
CHEMBL158344 51592 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 485 6 3 5 3.8 Cc1ccc(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cc4ccccc4s3)CC2)cc1 10.1016/j.bmcl.2003.11.070
10644957 119337 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 368 3 1 3 5.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(-c3ccccc3)c2n1 10.1021/jm000269t
CHEMBL344228 119337 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 368 3 1 3 5.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(-c3ccccc3)c2n1 10.1021/jm000269t
10421577 203896 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 235 2 1 2 3.4 Cc1[nH]c(-c2ccccc2)nc1-c1cccnc1 10.1016/s0960-894x(02)00090-2
CHEMBL6893 203896 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 235 2 1 2 3.4 Cc1[nH]c(-c2ccccc2)nc1-c1cccnc1 10.1016/s0960-894x(02)00090-2
44573616 193112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL522702 193112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 461 3 1 3 4.7 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44313596 105856 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 429 4 1 4 5.4 Cc1cc(C(=O)Nc2cccc(OC(F)(F)F)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL312748 105856 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 429 4 1 4 5.4 Cc1cc(C(=O)Nc2cccc(OC(F)(F)F)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44312927 103083 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 421 6 2 7 3.3 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccccn4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL307462 103083 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 421 6 2 7 3.3 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4ccccn4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
10497816 27688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3F)cc2n1 10.1021/jm000269t
CHEMBL137008 27688 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 2 1 3 4.1 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3F)cc2n1 10.1021/jm000269t
44573531 193199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 376 4 1 3 4.5 CC(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL523364 193199 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 376 4 1 3 4.5 CC(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
70693067 76896 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 368 4 1 3 4.4 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070142 76896 0 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 368 4 1 3 4.4 CCCS(=O)(=O)c1ccc2[nH]c(-c3cccc(C(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.07.020
11110677 11048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cccc(NC(=O)CCc3ccncc3)c21 10.1021/jm011125x
CHEMBL117684 11048 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cccc(NC(=O)CCc3ccncc3)c21 10.1021/jm011125x
23283666 103426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 582 10 2 4 6.9 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC1)C2Cc1ccccc1 10.1021/jm990468g
CHEMBL3084874 103426 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 582 10 2 4 6.9 COc1ccc2c(c1)CCC(NC[C@H]1CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC1)C2Cc1ccccc1 10.1021/jm990468g
11727519 53772 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 339 6 2 2 4.7 O=C(CCCc1ccccc1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
CHEMBL160389 53772 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 339 6 2 2 4.7 O=C(CCCc1ccccc1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
10596340 115493 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 2 1 3 4.7 Cc1nc(N2CCCCC2)c2[nH]c(C34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)cc2n1 10.1021/jm000269t
CHEMBL335145 115493 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 2 1 3 4.7 Cc1nc(N2CCCCC2)c2[nH]c(C34C[C@H]5C[C@@H](C3)C[C@@H](C4)C5)cc2n1 10.1021/jm000269t
44377450 55578 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL162093 55578 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44579809 193274 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 396 1 1 3 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(Br)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL523943 193274 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 396 1 1 3 5.0 O=C1O[C@]2(CC[C@H](c3nc4cc(Br)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
18735143 163500 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
CHEMBL42020 163500 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 482 6 2 5 3.6 CC(C)(C)OC(=O)NC1CCN(CC(=O)NC2CCc3cc(F)ccc3C2Cc2cccnc2)C1 10.1016/s0960-894x(00)00311-5
10429613 163339 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL419086 163339 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
11001068 205070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 300 4 3 3 3.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(O)cc1 10.1021/jm0004547
CHEMBL77311 205070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 300 4 3 3 3.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(O)cc1 10.1021/jm0004547
22934131 97037 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL266904 97037 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3ccccn3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
10833009 28335 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 334 4 1 3 4.8 CC(C)Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137464 28335 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 334 4 1 3 4.8 CC(C)Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44390369 64610 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL181727 64610 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 629 9 1 7 5.9 CN(C)c1nc(NCC2CCC(CN(C)S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
70695116 76892 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 300 4 1 3 3.4 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccccc3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070138 76892 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 300 4 1 3 3.4 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccccc3)nc2c1 10.1016/j.bmcl.2012.07.020
10005032 59222 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 472 8 2 3 5.9 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00177-3
CHEMBL17022 59222 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5Compound was tested for its affinity to bind with Neuropeptide Y receptor type 5
ChEMBL 472 8 2 3 5.9 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(00)00177-3
44579808 173360 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 1 1 3 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL452726 173360 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 1 1 3 5.3 O=C1O[C@]2(CC[C@H](c3nc4cc(C(F)(F)F)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
9967563 187655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cncnc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL495036 187655 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cncnc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
11002935 52072 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 4 2 2 5.1 O=C(Cc1ccc2ccccc2c1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
CHEMBL158732 52072 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 4 2 2 5.1 O=C(Cc1ccc2ccccc2c1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
44370214 47007 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 547 9 3 5 5.7 CC(C)c1cc(C(C)C)c(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cccs3)CC2)c(C(C)C)c1 10.1016/j.bmcl.2003.11.070
CHEMBL154168 47007 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 547 9 3 5 5.7 CC(C)c1cc(C(C)C)c(S(=O)(=O)NC[C@H]2CC[C@H](C(=O)NNC(=O)c3cccs3)CC2)c(C(C)C)c1 10.1016/j.bmcl.2003.11.070
10517831 115356 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 1 4 3.3 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)nc2n1 10.1021/jm000269t
CHEMBL334960 115356 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 1 4 3.3 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)nc2n1 10.1021/jm000269t
44390499 129657 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL367355 129657 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 579 8 2 6 6.0 CN(C)c1nc(NCC2CCC(CNC(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10496226 28086 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 324 3 1 4 4.3 CSc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137296 28086 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 324 3 1 4 4.3 CSc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44313099 103080 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 470 6 2 6 5.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc5ccccc45)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL307458 103080 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 470 6 2 6 5.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4cccc5ccccc45)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
44370215 169055 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 455 6 3 5 2.9 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
CHEMBL439638 169055 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 455 6 3 5 2.9 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Cl)cc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
71519332 86177 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 412 5 1 3 5.2 CCS(=O)(=O)c1ccc2[nH]c(C(F)(F)c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312080 86177 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 412 5 1 3 5.2 CCS(=O)(=O)c1ccc2[nH]c(C(F)(F)c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
44287999 162487 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41673 162487 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 471 11 4 3 3.2 C[C@@H](NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccccc1 10.1016/s0960-894x(00)00292-4
44312707 204947 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 461 7 2 6 4.8 CNc1cc(-c2ccc(NS(=O)(=O)c3ccc(N(C)C)cc3)cc2)nn1-c1ccc(C)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL76411 204947 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 461 7 2 6 4.8 CNc1cc(-c2ccc(NS(=O)(=O)c3ccc(N(C)C)cc3)cc2)nn1-c1ccc(C)cc1 10.1016/s0960-894x(01)00448-6
44580504 193180 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 2 1 4 3.2 O=C1OC2(CCN(Cc3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL523235 193180 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 2 1 4 3.2 O=C1OC2(CCN(Cc3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
45481806 197852 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 460 2 1 5 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nc4cc(Cl)ccc4o3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572460 197852 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 460 2 1 5 3.8 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nc4cc(Cl)ccc4o3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
18004942 187516 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 420 2 2 3 2.9 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccccc3Cl)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL494346 187516 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 420 2 2 3 2.9 NS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccccc3Cl)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
44460453 104175 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 431 4 1 6 3.7 O=C([C@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL309685 104175 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 431 4 1 6 3.7 O=C([C@H]1CCCO1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
9867212 104895 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL311229 104895 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 4 1 6 3.9 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)[C@H]4CCCO4)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44461116 107136 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 399 4 1 5 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)C(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL316153 107136 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 399 4 1 5 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)C(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44460972 205392 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 4 1 4 5.0 O=C1CCCN1[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL80003 205392 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 4 1 4 5.0 O=C1CCCN1[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44344468 103439 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 468 9 3 4 4.7 C=CCC1c2ccc(O)cc2CCC1NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
CHEMBL3084889 103439 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 468 9 3 4 4.7 C=CCC1c2ccc(O)cc2CCC1NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
44344599 110393 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CC[C@H](NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
CHEMBL324311 110393 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 522 8 2 5 3.0 O=C(CN1CC[C@H](NS(=O)(=O)c2ccccc2)C1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1021/jm990468g
11133371 205151 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 410 6 2 3 5.7 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/jm0004547
CHEMBL78109 205151 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 410 6 2 3 5.7 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccc(Cl)cc2)cc1 10.1021/jm0004547
44579887 193093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)no1 10.1016/j.bmcl.2008.08.021
CHEMBL522589 193093 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 6 4.6 Cc1nc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)no1 10.1016/j.bmcl.2008.08.021
11792636 29094 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 4 1 3 4.0 Cc1nc(N2CCCCC2)c2nc(CCc3ccccc3)cc-2[nH]1 10.1021/jm000269t
CHEMBL138118 29094 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 4 1 3 4.0 Cc1nc(N2CCCCC2)c2nc(CCc3ccccc3)cc-2[nH]1 10.1021/jm000269t
45481799 198054 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL574085 198054 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3cnc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
46226606 201843 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
CHEMBL607088 201843 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant Y5 receptorDisplacement of [125I]PYY from human recombinant Y5 receptor
ChEMBL 388 3 2 5 3.7 O=C1O[C@]2(CC[C@H](C(=O)Nc3cc(-c4ccccc4)[nH]n3)CC2)c2cccnc21 10.1016/j.bmc.2009.08.019
9947469 187268 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(Cl)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL492778 187268 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(Cl)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
23442561 67559 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cccc(F)c2)s1 10.1016/j.bmcl.2005.05.009
CHEMBL189810 67559 0 None - 0 Mouse 8.3 pIC50 = 8.3 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2cccc(F)c2)s1 10.1016/j.bmcl.2005.05.009
22325333 184327 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4c(Cl)cc(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL484268 184327 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.5 O=C1OC2(CCN(c3nc4c(Cl)cc(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
9866472 187872 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 414 2 1 5 3.8 O=C1Cc2ccccc2C2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)O1 10.1016/j.bmcl.2009.05.013
CHEMBL496393 187872 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 414 2 1 5 3.8 O=C1Cc2ccccc2C2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)O1 10.1016/j.bmcl.2009.05.013
22934124 161775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 260 1 1 1 4.2 c1ccc(-c2nc3c([nH]2)-c2ccccc2CCC3)cc1 10.1016/s0960-894x(02)00090-2
CHEMBL414020 161775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 260 1 1 1 4.2 c1ccc(-c2nc3c([nH]2)-c2ccccc2CCC3)cc1 10.1016/s0960-894x(02)00090-2
25211875 192649 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 7 3.5 Cn1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)n1 10.1016/j.bmcl.2008.08.021
CHEMBL521750 192649 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 400 2 1 7 3.5 Cn1nnc(-c2ccc3[nH]c([C@H]4CC[C@@]5(CC4)OC(=O)c4ccccc45)nc3c2)n1 10.1016/j.bmcl.2008.08.021
10098098 12925 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4=O)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL1189130 12925 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4=O)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL538079 12925 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4c(c3)-c3ccccc3C4=O)CC1)C(=O)OC2 10.1021/jm049599u
9984570 13083 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 496 5 1 5 5.7 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(C)c54)CC3)ccc21 10.1021/jm049599u
CHEMBL1190216 13083 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 496 5 1 5 5.7 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(C)c54)CC3)ccc21 10.1021/jm049599u
CHEMBL540365 13083 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 496 5 1 5 5.7 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(C)c54)CC3)ccc21 10.1021/jm049599u
44580546 188133 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 337 1 1 4 3.4 O=C1OC2(CCN(c3nc4c(F)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL498396 188133 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 337 1 1 4 3.4 O=C1OC2(CCN(c3nc4c(F)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
10981271 205108 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 360 6 1 2 5.6 C[C@@H](Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77719 205108 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 360 6 1 2 5.6 C[C@@H](Cc1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
11068838 103580 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL308625 103580 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
22325347 188085 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4c(Cl)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL497972 188085 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4c(Cl)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44573534 193079 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 364 4 1 3 4.3 COc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL522513 193079 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 364 4 1 3 4.3 COc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
10640471 29157 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 334 3 1 4 4.1 CC(=O)c1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
CHEMBL138172 29157 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 334 3 1 4 4.1 CC(=O)c1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
9905079 28524 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 4 1 4 4.1 Cc1nc2cc(-c3ccccc3)nc-2c(N(C)Cc2ccco2)[nH]1 10.1021/jm000269t
CHEMBL137613 28524 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 318 4 1 4 4.1 Cc1nc2cc(-c3ccccc3)nc-2c(N(C)Cc2ccco2)[nH]1 10.1021/jm000269t
44263876 97011 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 276 2 1 2 3.9 COc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CC2 10.1016/s0960-894x(02)00090-2
CHEMBL266637 97011 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 276 2 1 2 3.9 COc1ccc2c(c1)-c1nc(-c3ccccc3)[nH]c1CC2 10.1016/s0960-894x(02)00090-2
44377691 57146 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 506 8 3 5 4.0 Nc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL164586 57146 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 506 8 3 5 4.0 Nc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
9871208 178684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 516 7 2 5 4.2 O=C(CN1CCC(NC(=O)Oc2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL46799 178684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 516 7 2 5 4.2 O=C(CN1CCC(NC(=O)Oc2ccccc2)CC1)NC1CCc2cc(F)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
44313224 103026 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 379 3 1 3 5.1 Cc1cc(C(=O)Nc2cccc(Cl)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL306993 103026 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 379 3 1 3 5.1 Cc1cc(C(=O)Nc2cccc(Cl)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
10572176 28180 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 349 4 1 4 3.8 Cc1nc2cc(-c3ccccc3)nc-2c(N2CCCCC2CN(C)C)[nH]1 10.1021/jm000269t
CHEMBL137356 28180 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 349 4 1 4 3.8 Cc1nc2cc(-c3ccccc3)nc-2c(N2CCCCC2CN(C)C)[nH]1 10.1021/jm000269t
10688707 28283 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(C)c2n1 10.1021/jm000269t
CHEMBL137427 28283 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 306 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(C)c2n1 10.1021/jm000269t
9889267 98878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 436 4 1 7 3.1 O=C(Nc1nccs1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00018-5
CHEMBL279073 98878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 436 4 1 7 3.1 O=C(Nc1nccs1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00018-5
44344283 12952 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 507 13 2 5 4.9 COc1ccc2c(c1)CCC(NCCCCCCNS(=O)(=O)c1ccccc1)C2Cc1cccnc1 10.1021/jm990468g
CHEMBL118931 12952 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 507 13 2 5 4.9 COc1ccc2c(c1)CCC(NCCCCCCNS(=O)(=O)c1ccccc1)C2Cc1cccnc1 10.1021/jm990468g
9889267 98878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 436 4 1 7 3.1 O=C(Nc1nccs1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
CHEMBL279073 98878 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Tested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptorTested for the inhibition of [125I]PYY binding to HEK 293 cells stably expressed with human neuropeptide NPY Y5 receptor
ChEMBL 436 4 1 7 3.1 O=C(Nc1nccs1)C1CCN(C(=O)Cn2c(=O)sc3ccc(Cl)cc32)CC1 10.1016/s0960-894x(02)00113-0
136058109 102155 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 485 6 2 4 4.9 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4cc(Cl)ccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
CHEMBL302584 102155 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 485 6 2 4 4.9 O=S(=O)(NC[C@H]1CC[C@H](CNC2=NC3CCc4cc(Cl)ccc4C3C2)CC1)c1ccccc1 10.1016/s0960-894x(99)00676-9
22054806 187454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 298 3 1 2 4.0 c1ccc(C2=NC(c3ccccc3)(c3ccccc3)CN2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL493970 187454 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 298 3 1 2 4.0 c1ccc(C2=NC(c3ccccc3)(c3ccccc3)CN2)cc1 10.1016/j.bmcl.2009.01.101
9902517 187493 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 340 3 1 3 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccs3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL494175 187493 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 340 3 1 3 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccs3)=N2)cc1 10.1016/j.bmcl.2009.01.101
10437616 60511 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5c(Cl)cccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL175657 60511 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5c(Cl)cccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL557817 60511 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 516 5 1 5 6.0 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5c(Cl)cccc54)CC3)ccc21 10.1021/jm049599u
10590336 119407 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 300 3 2 3 4.7 Cc1nc(Nc2ccccc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL344692 119407 1 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 300 3 2 3 4.7 Cc1nc(Nc2ccccc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10518886 119423 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 308 3 1 4 3.6 COc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL344844 119423 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 308 3 1 4 3.6 COc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44377722 57195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL164971 57195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 535 10 2 5 4.6 COc1ccc2c(c1)CC(CNCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
10254802 127225 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 485 5 1 6 5.2 COc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4oc5ccccc5c4c3)CC1)C(=O)OC2 10.1021/jm049599u
CHEMBL365777 127225 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 485 5 1 6 5.2 COc1cccc2c1N(C1CCN(CC(=O)Nc3ccc4oc5ccccc5c4c3)CC1)C(=O)OC2 10.1021/jm049599u
44580748 187891 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 412 3 2 6 2.6 CS(=O)(=O)Nc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL496537 187891 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 412 3 2 6 2.6 CS(=O)(=O)Nc1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44379364 58117 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 551 10 3 6 3.7 COc1ccc2c(c1)CC(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
CHEMBL167621 58117 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 551 10 3 6 3.7 COc1ccc2c(c1)CC(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00018-5
