Ligand source activities (1 row/activity)





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56841989 220199 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 220199 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 220199 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 220199 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 220257 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 217805 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 190351 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 190351 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 220154 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 220274 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 220154 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 220274 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 217801 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 217800 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 220229 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 220229 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 215992 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 220185 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 220185 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 217799 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 220152 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 10556 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 10556 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 10556 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 220152 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 220180 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 217802 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 220310 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 220180 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 220310 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 220633 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 217802 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 220147 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 220243 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 220147 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 220243 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 220236 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 220309 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 220236 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 220309 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 220192 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 220192 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 220169 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 220169 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 220316 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 220178 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 220292 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 220178 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 220292 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 220208 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 220216 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 220208 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 220216 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 220633 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 72751 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 72751 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 104933 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 104933 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 72746 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 72746 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 71361 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 71361 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 195737 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 195737 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 206822 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 206822 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 72749 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 72749 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 190983 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 190983 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 194635 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 194635 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 194800 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 194800 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 72744 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 72744 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 72753 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 72753 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 72742 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 72742 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 78015 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 78015 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 66727 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 66727 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 78042 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 78042 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 78040 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 78040 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 185308 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 185308 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 117365 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 117365 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 70022 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 70022 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 185601 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 185601 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 171647 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 171647 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 78038 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 78038 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 78016 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 78016 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 78013 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 78013 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 69570 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 69570 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 78021 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 78021 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 105357 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 105357 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 78033 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 78033 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 193857 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 193857 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 67823 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 67823 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 78036 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 78036 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 193819 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 193819 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 104907 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 104907 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 105626 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 105626 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 7686 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 7686 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 7686 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 7686 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 58631 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 58631 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 65810 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 65810 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 173913 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 173913 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 78019 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 78019 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 78030 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 78030 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 67064 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 67064 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 66517 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 66517 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 105330 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 105330 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 171647 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 171647 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 105599 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 105599 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 72743 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 72743 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 72759 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 72759 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 72745 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 72745 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 78017 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 78017 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 78029 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 78029 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 105667 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 105667 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 78014 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 78014 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 66788 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 66788 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 68144 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 68144 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 195781 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 195781 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 72726 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 72726 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 78035 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 78035 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 117329 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 117329 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 170003 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 170003 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 65864 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 65864 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 66959 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 66959 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 67212 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 67212 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 105698 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 105698 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 67176 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 67176 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 72741 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 72741 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 66385 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 66385 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 185421 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 185421 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 68163 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 68163 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 78034 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 78034 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 105466 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 105466 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 72750 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 72750 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 193750 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 193750 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 70033 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 70033 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 50493 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 50493 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 67043 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 67043 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 67124 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 67124 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 78037 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 78037 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 185594 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 185594 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 66895 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 66895 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 105327 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 105327 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 117329 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 117329 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 193927 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 193927 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 8988 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 8988 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 8988 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 196250 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 196250 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 194779 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 194779 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 78032 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 78032 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 78043 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 78043 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 199872 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 199872 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 199428 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 199428 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 78020 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 78020 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 105241 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 105241 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 78039 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 78039 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 57786 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 57786 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 185478 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 185478 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 78041 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 78041 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 69569 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 69569 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 72752 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 72752 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 67158 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 67158 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 185419 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 185419 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 196146 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 196146 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 78018 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 78018 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 72748 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 72748 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 196170 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 196170 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 72747 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 72747 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 78031 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 78031 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 24317 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 24317 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 24352 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 24352 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 24383 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 24383 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 24316 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 24316 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 24414 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 24414 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 24561 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 24561 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 24351 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 24351 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 24213 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 24213 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 24413 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 24413 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 24451 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 24451 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 24524 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 24524 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 24214 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 24214 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 24251 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 24251 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 24252 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 24252 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 24523 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 24523 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 25872 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 25872 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 24452 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 24452 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 24488 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 24488 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 25871 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 25871 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 24562 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 24562 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 24382 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 24382 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 24594 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 24594 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 25886 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 25886 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 25906 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 25906 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 25999 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 25999 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 21781 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 21781 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 25939 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 25939 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 24176 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 24176 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 21784 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 21784 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 21825 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 21825 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 25887 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 25887 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 25973 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 25973 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 26000 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 26000 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 21782 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 21782 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 21795 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 21795 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 72751 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 72751 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 72749 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 72749 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 24286 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 24286 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 21763 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 21763 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 21770 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 21770 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 21771 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 21771 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 72756 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 72756 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 72758 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 72758 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 21826 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 21826 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 25851 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 25851 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 25923 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 25923 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 25956 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 25956 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 72746 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 72746 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 72744 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 72744 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 72744 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 72744 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 24489 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 24489 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 21764 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 21764 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 21808 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 21808 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 26110 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 26110 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 72757 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 72757 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 72743 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 72743 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 24068 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 24068 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 24068 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 24068 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 21806 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 21806 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 109715 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 109715 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 21761 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 21761 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 72741 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 72741 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 21827 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 21827 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 21827 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 21827 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 72759 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 72759 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 108541 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 108541 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 108541 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 25852 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 25852 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 25972 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 25972 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 72754 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 