Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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162660600 181290 None 0 Human Functional pEC50 = 10.9 10.9 1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4337 106 62 64 -24.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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)CSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4761047 181290 None 0 Human Functional pEC50 = 10.9 10.9 1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4337 106 62 64 -24.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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)CSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
168281065 191120 None 0 Human Functional pEC50 = 10.9 10.9 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3920 140 55 53 -10.5 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCN=[N+]=[N-])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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5186705 191120 None 0 Human Functional pEC50 = 10.9 10.9 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3920 140 55 53 -10.5 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCN=[N+]=[N-])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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL4126027 215468 None 0 Human Functional pEC50 = 10.8 10.8 74 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon 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
137634214 156738 None 0 Human Functional pEC50 = 10.8 10.8 1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4121 139 65 62 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4069307 156738 None 0 Human Functional pEC50 = 10.8 10.8 1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4121 139 65 62 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4226451 215762 None 0 Human Functional pEC50 = 10.8 10.8 7 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
155523482 170899 None 0 Human Functional pEC50 = 10.8 10.8 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3480 112 54 51 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4453136 170899 None 0 Human Functional pEC50 = 10.8 10.8 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3480 112 54 51 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168292950 192256 None 0 Human Functional pEC50 = 10.8 10.8 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3881 137 56 53 -12.5 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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5203806 192256 None 0 Human Functional pEC50 = 10.8 10.8 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3881 137 56 53 -12.5 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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
168284782 191797 None 0 Human Functional pEC50 = 10.7 10.7 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3907 139 55 53 -10.3 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCN=[N+]=[N-])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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5196728 191797 None 0 Human Functional pEC50 = 10.7 10.7 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3907 139 55 53 -10.3 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCN=[N+]=[N-])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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5314341 218197 None 0 Mouse Functional pEC50 = 10.7 10.7 -2 5
Agonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assayAgonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay
ChEMBL None None None None 10.1016/j.bmc.2017.10.047
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 10.7 10.7 -3 5
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL None None None None 10.1021/acs.jmedchem.6b00840
137642925 158216 None 0 Mouse Functional pEC50 = 10.6 10.6 - 1
Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4579 156 66 65 -22.3 CCCCCCCCCCCCCCCC(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.7b00174
CHEMBL4086979 158216 None 0 Mouse Functional pEC50 = 10.6 10.6 - 1
Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4579 156 66 65 -22.3 CCCCCCCCCCCCCCCC(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.7b00174
137659233 159239 None 0 Human Functional pEC50 = 10.6 10.6 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4098061 159239 None 0 Human Functional pEC50 = 10.6 10.6 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.7b00174
155533592 171993 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4469604 171993 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4126953 215477 None 0 Human Functional pEC50 = 10.6 10.6 74 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon 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
CHEMBL4226514 215763 None 0 Human Functional pEC50 = 10.6 10.6 -1 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
137659233 159239 None 0 Human Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4098061 159239 None 0 Human Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4126738 215473 None 0 Human Functional pEC50 = 10.5 10.5 70 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon 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
CHEMBL4227045 215768 None 0 Human Functional pEC50 = 10.5 10.5 -1 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
168283329 190883 None 0 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3823 134 55 52 -12.3 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](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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5183317 190883 None 0 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3823 134 55 52 -12.3 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](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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
168283329 190883 None 0 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3823 134 55 52 -12.3 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](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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5183317 190883 None 0 Human Functional pEC50 = 10.5 10.5 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3823 134 55 52 -12.3 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](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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00218
155532202 171806 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4466715 171806 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4226613 215764 None 0 Human Functional pEC50 = 10.5 10.5 -1 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
155562429 175336 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4571762 175336 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168287225 191824 None 0 Human Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3937 138 57 53 -12.2 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](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](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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5197042 191824 None 0 Human Functional pEC50 = 10.5 10.5 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3937 138 57 53 -12.2 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](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](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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
155526545 171230 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4458230 171230 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