10639971 28639 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 3 4.7 Cc1nc(-c2ccsc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL137724 28639 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 3 4.7 Cc1nc(-c2ccsc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
9880873 193195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccnn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL523338 193195 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccnn3)=N2)cc1 10.1016/j.bmcl.2009.01.101
44390385 122516 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360117 122516 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 565 9 2 6 6.4 CN(C)c1nc(NCC2CCC(CNCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
10685661 119186 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 264 2 1 3 3.1 Cc1nc(N2CCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL343153 119186 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 264 2 1 3 3.1 Cc1nc(N2CCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
136058112 203731 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 481 7 2 5 4.3 COc1ccc2c(c1)CCC1N=C(NC[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4)CC3)CC21 10.1016/s0960-894x(99)00676-9
CHEMBL67768 203731 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 481 7 2 5 4.3 COc1ccc2c(c1)CCC1N=C(NC[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4)CC3)CC21 10.1016/s0960-894x(99)00676-9
44263987 204318 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 250 1 2 2 3.0 c1ccc2c(c1)CCCc1nc(-c3c[nH]cn3)[nH]c1-2 10.1016/s0960-894x(02)00090-2
CHEMBL7147 204318 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 250 1 2 2 3.0 c1ccc2c(c1)CCCc1nc(-c3c[nH]cn3)[nH]c1-2 10.1016/s0960-894x(02)00090-2
44313495 204813 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 4.8 Cc1ccccc1NC(=O)c1cc(C)n(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(01)00449-8
CHEMBL75163 204813 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 4.8 Cc1ccccc1NC(=O)c1cc(C)n(-c2cccc(C(F)(F)F)c2)n1 10.1016/s0960-894x(01)00449-8
70695121 76916 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 393 5 1 5 3.6 CCCS(=O)(=O)c1ccc2[nH]c(-c3cn(-c4ccccc4)ccc3=O)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070162 76916 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 393 5 1 5 3.6 CCCS(=O)(=O)c1ccc2[nH]c(-c3cn(-c4ccccc4)ccc3=O)nc2c1 10.1016/j.bmcl.2012.07.020
44580746 188059 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 390 2 1 5 2.9 CN(C)C(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL497785 188059 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 390 2 1 5 2.9 CN(C)C(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
10714258 119278 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 370 2 1 3 4.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(Br)c2n1 10.1021/jm000269t
CHEMBL343766 119278 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 370 2 1 3 4.7 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)c(Br)c2n1 10.1021/jm000269t
2821670 168456 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccc(Cl)cc2)n[nH]1)C1Cc2ccccc2C1 10.1016/j.bmcl.2009.02.035
CHEMBL435036 168456 2 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccc(Cl)cc2)n[nH]1)C1Cc2ccccc2C1 10.1016/j.bmcl.2009.02.035
44573533 187463 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 364 4 2 3 3.8 OCc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL493998 187463 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 364 4 2 3 3.8 OCc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
10833804 119142 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 346 2 1 3 4.6 FC(F)(F)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL342818 119142 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 346 2 1 3 4.6 FC(F)(F)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44460907 104366 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 6 2 4 5.3 O=C(CC1CC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL310119 104366 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 427 6 2 4 5.3 O=C(CC1CC1)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461208 104745 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 442 7 2 5 4.1 O=C(CNCC1CC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL310674 104745 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 442 7 2 5 4.1 O=C(CNCC1CC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460957 205308 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 8 2 5 4.9 CCCN(C)CC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79308 205308 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 8 2 5 4.9 CCCN(C)CC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461198 205346 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 7 2 4 5.7 CCCCC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79659 205346 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 429 7 2 4 5.7 CCCCC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461210 205347 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 472 7 2 6 3.9 O=C(CNCC1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL79663 205347 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 472 7 2 6 3.9 O=C(CNCC1CCCO1)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460963 205554 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 438 5 1 5 4.4 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccccc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81104 205554 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 438 5 1 5 4.4 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccccc2-3)CC1 10.1016/j.bmcl.2004.03.014
44461179 205657 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 5 2 4 4.9 O=C(N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)C1CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81982 205657 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 5 2 4 4.9 O=C(N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1)C1CC1 10.1016/j.bmcl.2004.03.014
10295464 205701 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against rat neuropeptide Y5 receptorIn vitro binding affinity against rat neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82374 205701 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against rat neuropeptide Y5 receptorIn vitro binding affinity against rat neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
9827743 166385 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 511 6 3 7 3.9 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2cc(O)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL42762 166385 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 511 6 3 7 3.9 O=C(CN1CCC(n2c(O)nc3ccccc32)CC1)NC1CCc2cc(O)ccc2C1Cc1cccnc1 10.1016/s0960-894x(00)00311-5
9955865 123678 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 459 10 2 7 3.8 COc1ccc(C)cc1S(=O)(=O)NCCCNc1nc(C(=O)c2ccccc2C)cs1 10.1016/j.bmcl.2005.05.009
CHEMBL362131 123678 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 459 10 2 7 3.8 COc1ccc(C)cc1S(=O)(=O)NCCCNc1nc(C(=O)c2ccccc2C)cs1 10.1016/j.bmcl.2005.05.009
45481810 198535 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL578013 198535 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 436 2 1 4 3.6 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44583507 188071 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL497839 188071 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3ccc(-c4ccccc4)nn3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
44271231 60428 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 536 7 2 7 2.0 NS(=O)(=O)c1ccc(CCNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
CHEMBL17513 60428 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with Human NPY-Y5 cDNA (compound prepared by manual synthesis technique)
ChEMBL 536 7 2 7 2.0 NS(=O)(=O)c1ccc(CCNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
10294504 187211 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 402 3 1 2 5.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(C(F)(F)F)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL492388 187211 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 402 3 1 2 5.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccc(C(F)(F)F)c3)=N2)cc1 10.1016/j.bmcl.2009.01.101
22934136 167108 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL429006 167108 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 291 2 1 3 3.6 COc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
70684601 76895 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070141 76895 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 376 5 1 3 5.1 CCCS(=O)(=O)c1ccc2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2c1 10.1016/j.bmcl.2012.07.020
22934142 204326 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL7149 204326 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 275 1 1 2 3.9 Cc1ccc2c(c1)-c1nc(-c3ccncc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
22934118 204665 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
CHEMBL7370 204665 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 279 1 1 2 3.8 Fc1ccc2c(c1)-c1nc(-c3cccnc3)[nH]c1CCC2 10.1016/s0960-894x(02)00090-2
9885994 205098 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77639 205098 0 None - 1 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
22325336 188958 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL508271 188958 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 353 1 1 4 3.9 O=C1OC2(CCN(c3nc4cc(Cl)ccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44580100 186923 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 371 1 1 4 4.0 O=C1OC2(CCN(c3nc4cc(Cl)c(F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL490008 186923 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 371 1 1 4 4.0 O=C1OC2(CCN(c3nc4cc(Cl)c(F)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
71454969 81338 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 2 5 2.9 CCCS(=O)(=O)c1ccc2[nH]c(N3CCNC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
CHEMBL2159157 81338 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 384 5 2 5 2.9 CCCS(=O)(=O)c1ccc2[nH]c(N3CCNC(c4ccccc4)C3)nc2c1 10.1016/j.bmcl.2012.09.025
9825755 203494 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 465 5 2 4 3.8 O=C(NC1=NC2CCc3ccccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
CHEMBL66168 203494 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 465 5 2 4 3.8 O=C(NC1=NC2CCc3ccccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
10459583 12901 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 491 6 1 5 5.7 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
CHEMBL1188975 12901 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 491 6 1 5 5.7 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
CHEMBL537858 12901 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 491 6 1 5 5.7 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm049599u
10571295 119152 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 335 2 1 4 2.6 CC(=O)N1CCN(c2[nH]c(C)nc3cc(-c4ccccc4)nc2-3)CC1 10.1021/jm000269t
CHEMBL342918 119152 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 335 2 1 4 2.6 CC(=O)N1CCN(c2[nH]c(C)nc3cc(-c4ccccc4)nc2-3)CC1 10.1021/jm000269t
71519333 86178 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 402 5 1 3 5.1 CCS(=O)(=O)c1ccc2[nH]c(C3(c4ccc(-c5ccccc5)cc4)CC3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312081 86178 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 402 5 1 3 5.1 CCS(=O)(=O)c1ccc2[nH]c(C3(c4ccc(-c5ccccc5)cc4)CC3)nc2c1 10.1016/j.bmcl.2012.11.005
70697152 76899 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 375 5 1 2 5.7 CCCS(=O)(=O)c1ccc2cc(-c3cccc(-c4ccccc4)c3)[nH]c2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070145 76899 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 375 5 1 2 5.7 CCCS(=O)(=O)c1ccc2cc(-c3cccc(-c4ccccc4)c3)[nH]c2c1 10.1016/j.bmcl.2012.07.020
44461116 107136 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 399 4 1 5 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)C(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
CHEMBL316153 107136 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ responseIn vitro binding affinity against human neuropeptide Y5 receptor measured as Ca+ response
ChEMBL 399 4 1 5 4.4 Cc1ccc2c(c1)-c1nc(NCC3CCN(C(=O)C(C)C)CC3)sc1CCO2 10.1016/j.bmcl.2004.03.014
44264067 204039 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 262 1 1 2 3.7 c1ccc(-c2nc3c([nH]2)CCOc2ccccc2-3)cc1 10.1016/s0960-894x(02)00090-2
CHEMBL6985 204039 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 262 1 1 2 3.7 c1ccc(-c2nc3c([nH]2)CCOc2ccccc2-3)cc1 10.1016/s0960-894x(02)00090-2
44313510 103805 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 4.8 Cc1cccc(NC(=O)c2cc(C)n(-c3cccc(C(F)(F)F)c3)n2)c1 10.1016/s0960-894x(01)00449-8
CHEMBL309055 103805 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 359 3 1 3 4.8 Cc1cccc(NC(=O)c2cc(C)n(-c3cccc(C(F)(F)F)c3)n2)c1 10.1016/s0960-894x(01)00449-8
44312968 204880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 472 5 2 5 5.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL75827 204880 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 472 5 2 5 5.3 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(C(F)(F)F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
9998721 64375 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 362 4 1 4 5.4 Cc1ccccc1C(=O)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
CHEMBL181304 64375 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 362 4 1 4 5.4 Cc1ccccc1C(=O)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
44573408 192657 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccc3Cl)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL521844 192657 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 368 3 1 2 4.9 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccccc3Cl)=N2)cc1 10.1016/j.bmcl.2009.01.101
23442539 124084 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cccc(F)c2)n1 10.1016/j.bmcl.2005.05.009
CHEMBL363279 124084 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cccc(F)c2)n1 10.1016/j.bmcl.2005.05.009
10589936 28023 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 258 3 1 3 3.2 CCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
CHEMBL137258 28023 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 258 3 1 3 3.2 CCCc1cc2[nH]c(C)nc(N3CCCCC3)c-2n1 10.1021/jm000269t
44377731 57442 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 507 8 2 5 4.1 COc1ccc2c(c1)CC(NC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL165506 57442 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 507 8 2 5 4.1 COc1ccc2c(c1)CC(NC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44379411 120467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 523 10 3 6 3.3 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CC2 10.1016/s0960-894x(02)00018-5
CHEMBL354111 120467 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5Inhibition of 125 I-PYY binding to human Neuropeptide Y receptor type 5
ChEMBL 523 10 3 6 3.3 COc1ccc2c(c1)C(O)(CNCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CC2 10.1016/s0960-894x(02)00018-5
10808680 28078 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 326 2 1 3 4.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3Cl)cc2n1 10.1021/jm000269t
CHEMBL137290 28078 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 326 2 1 3 4.6 Cc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3Cl)cc2n1 10.1021/jm000269t
44312956 103167 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 488 6 2 6 5.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL308110 103167 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 488 6 2 6 5.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(OC(F)(F)F)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
10645176 27848 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 372 4 1 4 5.2 Cc1nc(N2CCCCC2)c2nc(CSc3ccc(Cl)cc3)cc-2[nH]1 10.1021/jm000269t
CHEMBL137125 27848 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 372 4 1 4 5.2 Cc1nc(N2CCCCC2)c2nc(CSc3ccc(Cl)cc3)cc-2[nH]1 10.1021/jm000269t
44313486 204772 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 471 3 1 3 5.1 Cc1cc(C(=O)Nc2cccc(I)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL74777 204772 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 471 3 1 3 5.1 Cc1cc(C(=O)Nc2cccc(I)c2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44377440 57451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 551 10 2 6 4.4 COc1cc2c(cc1OC)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL165556 57451 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 551 10 2 6 4.4 COc1cc2c(cc1OC)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44377661 119917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 593 12 2 7 4.3 CCOC(=O)COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL349386 119917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 593 12 2 7 4.3 CCOC(=O)COc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44287971 163442 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL41981 163442 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 487 12 6 4 2.4 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](CO)c1ccccc1 10.1016/s0960-894x(00)00292-4
9969726 205588 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 375 3 1 5 3.6 CC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81442 205588 1 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 375 3 1 5 3.6 CC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
9799669 205810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 373 3 1 4 4.1 CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL83255 205810 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 373 3 1 4 4.1 CC(=O)N1CCC(CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10324940 13842 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)C(=O)c1ccccc1-2 10.1021/jm049599u
CHEMBL1195875 13842 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)C(=O)c1ccccc1-2 10.1021/jm049599u
CHEMBL555513 13842 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 501 4 1 5 5.1 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)C(=O)c1ccccc1-2 10.1021/jm049599u
10969955 110588 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against rat Neuropeptide Y receptor Y5Binding affinity against rat Neuropeptide Y receptor Y5
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL325475 110588 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity against rat Neuropeptide Y receptor Y5Binding affinity against rat Neuropeptide Y receptor Y5
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
1639804 13372 11 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 323 2 1 3 3.7 CCn1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL119247 13372 11 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 323 2 1 3 3.7 CCn1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
44460467 164557 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 6 1 5 4.9 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(C)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL421521 164557 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 413 6 1 5 4.9 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(C)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44460946 205545 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 472 5 1 5 5.1 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81024 205545 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 472 5 1 5 5.1 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCCc2ccc(Cl)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10295464 205701 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82374 205701 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 417 6 1 5 4.7 CCCCC(=O)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
23283663 103417 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 537 9 3 5 4.9 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(O)ccc3C2Cc2cccnc2)CC1)c1ccccc1F 10.1021/jm990468g
CHEMBL3084864 103417 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 537 9 3 5 4.9 O=S(=O)(NC[C@H]1CC[C@H](CNC2CCc3cc(O)ccc3C2Cc2cccnc2)CC1)c1ccccc1F 10.1021/jm990468g
45481640 197910 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 420 2 1 4 3.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL572909 197910 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 420 2 1 4 3.1 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccc(Cl)cn3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
71519003 86167 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 386 5 1 5 4.0 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(OC(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312070 86167 0 None - 0 Mouse 8.2 pIC50 = 8.2 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 386 5 1 5 4.0 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(OC(F)(F)F)c3)nc2c1 10.1016/j.bmcl.2012.11.005
9880835 187654 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccnc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL495034 187654 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 335 3 1 3 3.7 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cccnc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
22934127 161798 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1cncc(-c2nc3c([nH]2)-c2ccccc2CCC3)c1 10.1016/s0960-894x(02)00090-2
CHEMBL414205 161798 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5Concentration that inhibited 50% of binding of 125 I -PYY ligand to human Neuropeptide Y receptor type 5
ChEMBL 261 1 1 2 3.6 c1cncc(-c2nc3c([nH]2)-c2ccccc2CCC3)c1 10.1016/s0960-894x(02)00090-2
44573575 187205 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccnc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL492371 187205 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccnc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
45487535 197238 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
CHEMBL568337 197238 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk cells
ChEMBL 418 3 1 6 3.9 O=C1O[C@]2(CC[C@H](C(=O)Nc3ncc(-c4ccc(F)cc4)cn3)CC2)c2cccnc21 10.1016/j.bmcl.2009.07.103
44573575 187205 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccnc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492371 187205 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3ccnc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
70693070 76913 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 407 3 1 5 4.0 CC(C)(C)S(=O)(=O)c1ccc2[nH]c(-c3ccc(=O)n(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
CHEMBL2070159 76913 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from mouse NPY Y5 receptorDisplacement of [125I]PYY from mouse NPY Y5 receptor
ChEMBL 407 3 1 5 4.0 CC(C)(C)S(=O)(=O)c1ccc2[nH]c(-c3ccc(=O)n(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.07.020
10096226 63496 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 469 6 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm049599u
CHEMBL179972 63496 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 469 6 1 5 4.5 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc(C(=O)c2ccccc2)cc1 10.1021/jm049599u
21956072 193120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 376 2 1 5 4.1 COC(=O)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
CHEMBL522768 193120 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 376 2 1 5 4.1 COC(=O)c1ccc2[nH]c([C@H]3CC[C@@]4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.021
10051692 44589 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 499 6 3 5 3.1 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Br)cc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
CHEMBL152016 44589 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 499 6 3 5 3.1 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccc(Br)cc2)CC1)c1cccs1 10.1016/j.bmcl.2003.11.070
10025916 63266 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 434 4 1 5 3.9 O=C(CN1CCC(N2C(=O)OCc3cc(F)ccc32)CC1)Nc1ccc2ncccc2c1 10.1021/jm049599u
CHEMBL179154 63266 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 434 4 1 5 3.9 O=C(CN1CCC(N2C(=O)OCc3cc(F)ccc32)CC1)Nc1ccc2ncccc2c1 10.1021/jm049599u
44583560 192644 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 405 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3nc(-c4ccccc4)cs3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
CHEMBL521723 192644 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant NPY Y5 receptor expressed in mouse LMtk- cells
ChEMBL 405 2 1 5 4.5 O=C1OC2(CCN(C(=O)Nc3nc(-c4ccccc4)cs3)CC2)c2ccccc21 10.1016/j.bmcl.2009.05.013
10971233 205033 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 392 6 2 3 5.5 C[C@H]([C@@H](O)c1ccccc1)N(C)/C(S)=N/c1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77010 205033 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 392 6 2 3 5.5 C[C@H]([C@@H](O)c1ccccc1)N(C)/C(S)=N/c1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
10958843 111218 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.2 CCn1c2ccccc2c2cc(C(=O)NCCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL326491 111218 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.2 CCn1c2ccccc2c2cc(C(=O)NCCc3ccncc3)ccc21 10.1021/jm011125x