72754 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 21760 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 21760 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 21762 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 21762 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 25922 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 25922 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 72745 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 72745 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 72742 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 72742 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 211877 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 211877 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 25957 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 25957 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 21754 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 21754 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 72752 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 72752 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 72753 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 72753 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 21807 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 21807 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 21809 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 21809 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 25985 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 25985 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 21805 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 21805 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 26111 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 26111 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 72726 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 72726 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 72747 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 72747 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 170118 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 170118 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 24287 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 24287 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 21769 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 21769 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 21794 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 21794 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 21797 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 21797 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 25907 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 25907 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 25984 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 25984 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 74594 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 74594 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 21740 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 21740 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 211949 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 211949 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 21783 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 21783 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 72755 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 72755 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 72748 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 72748 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 21796 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 21796 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 26015 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 26015 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 25940 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 25940 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 72750 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 72750 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 7124 0 None 1 5 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12069595
1522 7124 0 None -1 5 Rat 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12069595
11589975 8455 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 8455 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 220199 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 220199 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 220199 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 220199 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 220185 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 220216 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 220147 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 220147 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 220185 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 220216 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 220292 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 220292 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 220246 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 220274 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 220246 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 220274 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 135260 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 135260 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 83677 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 83677 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 83680 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 83680 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 135263 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 135263 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 125756 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 125756 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 135258 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 135258 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 193983 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 193983 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 83576 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 83576 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 88123 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 88123 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 135257 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 135257 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 135262 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 135262 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 135264 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 135264 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 105239 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 105239 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 132220 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 132220 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 88121 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 88121 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 83690 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 83690 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 88114 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 88114 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 32361 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 32361 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 36159 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 36159 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 126060 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 126060 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 83686 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 83686 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 135255 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 135255 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 135256 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 135256 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 34991 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 34991 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 177584 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 177584 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 132230 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 132230 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 83669 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 83669 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 88118 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 88118 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 88118 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 88118 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 83666 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 83666 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 209566 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 209566 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 209566 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 209566 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 35084 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 35084 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 125991 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 125991 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 135271 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 135271 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 211926 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 211926 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 83676 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 83676 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 64928 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 64928 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 83684 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 83684 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 131180 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 131180 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 194459 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 194459 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 194459 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 194459 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 132232 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 132232 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 65907 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 65907 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 66729 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 66729 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 88112 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 88112 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 135275 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 135275 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 204379 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 204379 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 135279 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 135279 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 132219 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 132219 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 199841 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 199841 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 132229 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 132229 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 204991 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 204991 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 132231 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 132231 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 200080 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 200080 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 34570 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 34570 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 125342 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 125342 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 135269 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 135269 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 64347 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 64347 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 65907 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 65907 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 132217 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 132217 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 176116 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 176116 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 105303 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 105303 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 88122 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 88122 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 135267 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 135267 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 135272 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 135272 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 88127 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 88127 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 135257 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 135257 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 199866 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 199866 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 199866 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 199866 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 200203 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 200203 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 194526 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 194526 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 194822 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 194822 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 194013 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 194013 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 88126 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 88126 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 73929 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 73929 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 105684 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 105684 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 135262 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 135262 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 135261 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 135261 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 200019 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 200019 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 200019 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 200019 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 206505 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 206505 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 67326 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 67326 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 135265 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 135265 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 135268 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 135268 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 176164 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 176164 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 199386 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 199386 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 206849 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 206849 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 194348 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 194348 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 194348 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 194348 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 194469 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 194469 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 194469 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 194469 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 199384 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 199384 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 210822 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 210822 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 20815 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 20815 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 117366 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 117366 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 194817 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 194817 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 212438 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 212438 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 126705 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 126705 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 120092 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 120092 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 131824 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 131824 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 88129 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 88129 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 135276 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 135276 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 88125 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 88125 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 122199 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 122199 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 132228 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 132228 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 194534 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 194534 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 194621 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 194621 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 199938 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 199938 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 105309 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 105309 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 33096 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 33096 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 194687 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 194687 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 208608 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 208608 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 199972 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 199972 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 64900 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 64900 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 105309 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 105309 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 205161 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 205161 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 200260 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 200260 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 206748 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 206748 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 206822 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 206822 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 200073 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 200073 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 200080 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 200080 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 7686 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 7686 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 7686 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 7686 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 175968 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 175968 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 88119 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 88119 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 135259 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 135259 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 204832 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 204832 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 7686 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 7686 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 7686 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 7686 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 199841 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 199841 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 200094 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 200094 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 64863 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 64863 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 67185 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 67185 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 67326 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 67326 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 88124 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 88124 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 135270 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 135270 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 132224 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 132224 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 132225 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 132225 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 203860 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 203860 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 205692 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 205692 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 206564 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 206564 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 199834 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 199834 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 105684 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 105684 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 132211 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 132211 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 190983 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 190983 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 75672 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 75672 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 132576 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 132576 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 135280 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 135280 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 123508 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 123508 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 103731 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 103731 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 194650 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 194650 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 193848 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 193848 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 193927 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 193927 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 193927 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 193927 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 206599 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 206599 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 105562 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 105562 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 34800 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 34800 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 132222 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 