155566739 175985 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4586269 175985 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168296994 192430 None 0 Human Functional pEC50 = 10.4 10.4 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3839 135 56 53 -13.4 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](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](CO)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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5206399 192430 None 0 Human Functional pEC50 = 10.4 10.4 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3839 135 56 53 -13.4 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](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](CO)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)C(=O)O 10.1021/acsmedchemlett.2c00217
168286525 191472 None 0 Human Functional pEC50 = 10.4 10.4 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3835 133 54 51 -10.5 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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5192132 191472 None 0 Human Functional pEC50 = 10.4 10.4 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3835 133 54 51 -10.5 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](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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
155564592 175641 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3479 112 54 50 -16.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4578443 175641 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3479 112 54 50 -16.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4225340 215755 None 0 Human Functional pEC50 = 10.4 10.4 -1 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
CHEMBL1222098 211101 None 0 Human Functional pEC50 = 10.3 10.3 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](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)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222088 211091 None 0 Human Functional pEC50 = 10.3 10.3 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)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](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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168285487 191764 None 0 Human Functional pEC50 = 10.3 10.3 -2 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4110 145 58 56 -11.9 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](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(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5196180 191764 None 0 Human Functional pEC50 = 10.3 10.3 -2 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4110 145 58 56 -11.9 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](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(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222076 211080 None 0 Human Functional pEC50 = 10.3 10.3 3 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168278702 191248 None 0 Human Functional pEC50 = 10.3 10.3 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4151 152 57 57 -10.8 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCNC(=O)COCCOCCNC(=O)CCCCN=[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](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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5188299 191248 None 0 Human Functional pEC50 = 10.3 10.3 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4151 152 57 57 -10.8 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CCCCNC(=O)COCCOCCNC(=O)CCCCN=[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](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)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL1222077 211081 None 0 Human Functional pEC50 = 10.3 10.3 20 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
49864558 15664 None 0 Human Functional pEC50 = 10.3 10.3 2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
91933345 15664 None 0 Human Functional pEC50 = 10.3 10.3 2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222080 15664 None 0 Human Functional pEC50 = 10.3 10.3 2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
162656099 180836 None 0 Human Functional pEC50 = 10.3 10.3 -3 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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]1CCNC(=O)CCCC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4755815 180836 None 0 Human Functional pEC50 = 10.3 10.3 -3 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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]1CCNC(=O)CCCC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
49864615 15674 None 0 Human Functional pEC50 = 10.3 10.3 -4 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3362 96 47 47 -11.9 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(C)CN[C@@H](Cc2cnc[nH]2)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222174 15674 None 0 Human Functional pEC50 = 10.3 10.3 -4 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3362 96 47 47 -11.9 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(C)CN[C@@H](Cc2cnc[nH]2)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222099 211102 None 0 Human Functional pEC50 = 10.2 10.2 -1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=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)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
168296031 192395 None 0 Human Functional pEC50 = 10.2 10.2 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4091 144 58 55 -12.2 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](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](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5205970 192395 None 0 Human Functional pEC50 = 10.2 10.2 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4091 144 58 55 -12.2 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](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](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
162652123 180450 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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]1CCCCNC(=O)CC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4751319 180450 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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]1CCCCNC(=O)CC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
168271903 190711 None 0 Human Functional pEC50 = 10.2 10.2 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4194 149 61 57 -13.2 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](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](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(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5180732 190711 None 0 Human Functional pEC50 = 10.2 10.2 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4194 149 61 57 -13.2 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](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](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(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 10.2 10.2 -3 5
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
168274917 190359 None 0 Human Functional pEC50 = 10.2 10.2 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3851 135 55 52 -11.7 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](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](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(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5175260 190359 None 0 Human Functional pEC50 = 10.2 10.2 2 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3851 135 55 52 -11.7 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](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](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(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222082 211085 None 0 Human Functional pEC50 = 10.2 10.2 8 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222087 211090 None 0 Human Functional pEC50 = 10.2 10.2 -2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by 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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222090 211093 None 0 Human Functional pEC50 = 10.2 10.2 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222079 211083 None 0 Human Functional pEC50 = 10.2 10.2 3 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 10.2 10.2 -3 5