44312687 204650 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 491 6 2 7 3.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4c[n+](C(F)(F)F)ccn4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL73619 204650 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 491 6 2 7 3.1 COc1ccc(S(=O)(=O)Nc2ccc(-c3cc(N)n(-c4c[n+](C(F)(F)F)ccn4)n3)cc2)cc1 10.1016/s0960-894x(01)00448-6
44460506 105410 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 5 1 6 4.0 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL311824 105410 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 458 5 1 6 4.0 O=C(CN1CCCCC1)N1CCC(CNc2nc3c(s2)CCOc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
11079077 204952 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 366 6 1 2 6.3 CC(CC1CCCCC1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL76422 204952 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 366 6 1 2 6.3 CC(CC1CCCCC1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
11089837 11020 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.9 Cc1c(NC(=O)N2CCOCC2)cc(C)c2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL117469 11020 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.9 Cc1c(NC(=O)N2CCOCC2)cc(C)c2c1c1ccccc1n2C(C)C 10.1021/jm011125x
44377461 55579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 505 8 2 4 4.7 Cc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL162094 55579 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 505 8 2 4 4.7 Cc1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
10637486 27581 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 2 4 2.3 Cc1nc(N2CCNCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL136940 27581 1 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 293 2 2 4 2.3 Cc1nc(N2CCNCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10667042 26015 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 336 4 2 4 3.7 Cc1nc(N2CCCCC2CCO)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL135485 26015 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 336 4 2 4 3.7 Cc1nc(N2CCCCC2CCO)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10641357 28473 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 7 2 4 3.7 CCOCCCNc1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
CHEMBL137557 28473 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 310 7 2 4 3.7 CCOCCCNc1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
10642052 115126 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.7 CCC1CCCCN1c1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
CHEMBL334373 115126 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.7 CCC1CCCCN1c1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
44580547 193480 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 1 1 4 3.5 Cc1cccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc12 10.1016/j.bmcl.2008.08.018
CHEMBL526641 193480 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 333 1 1 4 3.5 Cc1cccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc12 10.1016/j.bmcl.2008.08.018
12018680 164683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(N)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL421695 164683 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 419 5 3 6 3.8 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc(N)cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44377689 58082 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL167318 58082 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 521 9 2 5 4.4 COc1ccc2c(c1)CC(NCCN1CCC(CNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
44344244 103416 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 484 8 2 3 4.7 C=CCC1c2ccc(F)cc2CCC1NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
CHEMBL3084863 103416 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 484 8 2 3 4.7 C=CCC1c2ccc(F)cc2CCC1NC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1021/jm990468g
9871512 166393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 525 7 2 7 4.2 COc1ccc2c(c1)CCC(NC(=O)CN1CCC(n3c(O)nc4ccccc43)CC1)C2Cc1cccnc1 10.1016/s0960-894x(00)00311-5
CHEMBL42768 166393 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell lineInhibition of binding of radioligand [125I]PYY to the human Neuropeptide Y receptor type 5, using a stably transfected HEK293 cell line
ChEMBL 525 7 2 7 4.2 COc1ccc2c(c1)CCC(NC(=O)CN1CCC(n3c(O)nc4ccccc43)CC1)C2Cc1cccnc1 10.1016/s0960-894x(00)00311-5
11795098 116414 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 397 4 2 4 4.9 O=C(Nc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1)c1ccccc1 10.1021/jm000269t
CHEMBL336029 116414 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 397 4 2 4 4.9 O=C(Nc1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1)c1ccccc1 10.1021/jm000269t
10549405 30458 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 371 3 1 5 2.0 Cc1nc(N2CCN(S(C)(=O)=O)CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL139270 30458 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 371 3 1 5 2.0 Cc1nc(N2CCN(S(C)(=O)=O)CC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10948789 103579 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 375 7 1 3 4.6 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Cc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL308623 103579 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 375 7 1 3 4.6 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Cc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
44288112 100208 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
CHEMBL288355 100208 1 None - 0 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 487 11 5 4 2.9 CC(NC(=O)C(CCCN=C(N)N)NC(=O)C(c1ccccc1)c1ccccc1)c1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
44313496 204814 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 345 3 1 3 4.7 Cc1cc(C(=O)Nc2cc(Cl)cc(Cl)c2)nn1-c1ccccc1 10.1016/s0960-894x(01)00449-8
CHEMBL75193 204814 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 345 3 1 3 4.7 Cc1cc(C(=O)Nc2cc(Cl)cc(Cl)c2)nn1-c1ccccc1 10.1016/s0960-894x(01)00449-8
44313228 204615 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 410 4 1 4 5.2 Cc1cc(C(=O)Nc2ccccc2-n2cccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL73351 204615 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 410 4 1 4 5.2 Cc1cc(C(=O)Nc2ccccc2-n2cccc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
44401578 12961 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 512 6 1 6 5.4 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(OC)c54)CC3)ccc21 10.1021/jm049599u
CHEMBL1189371 12961 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 512 6 1 6 5.4 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(OC)c54)CC3)ccc21 10.1021/jm049599u
CHEMBL538569 12961 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 512 6 1 6 5.4 CCn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5cccc(OC)c54)CC3)ccc21 10.1021/jm049599u
10926986 12629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 379 3 1 3 5.4 CC(C)c1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
CHEMBL118710 12629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 379 3 1 3 5.4 CC(C)c1c(NC(=O)N2CCOCC2)ccc2c1c1ccccc1n2C(C)C 10.1021/jm011125x
44287938 100410 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
CHEMBL290175 100410 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 631 13 4 4 5.4 N/C(=N/CCCC(NC(=O)Cc1ccc(-c2ccccc2)cc1)C(=O)N1CCCc2cc(O)ccc2C1)NCCCc1ccccc1 10.1016/s0960-894x(00)00292-4
10893873 13616 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.7 CC(C)(C)Cn1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
CHEMBL119426 13616 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 365 2 1 3 4.7 CC(C)(C)Cn1c2ccccc2c2cc(NC(=O)N3CCOCC3)ccc21 10.1021/jm011125x
44460815 205252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 416 4 2 5 3.0 CC(=O)NC1CCN(CC(=O)Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL78901 205252 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 416 4 2 5 3.0 CC(=O)NC1CCN(CC(=O)Nc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
44401552 165906 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL425012 165906 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 572 8 2 6 5.5 O=S(=O)(NCC1CCC(CNc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
10500401 27819 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 9 2 3 5.9 CCCCCC(CC)CNc1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
CHEMBL137102 27819 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 350 9 2 3 5.9 CCCCCC(CC)CNc1[nH]c(C)nc2cc(-c3ccccc3)nc1-2 10.1021/jm000269t
10737530 119421 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc(F)ccc3F)cc2n1 10.1021/jm000269t
CHEMBL344820 119421 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 328 2 1 3 4.2 Cc1nc(N2CCCCC2)c2[nH]c(-c3cc(F)ccc3F)cc2n1 10.1021/jm000269t
12018679 204604 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 449 6 2 7 4.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc([N+](=O)[O-])cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
CHEMBL73251 204604 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 in HEK 293 cell line, using [125I]PYY as radioligand
ChEMBL 449 6 2 7 4.1 Cc1ccc(-n2nc(-c3ccc(NS(=O)(=O)c4ccc([N+](=O)[O-])cc4)cc3)cc2N)cc1 10.1016/s0960-894x(01)00448-6
44377460 52735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 536 9 2 6 4.3 O=[N+]([O-])c1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL159450 52735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 536 9 2 6 4.3 O=[N+]([O-])c1ccc2c(c1)CC(NCC1CCN(CCNS(=O)(=O)c3cccc4ccccc34)CC1)CCC2 10.1016/s0960-894x(02)00002-1
11015360 11292 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 422 6 1 5 3.4 CN(C)S(=O)(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
CHEMBL117922 11292 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 422 6 1 5 3.4 CN(C)S(=O)(=O)n1c2ccccc2c2cc(NC(=O)CCc3ccncc3)ccc21 10.1021/jm011125x
44579845 193123 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 1 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL522788 193123 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 386 1 1 3 5.6 O=C1O[C@]2(CC[C@H](c3nc4cc(Cl)c(Cl)cc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
10347241 13932 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 4 2 5 5.0 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
CHEMBL1196486 13932 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 4 2 5 5.0 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
CHEMBL557172 13932 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 503 4 2 5 5.0 O=C(CN1CCC(N2C(=O)OCc3cc(Cl)ccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
10971892 103173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 422 7 1 2 6.9 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C(Cc1ccccc1)c1ccccc1 10.1021/jm0004547
CHEMBL308130 103173 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 422 7 1 2 6.9 CN(C(=O)Nc1ccc(Oc2ccccc2)cc1)C(Cc1ccccc1)c1ccccc1 10.1021/jm0004547
44573697 187210 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 351 3 2 3 2.9 O=c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)[nH]1 10.1016/j.bmcl.2009.01.101
CHEMBL492377 187210 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 351 3 2 3 2.9 O=c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)[nH]1 10.1016/j.bmcl.2009.01.101
9952193 100586 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 387 6 2 4 4.4 COc1ccc(-c2cc(NC(=O)Cc3ccc4ccccc4c3)[nH]n2)cc1OC 10.1021/jm980521l
CHEMBL291666 100586 0 None - 1 Rat 8.1 pIC50 = 8.1 Binding
The compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in ratThe compound was tested for the binding affinity against Neuropeptide Y receptor type 5 in rat
ChEMBL 387 6 2 4 4.4 COc1ccc(-c2cc(NC(=O)Cc3ccc4ccccc4c3)[nH]n2)cc1OC 10.1021/jm980521l
10689108 25740 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 312 3 1 3 4.3 Cc1nc(N2CCCCC2)c2nc(CC3CCCCC3)cc-2[nH]1 10.1021/jm000269t
CHEMBL135261 25740 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 312 3 1 3 4.3 Cc1nc(N2CCCCC2)c2nc(CC3CCCCC3)cc-2[nH]1 10.1021/jm000269t
9947073 193086 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 362 4 1 3 4.1 O=Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL522539 193086 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 362 4 1 3 4.1 O=Cc1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
9983662 13956 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 469 4 2 5 4.3 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
CHEMBL1196677 13956 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 469 4 2 5 4.3 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
CHEMBL557802 13956 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 469 4 2 5 4.3 O=C(CN1CCC(N2C(=O)OCc3ccccc32)CC1)Nc1ccc2c(c1)-c1ccccc1C2O 10.1021/jm049599u
45481802 198408 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 472 3 1 6 3.7 COc1cccc2sc(NC(=O)N3CCC4(CC3)CN(S(C)(=O)=O)c3ccccc34)nc12 10.1016/j.bmc.2009.05.064
CHEMBL576941 198408 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 472 3 1 6 3.7 COc1cccc2sc(NC(=O)N3CCC4(CC3)CN(S(C)(=O)=O)c3ccccc34)nc12 10.1016/j.bmc.2009.05.064
9908720 204636 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 396 3 1 4 5.0 Cc1cc(C(=O)Nc2cccc3cnccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL73534 204636 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 396 3 1 4 5.0 Cc1cc(C(=O)Nc2cccc3cnccc23)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
71518853 86161 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 350 5 1 4 3.6 CCS(=O)(=O)c1ccc2[nH]c(OCc3cccc(Cl)c3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312064 86161 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 350 5 1 4 3.6 CCS(=O)(=O)c1ccc2[nH]c(OCc3cccc(Cl)c3)nc2c1 10.1016/j.bmcl.2012.11.005
44313572 204922 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 363 3 1 3 4.6 Cc1cc(C(=O)Nc2ccc(F)cc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
CHEMBL76218 204922 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligandBinding affinity to human neuropeptide Y receptor type 5 (NPY5) in HEK 293 cell line assayed by using [125I]PYY as radioligand
ChEMBL 363 3 1 3 4.6 Cc1cc(C(=O)Nc2ccc(F)cc2)nn1-c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(01)00449-8
11099994 10130 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2ccc(NC(=O)CCc3ccncc3)cc21 10.1021/jm011125x
CHEMBL115690 10130 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)Binding affinity to the human Neuropeptide Y receptor Y5 (NPY5)
ChEMBL 343 5 1 3 4.8 CCn1c2ccccc2c2ccc(NC(=O)CCc3ccncc3)cc21 10.1021/jm011125x
21129772 169424 4 None -309 8 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
CHEMBL44246 169424 4 None -309 8 Human 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cellsInhibition of binding of [3H]propionyl-NPY (1 nM) to Neuropeptide Y receptor type 5 in HEC-1-B cells
ChEMBL 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1016/s0960-894x(00)00292-4
11056043 120050 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 311 4 2 2 3.9 O=C(Cc1ccccc1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
CHEMBL350463 120050 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 311 4 2 2 3.9 O=C(Cc1ccccc1)Nc1cc(-c2ccc(Cl)cc2)n[nH]1 10.1021/jm025513q
44460921 205706 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 430 6 2 5 4.1 CN(C)CC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL82408 205706 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 430 6 2 5 4.1 CN(C)CC(=O)N[C@H]1CC[C@H](CNc2nc3c(s2)CCCc2ccc(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
10779945 168580 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 5.0 Cc1nc(C2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL435825 168580 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 291 2 1 2 5.0 Cc1nc(C2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
44580594 188102 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4c(C(F)(F)F)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL498166 188102 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 387 1 1 4 4.2 O=C1OC2(CCN(c3nc4c(C(F)(F)F)cccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
10498514 119216 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.7 CC(C)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL343330 119216 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 320 3 1 3 4.7 CC(C)c1nc(N2CCCCC2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
22325350 184326 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 397 2 1 6 2.6 CS(=O)(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
CHEMBL484267 184326 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 397 2 1 6 2.6 CS(=O)(=O)c1ccc2[nH]c(N3CCC4(CC3)OC(=O)c3ccccc34)nc2c1 10.1016/j.bmcl.2008.08.018
44377468 56500 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 525 8 2 4 5.0 O=S(=O)(NCCN1CCC(CNC2CCCc3ccc(Cl)cc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
CHEMBL163470 56500 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 525 8 2 4 5.0 O=S(=O)(NCCN1CCC(CNC2CCCc3ccc(Cl)cc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00002-1
10734658 27604 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 286 2 1 3 4.0 Cc1nc(-c2cccnc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
CHEMBL136959 27604 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 286 2 1 3 4.0 Cc1nc(-c2cccnc2)c2[nH]c(-c3ccccc3)cc2n1 10.1021/jm000269t
10789271 164856 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 404 4 1 5 3.8 Cc1nc(N2CCCCC2)c2nc(CS(=O)(=O)c3ccc(Cl)cc3)cc-2[nH]1 10.1021/jm000269t
CHEMBL421913 164856 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 404 4 1 5 3.8 Cc1nc(N2CCCCC2)c2nc(CS(=O)(=O)c3ccc(Cl)cc3)cc-2[nH]1 10.1021/jm000269t
44377854 120113 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 507 10 2 5 3.8 COc1ccc2c(c1)CC(CNCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
CHEMBL351082 120113 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Concentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptorConcentration that inhibited 50% of total specific binding of [125I]PYY ligand to human NPY-Y5 receptor
ChEMBL 507 10 2 5 3.8 COc1ccc2c(c1)CC(CNCC1CN(CCNS(=O)(=O)c3cccc4ccccc34)C1)CCC2 10.1016/s0960-894x(02)00002-1
10075283 12979 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc3c(c2)C(=O)c2ccccc2-3)CC1 10.1021/jm049599u
CHEMBL1189496 12979 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc3c(c2)C(=O)c2ccccc2-3)CC1 10.1021/jm049599u
CHEMBL538823 12979 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 481 4 1 5 4.8 Cc1ccc2c(c1)COC(=O)N2C1CCN(CC(=O)Nc2ccc3c(c2)C(=O)c2ccccc2-3)CC1 10.1021/jm049599u
12078329 29447 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 324 3 1 3 3.9 Cc1nc(N2CCCCC2)c2nc(Cc3ccc(F)cc3)cc-2[nH]1 10.1021/jm000269t
CHEMBL138435 29447 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 324 3 1 3 3.9 Cc1nc(N2CCCCC2)c2nc(Cc3ccc(F)cc3)cc-2[nH]1 10.1021/jm000269t
44401449 71094 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
CHEMBL195346 71094 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 544 6 2 6 5.0 O=S(=O)(NC1CCC(Nc2ncc3ccccc3n2)CC1)c1ccc(Br)cc1OC(F)(F)F 10.1016/j.bmcl.2005.03.052
11204090 63507 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL180003 63507 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 587 7 2 7 5.1 CN(C)c1nc(N[C@H]2CC[C@@H](NS(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
44390118 123909 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 366 4 1 4 5.3 O=C(c1cccc(F)c1)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
CHEMBL362795 123909 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against Neuropeptide Y receptor type 5 in mouseInhibitory concentration against Neuropeptide Y receptor type 5 in mouse
ChEMBL 366 4 1 4 5.3 O=C(c1cccc(F)c1)c1cnc(Nc2cccc(C(F)(F)F)c2)s1 10.1016/j.bmcl.2005.01.063
11342160 122935 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
CHEMBL360671 122935 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYYInhibitory activity against constitutively activated human Neuropeptide Y receptor Y5 transiently expressed in COS-1 cells using [125I]PYY
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.03.052
11342160 122935 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
CHEMBL360671 122935 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cellsInhibitory activity against neuropeptide Y receptor type 5 by using [125I]PYY as radioligand expressed in COS-1 cells
ChEMBL 573 6 1 7 4.6 CN(C)c1nc(NC2CCN(S(=O)(=O)c3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12 10.1016/j.bmcl.2005.05.121
9934923 102641 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 481 5 3 5 3.5 O=C(NC1=NC2CCc3cc(O)ccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
CHEMBL304353 102641 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 481 5 3 5 3.5 O=C(NC1=NC2CCc3cc(O)ccc3C2C1)[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2)CC1 10.1016/s0960-894x(99)00676-9
9847333 198150 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 465 3 1 5 3.4 Cn1ccnc1-c1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmc.2009.05.064
CHEMBL574772 198150 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 465 3 1 5 3.4 Cn1ccnc1-c1ccc(NC(=O)N2CCC3(CC2)CN(S(C)(=O)=O)c2ccccc23)cc1 10.1016/j.bmc.2009.05.064
11057893 205114 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1cccc(Oc2ccccc2)c1 10.1021/jm0004547
CHEMBL77769 205114 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 376 6 2 3 5.1 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Nc1cccc(Oc2ccccc2)c1 10.1021/jm0004547
23442513 67000 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 517 9 2 6 5.1 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)n1 10.1016/j.bmcl.2005.05.009
CHEMBL186916 67000 0 None - 0 Mouse 8.1 pIC50 = 8.1 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 517 9 2 6 5.1 Cc1ccccc1C(=O)c1csc(NCCCNS(=O)(=O)c2cc(C(F)(F)F)ccc2Cl)n1 10.1016/j.bmcl.2005.05.009
44271231 60428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 536 7 2 7 2.0 NS(=O)(=O)c1ccc(CCNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
CHEMBL17513 60428 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)Inhibitory concentration of total specific binding of [125I]- -PYY to HEK 293 cells transfected with the Human NPY-Y5 cDNA (compound prepared by parallel synthesis technique)
ChEMBL 536 7 2 7 2.0 NS(=O)(=O)c1ccc(CCNC(=O)C2CCN(C(=O)Cn3c(=O)sc4ccc(Cl)cc43)CC2)cc1 10.1016/s0960-894x(02)00113-0
20587799 191678 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 347 1 1 4 3.8 Cc1cc2nc(N3CCC4(CC3)OC(=O)c3ccccc34)[nH]c2cc1C 10.1016/j.bmcl.2008.08.018
CHEMBL519651 191678 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 347 1 1 4 3.8 Cc1cc2nc(N3CCC4(CC3)OC(=O)c3ccccc34)[nH]c2cc1C 10.1016/j.bmcl.2008.08.018
10223395 187722 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 412 4 1 4 3.7 CS(=O)(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
CHEMBL495369 187722 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 412 4 1 4 3.7 CS(=O)(=O)c1cccc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1016/j.bmcl.2009.01.101
44580222 184172 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 363 1 1 6 3.0 O=C1OC2(CCN(c3nc4cc5c(cc4[nH]3)OCO5)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL483040 184172 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 363 1 1 6 3.0 O=C1OC2(CCN(c3nc4cc5c(cc4[nH]3)OCO5)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
71519164 86169 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 378 5 1 4 4.8 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312072 86169 0 None - 0 Mouse 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 378 5 1 4 4.8 CCS(=O)(=O)c1ccc2[nH]c(Oc3cccc(-c4ccccc4)c3)nc2c1 10.1016/j.bmcl.2012.11.005
9983624 13941 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 468 4 1 5 4.9 Cn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5ccccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL1196584 13941 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 468 4 1 5 4.9 Cn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5ccccc54)CC3)ccc21 10.1021/jm049599u
CHEMBL557540 13941 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cellsInhibition of [125I]PYY binding to the rat NPY Y5 receptor in C6 cells
ChEMBL 468 4 1 5 4.9 Cn1c2ccccc2c2cc(NC(=O)CN3CCC(N4C(=O)OCc5ccccc54)CC3)ccc21 10.1021/jm049599u
44573615 187233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nccc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
CHEMBL492567 187233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity to human neuropeptide Y5 receptorBinding affinity to human neuropeptide Y5 receptor
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nccc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmc.2009.05.064
44573615 187233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nccc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
CHEMBL492567 187233 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant Y5 receptor expressed in mouse LMtk cells
ChEMBL 463 3 1 5 3.5 CS(=O)(=O)N1CC2(CCN(C(=O)Nc3nccc(-c4ccccc4)n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.02.035
9888989 203824 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 431 9 1 4 5.2 COc1ccc2c(c1)CCC(NCCc1ccc(OC)c(OC)c1)C2Cc1ccccc1 10.1021/jm990468g
CHEMBL68467 203824 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.Inhibition of [125I]-PYY binding to recombinant NPY Y5 receptor on HEK293 cell membranes.