132222 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 132227 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 132227 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 194634 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 194634 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 204802 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 204802 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 203838 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 203838 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 203867 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 203867 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 204420 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 204420 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 205747 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 205747 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 205758 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 205758 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 194533 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 194533 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 194652 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 194652 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 203867 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 203867 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 83685 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 83685 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 135281 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 135281 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 203839 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 203839 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 194759 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 194759 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 83672 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 83672 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 83687 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 83687 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 35325 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 35325 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 194746 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 194746 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 194801 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 194801 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 110190 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 110190 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 110189 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 110189 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 199854 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 199854 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 17784 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 17784 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 110220 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 110220 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 66426 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 66426 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 35020 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 35020 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 37449 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 37449 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 211639 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 211639 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 212480 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 212480 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 19659 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 19659 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 19659 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 105212 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 105212 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 64922 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 64922 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 190977 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 190977 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 193652 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 193652 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 168471 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 168471 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 199687 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 199687 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 19761 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 19761 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 19761 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 33055 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 33055 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 205231 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 205231 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 64883 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 64883 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 110200 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 110200 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 110206 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 110206 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 176194 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 176194 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 73706 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 73706 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 73908 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 73908 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 19911 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 19911 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 19911 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 55201 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 55201 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 83673 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 83673 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 194938 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 194938 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 104033 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 104033 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 210319 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 210319 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 35301 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 35301 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 109691 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 109691 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 92950 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 92950 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 19590 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 19590 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 19590 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 110267 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 110267 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 170875 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 170875 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 169351 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 169351 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 117389 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 117389 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 110227 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 110227 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 92935 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 92935 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 57041 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 57041 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 125575 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 125575 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 78129 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 78129 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 71117 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 71117 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 123454 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 123454 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 174586 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 174586 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 211765 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 211765 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 211949 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 211949 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 103840 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 103840 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 104139 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 104139 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 176014 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 176014 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 64915 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 64915 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 194839 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 194839 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 194048 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 194048 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 123423 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 123423 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 211741 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 211741 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 20698 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 20698 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 20698 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 70274 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 70274 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 19598 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 19598 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 19598 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 194564 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 194564 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 70245 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 70245 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 34803 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 34803 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 199919 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 199919 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 63938 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 63938 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 172908 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 172908 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 126027 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 126027 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 172142 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 172142 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 194882 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 194882 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 70539 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 70539 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 54818 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 54818 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 211605 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 211605 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 57860 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 57860 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 76266 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 76266 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 176490 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 176490 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 174558 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 174558 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 174558 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 174558 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 199875 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 199875 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 170121 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 170121 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 212390 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 212390 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 212391 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 212391 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 212641 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 212641 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 88116 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 88116 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 35019 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 35019 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 125557 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 125557 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 211749 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 211749 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 212144 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 212144 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 77216 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 77216 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 125959 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 125959 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 126843 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 126843 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 126843 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 126843 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 179860 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 179860 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 85130 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 85130 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 126000 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 126000 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 67128 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 67128 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 194248 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 194248 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 199444 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 199444 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 199912 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 199912 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 35401 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 35401 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 194547 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 194547 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 112599 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 112599 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 174831 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 174831 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 211839 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 211839 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 109933 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 109933 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 69560 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 69560 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 35223 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 35223 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 200140 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 200140 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 199975 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 199975 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 212365 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 212365 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 212457 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 212457 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 175465 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 175465 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 133074 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 133074 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 105303 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 105303 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 88115 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 88115 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 19648 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 19648 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 19648 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 126075 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 126075 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 108084 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 108084 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 54071 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 54071 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 109920 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 109920 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 33342 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 33342 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 212085 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 212085 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 212718 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 212718 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 193992 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 193992 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 212435 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 212435 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 71250 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 71250 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 199422 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 199422 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 112598 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 112598 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 110213 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 110213 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 71318 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 71318 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 58631 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 58631 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 58631 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 58631 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 34960 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 34960 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 126814 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 126814 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 88117 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 88117 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 112263 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 112263 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 20718 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 20718 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 20718 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 200118 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 200118 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 204625 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 204625 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 17804 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 17804 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 117365 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 117365 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 170239 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 170239 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 204024 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 204024 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 205721 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 205721 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 204024 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 204024 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 206600 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 206600 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 200067 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 200067 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 199851 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 199851 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 111059 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 111059 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 112404 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 112404 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 112759 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 112759 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 112905 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 112905 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 174803 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 174803 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 212371 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 212371 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 212383 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 212383 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 212453 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 212453 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 212738 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 212738 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 66729 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 66729 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 194347 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 194347 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 203976 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 203976 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 193651 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 193651 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 203976 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 203976 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 206910 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 206910 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 208146 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 208146 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 194347 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 194347 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 206822 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 206822 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 206849 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 206849 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 32513 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 32513 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 190980 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 190980 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 204629 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 204629 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 203584 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 203584 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 205532 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 205532 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 205723 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 205723 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 200152 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 200152 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 193801 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 193801 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 193852 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 193852 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 206880 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 206880 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 208634 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 208634 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 206819 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 206819 