Ligand source activities (1 row/activity)





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

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

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

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

CHEMBL4127525 219801 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4126812 219795 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)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](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4129347 219815 0 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4226634 220084 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4128194 219808 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4130225 219825 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4227180 220088 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(N)=O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4225594 220077 0 None -28 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
CHEMBL4224968 220072 0 None -11 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4126027 219787 0 None -74 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4128125 219807 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4226185 220079 0 None -41 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4225795 220078 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
163242286 199694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assayPositive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assay
ChEMBL 504 8 2 4 8.1 COc1ccc2c(c1-c1cc(F)c(O)c(NCC(C)C)c1)CCN(C(C)c1ccc(C(C)C)cc1)[C@@H]2C 10.1021/acsmedchemlett.2c00220
CHEMBL5196841 199694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assayPositive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assay
ChEMBL 504 8 2 4 8.1 COc1ccc2c(c1-c1cc(F)c(O)c(NCC(C)C)c1)CCN(C(C)c1ccc(C(C)C)cc1)[C@@H]2C 10.1021/acsmedchemlett.2c00220
CHEMBL5222174 199694 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Positive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assayPositive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assay
ChEMBL 504 8 2 4 8.1 COc1ccc2c(c1-c1cc(F)c(O)c(NCC(C)C)c1)CCN(C(C)c1ccc(C(C)C)cc1)[C@@H]2C 10.1021/acsmedchemlett.2c00220
CHEMBL4130148 219824 0 None -37 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.8b00292
CHEMBL4130044 219819 0 None -3388 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.8b00292
CHEMBL4126738 219792 0 None -70 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)[C@H](CCN[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4126953 219796 0 None -74 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4224701 220068 0 None -30 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4226514 220082 0 None -144 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4225340 220074 0 None -69 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4229251 220095 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(=O)O 10.1016/j.bmc.2017.10.047
163242274 197628 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assayPositive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assay
ChEMBL 447 5 1 3 7.3 COc1ccc2c(c1-c1cc(C)c(O)c(F)c1)CCN(C(C)c1ccc(C(C)C)cc1)[C@@H]2C 10.1021/acsmedchemlett.2c00220
CHEMBL5184469 197628 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Positive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assayPositive allosteric modulator activity at human GIPR expressed in HEK293 cells assessed as potentiation of intracellular cAMP accumulation incubated for 30 mins in presence of GIPR agonist GIP(I-42) by HTRF assay
ChEMBL 447 5 1 3 7.3 COc1ccc2c(c1-c1cc(C)c(O)c(F)c1)CCN(C(C)c1ccc(C(C)C)cc1)[C@@H]2C 10.1021/acsmedchemlett.2c00220
CHEMBL4227861 220093 0 None -38 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
CHEMBL4226451 220081 0 None -371 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)CN(C)C(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL4226613 220083 0 None -288 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
CHEMBL4227045 220087 0 None -316 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GIP receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
122189709 130154 0 None -239 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616688 130154 0 None -239 2 Human 6.0 pIC50 = 6 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
11570626 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
122189708 130153 0 None -213 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616687 130153 0 None -213 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
57403703 75745 0 None -41 3 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922842 75745 0 None -41 3 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11585452 88165 0 None -47 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159338 88165 0 None -47 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
11950972 168011 0 None -3 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411832 168011 0 None -3 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11952214 93594 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232242 93594 0 None -6 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
44431020 174418 0 None -123 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL430163 174418 0 None -123 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
122189722 130168 0 None -295 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616701 130168 0 None -295 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
16100296 209618 46 None -23 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL62444 209618 46 None -23 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
11952211 94726 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL234087 94726 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60171059 88177 0 None -407 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159349 88177 0 None -407 4 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
122189577 130125 0 None -588 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616588 130125 0 None -588 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
54765285 75770 0 None -128 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIP receptor assessed as inhibition of cAMP productionAntagonist activity at human GIP receptor assessed as inhibition of cAMP production
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922933 75770 0 None -128 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GIP receptor assessed as inhibition of cAMP productionAntagonist activity at human GIP receptor assessed as inhibition of cAMP production
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
54765284 75743 0 None -165 3 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922840 75743 0 None -165 3 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57391489 75744 0 None -141 3 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922841 75744 0 None -141 3 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
60171062 88180 0 None -104 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159352 88180 0 None -104 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11950795 93593 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232241 93593 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11950794 168010 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411831 168010 0 None -5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60170970 88175 0 None -199 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159347 88175 0 None -199 4 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11678967 88157 0 None -29 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
CHEMBL2159330 88157 0 None -29 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
11949739 168012 0 None -57 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411833 168012 0 None -57 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60171061 88179 0 None -114 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159351 88179 0 None -114 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
53469443 117084 1 None -63 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR assessed as inhibition of cAMP productionAntagonist activity at human GIPR assessed as inhibition of cAMP production
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238246 117084 1 None -63 3 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR assessed as inhibition of cAMP productionAntagonist activity at human GIPR assessed as inhibition of cAMP production
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10324097 63636 0 None -15 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643955 63636 0 None -15 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