ChEMBL 431 9 1 4 5.2 COc1ccc2c(c1)CCC(NCCc1ccc(OC)c(OC)c1)C2Cc1ccccc1 10.1021/jm990468g
22257112 102902 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 495 6 2 5 3.8 COc1ccc2c(c1)CCC1N=C(NC(=O)[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4)CC3)CC21 10.1016/s0960-894x(99)00676-9
CHEMBL305987 102902 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity for human Neuropeptide Y receptor type 5 in HEK293 cellsBinding affinity for human Neuropeptide Y receptor type 5 in HEK293 cells
ChEMBL 495 6 2 5 3.8 COc1ccc2c(c1)CCC1N=C(NC(=O)[C@H]3CC[C@H](CNS(=O)(=O)c4ccccc4)CC3)CC21 10.1016/s0960-894x(99)00676-9
44580505 187809 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.7 O=C1O[C@]2(CC[C@H](c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
CHEMBL495930 187809 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human NPY Y5 receptor transfected in mouse LMtk cellsBinding affinity to human NPY Y5 receptor transfected in mouse LMtk cells
ChEMBL 319 1 1 4 3.7 O=C1O[C@]2(CC[C@H](c3nc4cccnc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.018
44579794 187045 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 318 1 1 3 4.3 O=C1O[C@]2(CC[C@H](c3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
CHEMBL491020 187045 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cellsDisplacement of [125I]PYY from human recombinant NPYY5 receptor expressed in mouse LMtk cells
ChEMBL 318 1 1 3 4.3 O=C1O[C@]2(CC[C@H](c3nc4ccccc4[nH]3)CC2)c2ccccc21 10.1016/j.bmcl.2008.08.021
10758195 78519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 3 1 4 3.9 COc1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
CHEMBL2111927 78519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 322 3 1 4 3.9 COc1c(-c2ccccc2)[nH]c2c(N3CCCCC3)nc(C)nc12 10.1021/jm000269t
44370202 120074 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 522 6 3 6 4.0 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3cccnc23)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
CHEMBL350684 120074 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Human Neuropeptide Y5 receptor binding affinityHuman Neuropeptide Y5 receptor binding affinity
ChEMBL 522 6 3 6 4.0 O=C(NNC(=O)[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3cccnc23)CC1)c1cc2ccccc2s1 10.1016/j.bmcl.2003.11.070
9967784 188856 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 340 3 1 3 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccsc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
CHEMBL506812 188856 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase-deficient mouse LM cells
ChEMBL 340 3 1 3 4.3 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3ccsc3)=N2)cc1 10.1016/j.bmcl.2009.01.101
9819988 28592 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 354 3 1 3 5.2 c1ccc(-c2cc3nc(-c4ccccc4)[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
CHEMBL137669 28592 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Affinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assayAffinity for human neuropeptide Y receptor Y5, binding was evaluated in an in vitro radioligand [125I]PYY binding assay
ChEMBL 354 3 1 3 5.2 c1ccc(-c2cc3nc(-c4ccccc4)[nH]c(N4CCCCC4)c-3n2)cc1 10.1021/jm000269t
10970790 205066 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 6 1 3 5.2 C[C@H](C(=O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL77255 205066 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 374 6 1 3 5.2 C[C@H](C(=O)c1ccccc1)N(C)C(=O)Nc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
11111618 205470 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 377 6 1 4 5.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Oc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
CHEMBL80465 205470 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory activity tested against Human Neuropeptide Y5 Receptor.Inhibitory activity tested against Human Neuropeptide Y5 Receptor.
ChEMBL 377 6 1 4 5.0 C[C@H]([C@@H](O)c1ccccc1)N(C)C(=O)Oc1ccc(Oc2ccccc2)cc1 10.1021/jm0004547
71519167 86173 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)cn3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312076 86173 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 379 5 1 5 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(-c4ccccc4)cn3)nc2c1 10.1016/j.bmcl.2012.11.005
71519002 86166 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(C(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
CHEMBL2312069 86166 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]PYY from mouse NPY-Y5 receptorDisplacement of [125I]PYY from mouse NPY-Y5 receptor
ChEMBL 370 4 1 4 4.2 CCS(=O)(=O)c1ccc2[nH]c(Oc3ccc(C(F)(F)F)cc3)nc2c1 10.1016/j.bmcl.2012.11.005
44461106 205575 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 437 4 1 5 4.8 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(Cl)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
CHEMBL81337 205575 0 None - 0 Human 7.0 pIC50 = 7 Binding
In vitro binding affinity against human neuropeptide Y5 receptorIn vitro binding affinity against human neuropeptide Y5 receptor
ChEMBL 437 4 1 5 4.8 CC(C)C(=O)N1CCC(CNc2nc3c(s2)CCOc2cc(Cl)c(F)cc2-3)CC1 10.1016/j.bmcl.2004.03.014
23442587 67177 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2ccc(F)cc2)s1 10.1016/j.bmcl.2005.05.009
CHEMBL187729 67177 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Inhibitory concentration against mouse NPY5 receptor at 1 umInhibitory concentration against mouse NPY5 receptor at 1 um
ChEMBL 433 9 2 6 3.6 Cc1ccccc1C(=O)c1cnc(NCCCNS(=O)(=O)c2ccc(F)cc2)s1 10.1016/j.bmcl.2005.05.009
44302732 202736 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 363 6 1 3 4.9 CC(C)Cn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL61880 202736 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 363 6 1 3 4.9 CC(C)Cn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
56683704 65370 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 457 7 2 5 2.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL1829320 65370 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 457 7 2 5 2.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
57345521 73312 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013020 73312 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL4284905 213450 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4284905 213450 0 None -1 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
10273848 155369 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 423 4 1 3 3.5 CN(C(=O)Nc1ccc(-c2cc(F)cc(F)c2)cc1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL403414 155369 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 423 4 1 3 3.5 CN(C(=O)Nc1ccc(-c2cc(F)cc(F)c2)cc1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
56841989 213420 6 None -2 7 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -2 7 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
57345520 73304 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 427 7 2 4 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013012 73304 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 427 7 2 4 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
56841989 213420 6 None -2 7 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281479 213420 6 None -2 7 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
56666778 65373 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 459 7 2 5 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829323 65373 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 459 7 2 5 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL4277590 213373 0 None -1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 213464 0 None -63 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
CHEMBL4277590 213373 0 None -1 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4286615 213464 0 None -63 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
70685339 73483 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 434 3 1 5 4.5 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016732 73483 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 434 3 1 5 4.5 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2012.02.098
10203845 155584 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 443 5 1 3 3.4 CCS(=O)(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL404461 155584 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 443 5 1 3 3.4 CCS(=O)(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
70681111 73449 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 435 3 1 6 3.9 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016682 73449 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 435 3 1 6 3.9 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
56683705 65372 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 473 7 2 5 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829322 65372 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 473 7 2 5 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
44139479 192701 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@@H]1NC(c2cccc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL521947 192701 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@@H]1NC(c2cccc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
56666779 65376 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 441 7 2 4 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL1829326 65376 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 441 7 2 4 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
22458813 200220 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 351 5 1 4 3.5 CCn1c2ccccc2c2cc(NC(=O)CCN3CCOCC3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL59680 200220 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 351 5 1 4 3.5 CCn1c2ccccc2c2cc(NC(=O)CCN3CCOCC3)ccc21 10.1016/s0960-894x(03)00329-9
57404430 73491 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 429 3 1 6 4.0 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016740 73491 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 429 3 1 6 4.0 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
56666779 65376 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 4 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829326 65376 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 4 3.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
56666777 65371 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 443 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL1829321 65371 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 443 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
70687454 73302 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 459 7 2 6 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2c(=O)sc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013010 73302 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 459 7 2 6 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2c(=O)sc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
70683225 73314 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013022 73314 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cccc(Cl)c32)CC1 10.1016/j.bmcl.2012.01.117
70681101 73317 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 427 7 2 4 2.9 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(F)c(F)cc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013025 73317 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 427 7 2 4 2.9 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(F)c(F)cc32)CC1 10.1016/j.bmcl.2012.01.117
57404430 73490 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 429 3 1 6 4.0 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016739 73490 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 429 3 1 6 4.0 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@]2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
56683704 65370 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 457 7 2 5 2.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829320 65370 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 457 7 2 5 2.1 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
44138706 186977 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2ccnc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL490561 186977 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2ccnc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
44139234 193168 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL523134 193168 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
70685315 73313 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013021 73313 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2012.01.117
44139732 12698 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 387 4 1 6 3.2 COc1ccc([C@]2(c3ccc(F)cc3)N=C(c3cc(C#N)ccn3)N[C@H]2C)cn1 10.1021/jm900110t
CHEMBL1187514 12698 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 387 4 1 6 3.2 COc1ccc([C@]2(c3ccc(F)cc3)N=C(c3cc(C#N)ccn3)N[C@H]2C)cn1 10.1021/jm900110t
CHEMBL506163 12698 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 387 4 1 6 3.2 COc1ccc([C@]2(c3ccc(F)cc3)N=C(c3cc(C#N)ccn3)N[C@H]2C)cn1 10.1021/jm900110t
70693715 73308 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 455 7 2 4 3.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CC(C)(C)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013016 73308 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 455 7 2 4 3.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CC(C)(C)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
10298415 166792 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 462 4 1 4 3.0 CN(C(=O)NC1CCN(c2cc(Cl)cc(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL428423 166792 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 462 4 1 4 3.0 CN(C(=O)NC1CCN(c2cc(Cl)cc(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
9930778 55148 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to the human Neuropeptide Y receptor type 5 was determined using [125I]- [PYY] as radioligandBinding affinity to the human Neuropeptide Y receptor type 5 was determined using [125I]- [PYY] as radioligand
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1021/jm025584p
CHEMBL161724 55148 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Binding affinity to the human Neuropeptide Y receptor type 5 was determined using [125I]- [PYY] as radioligandBinding affinity to the human Neuropeptide Y receptor type 5 was determined using [125I]- [PYY] as radioligand
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1021/jm025584p
9930778 55148 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1016/j.bmcl.2012.02.098
CHEMBL161724 55148 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1016/j.bmcl.2012.02.098
70685316 73316 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 4 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccc(F)cc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013024 73316 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 4 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccc(F)cc32)CC1 10.1016/j.bmcl.2012.01.117
10159722 95085 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 429 4 1 3 3.1 CN(C(=O)N[C@H]1CC[C@H](c2cc(F)cc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255353 95085 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 429 4 1 3 3.1 CN(C(=O)N[C@H]1CC[C@H](c2cc(F)cc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL4278700 213390 0 None -12 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
42630820 187078 10 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human NPYY5 receptorBinding affinity to human NPYY5 receptor
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL491288 187078 10 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human NPYY5 receptorBinding affinity to human NPYY5 receptor
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL4278700 213390 0 None -12 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
42630820 187078 10 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL491288 187078 10 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
54141274 66617 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 475 7 3 6 4.6 Nc1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC2)nc2ccccc12 10.1016/j.bmcl.2011.06.124
CHEMBL1836102 66617 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 475 7 3 6 4.6 Nc1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC2)nc2ccccc12 10.1016/j.bmcl.2011.06.124
CHEMBL1852685 66617 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 475 7 3 6 4.6 Nc1nc(NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC2)nc2ccccc12 10.1016/j.bmcl.2011.06.124
44138709 186890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cccc(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL489726 186890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cccc(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
44138709 186890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cccc(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL489726 186890 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cccc(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
10041217 101032 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 312 2 1 3 4.7 CCn1c2ccccc2c2cc(-c3nc4ccc[nH]c-4n3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL294560 101032 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 312 2 1 3 4.7 CCn1c2ccccc2c2cc(-c3nc4ccc[nH]c-4n3)ccc21 10.1016/s0960-894x(03)00329-9
70693714 73307 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 429 7 2 4 2.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3c2ccc(F)c3F)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013015 73307 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 429 7 2 4 2.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3c2ccc(F)c3F)CC1 10.1016/j.bmcl.2012.01.117
70693717 73310 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 391 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013018 73310 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 391 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
10272799 155459 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 407 4 1 2 4.0 CCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL403918 155459 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 407 4 1 2 4.0 CCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL4279973 213401 0 None -10 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10062681 111216 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL326483 111216 1 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL4279973 213401 0 None -10 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
11491176 200043 38 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmcl.2012.02.098
CHEMBL595573 200043 38 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 406 3 1 6 3.6 O=C1O[C@]2(CC[C@H](C(=O)Nc3ccn(-c4ccccc4F)n3)CC2)c2cnccc21 10.1016/j.bmcl.2012.02.098
44139478 186941 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL490123 186941 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
9930778 55148 0 None -1 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity to the rat Neuropeptide Y receptor type 5 was determined using [125I]- [Leu31,Pro34]PYY as radioligandBinding affinity to the rat Neuropeptide Y receptor type 5 was determined using [125I]- [Leu31,Pro34]PYY as radioligand
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1021/jm025584p
CHEMBL161724 55148 0 None -1 2 Rat 8.8 pKi = 8.8 Binding
Binding affinity to the rat Neuropeptide Y receptor type 5 was determined using [125I]- [Leu31,Pro34]PYY as radioligandBinding affinity to the rat Neuropeptide Y receptor type 5 was determined using [125I]- [Leu31,Pro34]PYY as radioligand
ChEMBL 362 6 1 5 4.2 CC(C)(C)OCCOc1ccc(-c2nc(-c3cccc(C#N)c3)c[nH]2)cn1 10.1021/jm025584p
70691635 73311 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013019 73311 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 425 7 2 4 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3c(Cl)cccc32)CC1 10.1016/j.bmcl.2012.01.117
20647089 67821 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 397 12 2 6 3.0 CCN(CC)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909727 67821 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 397 12 2 6 3.0 CCN(CC)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
56663345 65374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 491 7 2 6 1.9 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCS(=O)(=O)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829324 65374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 491 7 2 6 1.9 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCS(=O)(=O)c3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
44138708 12631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 1 4 4.1 C[C@@H]1NC(c2cc(Cl)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL1187117 12631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 1 4 4.1 C[C@@H]1NC(c2cc(Cl)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL490903 12631 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 1 4 4.1 C[C@@H]1NC(c2cc(Cl)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
70693716 73309 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 407 8 2 4 2.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CCN2CCc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013017 73309 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 407 8 2 4 2.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CCN2CCc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
10293988 95644 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 3 1 2 3.6 CC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257940 95644 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 3 1 2 3.6 CC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
20647101 68005 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 446 11 2 7 4.1 COc1ccc(C)cc1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912082 68005 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 446 11 2 7 4.1 COc1ccc(C)cc1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
44138579 12632 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 350 3 1 4 3.4 C[C@@H]1NC(c2cnccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL1187124 12632 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 350 3 1 4 3.4 C[C@@H]1NC(c2cnccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL491119 12632 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 350 3 1 4 3.4 C[C@@H]1NC(c2cnccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
10017062 202743 1 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 289 2 1 2 4.8 CCn1c2ccccc2c2cc(-c3nc(C)c(C)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL61934 202743 1 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 289 2 1 2 4.8 CCn1c2ccccc2c2cc(-c3nc(C)c(C)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL4276961 213368 0 None -1000 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.8b01046
70689521 73486 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 420 3 1 4 4.8 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OCc1ccccc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016735 73486 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 420 3 1 4 4.8 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)OCc1ccccc12 10.1016/j.bmcl.2012.02.098
76321859 105720 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 428 5 1 3 4.3 CCN1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
CHEMBL3126050 105720 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 428 5 1 3 4.3 CCN1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
70693713 73303 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 6 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2c(=O)oc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013011 73303 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 6 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2c(=O)oc3ccccc32)CC1 10.1016/j.bmcl.2012.01.117
10970274 120075 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 354 3 2 3 4.0 O=C(Nc1cc(-c2ccncc2)[nH]n1)C1Cc2ccc3ccccc3c2C1 10.1021/jm025513q
CHEMBL350690 120075 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 354 3 2 3 4.0 O=C(Nc1cc(-c2ccncc2)[nH]n1)C1Cc2ccc3ccccc3c2C1 10.1021/jm025513q
21336489 79496 0 None 1737 2 Human 8.0 pKi = 8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 441 8 3 4 3.7 Nc1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL2113711 79496 0 None 1737 2 Human 8.0 pKi = 8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 441 8 3 4 3.7 Nc1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
21336507 189692 0 None 1288 2 Human 8.0 pKi = 8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
CHEMBL51542 189692 0 None 1288 2 Human 8.0 pKi = 8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
CHEMBL4285633 213457 0 None -39 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287469 213470 0 None -1 3 Human 7.0 pKi = 7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](CC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C)CC(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4288294 213478 0 None -15 4 Human 7.0 pKi = 7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277697 213376 0 None -25 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281120 213414 0 None -3 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290488 213496 0 None -1 4 Human 6.0 pKi = 6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
164626032 186534 0 None -1000 2 Human 5.0 pKi = 5 Binding
Displacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysis
ChEMBL 976 33 19 13 -3.4 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)NC(=O)NCCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
CHEMBL4877802 186534 0 None -1000 2 Human 5.0 pKi = 5 Binding
Displacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysis
ChEMBL 976 33 19 13 -3.4 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)NC(=O)NCCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c01574
10020909 101852 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 352 3 1 3 5.6 CCn1c2ccccc2c2cc(-c3nc(C)c(-c4ccccn4)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL300543 101852 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 352 3 1 3 5.6 CCn1c2ccccc2c2cc(-c3nc(C)c(-c4ccccn4)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
44294762 101526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 496 8 3 5 4.7 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2[N+](=O)[O-])CC1)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
CHEMBL298168 101526 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 496 8 3 5 4.7 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccccc2[N+](=O)[O-])CC1)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
20647087 67990 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 394 9 2 6 3.2 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C(F)(F)F 10.1016/j.bmcl.2011.08.072