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 132226 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 132226 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 211401 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 211401 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 205712 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 205712 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 194528 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 194528 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 193645 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 193645 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 206819 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 206819 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 66313 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 66313 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 67185 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 67185 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 207922 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 207922 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 194800 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 194800 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 204834 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 204834 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 205235 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 205235 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 193927 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 193927 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 199958 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 199958 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 193849 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 193849 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 193877 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 193877 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 206716 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 206716 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 206749 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 206749 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 205287 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 205287 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 83689 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 83689 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 206597 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 206597 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 76808 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 76808 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 204627 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 204627 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 203618 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 203618 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 181420 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 181420 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 66313 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 66313 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 175968 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 175968 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 92951 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 92951 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 194635 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 194635 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 204962 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 204962 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 203586 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 203586 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 208527 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 208527 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 200035 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 200035 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 83675 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 83675 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 76357 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 76357 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 19671 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 19671 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 19671 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 204928 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 204928 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 208640 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 208640 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 70746 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 70746 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 66426 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 66426 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 92945 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 92945 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 132215 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 132215 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 132223 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 132223 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 7686 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 7686 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 7686 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 7686 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 205802 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 205802 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 194527 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 194527 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 205802 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 205802 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 206911 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 206911 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 7686 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 7686 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 7686 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 7686 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 111672 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 111672 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 105562 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 105562 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 92947 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 92947 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 126231 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 126231 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 200188 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 200188 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 110188 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 110188 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 210865 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 210865 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 194823 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 194823 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 193767 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 193767 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 212178 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 212178 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 212721 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 212721 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 19591 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 19591 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 19591 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 109715 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 109715 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 139264 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 139264 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 54625 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 54625 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 194017 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 194017 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 67105 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 67105 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 85358 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 85358 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 212527 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 212527 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 110217 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 110217 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 19639 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 19639 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 19639 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 83681 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 83681 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 67119 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 67119 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 126642 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 126642 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 174902 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 174902 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 112396 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 112396 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 112288 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 112288 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 119870 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 119870 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 108291 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 108291 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 92943 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 92943 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 35506 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 35506 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 123489 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 123489 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 175293 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 175293 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 70606 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 70606 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 16936 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 16936 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 109921 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 109921 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 193987 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 193987 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 193987 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 193987 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 212320 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 212320 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 110195 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 110195 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 20781 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 20781 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 20781 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 117396 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 117396 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 36164 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 36164 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 211493 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 211493 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 175917 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 175917 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 176286 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 176286 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 212136 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 212136 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 64324 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 64324 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 211854 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 211854 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 125561 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 125561 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 71320 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 71320 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 212388 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 212388 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 211658 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 211658 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 210741 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 210741 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 92937 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 92937 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 110917 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 110917 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 111169 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 111169 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 19951 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 19951 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 19951 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 108005 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 108005 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 34764 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 34764 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 194639 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 194639 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 34360 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 34360 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 173140 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 173140 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 212589 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 212589 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 206565 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 206565 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 19638 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 19638 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 19638 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 172987 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 172987 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 35481 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 35481 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 168613 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 168613 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 211727 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 211727 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 20279 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 20279 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 110214 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 110214 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 18415 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 18415 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 194241 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 194241 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 7299 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 7299 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 7299 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 175981 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 175981 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 35445 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 35445 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 200189 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 200189 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 212147 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 212147 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 165564 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 165564 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 179361 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 179361 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 53036 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 53036 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 36047 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 36047 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 211754 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 211754 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 33994 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 33994 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 211276 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 211276 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 112403 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 112403 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 170418 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 170418 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 211706 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 211706 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 111525 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 111525 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 34528 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 34528 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 132221 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 132221 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 194468 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 194468 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 200071 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 200071 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 205238 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 205238 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 17104 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 17104 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 117329 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 117329 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 174869 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 174869 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 203625 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 203625 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 194093 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 194093 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 194468 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 194468 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 200071 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 200071 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 104907 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 104907 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 111520 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 111520 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 212332 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 212332 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 212659 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 212659 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 88128 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 88128 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 135273 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 135273 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 203585 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 203585 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 199484 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 199484 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 211847 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 211847 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 204630 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 204630 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 205118 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 205118 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 132218 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 132218 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 204801 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 204801 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 193750 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 193750 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 170032 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 170032 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 204664 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 204664 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 205160 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 205160 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 199720 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 199720 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 194779 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 194779 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 199838 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 199838 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 135278 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 135278 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 190894 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 190894 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 63954 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 63954 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 92949 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 92949 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 132212 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 132212 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 105216 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 105216 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 204628 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 204628 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 194622 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 194622 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 206506 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 206506 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 29827 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 29827 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 211433 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 211433 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 195051 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 195051 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 19584 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 19584 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 19584 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 170341 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 170341 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 118164 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 118164 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 194271 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 194271 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 20748 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 20748 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 20748 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 77041 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 77041 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 109931 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 109931 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 175924 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 175924 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 76611 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 76611 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 83679 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 83679 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 63947 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 63947 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 35261 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 35261 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 60787 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 60787 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 92939 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 