11950971 157683 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL395759 157683 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60170971 88176 0 None -263 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159348 88176 0 None -263 3 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
10436553 63634 0 None 1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643953 63634 0 None 1 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
11950075 93589 0 None -9 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232224 93589 0 None -9 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11444850 75742 0 None -54 3 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922839 75742 0 None -54 3 Human 6.5 pIC50 = 6.5 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11952035 158249 0 None -3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL396215 158249 0 None -3 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10053841 63698 0 None -85 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644182 63698 0 None -85 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
57518490 88164 0 None -56 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159337 88164 0 None -56 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
60170767 88154 0 None -54 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159327 88154 0 None -54 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
11952394 93787 0 None -660 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232448 93787 0 None -660 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11331120 75737 0 None -81 3 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922834 75737 0 None -81 3 Human 6.4 pIC50 = 6.4 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11585375 88166 0 None -30 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159339 88166 0 None -30 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
53323247 63633 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 444 6 1 4 6.2 O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643952 63633 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 444 6 1 4 6.2 O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11949740 163504 0 None -194 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL407028 163504 0 None -194 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10054055 79095 12 None -7 3 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulationInhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulation
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198387 79095 12 None -7 3 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulationInhibitory concentration against human gastric inhibitory polypeptide receptor (hGIP) mediated cAMP accumulation
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
60170857 88170 0 None -56 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159342 88170 0 None -56 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11699553 88155 0 None -72 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
CHEMBL2159328 88155 0 None -72 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
11952035 93592 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232239 93592 0 None -10 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
23550062 63632 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1643951 63632 0 None -3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
60170855 88162 0 None -15 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159335 88162 0 None -15 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
60171060 88178 0 None -158 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159350 88178 0 None -158 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
11456187 75738 2 None -40 3 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922835 75738 2 None -40 3 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GIP receptor by cAMP assayInhibition of human GIP receptor by cAMP assay
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11757679 63694 0 None -54 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1644178 63694 0 None -54 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
164616962 191972 0 None -141 6 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GIPR expressed in HEK293 cells assessed as inhibition of GIP-induced cAMP productionAntagonist activity at human GIPR expressed in HEK293 cells assessed as inhibition of GIP-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857523 191972 0 None -141 6 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GIPR expressed in HEK293 cells assessed as inhibition of GIP-induced cAMP productionAntagonist activity at human GIPR expressed in HEK293 cells assessed as inhibition of GIP-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
10077369 63704 0 None -14 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644188 63704 0 None -14 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
11952211 160520 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL398180 160520 0 None -7 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11952213 93533 0 None -2 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232037 93533 0 None -2 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIP receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
9985625 63699 0 None -89 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
CHEMBL1644183 63699 0 None -89 5 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
10415723 63700 0 None -63 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644184 63700 0 None -63 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11657413 88158 0 None -44 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
CHEMBL2159331 88158 0 None -44 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
11756248 63689 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644173 63689 0 None -6 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
122189714 130159 0 None -301 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616693 130159 0 None -301 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assayAntagonist activity against human glucose dependent insulinotropic peptide receptor by cAMP accumulation assay
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
9985625 63699 0 None -89 5 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None -89 5 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
60170856 88169 0 None -128 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159341 88169 0 None -128 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11527207 88168 0 None -81 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
CHEMBL2159340 88168 0 None -81 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
11592461 88171 0 None -64 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159343 88171 0 None -64 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
10097880 63635 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643954 63635 0 None -1 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11621378 88181 3 None -131 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159353 88181 3 None -131 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
13316 9239 0 None -346 4 Rat 6.1 pIC50 = 6.1 Functional
<i>In vitro</i> potency in GIPR recombinant cells<i>In vitro</i> potency in GIPR recombinant cells
Guide to Pharmacology None None None None 38316982
13316 9239 0 None -17 4 Human 7.4 pIC50 = 7.4 Functional
<i>In vitro</i> potency in GIPR recombinant cells<i>In vitro</i> potency in GIPR recombinant cells
Guide to Pharmacology None None None None 38316982
8970 8731 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Measuring <i>in vitro</i> inhibition of native GIP-induced cAMP accumulation at [GIP] of 10 pM and 1 nM.Measuring <i>in vitro</i> inhibition of native GIP-induced cAMP accumulation at [GIP] of 10 pM and 1 nM.
Guide to Pharmacology None None None None 16608883
11570626 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
9135 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
CHEMBL1933349 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
DB12044 9328 46 None -63 9 Human 6.0 pIC50 = 6.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
11998 9305 0 None -24 2 Mouse 6.6 pIC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35710141
11998 9305 0 None 24 2 Human 8.0 pIC50 = 8.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 35710141
3542 8548 0 None - 1 Rat 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399
1128 8580 0 None - 1 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399
155817389 8580 0 None - 1 Rat 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399
1130 8582 0 None - 1 Rat 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399
1129 8581 0 None - 1 Rat 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399
155817390 8581 0 None - 1 Rat 8.5 pIC50 None 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9226399