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None None 10.1038/nchembio.209
155517094 170271 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4444485 170271 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222091 211094 None 0 Human Functional pEC50 = 10.1 10.1 -1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)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(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)[C@@H](C)O 10.1038/nchembio.209
168290869 192082 None 0 Human Functional pEC50 = 10.1 10.1 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3837 134 55 52 -12.0 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](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)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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5201113 192082 None 0 Human Functional pEC50 = 10.1 10.1 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3837 134 55 52 -12.0 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](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)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](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)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222101 211104 None 0 Human Functional pEC50 = 10.1 10.1 2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC1=O 10.1038/nchembio.209
CHEMBL1222085 211088 None 0 Human Functional pEC50 = 10.1 10.1 -1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222100 211103 None 0 Human Functional pEC50 = 10.1 10.1 3 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 10.1 10.1 -3 5
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
CHEMBL1222092 211095 None 0 Human Functional pEC50 = 10.1 10.1 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4175452 215694 None 0 Human Functional pEC50 = 10.1 10.1 7 2
Agonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF methodAgonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF method
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2022.115036
155512720 169789 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4437733 169789 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccncc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222089 211092 None 0 Human Functional pEC50 = 10.1 10.1 -3 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168298565 192781 None 0 Human Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4643 155 67 66 -21.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(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(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5218881 192781 None 0 Human Functional pEC50 = 10.0 10.0 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4643 155 67 66 -21.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(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(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL1222078 211082 None 0 Human Functional pEC50 = 10 10.0 2 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1c[nH]cn1)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222081 211084 None 0 Human Functional pEC50 = 10 10.0 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCS(=O)(=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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168271945 190208 None 0 Human Functional pEC50 = 10 10.0 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3941 140 59 55 -15.0 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](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](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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5172868 190208 None 0 Human Functional pEC50 = 10 10.0 1 2
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3941 140 59 55 -15.0 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](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](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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
162648287 180011 None 0 Human Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4210 122 64 63 -28.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](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](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4745985 180011 None 0 Human Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4210 122 64 63 -28.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](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](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL1222097 211100 None 0 Human Functional pEC50 = 9.9 9.9 1 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
137662302 159336 None 0 Human Functional pEC50 = 9.9 9.9 13 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 4314 132 64 64 -25.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)O 10.1021/acs.jmedchem.7b00174
CHEMBL4098991 159336 None 0 Human Functional pEC50 = 9.9 9.9 13 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 4314 132 64 64 -25.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)O 10.1021/acs.jmedchem.7b00174
162648841 179952 None 0 Human Functional pEC50 = 9.9 9.9 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4745235 179952 None 0 Human Functional pEC50 = 9.9 9.9 -1 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL1222083 211086 None 0 Human Functional pEC50 = 9.9 9.9 4 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222084 211087 None 0 Human Functional pEC50 = 9.9 9.9 4 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168299170 192807 None 0 Human Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4628 153 66 65 -20.5 CCCCCCCCCCCCCCCC(=O)N[C@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5219454 192807 None 0 Human Functional pEC50 = 9.9 9.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4628 153 66 65 -20.5 CCCCCCCCCCCCCCCC(=O)N[C@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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(=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(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL1222075 211079 None 0 Human Functional pEC50 = 9.8 9.8 3 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4227861 215774 None 0 Human Functional pEC50 = 9.8 9.8 -1 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
168298728 192839 None 0 Human Functional pEC50 = 9.8 9.8 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4261 133 64 63 -25.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220251 192839 None 0 Human Functional pEC50 = 9.8 9.8 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4261 133 64 63 -25.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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(N)=O 10.1016/j.ejmech.2020.113118
172439005 195306 None 0 Human Functional pEC50 = 9.7 9.7 -3 2
Agonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF methodAgonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF method
ChEMBL 4379 138 67 66 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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)N[C@@H](CS)C(N)=O 10.1016/j.ejmech.2022.115036
CHEMBL5400455 195306 None 0 Human Functional pEC50 = 9.7 9.7 -3 2
Agonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF methodAgonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF method