92939 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 35205 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 35205 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 104009 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 104009 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 194234 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 194234 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 128923 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 128923 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 171669 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 171669 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 19778 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 19778 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 123024 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 123024 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 110204 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 110204 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 110880 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 110880 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 17813 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 17813 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 210300 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 210300 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 211770 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 211770 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 117175 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 117175 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 119676 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 119676 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 199651 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 199651 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 211504 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 211504 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 109669 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 109669 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 123459 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 123459 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 179846 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 179846 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 107030 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 107030 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 200171 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 200171 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 176849 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 176849 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 211399 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 211399 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 212381 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 212381 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 172924 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 172924 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 63957 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 63957 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 212172 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 212172 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 83683 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 83683 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 34945 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 34945 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 211734 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 211734 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 186624 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 186624 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 186624 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 186624 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 83682 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 83682 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 108854 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 108854 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 108854 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 126937 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 126937 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 200057 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 200057 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 194046 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 194046 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 172414 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 172414 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 19599 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 19599 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 19599 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 20799 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 20799 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 71125 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 71125 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 194085 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 194085 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 110935 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 110935 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 171472 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 171472 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 212447 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 212447 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 212663 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 212663 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 111661 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 111661 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 111661 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 211852 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 211852 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 92946 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 92946 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 132213 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 132213 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 132216 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 132216 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 199955 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 199955 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 205063 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 205063 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 199955 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 199955 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 209453 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 209453 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 205105 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 205105 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 206883 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 206883 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 70644 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 70644 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 135274 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 135274 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 88120 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 88120 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 193819 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 193819 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 194020 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 194020 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 92938 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 92938 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 206599 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 206599 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 66031 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 66031 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 132214 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 132214 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 205804 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 205804 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 193879 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 193879 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 80223 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 80223 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 80223 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 80223 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 206748 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 206748 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 64863 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 64863 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 105216 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 105216 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 190984 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 190984 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 179541 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 179541 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 194301 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 194301 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 205104 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 205104 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 76596 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 76596 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 87933 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 87933 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 117118 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 117118 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 211206 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 211206 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 212103 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 212103 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 111672 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 111672 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 110205 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 110205 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 83678 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 83678 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 35058 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 35058 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 123575 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 123575 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 83668 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 83668 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 171941 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 171941 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 204835 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 204835 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 212086 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 212086 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 77682 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 77682 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 92940 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 92940 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 58366 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 58366 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 126115 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 126115 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 210675 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 210675 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 199891 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 199891 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 112633 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 112633 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 109860 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 109860 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 34461 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 34461 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 199978 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 199978 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 83671 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 83671 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 17820 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 17820 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 110203 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 110203 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 60546 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 60546 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 122271 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 122271 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 62352 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 62352 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 200053 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 200053 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 170279 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 170279 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 170118 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 170118 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 211849 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 211849 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 103812 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 103812 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 35108 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 35108 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 71384 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 71384 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 83667 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 83667 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 65996 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 65996 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 180139 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 180139 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 194434 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 194434 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 58846 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 58846 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 53781 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 53781 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 122134 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 122134 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 136435 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 136435 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 34859 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 34859 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 109857 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 109857 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 175834 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 175834 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 92952 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 92952 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 169266 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 169266 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 211726 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 211726 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 199959 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 199959 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 204631 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 204631 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 194295 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 194295 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 110952 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 110952 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 111672 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 111672 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 113913 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 113913 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 212171 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 212171 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 110216 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 110216 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 117170 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 117170 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 211930 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 211930 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 199872 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 199872 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 35867 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 35867 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 204833 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 204833 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 208622 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 208622 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 194047 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 194047 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 74333 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 74333 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 191106 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 191106 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 194651 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 194651 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 168554 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 168554 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 199428 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 199428 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 19697 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 19697 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 19697 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 19855 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 19855 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 19855 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 194912 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 194912 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 211887 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 211887 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 110357 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 110357 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 194864 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 194864 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 199858 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 199858 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 35930 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 35930 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 35297 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 35297 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 103786 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 103786 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 63920 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 63920 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 185463 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 185463 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 109803 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 109803 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 34953 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 34953 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 35056 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 35056 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 105654 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 105654 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 19724 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 19724 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 105654 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 105654 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 108932 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 108932 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 194233 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 194233 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 194272 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 194272 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 67285 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 67285 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 67285 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 126185 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 126185 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 126201 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 126201 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 63969 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 63969 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 134003 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 134003 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 194670 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 194670 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 64891 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 64891 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 35412 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 35412 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 199974 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 199974 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 129294 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 129294 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 125964 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 125964 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 210510 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 210510 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 211097 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 211097 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 211592 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 211592 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 83691 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 83691 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 194838 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 194838 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 126056 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 126056 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 175235 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 175235 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 194242 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 194242 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 125920 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 125920 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 111143 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 111143 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 111522 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 111522 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 212087 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 212087 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 212125 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 212125 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 212126 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 212126 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 212333 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 212333 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 212436 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 212436 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 212480 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 212480 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 173164 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 173164 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 130456 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 130456 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 205314 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 