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

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

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

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

2540 11173 111 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GIPR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GIPR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 11173 111 None - 4 Human 4.7 pAC50 = 4.7 Binding
Binding affinity towards human GIPR in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GIPR in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL5072364 221058 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(C)C)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C nan
CHEMBL5077951 221304 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C)C(C)C nan
CHEMBL5075905 221182 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C nan
CHEMBL5087366 221868 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(N)=O)C(C)C)[C@@H](C)CC nan
CHEMBL5090950 222065 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C nan
CHEMBL5083589 221651 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(N)=O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)C(C)C nan
11410779 195010 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL499372 195010 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
22496431 176605 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 647 11 2 5 9.6 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(Cl)cc3)c(-c3ccccc3)s2)cc1 10.1021/jm8016249
CHEMBL443971 176605 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 647 11 2 5 9.6 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(Cl)cc3)c(-c3ccccc3)s2)cc1 10.1021/jm8016249
22496459 194021 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
9985258 185762 10 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
22496373 194281 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.4 O=C(O)CCNC(=O)c1ccc(CN(c2nc(-c3ccc(Cl)c(Cl)c3)cs2)C2CCCc3ccccc32)cc1 10.1021/jm8016249
CHEMBL494248 194281 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.4 O=C(O)CCNC(=O)c1ccc(CN(c2nc(-c3ccc(Cl)c(Cl)c3)cs2)C2CCCc3ccccc32)cc1 10.1021/jm8016249
10167904 180437 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 615 10 4 5 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL453457 180437 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 615 10 4 5 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
164616962 191972 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Antagonist activity at mouse GIPR expressed in CHO-K1 cells assessed as inhibition of GIP-induced cAMP productionAntagonist activity at mouse GIPR expressed in CHO-K1 cells assessed as inhibition of GIP-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857523 191972 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Antagonist activity at mouse GIPR expressed in CHO-K1 cells assessed as inhibition of GIP-induced cAMP productionAntagonist activity at mouse GIPR expressed in CHO-K1 cells assessed as inhibition of GIP-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
CHEMBL5088990 221966 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C nan
9914410 193236 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 513 9 4 4 5.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccccc2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487662 193236 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 513 9 4 4 5.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccccc2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
9916972 181808 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 613 10 4 5 6.2 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL456738 181808 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 613 10 4 5 6.2 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
10282370 195476 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 608 9 4 5 6.0 N#Cc1ccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc1C(F)(F)F 10.1021/jm7015599
CHEMBL504245 195476 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 608 9 4 5 6.0 N#Cc1ccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc1C(F)(F)F 10.1021/jm7015599
CHEMBL5078233 221324 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C)C(C)C nan
11169089 195075 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL500315 195075 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
22496365 195632 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 621 11 2 6 8.2 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL506800 195632 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 621 11 2 6 8.2 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496384 193926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL491920 193926 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10257357 148616 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL386446 148616 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10282059 180003 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 593 9 4 4 5.9 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Br)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL452311 180003 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 593 9 4 4 5.9 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Br)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
10369510 179897 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 523 8 4 4 5.1 Cc1cc(C)cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)c1 10.1021/jm7015599
CHEMBL452067 179897 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 523 8 4 4 5.1 Cc1cc(C)cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)c1 10.1021/jm7015599
44561438 196182 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL513067 196182 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
10282162 179200 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 599 9 4 4 6.2 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(F)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL447684 179200 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 599 9 4 4 6.2 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(F)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10145603 195849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 611 10 4 5 6.1 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL509710 195849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 611 10 4 5 6.1 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
16100296 79187 46 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
CHEMBL198736 79187 46 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
44561439 197980 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL518939 197980 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
22496449 181216 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496557 200040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL523847 200040 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