CHEMBL1912067 67990 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 394 9 2 6 3.2 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C(F)(F)F 10.1016/j.bmcl.2011.08.072
22458796 100740 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 335 5 1 3 4.2 CCn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL292729 100740 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 335 5 1 3 4.2 CCn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
70687474 73494 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 456 4 1 5 5.1 CCN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
CHEMBL2016743 73494 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 456 4 1 5 5.1 CCN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
136000676 62788 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 2 4 2.9 C[C@@H]1NC(c2c[nH]c(=O)c(F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1784123 62788 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 2 4 2.9 C[C@@H]1NC(c2c[nH]c(=O)c(F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
21336511 191147 0 None 323 2 Human 8.0 pKi = 8.0 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL51884 191147 0 None 323 2 Human 8.0 pKi = 8.0 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
57392816 68001 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 10 2 6 4.0 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CCCCC1 10.1016/j.bmcl.2011.08.072
CHEMBL1912078 68001 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 10 2 6 4.0 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CCCCC1 10.1016/j.bmcl.2011.08.072
56683706 65378 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 431 8 2 5 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(F)c(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829328 65378 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 431 8 2 5 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(F)c(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
57403258 68007 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 406 10 2 8 2.5 Cn1cnc(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)c1 10.1016/j.bmcl.2011.08.072
CHEMBL1912084 68007 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 406 10 2 8 2.5 Cn1cnc(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)c1 10.1016/j.bmcl.2011.08.072
CHEMBL2110365 209213 4 None -426 4 Human 6.9 pKi = 6.9 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
44345744 113965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 339 2 1 2 5.6 Clc1ccc(-c2c[nH]c(-c3nccc4ccccc34)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL332598 113965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 339 2 1 2 5.6 Clc1ccc(-c2c[nH]c(-c3nccc4ccccc34)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL2440183 210474 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Binding affinity to Y5 receptor (unknown origin)Binding affinity to Y5 receptor (unknown origin)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)[C@H]1C(=O)OC)[C@@H](C)O)[C@@H](C)CC 10.1021/jm4008505
46209585 67991 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 368 10 2 6 3.1 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912068 67991 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 368 10 2 6 3.1 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
10247746 102726 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 357 4 1 4 3.8 CCn1c(=O)c2ccc(NC(=O)Cc3ccncc3)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL304896 102726 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 357 4 1 4 3.8 CCn1c(=O)c2ccc(NC(=O)Cc3ccncc3)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
46912327 105719 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 428 4 1 3 4.3 CN1CCCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
CHEMBL3126049 105719 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 428 4 1 3 4.3 CN1CCCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
10435289 170983 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 480 8 2 5 4.5 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3c(c2)OCCO3)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
CHEMBL445613 170983 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 480 8 2 5 4.5 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3c(c2)OCCO3)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
70689510 73320 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 391 7 3 3 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013028 73320 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 391 7 3 3 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cc2c[nH]c3ccccc23)CC1 10.1016/j.bmcl.2012.01.117
11078256 52312 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2cccc(Cl)c2)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
CHEMBL158940 52312 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2cccc(Cl)c2)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
44294942 186527 0 None 58 2 Human 6.9 pKi = 6.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 446 11 2 3 5.6 O=S(=O)(NCCCCCCNCc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
CHEMBL48777 186527 0 None 58 2 Human 6.9 pKi = 6.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 446 11 2 3 5.6 O=S(=O)(NCCCCCCNCc1ccc2ccccc2c1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
CHEMBL4280392 213406 0 None -100 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
44350924 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
91929378 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL439122 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4280898 213410 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None -645 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4289416 213486 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291705 213510 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NC)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10045322 62517 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 1 5 2.7 C[C@@H]1NC(c2ccc(=O)n(C)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1782077 62517 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 1 5 2.7 C[C@@H]1NC(c2ccc(=O)n(C)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
10202875 95084 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 428 4 1 4 2.4 CN(C(=O)NC1CCN(c2cccc(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255352 95084 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 428 4 1 4 2.4 CN(C(=O)NC1CCN(c2cccc(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL4280392 213406 0 None -100 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
20610118 155404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 428 4 1 4 2.4 CN(C(=O)NC1CCN(c2ccc(Cl)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL403622 155404 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 428 4 1 4 2.4 CN(C(=O)NC1CCN(c2ccc(Cl)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
44350924 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
91929378 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL439122 168988 0 None -234 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL 2220 73 32 30 -7.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)[C@@H](C)CC 10.1021/acs.jmedchem.8b01046
CHEMBL4280898 213410 0 None -2 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283257 213437 0 None -645 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4289416 213486 0 None -8 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291705 213510 0 None -1 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NC)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
2226619 202735 10 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 306 2 1 2 4.3 CCn1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL61879 202735 10 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 306 2 1 2 4.3 CCn1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
44345803 117300 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 235 2 1 2 3.4 Cc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL339652 117300 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 235 2 1 2 3.4 Cc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
56673734 65381 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 429 8 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829331 65381 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 429 8 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
9886706 178642 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 390 1 1 4 5.3 O=C1CC2(CCC2)CC(O)=C1C1C2=C(CC3(CCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL467558 178642 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 390 1 1 4 5.3 O=C1CC2(CCC2)CC(O)=C1C1C2=C(CC3(CCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
1202745 189002 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL508770 189002 2 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
9806472 161991 0 None 257 2 Human 7.9 pKi = 7.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
CHEMBL415926 161991 0 None 257 2 Human 7.9 pKi = 7.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00287-1
21336493 189207 0 None 1698 2 Human 7.9 pKi = 7.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccc3ccccc3n2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL51138 189207 0 None 1698 2 Human 7.9 pKi = 7.9 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccc3ccccc3n2)CC1 10.1016/s0960-894x(02)00287-1
127031281 139206 0 None -104 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1789 59 29 21 -2.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN/C(N)=N/C(=O)NCCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3785569 139206 0 None -104 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1789 59 29 21 -2.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN/C(N)=N/C(=O)NCCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787712 139206 0 None -104 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1789 59 29 21 -2.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN/C(N)=N/C(=O)NCCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
12250898 110542 1 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3ccccn3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL325171 110542 1 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3ccccn3)n2)cc1 10.1016/s0960-894x(03)00747-9
44138575 187036 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 373 3 2 5 2.5 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1021/jm900110t
CHEMBL490901 187036 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 373 3 2 5 2.5 C[C@@H]1NC(c2cc(C#N)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(=O)[nH]c1 10.1021/jm900110t
44345940 15583 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 281 4 1 4 3.2 COc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1OC 10.1016/s0960-894x(03)00747-9
CHEMBL122120 15583 1 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 281 4 1 4 3.2 COc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1OC 10.1016/s0960-894x(03)00747-9
9858246 101077 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 320 2 1 2 4.9 CC(C)n1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL294842 101077 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 320 2 1 2 4.9 CC(C)n1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
10450609 102281 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 351 3 1 2 6.2 CCn1c2ccccc2c2cc(-c3nc(C)c(-c4ccccc4)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL303325 102281 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 351 3 1 2 6.2 CCn1c2ccccc2c2cc(-c3nc(C)c(-c4ccccc4)[nH]3)ccc21 10.1016/s0960-894x(03)00329-9
10245014 162793 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 312 2 1 3 4.7 CCn1c2ccccc2c2cc(-c3nc4cc[nH]cc-4n3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL417225 162793 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 312 2 1 3 4.7 CCn1c2ccccc2c2cc(-c3nc4cc[nH]cc-4n3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL4279794 213399 0 None -63 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287140 213468 0 None -10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
20647122 67988 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 354 10 2 6 2.7 CCS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912065 67988 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 354 10 2 6 2.7 CCS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
57399737 67998 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 374 9 2 7 3.0 Cc1nc(C)c(-c2csc(NCCCCCNS(C)(=O)=O)n2)s1 10.1016/j.bmcl.2011.08.072
CHEMBL1912075 67998 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 374 9 2 7 3.0 Cc1nc(C)c(-c2csc(NCCCCCNS(C)(=O)=O)n2)s1 10.1016/j.bmcl.2011.08.072
155524657 170989 0 None -2754 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4456247 170989 0 None -2754 4 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](N)CCCC[C@@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
44294740 101549 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 470 11 3 5 4.4 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
CHEMBL298342 101549 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 470 11 3 5 4.4 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
12250900 111318 1 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3ccncc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL326736 111318 1 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3ccncc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL4283846 213443 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CO)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
57391020 68008 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 434 10 2 8 3.1 Cc1nn(C)c(C)c1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912085 68008 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 434 10 2 8 3.1 Cc1nn(C)c(C)c1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
10384590 200492 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 371 4 1 4 4.3 CC(C)n1c(=O)c2ccc(NC(=O)Cc3ccncc3)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL59866 200492 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 371 4 1 4 4.3 CC(C)n1c(=O)c2ccc(NC(=O)Cc3ccncc3)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
10332613 114441 3 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL333310 114441 3 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL4279794 213399 0 None -63 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287140 213468 0 None -10 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
70695681 78355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 383 7 3 3 3.9 O=C(O)CCc1cccc(CC(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)c1 10.1021/jm025513q
CHEMBL2110162 78355 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 383 7 3 3 3.9 O=C(O)CCc1cccc(CC(=O)Nc2cc(-c3ccc(Cl)cc3)n[nH]2)c1 10.1021/jm025513q
CHEMBL4283846 213443 0 None -3 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CO)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10160875 95396 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 446 4 1 4 2.5 CN(C(=O)NC1CCN(c2ccc(F)c(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL256885 95396 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 446 4 1 4 2.5 CN(C(=O)NC1CCN(c2ccc(F)c(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
20610116 98023 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 436 5 1 5 1.9 CC(=O)c1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
CHEMBL272964 98023 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 436 5 1 5 1.9 CC(=O)c1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
CHEMBL2440192 210481 0 None -32 3 Human 7.8 pKi = 7.8 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](N)Cc1ccc(O)cc1 10.1021/jm4008505
24950710 178815 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 418 1 1 4 6.1 O=C1CC2(CCCC2)CC(O)=C1C1C2=C(CC3(CCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL469173 178815 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 418 1 1 4 6.1 O=C1CC2(CCCC2)CC(O)=C1C1C2=C(CC3(CCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL4540843 213993 19 None -18 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysis
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
21336500 101674 0 None 190 2 Human 7.8 pKi = 7.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 500 10 3 4 4.8 O=S(=O)(NC[C@H]1CC[C@H](CNC(CO)Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL299295 101674 0 None 190 2 Human 7.8 pKi = 7.8 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 500 10 3 4 4.8 O=S(=O)(NC[C@H]1CC[C@H](CNC(CO)Cc2ccc(Cl)cc2)CC1)c1cccc2ccccc12 10.1016/s0960-894x(02)00287-1
CHEMBL4540843 213993 19 None -18 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysisDisplacement of [3H]propionyl-pNPY from human neuropeptide Y Y5 receptor in human HEC-1B cells measured after 90 mins by scintillation counting analysis
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)N)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.1c01574
57394524 67824 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 424 10 2 7 1.9 CN1CCN(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
CHEMBL1909730 67824 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 424 10 2 7 1.9 CN1CCN(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
57392815 67993 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 345 9 2 6 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2cccs2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912070 67993 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 345 9 2 6 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2cccs2)cs1 10.1016/j.bmcl.2011.08.072
56663346 65377 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 413 8 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3ccc(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829327 65377 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 413 8 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3ccc(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
57399726 67813 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 383 10 2 7 2.8 Cc1nccnc1-c1csc(NCCCCCNS(=O)(=O)C(C)C)n1 10.1016/j.bmcl.2011.08.072
CHEMBL1909719 67813 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 383 10 2 7 2.8 Cc1nccnc1-c1csc(NCCCCCNS(=O)(=O)C(C)C)n1 10.1016/j.bmcl.2011.08.072
70685340 73489 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 449 3 1 6 4.0 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)Cc1cnccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
CHEMBL2016738 73489 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 449 3 1 6 4.0 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)Cc1cnccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
20647107 68009 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 421 10 2 8 3.4 Cc1noc(C)c1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912086 68009 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 421 10 2 8 3.4 Cc1noc(C)c1S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
44345818 13729 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 269 2 1 2 4.1 Cc1[nH]c(-c2cccnc2)nc1-c1cccc(Cl)c1 10.1016/s0960-894x(03)00747-9
CHEMBL119507 13729 1 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 269 2 1 2 4.1 Cc1[nH]c(-c2cccnc2)nc1-c1cccc(Cl)c1 10.1016/s0960-894x(03)00747-9
56683702 65364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 481 7 2 5 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829314 65364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 481 7 2 5 3.3 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
56677038 65361 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 453 6 2 5 2.5 CC1(C)CC(=O)N(CC(=O)N[C@H]2CC[C@H](CNS(C)(=O)=O)CC2)c2ccccc2S1 10.1016/j.bmcl.2011.06.078
CHEMBL1829311 65361 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 453 6 2 5 2.5 CC1(C)CC(=O)N(CC(=O)N[C@H]2CC[C@H](CNS(C)(=O)=O)CC2)c2ccccc2S1 10.1016/j.bmcl.2011.06.078
12260207 178722 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 338 1 1 4 4.2 CC1CC(=O)C(C2C3=C(CC(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL468414 178722 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 338 1 1 4 4.2 CC1CC(=O)C(C2C3=C(CC(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
11475091 178554 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3ccc(Cl)cc32)=C(O)C1 10.1021/jm8003587
CHEMBL466946 178554 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3ccc(Cl)cc32)=C(O)C1 10.1021/jm8003587
44295007 101747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 633 12 3 5 4.9 Cc1ccc(S(=O)(=O)NC(Cc2ccccc2)C(=O)NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/s0960-894x(02)00288-3
CHEMBL299742 101747 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 633 12 3 5 4.9 Cc1ccc(S(=O)(=O)NC(Cc2ccccc2)C(=O)NC[C@H]2CC[C@H](CNS(=O)(=O)c3ccc4ccccc4c3)CC2)cc1 10.1016/s0960-894x(02)00288-3
CHEMBL4289021 213483 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290615 213497 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282168 213429 0 None -630 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
57399727 67816 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 425 9 2 6 4.4 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.08.072
CHEMBL1909722 67816 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 425 9 2 6 4.4 CC(C)S(=O)(=O)NCCCCCNc1nc2c(s1)CCSc1ccccc1-2 10.1016/j.bmcl.2011.08.072
46913706 105711 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 413 4 1 3 4.5 O=C1CCCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126041 105711 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 413 4 1 3 4.5 O=C1CCCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
9946965 193072 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 360 3 1 4 3.5 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1021/jm900110t
CHEMBL522456 193072 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 360 3 1 4 3.5 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)CN2)c1 10.1021/jm900110t
44139602 193275 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 357 3 1 6 2.9 C[C@@H]1NC(c2cnsn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL523945 193275 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 357 3 1 6 2.9 C[C@@H]1NC(c2cnsn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
70687457 73321 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 405 7 2 4 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cc2cn(C)c3ccccc23)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013029 73321 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 405 7 2 4 2.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cc2cn(C)c3ccccc23)CC1 10.1016/j.bmcl.2012.01.117
10112931 95050 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 421 5 1 2 4.4 CCCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255147 95050 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 421 5 1 2 4.4 CCCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
1504 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
1518 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
1521 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
24868177 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
44288922 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
77068007 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
90479759 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
CHEMBL438945 2807 8 None -9 10 Human 8.7 pKi = 8.7 Binding
Displacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometryDisplacement of Cy5-pNPY from human Y5 receptor expressed in human HEC-1B cells after 90 to 120 mins by flow cytometry
ChEMBL None None None None 10.1021/jm4008505
44139601 193249 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 351 3 1 5 2.8 C[C@@H]1NC(c2cnccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL523776 193249 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 351 3 1 5 2.8 C[C@@H]1NC(c2cnccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
70687455 73315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 4 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(F)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013023 73315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 409 7 2 4 2.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(F)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL429531 213537 15 None -27 4 Human 8.7 pKi = 8.7 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O 10.1021/jm010031k
70683239 73488 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 448 3 1 5 4.6 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
CHEMBL2016737 73488 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 448 3 1 5 4.6 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
9887225 187148 3 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1021/jm900110t
CHEMBL491930 187148 3 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 400 2 1 5 3.8 O=C1OC2(CCN(C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)c2ccccc21 10.1021/jm900110t
10112931 95050 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 421 5 1 2 4.4 CCCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255147 95050 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 421 5 1 2 4.4 CCCC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
44139599 187037 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 380 4 1 5 3.4 COc1ccnc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c1 10.1021/jm900110t
CHEMBL490902 187037 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 380 4 1 5 3.4 COc1ccnc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c1 10.1021/jm900110t
44138581 187142 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 427 4 1 5 3.4 C[C@@H]1NC(c2cccc(S(C)(=O)=O)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL491894 187142 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 427 4 1 5 3.4 C[C@@H]1NC(c2cccc(S(C)(=O)=O)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
10155282 198884 1 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 357 6 2 3 4.5 CCn1c2ccccc2c2cc(NC(=O)CNCc3ccccc3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL58424 198884 1 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 357 6 2 3 4.5 CCn1c2ccccc2c2cc(NC(=O)CNCc3ccccc3)ccc21 10.1016/s0960-894x(03)00329-9
54580489 62705 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1ccc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)[nH]c1=O 10.1016/j.bmc.2009.05.069
CHEMBL1783923 62705 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1ccc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)[nH]c1=O 10.1016/j.bmc.2009.05.069
44138577 193125 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 4 1 4 4.3 CC[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL522793 193125 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 388 4 1 4 4.3 CC[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