205314 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 194850 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 194850 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 67202 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 67202 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 193990 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 193990 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 173887 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 173887 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 83670 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 83670 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 211105 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 211105 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 211444 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 211444 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 211877 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 211877 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 195737 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 195737 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 193702 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 193702 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 88113 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 88113 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 210273 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 210273 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 19673 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 19673 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 19673 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 125930 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 125930 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 92953 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 92953 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 83674 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 83674 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 113913 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 113913 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 210818 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 210818 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 110582 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 110582 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 211659 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 211659 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 71149 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 71149 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 199436 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 199436 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 130862 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 130862 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 34796 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 34796 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 64216 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 64216 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 127245 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 127245 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 34851 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 34851 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 109944 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 109944 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 34621 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 34621 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 211551 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 211551 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 64225 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 64225 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 126695 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 126695 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 170221 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 170221 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 212367 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 212367 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 212589 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 212589 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 20614 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 20614 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 20614 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 117365 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 117365 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 20144 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 20144 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 171336 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 171336 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 212324 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 212324 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 212480 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 212480 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 110194 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 110194 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 204689 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 204689 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 92942 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 92942 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 194433 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 194433 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 168577 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 168577 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 193984 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 193984 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 204017 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 204017 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 193984 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 193984 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 83688 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 83688 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 70270 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 70270 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 199899 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 199899 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 51363 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 51363 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 70040 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 70040 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 199423 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 199423 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 211812 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 211812 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 117995 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 117995 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 211429 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 211429 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 112187 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 112187 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 211731 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 211731 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 17792 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 17792 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 62353 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 62353 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 34354 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 34354 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 32787 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 32787 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 35246 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 35246 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 121904 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 121904 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 200259 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 200259 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 171462 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 171462 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 64856 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 64856 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 110193 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 110193 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 173172 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 173172 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 123192 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 123192 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 37231 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 37231 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 110356 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 110356 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 106984 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 106984 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 211593 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 211593 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 211394 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 211394 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 19733 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 19733 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 19733 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 19401 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 19401 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 107186 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 107186 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 20388 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 20388 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 212031 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 212031 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 172685 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 172685 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 34592 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 34592 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 126199 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 126199 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 211383 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 211383 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 59509 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 59509 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 18064 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 18064 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 199902 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 199902 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 20704 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 20704 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 20704 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 109950 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 109950 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 193989 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 193989 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 107362 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 107362 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 32512 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 32512 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 199865 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 199865 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 20728 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 20728 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 20728 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 205187 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 205187 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 211415 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 211415 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 92936 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 92936 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 211701 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 211701 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 16902 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 16902 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 176203 4 None -309 9 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 176203 4 None -309 9 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 126828 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 126828 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 212485 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 212485 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 175359 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 175359 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 194881 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 194881 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 125994 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 125994 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 191105 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 191105 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 63274 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 63274 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 34377 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 34377 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 171635 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 171635 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 126891 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 126891 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 19751 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 19751 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 19751 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 36220 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 36220 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 77869 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 77869 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 70281 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 70281 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 130687 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 130687 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 129713 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 129713 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 129713 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 129713 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 109418 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 109418 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 204929 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 204929 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 211893 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 211893 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 73774 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 73774 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 67202 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 67202 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 198457 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 198457 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 194501 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 194501 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 190951 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 190951 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 92944 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 92944 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 20713 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 20713 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 20713 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 194012 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 194012 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 194012 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 194012 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 210603 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 210603 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 109679 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 109679 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 194588 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 194588 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 193824 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 193824 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 85294 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 85294 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 126852 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 126852 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 195635 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 195635 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 35365 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 35365 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 211845 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 211845 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 212249 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 212249 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 92948 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 92948 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 92941 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 92941 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 212354 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 212354 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 73951 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 73951 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 209515 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 209515 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 72144 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 72144 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 80087 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 80087 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 220229 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 220229 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 162148 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 162148 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 220199 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 220199 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 80079 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 80079 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 220199 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 220199 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 72147 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 72147 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 220152 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 220243 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 220152 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 220243 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 80258 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 80258 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 162363 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 162363 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 80224 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 80224 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 72146 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 72146 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 199480 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 199480 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 72150 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 72150 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 206999 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 206999 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 80266 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 80266 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 72150 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 72150 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 72145 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 72145 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 80077 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 80077 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 80089 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 80089 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 80092 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 80092 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 80265 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 80265 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 72144 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 72144 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 193756 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 193756 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 199947 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 199947 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 80088 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 80088 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 19470 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 19470 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 19470 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 80083 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 80083 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 173571 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 173571 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 61922 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 61922 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 61922 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 61922 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 80091 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 80091 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 101860 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 101860 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 220169 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 193857 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 193857 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 220169 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 193857 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 193857 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 73391 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 73391 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 73391 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 193669 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 193669 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 193669 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 193669 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 107809 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 107809 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 80082 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 80082 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 80085 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 80085 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 162238 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 162238 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 220180 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 117993 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 117993 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 220180 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 206822 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 206822 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 193720 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 193720 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 61922 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 61922 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 80086 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 80086 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 74596 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 74596 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 72148 