ChEMBL 4379 138 67 66 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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)N[C@@H](CS)C(N)=O 10.1016/j.ejmech.2022.115036
168284802 191859 None 0 Human Functional pEC50 = 9.6 9.6 4 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4104 144 57 55 -11.3 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)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](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(N)=O)C(=O)O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5197522 191859 None 0 Human Functional pEC50 = 9.6 9.6 4 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4104 144 57 55 -11.3 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)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](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(N)=O)C(=O)O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
168299650 192792 None 0 Human Functional pEC50 = 9.6 9.6 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4392 150 72 63 -24.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219122 192792 None 0 Human Functional pEC50 = 9.6 9.6 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4392 150 72 63 -24.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
168298631 192837 None 0 Human Functional pEC50 = 9.6 9.6 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4756 159 68 67 -20.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5220241 192837 None 0 Human Functional pEC50 = 9.6 9.6 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4756 159 68 67 -20.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O)C(=O)O 10.1016/j.ejmech.2020.113118
162657120 181008 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C/CCC[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](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](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4757675 181008 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C/CCC[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](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](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
168298518 192853 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3474 114 55 51 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL5220666 192853 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3474 114 55 51 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
172462313 196729 None 0 Human Functional pEC50 = 9.4 9.4 -4 2
Agonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF methodAgonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF method
ChEMBL 4315 139 66 65 -27.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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)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)N[C@@H](CS)C(N)=O 10.1016/j.ejmech.2022.115036
CHEMBL5431072 196729 None 0 Human Functional pEC50 = 9.4 9.4 -4 2
Agonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF methodAgonist activity at GCGR (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF method
ChEMBL 4315 139 66 65 -27.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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)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)N[C@@H](CS)C(N)=O 10.1016/j.ejmech.2022.115036
168299004 192862 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4453 151 73 65 -26.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5221090 192862 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4453 151 73 65 -26.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
168298163 192852 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3488 113 55 51 -18.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[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)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL5220630 192852 None 0 Human Functional pEC50 = 9.4 9.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3488 113 55 51 -18.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[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)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL4163714 215678 None 0 Human Functional pEC50 = 9.3 9.3 3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CS)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222086 211089 None 0 Human Functional pEC50 = 9.3 9.3 -30 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by 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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[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](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)C(C)C 10.1038/nchembio.209
168282938 190854 None 0 Human Functional pEC50 = 9.3 9.3 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4117 146 57 55 -10.0 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5182822 190854 None 0 Human Functional pEC50 = 9.3 9.3 -1 2
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4117 146 57 55 -10.0 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](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[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](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 9.3 9.3 -3 5
Agonist activity at human GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assayAgonist activity at human GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay
ChEMBL None None None None 10.1016/j.bmc.2017.10.047
162659870 181379 None 0 Human Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4338 104 61 64 -22.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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)CSCc2cc3cc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CSC3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4762061 181379 None 0 Human Functional pEC50 = 9.2 9.2 -2 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4338 104 61 64 -22.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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](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)CSCc2cc3cc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CSC3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
49864580 15665 None 0 Human Functional pEC50 = 9.2 9.2 -41 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3380 111 48 48 -12.0 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(C)CN[C@@H](Cc1cnc[nH]1)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222102 15665 None 0 Human Functional pEC50 = 9.2 9.2 -41 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3380 111 48 48 -12.0 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(C)CN[C@@H](Cc1cnc[nH]1)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4170727 215686 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168298382 192849 None 0 Human Functional pEC50 = 9.1 9.1 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4331 137 64 63 -22.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=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 10.1016/j.ejmech.2020.113118
CHEMBL5220497 192849 None 0 Human Functional pEC50 = 9.1 9.1 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4331 137 64 63 -22.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=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 10.1016/j.ejmech.2020.113118
CHEMBL4174154 215691 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4166241 215682 None 0 Human Functional pEC50 = 9.1 9.1 3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168298376 192844 None 0 Human Functional pEC50 = 9.0 9.0 -1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4467 150 73 65 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220372 192844 None 0 Human Functional pEC50 = 9.0 9.0 -1 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4467 150 73 65 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5314341 218197 None 0 Human Functional pEC50 = 9.0 9.0 -3 5