44561556 196058 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
CHEMBL511964 196058 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
10145290 180002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 595 10 3 4 7.0 CO[C@H](CNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1)C(=O)O 10.1021/jm7015599
CHEMBL452310 180002 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 595 10 3 4 7.0 CO[C@H](CNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1)C(=O)O 10.1021/jm7015599
10210150 192551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 573 9 4 5 5.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
CHEMBL486650 192551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 573 9 4 5 5.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
22496448 194100 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL493020 194100 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
22496457 179337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448561 179337 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
11249762 190620 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL480692 190620 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
10032265 193101 1 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487476 193101 1 None - 1 Human 6.5 pIC50 = 6.5 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
22496371 176705 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 605 10 2 5 8.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL444126 176705 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 605 10 2 5 8.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL5089388 221985 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C)C(C)C)C(C)C nan
11764614 195470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL504156 195470 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
16100334 90149 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
CHEMBL219384 90149 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
10211765 177713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 659 9 4 4 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Br)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL445532 177713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 659 9 4 4 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Br)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
22496384 193926 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL491920 193926 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
9871912 199403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 537 10 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccccc3)cs2)cc1 10.1021/jm8016249
CHEMBL521650 199403 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 537 10 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccccc3)cs2)cc1 10.1021/jm8016249
22496477 179556 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL451288 179556 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10257629 194054 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL5078651 221353 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assayBinding affinity towards GIP receptor in human HEK293 cells measured by fluorescence assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)C(C)C)C(C)C)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](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](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)C(C)C nan
10280734 199261 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 547 9 4 4 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL520893 199261 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 547 9 4 4 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10030697 185853 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10144347 201171 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 561 10 4 5 5.9 CSc1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
CHEMBL528775 201171 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 561 10 4 5 5.9 CSc1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
16100296 79187 46 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
CHEMBL198736 79187 46 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
22496358 194098 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL493019 194098 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10144925 198625 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL519903 198625 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10053886 198543 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10393937 195167 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496449 181216 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
11376210 190371 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
CHEMBL480113 190371 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
10211943 180021 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 675 11 4 7 5.4 CS(=O)(=O)c1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)ccc1OC(F)(F)F 10.1021/jm7015599
CHEMBL452451 180021 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 675 11 4 7 5.4 CS(=O)(=O)c1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)ccc1OC(F)(F)F 10.1021/jm7015599
10032265 193101 1 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487476 193101 1 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity to GIPR in rat liver membraneBinding affinity to GIPR in rat liver membrane
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
22496459 194021 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496457 179337 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448561 179337 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
22496477 179556 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL451288 179556 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
42617999 195154 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 624 10 3 6 6.3 O=C(NC[C@@H](O)C(=O)O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501392 195154 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 624 10 3 6 6.3 O=C(NC[C@@H](O)C(=O)O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496546 195231 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 649 10 2 5 8.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL502694 195231 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 649 10 2 5 8.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cs2)ccc1C(C)C 10.1021/jm8016249
11599295 190580 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL480501 190580 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human GIPBinding affinity against human GIP
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
22496557 200040 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL523847 200040 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