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 72148 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 19403 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 19403 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 19403 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 80084 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 80084 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 102419 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 102419 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 74780 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 74780 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 19404 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 19404 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 19404 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 209522 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 209522 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 220147 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 80261 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 80261 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 112497 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 112497 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 80078 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 80078 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 126853 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 126853 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 86271 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 86271 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 196471 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 196471 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 220236 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 220249 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 220257 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 220155 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 220193 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 220275 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 193313 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 193313 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 108629 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 108629 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 108303 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 108303 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 74765 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 74765 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 107516 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 107516 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 80269 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 80269 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 69562 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 69562 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 197926 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 197926 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 74776 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 74776 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 72152 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 72152 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 74782 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 74782 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 215992 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 120742 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 120742 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 217253 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 74766 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 74766 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 109503 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 109503 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 112496 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 112496 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 177762 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 177762 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 80095 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 80095 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 59086 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 59086 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 193306 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 193306 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 220185 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 175767 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 175767 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 175767 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 220189 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 220216 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 220265 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 220289 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 69291 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 69291 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 101859 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 101859 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 220185 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 162183 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 162183 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 175767 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 175767 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 175767 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 220189 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 220216 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 220265 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 220289 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 209514 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 209514 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 124078 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 124078 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 72155 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 72155 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 185421 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 185421 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 195781 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 195781 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 168770 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 168770 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 195986 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 195986 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 145984 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 145984 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 145984 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 117319 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 117319 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 193815 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 193815 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 22355 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 22355 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 107854 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 107854 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 109058 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 109058 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 169572 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 169572 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 220178 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 220247 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 74763 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 74763 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 74773 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 74773 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 177768 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 177768 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 108326 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 108326 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 118095 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 118095 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 220222 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 74783 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 74783 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 207271 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 207271 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 121218 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 121218 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 220178 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 220247 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 85130 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 85130 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 220222 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 102171 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 102171 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 104799 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 104799 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 217260 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 185594 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 185594 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 220772 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 108451 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 108451 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 220772 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 74599 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 74599 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 74768 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 74768 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 72151 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 72151 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 74588 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 74588 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 80264 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 80264 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 74784 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 74784 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 20501 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 20501 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 72138 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 72138 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 72135 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 72135 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 185501 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 185501 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 185333 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 185333 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 108524 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 108524 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 220262 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 220276 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 220208 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 74591 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 74591 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 112488 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 112488 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 199851 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 199851 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 200054 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 200054 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 80096 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 80096 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 101825 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 101825 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 9583 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 200028 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 200028 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 80090 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 80090 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 220316 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 80263 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 80263 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 193927 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 193927 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 101825 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 101825 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 193816 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 193816 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 193921 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 193921 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 205663 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 205663 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 69479 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 69479 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 199904 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 199904 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 102203 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 102203 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 69569 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 69569 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 69570 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 69570 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 102352 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 102352 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 59054 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 59054 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 69566 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 69566 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 220633 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 196170 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 196170 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 162352 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 162352 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 220262 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 220276 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 72136 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 72136 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 220208 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 107761 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 107761 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 21321 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 21321 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 72141 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 72141 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 116929 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 116929 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 72137 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 72137 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 179081 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 179081 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 208534 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 208534 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 185553 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 185553 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 80259 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 80259 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 145985 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 145985 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 145985 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 145985 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 182429 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 182429 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 72140 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 72140 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 120564 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 120564 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 108125 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 108125 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 80270 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 80270 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 168477 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 168477 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 168477 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 185308 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 185308 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 74778 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 74778 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 220309 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 171647 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 171647 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 220309 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 74771 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 74771 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 220209 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 220209 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 197848 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 197848 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 61706 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 61706 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 21234 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 21234 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 72133 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 72133 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 162333 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 162333 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 74777 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 74777 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 69481 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 69481 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 108801 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 108801 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 145994 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 145994 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 145994 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 196250 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 196250 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 74592 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 74592 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 112490 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 112490 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 199970 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 199970 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 199473 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 199473 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 220292 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 220292 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 193922 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 193922 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 173850 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 173850 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 174199 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 174199 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 74785 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 74785 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 108782 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 108782 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 69563 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 69563 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 72149 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 72149 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 102353 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 102353 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 23072 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 23072 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 72145 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 72145 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 80080 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 80080 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 171647 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 171647 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 69568 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 69568 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 193891 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 193891 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 74589 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 74589 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 69564 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 69564 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 72149 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 72149 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 220269 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 21329 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 21329 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 193833 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 193833 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 21425 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 21425 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 80271 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 80271 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 101941 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 101941 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 74781 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 74781 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 220283 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 104838 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 104838 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 164444 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 164444 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 220303 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 65996 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 65996 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 220283 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 168770 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 168770 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 220303 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 8988 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 8988 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 8988 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 8988 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 8988 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 8988 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 60610 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 60610 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 74590 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 74590 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 21337 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 21337 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 118144 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 118144 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 185478 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 185478 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 196146 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 196146 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 189087 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 189087 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 162364 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 162364 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 69484 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 69484 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 185419 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 185419 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 185601 