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2017.07.046
137650720 157372 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4213 135 59 61 -21.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)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(C)C)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(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4076828 157372 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4213 135 59 61 -21.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)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(C)C)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(N)=O 10.1021/acs.jmedchem.7b00174
137661599 159288 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 4447 149 73 65 -25.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)O 10.1016/j.ejmech.2017.07.046
CHEMBL4098545 159288 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 4447 149 73 65 -25.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)O 10.1016/j.ejmech.2017.07.046
137638423 156980 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4486 148 66 64 -22.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)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(C)C)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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)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)O 10.1021/acs.jmedchem.7b00174
CHEMBL4072029 156980 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4486 148 66 64 -22.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)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(C)C)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](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)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)O 10.1021/acs.jmedchem.7b00174
CHEMBL4167331 215684 None 0 Human Functional pEC50 = 8.9 8.9 4 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4162383 215674 None 0 Human Functional pEC50 = 8.9 8.9 1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
168299536 192801 None 0 Human Functional pEC50 = 8.9 8.9 -9 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3554 120 56 51 -16.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219263 192801 None 0 Human Functional pEC50 = 8.9 8.9 -9 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3554 120 56 51 -16.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
168299173 192808 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4346 136 64 63 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=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 10.1016/j.ejmech.2020.113118
CHEMBL5219458 192808 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4346 136 64 63 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=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 10.1016/j.ejmech.2020.113118
CHEMBL4159256 215668 None 0 Human Functional pEC50 = 8.9 8.9 -1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4160347 215671 None 0 Human Functional pEC50 = 8.9 8.9 7 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4167169 215683 None 0 Human Functional pEC50 = 8.9 8.9 1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4173061 215690 None 0 Human Functional pEC50 = 8.8 8.8 -1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4175452 215694 None 0 Human Functional pEC50 = 8.8 8.8 7 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168299127 192769 None 0 Human Functional pEC50 = 8.7 8.7 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3426 114 54 49 -16.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5218509 192769 None 0 Human Functional pEC50 = 8.7 8.7 -3 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3426 114 54 49 -16.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4162789 215675 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4159275 215669 None 0 Human Functional pEC50 = 7.8 7.8 3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4170976 215687 None 0 Human Functional pEC50 = 7.7 7.7 6 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
137634741 155989 None 0 Human Functional pEC50 = 8.6 8.6 -93 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4185 134 62 62 -26.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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)CNC(=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)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(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4060629 155989 None 0 Human Functional pEC50 = 8.6 8.6 -93 2
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4185 134 62 62 -26.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)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)CNC(=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)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(N)=O 10.1021/acs.jmedchem.7b00174
155532070 171819 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3451 112 52 52 -18.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4466856 171819 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3451 112 52 52 -18.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222095 211098 None 0 Human Functional pEC50 = 8.6 8.6 -85 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by 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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[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(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4169653 215685 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
168298006 192817 None 0 Human Functional pEC50 = 8.6 8.6 -21 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3569 119 56 51 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219646 192817 None 0 Human Functional pEC50 = 8.6 8.6 -21 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3569 119 56 51 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
168298501 192845 None 0 Human Functional pEC50 = 8.6 8.6 -16 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3583 120 56 51 -16.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220384 192845 None 0 Human Functional pEC50 = 8.6 8.6 -16 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3583 120 56 51 -16.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4174404 215693 None 0 Human Functional pEC50 = 8.6 8.6 3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4163731 215679 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=O)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4177064 215696 None 0 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4130148 215505 None 0 Human Functional pEC50 = 8.5 8.5 8 3
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon 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
CHEMBL4172444 215689 None 0 Human Functional pEC50 = 8.5 8.5 4 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222094 211097 None 0 Human Functional pEC50 = 8.4 8.4 -33 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4174382 215692 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168299788 192784 None 0 Human Functional pEC50 = 7.4 7.4 -177 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4276 132 64 63 -25.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[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)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(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5218999 192784 None 0 Human Functional pEC50 = 7.4 7.4 -177 2