20775916 193868 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 7.1 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL491352 193868 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 7.1 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
10257357 148616 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL386446 148616 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
20776097 176220 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 613 9 2 5 7.9 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL442651 176220 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 613 9 2 5 7.9 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10030697 185853 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10231964 192535 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NCC(O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL486634 192535 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NCC(O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
22496412 179483 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 593 10 2 5 8.6 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C4=CCCCC4)cc3)n2)cc1 10.1021/jm8016249
CHEMBL450411 179483 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 593 10 2 5 8.6 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C4=CCCCC4)cc3)n2)cc1 10.1021/jm8016249
22496395 194127 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 569 9 2 5 7.9 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)n2)cc1 10.1021/jm8016249
CHEMBL493233 194127 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 569 9 2 5 7.9 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)n2)cc1 10.1021/jm8016249
20776096 179340 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448584 179340 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10144633 179206 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 571 9 4 4 6.4 CC(C)(C)c1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
CHEMBL447742 179206 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 571 9 4 4 6.4 CC(C)(C)c1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
22496445 178585 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assayBinding affinity to human recombinant GIPR expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496451 184797 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 625 10 2 6 8.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(SC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL464663 184797 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 625 10 2 6 8.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(SC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10168348 181167 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 643 9 4 6 6.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc3c(c2)C(F)(F)OC(F)(F)O3)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL455214 181167 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 643 9 4 6 6.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc3c(c2)C(F)(F)OC(F)(F)O3)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10257629 194054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
10393937 195167 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10053886 198543 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
11764615 194991 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL499160 194991 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
16100300 144017 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL375167 144017 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
10232009 193240 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 583 9 4 4 6.5 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487668 193240 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 583 9 4 4 6.5 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
22496445 178585 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10483282 192552 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 577 8 4 4 5.8 Cc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL486651 192552 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human cloned GIPR expressed in BHK cellsBinding affinity to human cloned GIPR expressed in BHK cells
ChEMBL 577 8 4 4 5.8 Cc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc(C(F)(F)F)c1 10.1021/jm7015599
9985258 185762 10 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine GIP from human recombinant GIPR receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
57393426 76217 0 None -30 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933365 76217 0 None -30 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
57393425 76215 0 None -54 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933363 76215 0 None -54 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
57391686 76216 0 None -44 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933364 76216 0 None -44 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
57391686 76216 0 None -44 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933364 76216 0 None -44 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
57396928 76212 0 None -11 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933360 76212 0 None -11 3 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
57393426 76217 0 None -30 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933365 76217 0 None -30 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
57396928 76212 0 None -11 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933360 76212 0 None -11 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]GIP from human GIPRDisplacement of [125I]GIP from human GIPR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
8970 8731 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity for the human receptor expressed in COS7 cells.Binding affinity for the human receptor expressed in COS7 cells.
Guide to Pharmacology None None None None 16608883
3542 8548 0 None - 1 Human 8.7 pKd = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7589426
1126 8547 0 None - 1 Rat 8.6 pKd None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8795084
134813898 8732 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26572091
8972 8732 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26572091
155817505 8730 0 None - 1 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26572091
8971 8730 0 None - 1 Human 8.6 pKi = 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26572091
3542 8548 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26572091
11429 10605 0 None 31 2 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 30473097
156588324 10605 0 None 31 2 Human 9.9 pKi = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 30473097
8973 8729 0 None - 1 Human 9.1 pKi = 9.1 Binding
Value derived from ligand binding In a competitive binding assay.Value derived from ligand binding In a competitive binding assay.
Guide to Pharmacology None None None None 26572091