10202456 95428 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 422 4 1 3 3.2 CC(C)C(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257022 95428 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 422 4 1 3 3.2 CC(C)C(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
10047509 62795 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 416 4 1 5 3.6 C[C@@H]1NC(c2ccc(=O)n(C(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1784130 62795 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 416 4 1 5 3.6 C[C@@H]1NC(c2ccc(=O)n(C(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
10046270 62796 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 396 4 1 6 2.3 COn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784131 62796 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 396 4 1 6 2.3 COn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
10275303 95577 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 444 5 1 4 2.4 CCS(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257707 95577 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 444 5 1 4 2.4 CCS(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
11729353 52280 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 413 5 2 4 4.6 COc1ccc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)cc1OC 10.1021/jm025513q
CHEMBL158913 52280 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 413 5 2 4 4.6 COc1ccc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)cc1OC 10.1021/jm025513q
10363209 62792 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 394 4 1 5 3.2 CCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784127 62792 1 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 394 4 1 5 3.2 CCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL439904 213854 13 None -50 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from NPY5 receptor expressed in human HEK293 cellsDisplacement of [125I]PYY from NPY5 receptor expressed in human HEK293 cells
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
44577739 189391 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 422 5 1 4 6.6 CCC1(CC)CC(=O)C(C2C3=C(CC(CC)(CC)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL512996 189391 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 422 5 1 4 6.6 CCC1(CC)CC(=O)C(C2C3=C(CC(CC)(CC)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
10223183 155573 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 4 2.0 Cc1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
CHEMBL404398 155573 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 4 2.0 Cc1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
CHEMBL4289021 213483 0 None -7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290615 213497 0 None -1 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
56659886 65362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 467 7 2 5 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829312 65362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 467 7 2 5 2.9 CCS(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL4282168 213429 0 None -630 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
9922187 100984 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 295 4 1 3 3.3 CCn1c2ccccc2c2cc(NC(=O)CN(C)C)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL294286 100984 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 295 4 1 3 3.3 CCn1c2ccccc2c2cc(NC(=O)CN(C)C)ccc21 10.1016/s0960-894x(03)00329-9
44345949 14549 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
CHEMBL120332 14549 3 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
56677039 65367 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 423 7 2 5 1.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829317 65367 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 423 7 2 5 1.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
44345638 110152 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 305 3 1 3 4.0 FC(F)(F)Oc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL323658 110152 1 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 305 3 1 3 4.0 FC(F)(F)Oc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
56670210 65363 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 479 7 2 5 3.1 CC1(C)CC(=O)N(CC(=O)N[C@H]2CC[C@H](CNS(=O)(=O)C3CC3)CC2)c2ccccc2S1 10.1016/j.bmcl.2011.06.078
CHEMBL1829313 65363 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 479 7 2 5 3.1 CC1(C)CC(=O)N(CC(=O)N[C@H]2CC[C@H](CNS(=O)(=O)C3CC3)CC2)c2ccccc2S1 10.1016/j.bmcl.2011.06.078
85472343 172302 0 None -338 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4475071 172302 0 None -338 4 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1705 55 30 22 -4.0 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
23397122 201755 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 323 4 1 4 2.7 CCn1c(=O)c2cc(NC(=O)CN(C)C)ccc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL60667 201755 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 323 4 1 4 2.7 CCn1c(=O)c2cc(NC(=O)CN(C)C)ccc2c2ccccc21 10.1016/s0960-894x(03)00329-9
24950555 178774 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1cccc2c1OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL468847 178774 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1cccc2c1OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
70685339 73484 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 434 3 1 5 4.5 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016733 73484 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 434 3 1 5 4.5 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@@]2(CC1)OC(=O)c1ccccc12 10.1016/j.bmcl.2012.02.098
127030359 139207 0 None -186 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787528 139207 0 None -186 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787713 139207 0 None -186 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4535525 139207 0 None -186 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1845 61 29 21 -1.5 CCC(=O)NCCCCNC(=O)/N=C(\N)NCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
155561620 175650 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4581256 175650 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
56659887 65366 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 499 7 2 6 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCC(C)(C)S(=O)(=O)c3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829316 65366 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 499 7 2 6 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCC(C)(C)S(=O)(=O)c3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
44345719 113787 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 227 2 1 2 3.5 c1cncc(-c2nc(C3CCCCC3)c[nH]2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL332381 113787 1 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 227 2 1 2 3.5 c1cncc(-c2nc(C3CCCCC3)c[nH]2)c1 10.1016/s0960-894x(03)00747-9
21336486 101348 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 475 10 3 3 5.7 O=C(NCCCCCCNS(=O)(=O)c1cccc2ccccc12)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
CHEMBL296906 101348 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 475 10 3 3 5.7 O=C(NCCCCCCNS(=O)(=O)c1cccc2ccccc12)Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
70695858 73495 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 510 4 1 5 5.6 O=C1O[C@]2(CC[C@@H](N(CC(F)(F)F)C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)Cc2ccccc21 10.1016/j.bmcl.2012.02.098
CHEMBL2016744 73495 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 510 4 1 5 5.6 O=C1O[C@]2(CC[C@@H](N(CC(F)(F)F)C(=O)Nc3cnc(-c4ccccc4)cn3)CC2)Cc2ccccc21 10.1016/j.bmcl.2012.02.098
44283143 161698 0 None -1023 4 Human 5.6 pKi = 5.6 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
91931648 161698 0 None -1023 4 Human 5.6 pKi = 5.6 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
CHEMBL413455 161698 0 None -1023 4 Human 5.6 pKi = 5.6 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2361 75 32 32 -6.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm010031k
24950871 178529 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 446 1 1 4 6.9 O=C1CC2(CCCCC2)CC(O)=C1C1C2=C(CC3(CCCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
CHEMBL466756 178529 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 446 1 1 4 6.9 O=C1CC2(CCCCC2)CC(O)=C1C1C2=C(CC3(CCCCC3)CC2=O)Oc2ccccc21 10.1021/jm8003587
57391019 68003 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 543 12 2 8 4.5 O=C(OCc1ccccc1)N1CCC(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
CHEMBL1912080 68003 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 543 12 2 8 4.5 O=C(OCc1ccccc1)N1CCC(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
CHEMBL4294277 213530 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
9907999 164868 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL422012 164868 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL4294277 213530 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
57396288 67996 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 11 2 6 3.9 O=S(=O)(CC1CCCC1)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912073 67996 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 11 2 6 3.9 O=S(=O)(CC1CCCC1)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL4282216 213430 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CN(C(=N)N)C[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282216 213430 0 None -39 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CN(C(=N)N)C[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
21336503 191069 0 None 549 2 Human 7.6 pKi = 7.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2cccc3ccccc23)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
CHEMBL51874 191069 0 None 549 2 Human 7.6 pKi = 7.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 490 8 2 3 5.7 O=S(=O)(NC[C@H]1CC[C@H](CNCc2cccc3ccccc23)CC1)c1ccccc1C(F)(F)F 10.1016/s0960-894x(02)00287-1
11130476 54932 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 303 3 2 2 3.4 O=C(Nc1cc(-c2ccccc2)[nH]n1)C1Cc2ccccc2C1 10.1021/jm025513q
CHEMBL161398 54932 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 303 3 2 2 3.4 O=C(Nc1cc(-c2ccccc2)[nH]n1)C1Cc2ccccc2C1 10.1021/jm025513q
44345971 14462 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
CHEMBL120117 14462 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
56673731 65359 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 482 7 2 5 2.4 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829309 65359 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 482 7 2 5 2.4 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
10223847 155554 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 419 4 1 5 1.6 CN(C(=O)NC1CCN(c2cccc(C#N)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL404304 155554 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 419 4 1 5 1.6 CN(C(=O)NC1CCN(c2cccc(C#N)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
57398084 68002 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 409 10 3 7 2.5 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CCNCC1 10.1016/j.bmcl.2011.08.072
CHEMBL1912079 68002 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 409 10 3 7 2.5 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CCNCC1 10.1016/j.bmcl.2011.08.072
54584448 62707 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1ccc(=O)[nH]c1C1=N[C@@](c2ccc(F)cc2)(c2ccc(F)nc2)[C@H](C)N1 10.1016/j.bmc.2009.05.069
CHEMBL1783925 62707 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1ccc(=O)[nH]c1C1=N[C@@](c2ccc(F)cc2)(c2ccc(F)nc2)[C@H](C)N1 10.1016/j.bmc.2009.05.069
21336495 102024 0 None 1737 2 Human 7.6 pKi = 7.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccnc3ccccc23)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL301747 102024 0 None 1737 2 Human 7.6 pKi = 7.6 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 468 9 2 6 4.0 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCc2ccnc3ccccc23)CC1 10.1016/s0960-894x(02)00287-1
127029975 139216 0 None -56 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1675 55 28 20 -1.9 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3785576 139216 0 None -56 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1675 55 28 20 -1.9 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL3787766 139216 0 None -56 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1675 55 28 20 -1.9 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
24950556 189471 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(F)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL513701 189471 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(F)ccc32)=C(O)C1 10.1021/jm8003587
57398069 67817 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 370 10 2 7 2.0 CC(C)S(=O)(=O)NCCOCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909723 67817 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 370 10 2 7 2.0 CC(C)S(=O)(=O)NCCOCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
76332712 105713 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 415 4 1 4 4.4 C[C@@H]1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
CHEMBL3126043 105713 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 415 4 1 4 4.4 C[C@@H]1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
10178465 193191 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 390 4 2 5 2.9 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)[C@H](CO)N2)c1 10.1021/jm900110t
CHEMBL523305 193191 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 390 4 2 5 2.9 N#Cc1ccnc(C2=NC(c3ccc(F)cc3)(c3ccc(F)cc3)[C@H](CO)N2)c1 10.1021/jm900110t
44139356 192694 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 376 3 1 6 2.7 C[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)nc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL521932 192694 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 376 3 1 6 2.7 C[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)nc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL4292105 213513 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4292105 213513 0 None -7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
44139480 187143 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cncc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL491895 187143 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cncc(C#N)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
10181110 167071 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 430 4 1 4 2.0 CN(C(=O)NC1CCN(c2cc(F)cc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL428953 167071 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 430 4 1 4 2.0 CN(C(=O)NC1CCN(c2cc(F)cc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
10139329 167420 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 458 5 1 4 2.8 CC(C)S(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL429679 167420 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 458 5 1 4 2.8 CC(C)S(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
57398085 68010 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 437 10 2 8 3.8 Cc1nc(C)c(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)s1 10.1016/j.bmcl.2011.08.072
CHEMBL1912087 68010 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 437 10 2 8 3.8 Cc1nc(C)c(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)s1 10.1016/j.bmcl.2011.08.072
22458823 102005 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 349 5 1 3 4.8 CC(C)n1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL301638 102005 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 349 5 1 3 4.8 CC(C)n1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ccc21 10.1016/s0960-894x(03)00329-9
136088970 62789 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 400 3 2 4 3.4 C[C@@H]1NC(c2c[nH]c(=O)c(Cl)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1784124 62789 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 400 3 2 4 3.4 C[C@@H]1NC(c2c[nH]c(=O)c(Cl)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
56677041 65375 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 455 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829325 65375 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 455 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
10161574 95578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 458 6 1 4 2.8 CCCS(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257708 95578 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 458 6 1 4 2.8 CCCS(=O)(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
44345933 16300 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3ccncc3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL122527 16300 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3ccncc3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
56666777 65371 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 443 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829321 65371 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 443 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCOc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
70685314 73305 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 407 7 2 4 2.4 Cc1ccc2c(c1)CCN2CC(=O)N[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013013 73305 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 407 7 2 4 2.4 Cc1ccc2c(c1)CCN2CC(=O)N[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2012.01.117
9907999 164868 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL422012 164868 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
11742181 62794 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 4 1 5 3.8 CC(C)n1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784129 62794 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 4 1 5 3.8 CC(C)n1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
21031286 187112 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 376 3 1 6 2.7 C[C@@H]1NC(c2nccc(C#N)n2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL491567 187112 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 376 3 1 6 2.7 C[C@@H]1NC(c2nccc(C#N)n2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
57396265 67814 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 373 10 2 6 3.8 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccsc2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909720 67814 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 373 10 2 6 3.8 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccsc2)cs1 10.1016/j.bmcl.2011.08.072
136000677 62790 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 434 3 2 4 3.7 C[C@@H]1NC(c2c[nH]c(=O)c(C(F)(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1784125 62790 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 434 3 2 4 3.7 C[C@@H]1NC(c2c[nH]c(=O)c(C(F)(F)F)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
56677041 65375 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 455 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL1829325 65375 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 455 7 2 4 2.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL4290048 213490 0 None -25 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
44345934 14557 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3ccccn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL120377 14557 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3ccccn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
44139354 187054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL491107 187054 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 374 3 1 4 3.9 C[C@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
44345855 14653 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 246 2 1 3 3.0 N#Cc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL120538 14653 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 246 2 1 3 3.0 N#Cc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
70681118 73496 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 427 4 1 5 4.8 O=C(CC1CCC2(CC1)Cc1ccccc1C(=O)O2)Nc1cnc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.02.098
CHEMBL2016745 73496 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 427 4 1 5 4.8 O=C(CC1CCC2(CC1)Cc1ccccc1C(=O)O2)Nc1cnc(-c2ccccc2)cn1 10.1016/j.bmcl.2012.02.098
20610104 95166 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 394 4 1 4 1.7 CN(C(=O)NC1CCN(c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255800 95166 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 394 4 1 4 1.7 CN(C(=O)NC1CCN(c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
20647123 68006 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 10 2 7 3.8 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)c1cccs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912083 68006 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 408 10 2 7 3.8 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)c1cccs1 10.1016/j.bmcl.2011.08.072
CHEMBL4290891 213504 0 None 5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10295943 98062 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 424 5 1 5 1.7 COc1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
CHEMBL273180 98062 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 424 5 1 5 1.7 COc1cccc(N2CCC(NC(=O)N(C)C3CCN(S(C)(=O)=O)CC3)CC2)c1 10.1016/j.bmcl.2007.11.132
20610111 157665 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 430 4 1 4 2.0 CN(C(=O)NC1CCN(c2ccc(F)c(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL408153 157665 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 430 4 1 4 2.0 CN(C(=O)NC1CCN(c2ccc(F)c(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL4293564 213524 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N(C)[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10005032 59222 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 472 8 2 3 5.9 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2011.06.124
CHEMBL17022 59222 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 472 8 2 3 5.9 O=S(=O)(NC[C@H]1CC[C@H](CNCc2ccc3ccccc3c2)CC1)c1ccc2ccccc2c1 10.1016/j.bmcl.2011.06.124
CHEMBL4290891 213504 0 None 5 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
9806472 161991 0 None 257 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00288-3
CHEMBL415926 161991 0 None 257 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 476 8 2 3 5.3 O=S(=O)(NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1)c1ccc2ccccc2c1 10.1016/s0960-894x(02)00288-3
CHEMBL4293564 213524 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N(C)[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
1565 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm900110t
624746 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm900110t
CHEMBL491762 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm900110t
1565 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
624746 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
CHEMBL491762 2207 15 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10.1021/jm8003587
11002986 53836 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 363 5 2 4 3.4 COc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1OC 10.1021/jm025513q
CHEMBL160443 53836 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 363 5 2 4 3.4 COc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1OC 10.1021/jm025513q
57398068 67815 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 402 10 2 7 3.8 Cc1nc(C)c(-c2csc(NCCCCCNS(=O)(=O)C(C)C)n2)s1 10.1016/j.bmcl.2011.08.072
CHEMBL1909721 67815 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 402 10 2 7 3.8 Cc1nc(C)c(-c2csc(NCCCCCNS(=O)(=O)C(C)C)n2)s1 10.1016/j.bmcl.2011.08.072
44345935 14565 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 257 2 1 2 3.4 Fc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1F 10.1016/s0960-894x(03)00747-9
CHEMBL120431 14565 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 257 2 1 2 3.4 Fc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1F 10.1016/s0960-894x(03)00747-9
296732 111367 85 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 220 2 1 1 3.7 c1ccc(-c2c[nH]c(-c3ccccc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL327027 111367 85 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 220 2 1 1 3.7 c1ccc(-c2c[nH]c(-c3ccccc3)n2)cc1 10.1016/s0960-894x(03)00747-9
24950714 178699 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(F)cccc32)=C(O)C1 10.1021/jm8003587
CHEMBL468225 178699 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(F)cccc32)=C(O)C1 10.1021/jm8003587
24950712 189367 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Cl)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL512787 189367 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Cl)ccc32)=C(O)C1 10.1021/jm8003587
7068786 182308 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
CHEMBL478417 182308 2 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 366 1 1 4 5.0 CC1(C)CC(=O)C([C@@H]2C3=C(CC(C)(C)CC3=O)Oc3ccccc32)=C(O)C1 10.1021/jm8003587
10112368 155585 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2cccc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL404462 155585 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2cccc(F)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
54586366 62710 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 1 5 2.7 C[C@@H]1NC(c2cccc(=O)n2C)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783928 62710 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 1 5 2.7 C[C@@H]1NC(c2cccc(=O)n2C)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
9803547 178640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 444 1 1 4 5.8 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Br)ccc32)=C(O)C1 10.1021/jm8003587
CHEMBL467550 178640 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 444 1 1 4 5.8 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3cc(Br)ccc32)=C(O)C1 10.1021/jm8003587
24950557 178822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 380 1 1 4 5.3 Cc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL469256 178822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 380 1 1 4 5.3 Cc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
57396289 68000 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 443 9 2 6 5.1 Cc1c(-c2csc(NCCCCCNS(C)(=O)=O)n2)sc2ccc(Cl)cc12 10.1016/j.bmcl.2011.08.072
CHEMBL1912077 68000 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 443 9 2 6 5.1 Cc1c(-c2csc(NCCCCCNS(C)(=O)=O)n2)sc2ccc(Cl)cc12 10.1016/j.bmcl.2011.08.072
44345650 110627 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL325704 110627 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.2 FC(F)(F)c1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