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4276 132 64 63 -25.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[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)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(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4165144 215681 None 0 Human Functional pEC50 = 8.4 8.4 -1 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4159003 215667 None 0 Human Functional pEC50 = 8.4 8.4 19 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[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](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](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4160365 215672 None 0 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)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(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4130044 215500 None 0 Human Functional pEC50 = 7.4 7.4 -812 3
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon 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
CHEMBL4225594 215758 None 0 Human Functional pEC50 = 8.3 8.3 -173 3
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG 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
CHEMBL4159426 215670 None 0 Human Functional pEC50 = 8.3 8.3 6 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222093 211096 None 0 Human Functional pEC50 = 7.3 7.3 -275 2
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[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(=O)O)NC(=O)[C@H](C)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4161800 215673 None 0 Human Functional pEC50 = 8.2 8.2 -3 2
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
162655167 180906 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C\CCC[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](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](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4756489 180906 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C\CCC[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](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](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)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(N)=O 10.1021/acs.jmedchem.0c01500
164616962 185299 None 0 Human Functional pIC50 = 9.4 9.4 1 6
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-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 185299 None 0 Human Functional pIC50 = 9.4 9.4 1 6
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-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
164616962 185299 None 0 Mouse Functional pIC50 = 9.3 9.3 -1 6
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-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 185299 None 0 Mouse Functional pIC50 = 9.3 9.3 -1 6
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-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
122189698 123432 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
CHEMBL3616677 123432 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
71243036 110334 None 0 Human Functional pIC50 = 7 7.0 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 110334 None 0 Human Functional pIC50 = 7 7.0 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
16225394 69000 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922917 69000 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
57882748 140050 None 12 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL3799802 140050 None 12 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
57882748 140050 None 12 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799802 140050 None 12 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
60170767 81410 None 0 Human Functional pIC50 = 7 7.0 54 2
Antagonist activity at human GCGR 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 GCGR 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 81410 None 0 Human Functional pIC50 = 7 7.0 54 2
Antagonist activity at human GCGR 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 GCGR 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
11950971 150993 None 0 Human Functional pIC50 = 6.0 6.0 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 150993 None 0 Human Functional pIC50 = 6.0 6.0 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11570626 2550 None 32 Dog Functional pIC50 = 7.0 7.0 -6 8
Antagonist activity at dog GCGR 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 dog GCGR 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 2550 None 32 Dog Functional pIC50 = 7.0 7.0 -6 8
Antagonist activity at dog GCGR 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 dog GCGR 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 2550 None 32 Dog Functional pIC50 = 7.0 7.0 -6 8
Antagonist activity at dog GCGR 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 dog GCGR 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 2550 None 32 Dog Functional pIC50 = 7.0 7.0 -6 8
Antagonist activity at dog GCGR 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 dog GCGR 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
10370821 72156 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197851 72156 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11950794 161325 None 0 Human Functional pIC50 = 6.0 6.0 5 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 161325 None 0 Human Functional pIC50 = 6.0 6.0 5 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
60170969 81430 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR 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 GCGR 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 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159346 81430 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR 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 GCGR 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 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
127047254 140025 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
CHEMBL3799656 140025 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
122189570 123407 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(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
CHEMBL3616581 123407 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(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
122189579 123416 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616590 123416 None 0 Human Functional pIC50 = 8.0 8.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
11950794 161325 None 0 Human Functional pIC50 = 8.0 8.0 5 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 161325 None 0 Human Functional pIC50 = 8.0 8.0 5 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
44431020 167739 None 0 Human Functional pIC50 = 8.0 8.0 123 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 167739 None 0 Human Functional pIC50 = 8.0 8.0 123 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
60170970 81431 None 0 Human Functional pIC50 = 7.9 7.9 199 4
Antagonist activity at human GCGR 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 GCGR 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 81431 None 0 Human Functional pIC50 = 7.9 7.9 199 4
Antagonist activity at human GCGR 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 GCGR 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
57518490 81420 None 0 Human Functional pIC50 = 7.9 7.9 56 2
Antagonist activity at human GCGR 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 GCGR 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 81420 None 0 Human Functional pIC50 = 7.9 7.9 56 2
Antagonist activity at human GCGR 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 GCGR 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