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 185601 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 74775 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 74775 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 117404 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 117404 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 72157 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 72157 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 74597 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 74597 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 170013 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 170013 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 109401 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 109401 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 220183 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 220220 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 220274 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 21642 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 21642 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 220269 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 112492 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 112492 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 80081 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 80081 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 193670 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 193670 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 69561 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 69561 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 193819 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 193819 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 72158 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 72158 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 80268 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 80268 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 107768 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 107768 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 69567 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 69567 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 21458 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 21458 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 120602 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 120602 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 120701 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 120701 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 220183 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 220220 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 220274 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 181042 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 181042 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 101865 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 101865 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 169578 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 169578 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 112498 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 112498 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 185602 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 185602 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 108505 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 108505 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 193650 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 193650 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 69478 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 69478 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 72134 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 72134 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 108057 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 108057 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 107492 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 107492 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 74774 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 74774 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 74769 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 74769 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 57481 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 57481 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 194978 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 194978 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 180405 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 180405 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 219845 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 17245 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 17245 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 104384 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 104384 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 74770 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 74770 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 80223 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 80223 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 69565 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 69565 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 112486 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 112486 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 112493 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 112493 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 112494 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 112494 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 193668 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 193668 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 80093 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 80093 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 200037 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 200037 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 102258 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 102258 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 220211 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 220211 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 102111 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 102111 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 74423 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 74423 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 74593 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 74593 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 220145 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 220170 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 220145 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 220170 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 103635 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 103635 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 220270 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 74587 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 74587 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 102418 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 102418 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 161988 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 161988 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 21323 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 21323 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 74767 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 74767 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 182217 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 182217 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 171804 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 171804 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 162118 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 162118 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 175235 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 175235 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 188425 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 188425 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 12788 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 12788 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 112487 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 112487 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 102303 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 102303 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 69571 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 69571 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 69482 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 69482 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 72139 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 72139 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 74600 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 74600 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 72154 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 72154 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 69477 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 69477 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 217252 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 59206 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 59206 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 217832 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 220172 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 220192 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 69925 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 69925 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 69925 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 220172 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 220192 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 219644 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 121271 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 121271 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 112491 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 112491 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 69559 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 69559 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 171647 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 171647 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 69476 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 69476 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 161839 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 161839 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 74594 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 74594 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 185449 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 185449 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 179968 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 179968 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 179968 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 220586 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 112501 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 112501 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 193560 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 193560 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 195723 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 195723 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 199971 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 199971 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 86420 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 86420 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 74764 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 74764 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 74598 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 74598 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 166261 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 166261 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 166261 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 220154 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 220154 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 220246 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 220284 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 220310 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 220246 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 220284 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 220310 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 104402 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 104402 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 74779 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 74779 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 209341 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 209341 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 117408 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 117408 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 80262 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 80262 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 112489 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 112489 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 112500 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 112500 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 108541 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 108541 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 108541 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 107362 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 107362 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 72143 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 72143 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 69572 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 69572 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 69480 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 69480 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 69483 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 69483 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 193820 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 193820 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 104839 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 104839 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 80094 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 80094 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 74772 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 74772 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 58883 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 58883 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 74595 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 74595 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 185579 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 185579 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 104401 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 104401 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 80267 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 80267 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 195968 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 195968 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 80260 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 80260 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 72153 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 72153 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 162131 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 162131 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 112495 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 112495 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 112499 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 112499 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 72156 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 72156 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 60959 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 60959 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 107848 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 107848 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 185552 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 185552 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 200036 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 200036 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 72142 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 72142 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 222835 0 125I-hPP -295 13 Rat 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase None None None None None
126455957 222833 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 222837 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 220199 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 220199 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 7686 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 7686 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 7686 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 7686 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 222835 0 3H-Propionyl-NPY -1318 13 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase None None None None None
21129772 176203 4 125I-PYY -309 9 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 176203 4 125I-PYY -309 9 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 176203 4 125I-hPP -309 9 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 176203 4 125I-PYY -309 9 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 176203 4 125I-PYY -309 9 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 176203 4 125I-hPP -309 9 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 222835 0 125I-PYY -331131 13 Mouse 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase None None None None None
None 223014 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 223207 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 222835 0 125I-PYY -1318 13 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222837 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 222835 0 125I-PYY -295 13 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase None None None None None
None 222837 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 220199 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 220199 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 222837 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 8988 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 8988 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 8988 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 9084 0 None -25 5 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1549 9663 0 None -1 5 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1549 9663 0 None -1 5 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817422 9663 0 None -1 5 Human 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817422 9663 0 None -1 5 Rat 8.9 pKi = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1504 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1518 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1521 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
24868177 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44288922 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
77068007 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
90479759 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL438945 9583 8 None -9 10 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1504 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1518 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1521 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
24868177 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44288922 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
77068007 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
90479759 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL438945 9583 8 None -3 10 Rat 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1557 9660 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44328226 9660 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL439478 9660 0 None -3 3 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1529 8632 0 None -31622 5 Rat 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1513 9774 0 None -19952 6 Human 6.4 pKi None 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1513 9774 0 None -15848 6 Rat 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1557 9660 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44328226 9660 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL439478 9660 0 None 3 3 Rat 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1516 10016 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1516 10016 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
57339564 10016 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
57339564 10016 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91898411 10016 0 None -100 5 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91898411 10016 0 None -100 5 Rat 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1507 9658 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44351001 9658 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91929182 9658 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL265849 9658 0 None -38 7 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1565 8988 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 8988 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 8988 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 9658 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
44351001 9658 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
91929182 9658 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL265849 9658 0 None -15 7 Rat 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1510 9666 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817418 9666 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
16142730 9666 0 None -15 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1512 9777 0 None -501 6 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1554 10018 0 None -2 3 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1544 8282 0 None -1 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1544 8282 0 None 1 4 Rat 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1564 8893 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 8893 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 7123 0 None - 1 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1554 10018 0 None 2 3 Rat 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1527 9084 0 None -31 5 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1510 9666 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
155817418 9666 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
16142730 9666 0 None -3 6 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1561 9929 0 None - 1 Human 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1512 9777 0 None -70 6 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1512 9777 0 None -70 6 Rat 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1515 9826 0 None -19 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL269503 9826 0 None -19 6 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1524 9083 0 None -1 3 Rat 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12890716
1524 9083 0 None -1 3 Rat 9.0 pKi None 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1515 9826 0 None -15 6 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
CHEMBL269503 9826 0 None -15 6 Rat 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1524 9083 0 None 1 3 Human 9.1 pKi None 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8824284
1562 7686 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 7686 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 7686 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 7686 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