56663347 65383 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 445 8 2 5 3.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829333 65383 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 445 8 2 5 3.7 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCSc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
57392790 67822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 411 10 2 7 2.0 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)N1CCOCC1 10.1016/j.bmcl.2011.08.072
CHEMBL1909728 67822 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 411 10 2 7 2.0 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)N1CCOCC1 10.1016/j.bmcl.2011.08.072
10449735 163234 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 337 4 1 4 3.2 CC(C)n1c(=O)c2ccc(NC(=O)CN(C)C)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL418459 163234 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 337 4 1 4 3.2 CC(C)n1c(=O)c2ccc(NC(=O)CN(C)C)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
22288540 102624 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 320 2 1 2 4.2 CCN1Cc2ccc(NC(=O)C(F)(F)F)cc2-c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL304245 102624 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 320 2 1 2 4.2 CCN1Cc2ccc(NC(=O)C(F)(F)F)cc2-c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL4280250 213404 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283705 213441 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None -630 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
44345853 14870 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL120760 14870 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 289 2 1 2 4.4 Clc1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL4290048 213490 0 None -25 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
76325491 105715 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 457 4 1 4 5.4 CC(C)(C)C1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
CHEMBL3126045 105715 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 457 4 1 4 5.4 CC(C)(C)C1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
70681100 73306 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 411 7 2 4 2.2 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3cc(F)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013014 73306 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 411 7 2 4 2.2 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCc3cc(F)ccc32)CC1 10.1016/j.bmcl.2012.01.117
44139603 186891 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 356 3 1 5 3.5 C[C@@H]1NC(c2nccs2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL489732 186891 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 356 3 1 5 3.5 C[C@@H]1NC(c2nccs2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
136088969 62787 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c[nH]c1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784120 62787 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c[nH]c1=O 10.1016/j.bmc.2009.05.069
9923839 187040 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1021/jm900110t
CHEMBL490937 187040 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 336 3 1 4 3.0 Fc1ccc(C2(c3ccc(F)cc3)CNC(c3cnccn3)=N2)cc1 10.1021/jm900110t
56677043 65384 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 427 8 2 4 3.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829334 65384 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 427 8 2 4 3.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCCc3cc(Cl)ccc32)CC1 10.1016/j.bmcl.2011.06.078
70695857 73493 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 442 3 1 5 4.7 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
CHEMBL2016742 73493 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 442 3 1 5 4.7 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1ccccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
22458799 100991 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 329 4 1 3 4.4 CCn1c2ccccc2c2cc(NC(=O)Cc3ccncc3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL294305 100991 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 329 4 1 3 4.4 CCn1c2ccccc2c2cc(NC(=O)Cc3ccncc3)ccc21 10.1016/s0960-894x(03)00329-9
10364093 62793 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 5 1 5 3.6 CCCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784128 62793 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 5 1 5 3.6 CCCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
44345801 14686 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 305 3 1 3 4.0 FC(F)(F)Oc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL120586 14686 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 305 3 1 3 4.0 FC(F)(F)Oc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
44345737 113825 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 290 2 1 3 3.8 Clc1ccc(-c2c[nH]c(-c3cnccn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL332561 113825 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 290 2 1 3 3.8 Clc1ccc(-c2c[nH]c(-c3cnccn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
44345961 113924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 235 2 1 2 3.4 Cc1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
CHEMBL332582 113924 1 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 235 2 1 2 3.4 Cc1ccccc1-c1c[nH]c(-c2cccnc2)n1 10.1016/s0960-894x(03)00747-9
CHEMBL4280250 213404 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4283705 213441 0 None -3 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4290445 213495 0 None -630 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N(C)[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
155549336 174263 0 None -141 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@H](CCCC[C@@H](N)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4549208 174263 0 None -141 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@H](CCCC[C@@H](N)C(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
44453965 95090 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 395 4 1 5 1.1 CN(C(=O)NC1CCN(c2cccnc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL255390 95090 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 395 4 1 5 1.1 CN(C(=O)NC1CCN(c2cccnc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
10041884 162799 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 323 4 1 4 2.7 CCn1c(=O)c2ccc(NC(=O)CN(C)C)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL417236 162799 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 323 4 1 4 2.7 CCn1c(=O)c2ccc(NC(=O)CN(C)C)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
76321860 105721 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 442 5 1 3 4.7 CC(C)N1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
CHEMBL3126051 105721 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 442 5 1 3 4.7 CC(C)N1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
24950870 178823 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 394 2 1 4 5.6 CCc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL469257 178823 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 394 2 1 4 5.6 CCc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
44294983 101728 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 455 11 2 5 4.0 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])c1ccc2ccccc2c1 10.1016/s0960-894x(02)00288-3
CHEMBL299579 101728 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 455 11 2 5 4.0 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])c1ccc2ccccc2c1 10.1016/s0960-894x(02)00288-3
44294898 186871 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 490 7 2 3 4.8 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
CHEMBL48960 186871 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 490 7 2 3 4.8 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
54580488 62704 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cc[nH]c(=O)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783922 62704 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2cc[nH]c(=O)c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
56673732 65360 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 454 7 2 5 1.6 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCSc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829310 65360 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 454 7 2 5 1.6 CN(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)CCSc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
44295107 101280 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 607 15 3 5 4.7 Cc1ccc(S(=O)(=O)NC(Cc2ccccc2)C(=O)NCCCCCCNS(=O)(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(02)00288-3
CHEMBL296387 101280 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 607 15 3 5 4.7 Cc1ccc(S(=O)(=O)NC(Cc2ccccc2)C(=O)NCCCCCCNS(=O)(=O)c2cccc3ccccc23)cc1 10.1016/s0960-894x(02)00288-3
10336953 100716 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 334 2 1 3 3.7 CCn1c(=O)c2ccc(NC(=O)C(F)(F)F)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
CHEMBL292560 100716 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 334 2 1 3 3.7 CCn1c(=O)c2ccc(NC(=O)C(F)(F)F)cc2c2ccccc21 10.1016/s0960-894x(03)00329-9
57398083 67999 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 346 9 2 7 2.4 CS(=O)(=O)NCCCCCNc1nc(-c2nccs2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912076 67999 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 346 9 2 7 2.4 CS(=O)(=O)NCCCCCNc1nc(-c2nccs2)cs1 10.1016/j.bmcl.2011.08.072
57391018 67994 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 366 10 2 6 2.9 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CC1 10.1016/j.bmcl.2011.08.072
CHEMBL1912071 67994 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 366 10 2 6 2.9 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)C1CC1 10.1016/j.bmcl.2011.08.072
11099807 50707 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccccc2Cl)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
CHEMBL157588 50707 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccccc2Cl)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
22462213 188199 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 459 11 2 5 3.4 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
CHEMBL49906 188199 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 459 11 2 5 3.4 O=C(NCCCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
155547323 173626 0 None -41 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4533775 173626 0 None -41 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1590 51 25 19 -1.2 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL413426 213066 0 None -97 4 Human 6.3 pKi = 6.3 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](CSSC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)[C@@H](C)CC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC 10.1021/jm010031k
44345637 10473 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 339 2 1 2 5.6 Clc1ccc(-c2c[nH]c(-c3cc4ccccc4cn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
CHEMBL116488 10473 1 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 339 2 1 2 5.6 Clc1ccc(-c2c[nH]c(-c3cc4ccccc4cn3)n2)cc1Cl 10.1016/s0960-894x(03)00747-9
10183204 97608 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 462 4 1 4 3.0 CN(C(=O)NC1CCN(c2ccc(Cl)c(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL270890 97608 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 462 4 1 4 3.0 CN(C(=O)NC1CCN(c2ccc(Cl)c(Cl)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
57398081 67995 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 382 11 2 6 3.5 CCC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912072 67995 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 382 11 2 6 3.5 CCC(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
20629114 73448 47 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.02.098
CHEMBL2016681 73448 47 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 407 4 2 4 3.3 CC(C)(C)S(=O)(=O)N[C@H]1CC[C@H](C(=O)Nc2ccc(C(F)(F)F)cn2)CC1 10.1016/j.bmcl.2012.02.098
136000678 62791 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 396 4 2 5 2.7 COc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c[nH]c1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784126 62791 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 396 4 2 5 2.7 COc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)c[nH]c1=O 10.1016/j.bmc.2009.05.069
66677782 105709 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 1 4 3.5 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2ncc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126039 105709 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 1 4 3.5 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2ncc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
46913606 105716 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 2 3 3.5 O=C1NCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126046 105716 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 2 3 3.5 O=C1NCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
46913409 105717 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 414 4 1 3 3.9 CN1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
CHEMBL3126047 105717 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 414 4 1 3 3.9 CN1CCN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C1=O 10.1016/j.bmcl.2014.02.023
44139600 186889 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 393 4 2 5 2.5 C[C@@H]1NC(c2cc(C(N)=O)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL489725 186889 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 393 4 2 5 2.5 C[C@@H]1NC(c2cc(C(N)=O)ccn2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
70689509 73318 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 416 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(C#N)ccc32)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013026 73318 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 416 7 2 5 2.5 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)Cn2ccc3cc(C#N)ccc32)CC1 10.1016/j.bmcl.2012.01.117
44139481 193258 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cccc(C#N)n2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
CHEMBL523821 193258 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 375 3 1 5 3.3 C[C@@H]1NC(c2cccc(C#N)n2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1021/jm900110t
10224063 95483 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 422 5 1 3 3.4 CCCC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257248 95483 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 422 5 1 3 3.4 CCCC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL4282616 213432 0 None 3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4282616 213432 0 None 3 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(CCC(N)=O)CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10111188 95336 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 4 1 3 2.8 CN(C(=O)N[C@H]1CC[C@@H](c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL256592 95336 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 4 1 3 2.8 CN(C(=O)N[C@H]1CC[C@@H](c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
2317 67649 9 None -2 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 590 27 4 8 6.3 COc1ccccc1CNCCCCCCNCCSSCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmcl.2011.06.124
CHEMBL19060 67649 9 None -2 2 Human 5.3 pKi = 5.3 Binding
Binding affinity to NPY5 receptorBinding affinity to NPY5 receptor
ChEMBL 590 27 4 8 6.3 COc1ccccc1CNCCCCCCNCCSSCCNCCCCCCNCc1ccccc1OC 10.1016/j.bmcl.2011.06.124
57398070 67818 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 395 7 1 7 2.0 CC(C)S(=O)(=O)N1CCN(CCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
CHEMBL1909724 67818 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 395 7 1 7 2.0 CC(C)S(=O)(=O)N1CCN(CCNc2nc(-c3ccccn3)cs2)CC1 10.1016/j.bmcl.2011.08.072
CHEMBL4276796 213366 0 None -63 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4278746 213391 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4276796 213366 0 None -63 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4278746 213391 0 None -3 3 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
10820168 96860 0 None -147 4 Human 5.3 pKi = 5.3 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 1192 37 16 15 -2.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC 10.1021/jm010031k
CHEMBL265391 96860 0 None -147 4 Human 5.3 pKi = 5.3 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 1192 37 16 15 -2.3 CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)CC 10.1021/jm010031k
CHEMBL429005 213491 0 None -5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]PYY from NPY5 receptor expressed in human HEK293 cellsDisplacement of [125I]PYY from NPY5 receptor expressed in human HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2006.10.007
57403234 67812 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 368 10 2 6 3.1 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2cccnc2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909718 67812 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 368 10 2 6 3.1 CC(C)S(=O)(=O)NCCCCCNc1nc(-c2cccnc2)cs1 10.1016/j.bmcl.2011.08.072
10111188 95643 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 4 1 3 2.8 CN(C(=O)N[C@H]1CC[C@H](c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257939 95643 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 393 4 1 3 2.8 CN(C(=O)N[C@H]1CC[C@H](c2ccccc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
20610103 155209 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 4 2.0 Cc1ccccc1N1CCC(NC(=O)N(C)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL402557 155209 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 4 2.0 Cc1ccccc1N1CCC(NC(=O)N(C)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2007.11.132
12250899 14551 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL120336 14551 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 221 2 1 2 3.1 c1ccc(-c2c[nH]c(-c3cccnc3)n2)cc1 10.1016/s0960-894x(03)00747-9
57394537 67992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 340 9 2 6 2.3 CS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912069 67992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 340 9 2 6 2.3 CS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
155553742 175438 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1505 47 22 18 -0.4 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4576579 175438 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1505 47 22 18 -0.4 CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CCCCCCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
44345802 165025 3 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 251 3 1 3 3.1 COc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL422608 165025 3 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 251 3 1 3 3.1 COc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
10155286 155339 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 357 3 1 2 3.4 CC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL403223 155339 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 357 3 1 2 3.4 CC(=O)N1CCC(N(C)C(=O)N[C@H]2CC[C@H](c3ccccc3)CC2)CC1 10.1016/j.bmcl.2007.11.132
2821670 168456 2 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccc(Cl)cc2)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
CHEMBL435036 168456 2 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 337 3 2 2 4.1 O=C(Nc1cc(-c2ccc(Cl)cc2)n[nH]1)C1Cc2ccccc2C1 10.1021/jm025513q
2979261 181646 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1ccc2c(c1)C(C1=C(O)CC(C)(C)CC1=O)C1=C(CC(C)(C)CC1=O)O2 10.1021/jm8003587
CHEMBL477578 181646 7 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1ccc2c(c1)C(C1=C(O)CC(C)(C)CC1=O)C1=C(CC(C)(C)CC1=O)O2 10.1021/jm8003587
11640844 6016 0 None -199 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]pig PPY from human NPY5 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY5 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
CHEMBL1080298 6016 0 None -199 2 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]pig PPY from human NPY5 receptor expressed in CHOK1 cells by scintillation countingDisplacement of [125I]pig PPY from human NPY5 receptor expressed in CHOK1 cells by scintillation counting
ChEMBL 444 6 2 6 6.6 c1ccc([C@@H]2CCSC(Nc3ccc(CCNc4nc5ccccc5s4)cc3)=N2)cc1 10.1016/j.bmcl.2009.09.048
46913508 105710 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 1 4 3.5 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2cnc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126040 105710 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 400 4 1 4 3.5 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2cnc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
10294889 95528 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 3 3.0 CCC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL257457 95528 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 408 4 1 3 3.0 CCC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
10341402 62797 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 4 1 5 3.5 CCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)cc(C)c1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784132 62797 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 408 4 1 5 3.5 CCn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)cc(C)c1=O 10.1016/j.bmc.2009.05.069
54587390 62708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 2 4 2.9 C[C@@H]1NC(c2ccc(F)c(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783926 62708 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 384 3 2 4 2.9 C[C@@H]1NC(c2ccc(F)c(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
56683703 65365 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 467 7 2 5 3.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829315 65365 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 467 7 2 5 3.8 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2CCC(C)(C)Sc3ccccc32)CC1 10.1016/j.bmcl.2011.06.078
57403235 67825 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 457 16 2 8 2.2 COCCN(CCOC)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909731 67825 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 457 16 2 8 2.2 COCCN(CCOC)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
56673733 65380 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 429 8 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829330 65380 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 429 8 2 5 3.0 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3ccc(Cl)cc32)CC1 10.1016/j.bmcl.2011.06.078
136000663 62703 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2ccc[nH]c2=O)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783921 62703 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2ccc[nH]c2=O)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL2440182 210473 0 None -12 2 Human 6.2 pKi = 6.2 Binding
Binding affinity to Y5 receptor (unknown origin)Binding affinity to Y5 receptor (unknown origin)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]1[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H]2[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)[C@H]2C(=O)OC)[C@H]1C(=O)OC 10.1021/jm4008505
10892960 52432 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 333 4 2 3 3.4 COc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
CHEMBL159070 52432 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 333 4 2 3 3.4 COc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
CHEMBL3104112 211053 0 None -69 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to NPYY5 receptor (unknown origin)Binding affinity to NPYY5 receptor (unknown origin)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)c1cccnc1SCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2013.11.061
CHEMBL4279133 213393 0 None -7 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 213413 0 None -316 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
136000675 63151 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(=O)[nH]cc1C1=N[C@@](c2ccc(F)cc2)(c2ccc(F)nc2)[C@H](C)N1 10.1016/j.bmc.2009.05.069
CHEMBL1784121 63151 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(=O)[nH]cc1C1=N[C@@](c2ccc(F)cc2)(c2ccc(F)nc2)[C@H](C)N1 10.1016/j.bmc.2009.05.069
CHEMBL1789629 63151 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(=O)[nH]cc1C1=N[C@@](c2ccc(F)cc2)(c2ccc(F)nc2)[C@H](C)N1 10.1016/j.bmc.2009.05.069
CHEMBL4279133 213393 0 None -7 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CC(=O)O)Cc1ccc(O)cc1)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4281010 213413 0 None -316 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)[C@@H](C)CC)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL411117 212865 0 None -2454 4 Human 6.2 pKi = 6.2 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)OC)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)OC)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
44345854 114493 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 269 2 1 2 4.1 Cc1[nH]c(-c2cccnc2)nc1-c1ccc(Cl)cc1 10.1016/s0960-894x(03)00747-9
CHEMBL333509 114493 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 269 2 1 2 4.1 Cc1[nH]c(-c2cccnc2)nc1-c1ccc(Cl)cc1 10.1016/s0960-894x(03)00747-9
76332713 105714 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 415 4 1 4 4.4 C[C@H]1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
CHEMBL3126044 105714 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 415 4 1 4 4.4 C[C@H]1CN([C@H]2CC[C@@H](C(=O)Nc3ccc(-c4cc(F)cc(F)c4)cn3)CC2)C(=O)O1 10.1016/j.bmcl.2014.02.023
54583973 62785 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 410 5 1 6 2.7 CCOn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784119 62785 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 410 5 1 6 2.7 CCOn1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)ccc1=O 10.1016/j.bmc.2009.05.069
9907999 164868 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
CHEMBL422012 164868 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 382 4 2 3 4.5 CCc1cc(-c2cc(NC(=O)C3Cc4ccc5ccccc5c4C3)[nH]n2)ccn1 10.1021/jm025513q
136088971 62702 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2ccc(=O)[nH]c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783920 62702 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 366 3 2 4 2.7 C[C@@H]1NC(c2ccc(=O)[nH]c2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
9821993 155060 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 394 3 1 3 2.6 CC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL401726 155060 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 394 3 1 3 2.6 CC(=O)N1CCC(N(C)C(=O)NC2CCN(c3cc(F)cc(F)c3)CC2)CC1 10.1016/j.bmcl.2007.11.132