58353063 110300 None 0 Human Functional pIC50 = 7.0 7.0 31 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237900 110300 None 0 Human Functional pIC50 = 7.0 7.0 31 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353067 110336 None 0 Human Functional pIC50 = 7.0 7.0 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 110336 None 0 Human Functional pIC50 = 7.0 7.0 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352821 110316 None 0 Human Functional pIC50 = 6.0 6.0 28 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237915 110316 None 0 Human Functional pIC50 = 6.0 6.0 28 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44404227 72155 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197850 72155 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
9985625 56941 None 0 Human Functional pIC50 = 6.9 6.9 5 4
Antagonist activity at human GCGR 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 GCGR 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 56941 None 0 Human Functional pIC50 = 6.9 6.9 5 4
Antagonist activity at human GCGR 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 GCGR 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
11678967 81413 None 0 Human Functional pIC50 = 6.9 6.9 29 2
Antagonist activity at human GCGR 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 GCGR 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 81413 None 0 Human Functional pIC50 = 6.9 6.9 29 2
Antagonist activity at human GCGR 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 GCGR 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
10346647 140441 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL380771 140441 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10007881 166012 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL425024 166012 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
145967741 165286 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228690 165286 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
54765285 69017 None 0 Human Functional pIC50 = 7.9 7.9 128 2
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
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 69017 None 0 Human Functional pIC50 = 7.9 7.9 128 2
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
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
164628536 186571 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876736 186571 None 0 Human Functional pIC50 = 7.9 7.9 2 2
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11621378 81437 None 3 Human Functional pIC50 = 7.9 7.9 131 2
Antagonist activity at human GCGR 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 GCGR 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 81437 None 3 Human Functional pIC50 = 7.9 7.9 131 2
Antagonist activity at human GCGR 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 GCGR 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
11527207 81424 None 0 Human Functional pIC50 = 7.9 7.9 81 2
Antagonist activity at human GCGR 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 GCGR 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 81424 None 0 Human Functional pIC50 = 7.9 7.9 81 2
Antagonist activity at human GCGR 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 GCGR 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
122189693 123427 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616672 123427 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
135819137 92904 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
CHEMBL24388 92904 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
11250000 68928 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
CHEMBL1922704 68928 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
11387112 68935 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922711 68935 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
90655064 110347 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238228 110347 None 0 Human Functional pIC50 = 5.9 5.9 -1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046968 139990 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
CHEMBL3799439 139990 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
127046098 140170 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3800525 140170 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
11570626 2550 None 32 Mouse Functional pIC50 = 6.9 6.9 -7 8
Antagonist activity at mouse GCGR 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 mouse GCGR 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 2550 None 32 Mouse Functional pIC50 = 6.9 6.9 -7 8
Antagonist activity at mouse GCGR 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 mouse GCGR 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 2550 None 32 Mouse Functional pIC50 = 6.9 6.9 -7 8
Antagonist activity at mouse GCGR 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 mouse GCGR 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 2550 None 32 Mouse Functional pIC50 = 6.9 6.9 -7 8
Antagonist activity at mouse GCGR 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 mouse GCGR 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
1148 1924 None 28 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
619101 1924 None 28 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
CHEMBL179281 1924 None 28 Human Functional pIC50 = 6.9 6.9 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
164628244 186553 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876499 186553 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
145969571 165263 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228281 165263 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
11444850 68989 None 0 Human Functional pIC50 = 7.9 7.9 54 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68989 None 0 Human Functional pIC50 = 7.9 7.9 54 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
164616848 185055 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4853767 185055 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170857 81426 None 0 Human Functional pIC50 = 7.9 7.9 56 2
Antagonist activity at human GCGR 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 GCGR 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 81426 None 0 Human Functional pIC50 = 7.9 7.9 56 2
Antagonist activity at human GCGR 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 GCGR 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
122189575 123412 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616586 123412 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
11490222 68930 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(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
CHEMBL1922706 68930 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(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
71243005 110326 None 0 Human Functional pIC50 = 6.9 6.9 5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 10 2 6 7.3 CCCCC[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
CHEMBL3237925 110326 None 0 Human Functional pIC50 = 6.9 6.9 5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 10 2 6 7.3 CCCCC[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
58353046 110337 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 110337 None 0 Human Functional pIC50 = 6.9 6.9 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10077369 56946 None 0 Human Functional pIC50 = 5.9 5.9 14 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56946 None 0 Human Functional pIC50 = 5.9 5.9 14 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
127046644 139665 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3797325 139665 None 0 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