54752621 67819 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 369 10 2 6 2.2 CN(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909725 67819 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 369 10 2 6 2.2 CN(C)S(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
3107239 178670 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(Cl)cccc32)=C(O)C1 10.1021/jm8003587
CHEMBL467813 178670 1 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 400 1 1 4 5.7 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3c(Cl)cccc32)=C(O)C1 10.1021/jm8003587
155543070 173189 0 None -436 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4522438 173189 0 None -436 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL4570354 173189 0 None -436 4 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation countingDisplacement of [3H]propionyl-pNPY from human NPY Y5 receptor expressed in human HEC1b cells after 120 mins by liquid scintillation counting
ChEMBL 1761 57 30 22 -3.5 CCC(=O)N[C@@H](CCCC[C@H](N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.6b00309
CHEMBL438914 213807 16 None -275 4 Human 5.2 pKi = 5.2 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)OC)[C@@H](C)CC 10.1021/jm010031k
46913408 105724 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 399 4 1 3 4.1 O=C1CCCN1[C@H]1CC[C@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126054 105724 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 399 4 1 3 4.1 O=C1CCCN1[C@H]1CC[C@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
44294739 186781 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 442 9 3 5 3.6 O=C(NCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
CHEMBL48904 186781 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 442 9 3 5 3.6 O=C(NCCCCNS(=O)(=O)c1ccccc1[N+](=O)[O-])Nc1cccc2ccccc12 10.1016/s0960-894x(02)00288-3
44294789 188944 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 464 10 2 3 4.6 O=C(NCCCCCCNS(=O)(=O)c1cccc2ccccc12)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
CHEMBL50807 188944 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 464 10 2 3 4.6 O=C(NCCCCCCNS(=O)(=O)c1cccc2ccccc12)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
44295138 193192 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 535 8 2 5 4.8 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccc3cccc([N+](=O)[O-])c3c2)CC1)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
CHEMBL52332 193192 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 535 8 2 5 4.8 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2ccc3cccc([N+](=O)[O-])c3c2)CC1)C1CCc2ccccc2C1 10.1016/s0960-894x(02)00288-3
71461713 79645 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 364 6 1 4 4.3 CC(C)Cn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ncc21 10.1016/s0960-894x(03)00329-9
CHEMBL2115090 79645 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 364 6 1 4 4.3 CC(C)Cn1c2ccccc2c2cc(NC(=O)CCN3CCCC3)ncc21 10.1016/s0960-894x(03)00329-9
57396287 67989 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 468 11 2 8 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2ccn(S(=O)(=O)c3ccccc3)c2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912066 67989 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 468 11 2 8 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2ccn(S(=O)(=O)c3ccccc3)c2)cs1 10.1016/j.bmcl.2011.08.072
57392791 67823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 439 10 2 7 2.7 CC1CN(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC(C)O1 10.1016/j.bmcl.2011.08.072
CHEMBL1909729 67823 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 439 10 2 7 2.7 CC1CN(S(=O)(=O)NCCCCCNc2nc(-c3ccccn3)cs2)CC(C)O1 10.1016/j.bmcl.2011.08.072
44283050 159482 0 None -17378 4 Human 5.1 pKi = 5.1 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
91931647 159482 0 None -17378 4 Human 5.1 pKi = 5.1 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
CHEMBL410166 159482 0 None -17378 4 Human 5.1 pKi = 5.1 Binding
Affinity for cloned Y5 receptor using [125I]PYY as radioligandAffinity for cloned Y5 receptor using [125I]PYY as radioligand
ChEMBL 2323 60 32 30 -6.7 CC[C@H](C)[C@H](N)C(=O)N[C@H]1CCC(=O)NC[C@@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](NC(=O)[C@@H](N)[C@@H](C)CC)CCC(=O)NC[C@H](C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)CN[C@@H](Cc2ccc(O)cc2)C(N)=O)NC(=O)[C@@H]2CCCN2C1=O 10.1021/jm010031k
CHEMBL4277676 213375 0 None -100 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4277676 213375 0 None -100 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 213467 0 None -316 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291016 213505 0 None -7 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294418 213531 0 None -616 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
CHEMBL4287058 213467 0 None -316 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)CC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4291016 213505 0 None -7 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C 10.1021/acs.jmedchem.8b01046
CHEMBL4294418 213531 0 None -616 4 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assayDisplacement of [125I]-PYY(1 to 36 residues) from human Y5R expressed in HEK293 cell membranes after 2 hrs by scintillation proximity assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)O)[C@@H](C)O)C(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCCCCNC(=O)[C@H](CCCCN)NC1=O 10.1021/acs.jmedchem.8b01046
20610119 97626 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2ccc(F)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL270999 97626 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2ccc(F)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
20647096 68004 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 420 10 2 6 3.9 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)c1ccccc1F 10.1016/j.bmcl.2011.08.072
CHEMBL1912081 68004 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 420 10 2 6 3.9 O=S(=O)(NCCCCCNc1nc(-c2ccccn2)cs1)c1ccccc1F 10.1016/j.bmcl.2011.08.072
9972871 202562 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 313 2 1 4 4.1 CCn1c2ccccc2c2cc(-c3nc4c[nH]cnc-4n3)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL61175 202562 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 313 2 1 4 4.1 CCn1c2ccccc2c2cc(-c3nc4c[nH]cnc-4n3)ccc21 10.1016/s0960-894x(03)00329-9
44345820 110631 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
CHEMBL325727 110631 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cellsBinding affinity towards human neuropeptide Y receptor type 5 using [125I]-PYY as radioligand in baculovirus-infected Sf9 cells
ChEMBL 255 2 1 2 3.8 Clc1cccc(-c2c[nH]c(-c3cccnc3)n2)c1 10.1016/s0960-894x(03)00747-9
70683238 73487 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 420 3 1 4 4.7 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)COc1ccccc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016736 73487 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 420 3 1 4 4.7 CN(C(=O)Nc1ccn(-c2ccccc2F)n1)[C@H]1CC[C@]2(CC1)COc1ccccc12 10.1016/j.bmcl.2012.02.098
46913511 105712 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 401 4 1 4 4.0 O=C1OCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126042 105712 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 401 4 1 4 4.0 O=C1OCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
46913408 105723 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 399 4 1 3 4.1 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126053 105723 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 399 4 1 3 4.1 O=C1CCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
9982218 101764 6 None 2 6 Human 8.1 pKi = 8.1 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL1435188 101764 6 None 2 6 Human 8.1 pKi = 8.1 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
CHEMBL299879 101764 6 None 2 6 Human 8.1 pKi = 8.1 Binding
Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5Tested for radioligand binding affinity against membranes from COS-7 cells transiently transfected with Neuropeptide Y receptor type 5
ChEMBL 471 9 2 5 4.1 O=[N+]([O-])c1ccccc1S(=O)(=O)NC[C@H]1CC[C@H](CNCC2CCc3ccccc3C2)CC1 10.1016/s0960-894x(02)00287-1
9952193 100586 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 387 6 2 4 4.4 COc1ccc(-c2cc(NC(=O)Cc3ccc4ccccc4c3)[nH]n2)cc1OC 10.1021/jm025513q
CHEMBL291666 100586 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 387 6 2 4 4.4 COc1ccc(-c2cc(NC(=O)Cc3ccc4ccccc4c3)[nH]n2)cc1OC 10.1021/jm025513q
56659888 65369 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 5 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(F)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829319 65369 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 5 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3cc(F)ccc32)CC1 10.1016/j.bmcl.2011.06.078
10432823 62798 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 430 4 1 5 3.9 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)cn(C(F)F)c1=O 10.1016/j.bmc.2009.05.069
CHEMBL1784133 62798 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 430 4 1 5 3.9 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)cn(C(F)F)c1=O 10.1016/j.bmc.2009.05.069
54581508 62706 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)[nH]c(=O)c1 10.1016/j.bmc.2009.05.069
CHEMBL1783924 62706 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 380 3 2 4 3.0 Cc1cc(C2=N[C@@](c3ccc(F)cc3)(c3ccc(F)nc3)[C@H](C)N2)[nH]c(=O)c1 10.1016/j.bmc.2009.05.069
54582496 62709 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 400 3 2 4 3.4 C[C@@H]1NC(c2ccc(Cl)c(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
CHEMBL1783927 62709 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in mouse LMtk- cells
ChEMBL 400 3 2 4 3.4 C[C@@H]1NC(c2ccc(Cl)c(=O)[nH]2)=N[C@@]1(c1ccc(F)cc1)c1ccc(F)nc1 10.1016/j.bmc.2009.05.069
44139355 187041 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 402 5 1 4 4.7 CCC[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
CHEMBL490949 187041 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in mouse LMtk- cells
ChEMBL 402 5 1 4 4.7 CCC[C@@H]1NC(c2cc(C#N)ccn2)=NC1(c1ccc(F)cc1)c1ccc(F)cc1 10.1021/jm900110t
10205608 98063 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 472 4 1 4 2.5 CN(C(=O)NC1CCN(c2cccc(Br)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL273182 98063 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 472 4 1 4 2.5 CN(C(=O)NC1CCN(c2cccc(Br)c2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
70687456 73319 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 405 7 2 4 3.0 Cc1cc2ccccc2n1CC(=O)N[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2012.01.117
CHEMBL2013027 73319 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]peptide YY from human NPY5 receptorDisplacement of [125I]peptide YY from human NPY5 receptor
ChEMBL 405 7 2 4 3.0 Cc1cc2ccccc2n1CC(=O)N[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2012.01.117
57398082 67997 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 345 9 2 6 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2ccsc2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1912074 67997 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 345 9 2 6 3.0 CS(=O)(=O)NCCCCCNc1nc(-c2ccsc2)cs1 10.1016/j.bmcl.2011.08.072
11758930 52109 3 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 317 3 2 2 3.7 Cc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
CHEMBL158759 52109 3 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 317 3 2 2 3.7 Cc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
20647090 67820 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 341 9 3 6 1.6 NS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
CHEMBL1909726 67820 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assayBinding affinity to human cloned NPY Y5 receptor expressed in african green monkey COS7 cells by radioligand binding assay
ChEMBL 341 9 3 6 1.6 NS(=O)(=O)NCCCCCNc1nc(-c2ccccn2)cs1 10.1016/j.bmcl.2011.08.072
24950713 178800 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3ccc(F)cc32)=C(O)C1 10.1021/jm8003587
CHEMBL469041 178800 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 384 1 1 4 5.1 CC1(C)CC(=O)C(C2C3=C(CC(C)(C)CC3=O)Oc3ccc(F)cc32)=C(O)C1 10.1021/jm8003587
20610117 97625 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 472 4 1 4 2.5 CN(C(=O)NC1CCN(c2ccc(Br)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL270997 97625 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 472 4 1 4 2.5 CN(C(=O)NC1CCN(c2ccc(Br)cc2)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
70683240 73492 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 443 3 1 6 4.1 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1cnccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
CHEMBL2016741 73492 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 443 3 1 6 4.1 CN(C(=O)Nc1cnc(-c2ccccc2)cn1)[C@H]1CC[C@@]2(CC1)Cc1cnccc1C(=O)O2 10.1016/j.bmcl.2012.02.098
24950558 189189 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 410 3 1 5 5.4 CCOc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL511264 189189 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 410 3 1 5 5.4 CCOc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
70695856 73485 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 421 3 2 6 3.5 O=C(Nc1ccn(-c2ccccc2F)n1)NC1CCC2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
CHEMBL2016734 73485 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranesDisplacement of [125I]PPY from human recombinant NPYY5 receptor expressed in insect Sf9 membranes
ChEMBL 421 3 2 6 3.5 O=C(Nc1ccn(-c2ccccc2F)n1)NC1CCC2(CC1)OC(=O)c1ccncc12 10.1016/j.bmcl.2012.02.098
56677042 65379 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 425 9 2 6 2.4 COc1ccc2c(c1)OCCN2CCN[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829329 65379 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 425 9 2 6 2.4 COc1ccc2c(c1)OCCN2CCN[C@H]1CC[C@H](CNS(=O)(=O)C(C)C)CC1 10.1016/j.bmcl.2011.06.078
20610110 155352 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2ccccc2F)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
CHEMBL403282 155352 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cellsDisplacement of [125]PYY from human chimeric NPY Y5 receptor expressed in CHOK1 cells
ChEMBL 412 4 1 4 1.9 CN(C(=O)NC1CCN(c2ccccc2F)CC1)C1CCN(S(C)(=O)=O)CC1 10.1016/j.bmcl.2007.11.132
46913512 105718 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 414 4 2 3 3.9 O=C1NCCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126048 105718 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 414 4 2 3 3.9 O=C1NCCCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
76310949 105722 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 440 5 1 3 4.4 O=C1N(C2CC2)CCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
CHEMBL3126052 105722 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation countingDisplacement of [125I]PYY from human NPY5 receptor transfected in LM(tk-) cell membranes after 120 mins by solid scintillation counting
ChEMBL 440 5 1 3 4.4 O=C1N(C2CC2)CCN1[C@H]1CC[C@@H](C(=O)Nc2ccc(-c3cc(F)cc(F)c3)cn2)CC1 10.1016/j.bmcl.2014.02.023
46209598 65382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 463 8 2 5 3.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829332 65382 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 463 8 2 5 3.4 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NCCN2CCOc3cc(C(F)(F)F)ccc32)CC1 10.1016/j.bmcl.2011.06.078
11057532 54185 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 5 2 3 4.2 CC(C)Oc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
CHEMBL160722 54185 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cellsInhibition of [125I]PYY binding to human recombinant Neuropeptide Y receptor type 5 in LMtk-cells
ChEMBL 361 5 2 3 4.2 CC(C)Oc1ccc(-c2cc(NC(=O)C3Cc4ccccc4C3)[nH]n2)cc1 10.1021/jm025513q
9922092 101071 3 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 292 1 1 2 3.8 Cn1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
CHEMBL294822 101071 3 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligandBinding affinity towards human neuropeptide Y receptor type 5 using 125[I]-PYY as radioligand
ChEMBL 292 1 1 2 3.8 Cn1c2ccccc2c2cc(NC(=O)C(F)(F)F)ccc21 10.1016/s0960-894x(03)00329-9
9930634 178773 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
CHEMBL468846 178773 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cellsDisplacement of [125I]PYY from human recombinant neuropeptide Y5 receptor expressed in thymidine kinase deficient human LM cells
ChEMBL 396 2 1 5 5.0 COc1ccc2c(c1)OC1=C(C(=O)CC(C)(C)C1)C2C1=C(O)CC(C)(C)CC1=O 10.1021/jm8003587
44295115 193257 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 519 7 3 3 6.1 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(02)00288-3
CHEMBL52382 193257 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranesDisplacement of [125I]PYY from human Neuropeptide Y receptor type 5 in COS-7 cell membranes
ChEMBL 519 7 3 3 6.1 O=C(NC[C@H]1CC[C@H](CNS(=O)(=O)c2cccc3ccccc23)CC1)Nc1ccc(Cl)c(Cl)c1 10.1016/s0960-894x(02)00288-3
56677040 65368 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 5 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3ccc(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
CHEMBL1829318 65368 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation countingDisplacement of [125I]PYY from human NPY5 receptor expressed in thymidine kinase deficient mouse LM cells after 120 mins by scintillation counting
ChEMBL 441 7 2 5 1.6 CC(C)S(=O)(=O)NC[C@H]1CC[C@H](NC(=O)CN2C(=O)COc3ccc(F)cc32)CC1 10.1016/j.bmcl.2011.06.078
None 216056 0 125I-hPP -295 13 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
126455957 216054 0 125I-hPP -2 5 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 4307 134 63 59 -16.4 CC[C@H](C)[C@@H](C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N3CCC[C@H]3C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC4=CC=C(C=C4)O)C(=O)N[C@@H](CC5=CC=C(C=C5)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC6=CNC=N6)C(=O)N[C@@H](CC7=CC=C(C=C7)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC8=CC=C(C=C8)O)C(=O)N)NC(=O)[C@@H]9CCCN9C(=O)[C@H](CC1=CC=C(C=C1)O)N None
None 216058 0 125I-hPP -8317 8 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 444 3 1 3 7.0 C1C(CC2=CC=CC=C2C1C3=C(OC4=CC=CC=C4C3=O)O)C5=CC=C(C=C5)C6=CC=CC=C6 None
56841989 213420 6 125I-PYY -2 7 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C None
CHEMBL4281479 213420 6 125I-PYY -2 7 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C None
1562 899 13 125I-hPP 2 2 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 None
5312114 899 13 125I-hPP 2 2 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 None
CHEMBL17645 899 13 125I-hPP 2 2 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 None
CHEMBL195380 899 13 125I-hPP 2 2 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 None
None 216056 0 3H-Propionyl-NPY -1318 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
21129772 169424 4 125I-PYY -309 8 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
21129772 169424 4 125I-PYY -309 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
21129772 169424 4 125I-hPP -309 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
CHEMBL44246 169424 4 125I-PYY -309 8 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
CHEMBL44246 169424 4 125I-PYY -309 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
CHEMBL44246 169424 4 125I-hPP -309 8 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 473 11 6 4 2.6 N=C(N)NCCCC(NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 None
None 216056 0 125I-PYY -331131 13 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216235 0 125I-hPP -131 3 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 895 16 5 11 3.3 C1CCC(C1)(CC(=O)NC(CCCN=C(N)N)C(=O)NCCN2C(=O)N(N(C2=O)C3=CC=CC=C3)C4=CC=CC=C4)CC(=O)N5CCN(CC5)C6C7=CC=CC=C7C(=O)NC8=CC=CC=C68 None
None 216428 0 125I-hPP - 1 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 643 13 7 5 2.5 C1=CC=C(C=C1)C(C2=CC=CC=C2)C(=O)NC(CCCN=C(N)N)C(=O)NCC3=CC=C(C=C3)CNC(=O)N.C(=O)(C(F)(F)F)O None
None 216056 0 125I-PYY -1318 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216058 0 125I-PYY -8317 8 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 444 3 1 3 7.0 C1C(CC2=CC=CC=C2C1C3=C(OC4=CC=CC=C4C3=O)O)C5=CC=C(C=C5)C6=CC=CC=C6 None
None 216056 0 125I-PYY -295 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 216058 0 125I-PYY -162181 8 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 444 3 1 3 7.0 C1C(CC2=CC=CC=C2C1C3=C(OC4=CC=CC=C4C3=O)O)C5=CC=C(C=C5)C6=CC=CC=C6 None
56841989 213420 6 125I-PYY -17 7 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C None
CHEMBL4281479 213420 6 125I-PYY -17 7 Mouse 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase None None None CC[C@H](C)[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C None
None 216058 0 125I-PYY -8317 8 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 444 3 1 3 7.0 C1C(CC2=CC=CC=C2C1C3=C(OC4=CC=CC=C4C3=O)O)C5=CC=C(C=C5)C6=CC=CC=C6 None
1565 2207 15 None 1 2 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
624746 2207 15 None 1 2 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
CHEMBL491762 2207 15 None 1 2 Human 7.6 pKi = 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
1527 2304 0 None -25 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1549 2888 0 None -1 5 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1549 2888 0 None -1 5 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817422 2888 0 None -1 5 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817422 2888 0 None -1 5 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1504 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1518 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1521 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
24868177 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44288922 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
77068007 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
90479759 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL438945 2807 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1504 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1518 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1521 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
24868177 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44288922 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
77068007 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
90479759 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL438945 2807 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1557 2885 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44328226 2885 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL439478 2885 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1529 1851 0 None -31622 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1513 3003 0 None -19952 6 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1513 3003 0 None -15848 6 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1557 2885 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44328226 2885 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL439478 2885 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1516 3242 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1516 3242 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
57339564 3242 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
57339564 3242 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91898411 3242 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91898411 3242 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1507 2883 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44351001 2883 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91929182 2883 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL265849 2883 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1565 2207 15 None -1 2 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
624746 2207 15 None -1 2 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
CHEMBL491762 2207 15 None -1 2 Rat 7.5 pKi None 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 366 1 1 4 5.0 OC1=C(C(=O)CC(C1)(C)C)C1C2=C(Oc3c1cccc3)CC(CC2=O)(C)C 10872822
1507 2883 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44351001 2883 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91929182 2883 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL265849 2883 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1510 2891 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817418 2891 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
16142730 2891 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1512 3002 0 None -501 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1554 3244 0 None -2 3 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1544 1500 0 None -1 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1544 1500 0 None 1 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1564 2112 0 None - 1 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 8 2 5 4.9 O=N(=O)c1ccccc1S(=O)(=O)NC[C@@H]1CC[C@H](CC1)CNc1ccc2c(c1)cccc2 12890716
73755001 2112 0 None - 1 Rat 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 453 8 2 5 4.9 O=N(=O)c1ccccc1S(=O)(=O)NC[C@@H]1CC[C@H](CC1)CNc1ccc2c(c1)cccc2 12890716
1560 335 0 None - 1 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1554 3244 0 None 2 3 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1527 2304 0 None -31 5 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1510 2891 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817418 2891 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
16142730 2891 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1561 3155 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1512 3002 0 None -70 6 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1512 3002 0 None -70 6 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1515 3053 0 None -19 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL269503 3053 0 None -19 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1524 2303 0 None -1 3 Rat 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1524 2303 0 None -1 3 Rat 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1515 3053 0 None -15 6 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL269503 3053 0 None -15 6 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1524 2303 0 None 1 3 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1562 899 13 None 2 2 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 12890716
5312114 899 13 None 2 2 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 12890716
CHEMBL17645 899 13 None 2 2 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 12890716
CHEMBL195380 899 13 None 2 2 Rat 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 475 7 3 6 4.6 Nc1nc(NCC2CCC(CC2)CNS(=O)(=O)c2cccc3c2cccc3)nc2c1cccc2 12890716