44404227 72155 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197850 72155 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189708 123442 None 0 Human Functional pIC50 = 7.9 7.9 213 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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 123442 None 0 Human Functional pIC50 = 7.9 7.9 213 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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
122189715 123449 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616694 123449 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
54765284 68990 None 0 Human Functional pIC50 = 7.9 7.9 165 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68990 None 0 Human Functional pIC50 = 7.9 7.9 165 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
57393253 68994 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922844 68994 None 0 Human Functional pIC50 = 7.9 7.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11585375 81422 None 0 Human Functional pIC50 = 7.9 7.9 30 2
Antagonist activity at human GCGR 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 GCGR 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 81422 None 0 Human Functional pIC50 = 7.9 7.9 30 2
Antagonist activity at human GCGR 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 GCGR 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
11273570 68938 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(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
CHEMBL1922714 68938 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(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
122189694 123428 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616673 123428 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189723 123458 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616702 123458 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
16100296 205297 None 41 Human Functional pIC50 = 6.9 6.9 18 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 205297 None 41 Human Functional pIC50 = 6.9 6.9 18 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
58353013 110295 None 0 Human Functional pIC50 = 6.9 6.9 10 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237895 110295 None 0 Human Functional pIC50 = 6.9 6.9 10 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353544 110299 None 0 Human Functional pIC50 = 6.9 6.9 7 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 110299 None 0 Human Functional pIC50 = 6.9 6.9 7 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352803 110338 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 110338 None 0 Human Functional pIC50 = 6.9 6.9 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353232 110288 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237889 110288 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
127045652 139791 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798135 139791 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
127047253 140159 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3800473 140159 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
10437700 135445 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL372784 135445 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
16100296 72436 None 41 Human Functional pIC50 = 6.8 6.8 -1 4
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO 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 10.1016/j.bmcl.2005.06.101
CHEMBL198736 72436 None 41 Human Functional pIC50 = 6.8 6.8 -1 4
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO 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 10.1016/j.bmcl.2005.06.101
11950972 161326 None 0 Human Functional pIC50 = 5.8 5.8 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 161326 None 0 Human Functional pIC50 = 5.8 5.8 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11952213 86792 None 0 Human Functional pIC50 = 5.8 5.8 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86792 None 0 Human Functional pIC50 = 5.8 5.8 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
145967924 165223 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4227634 165223 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
11952035 151559 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 151559 None 0 Human Functional pIC50 = 7.8 7.8 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11570626 2550 None 32 Human Functional pIC50 = 7.8 7.8 3 8
Antagonist activity at human GCGR 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 GCGR 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 2550 None 32 Human Functional pIC50 = 7.8 7.8 3 8
Antagonist activity at human GCGR 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 GCGR 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 2550 None 32 Human Functional pIC50 = 7.8 7.8 3 8
Antagonist activity at human GCGR 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 GCGR 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 2550 None 32 Human Functional pIC50 = 7.8 7.8 3 8
Antagonist activity at human GCGR 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 GCGR 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
60170971 81432 None 0 Human Functional pIC50 = 7.8 7.8 186 3
Antagonist activity at human GCGR 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 GCGR 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 81432 None 0 Human Functional pIC50 = 7.8 7.8 186 3
Antagonist activity at human GCGR 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 GCGR 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
45381379 110329 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(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
CHEMBL3237928 110329 None 0 Human Functional pIC50 = 6.8 6.8 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(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
16225393 69005 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922922 69005 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
127046099 139997 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799468 139997 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
11757662 72282 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198214 72282 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44389598 64893 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 64893 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
11331120 68984 None 0 Human Functional pIC50 = 7.8 7.8 81 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68984 None 0 Human Functional pIC50 = 7.8 7.8 81 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
10324097 56878 None 0 Human Functional pIC50 = 6.8 6.8 15 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56878 None 0 Human Functional pIC50 = 6.8 6.8 15 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
58353838 110339 None 0 Human Functional pIC50 = 6.8 6.8 5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238220 110339 None 0 Human Functional pIC50 = 6.8 6.8 5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352840 110290 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)c(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237890 110290 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)c(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
90655066 110346 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ncccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238227 110346 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ncccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047904 139916 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799017 139916 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10416067 71837 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL196844 71837 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
10073298 70579 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 467 4 2 5 4.5 CC(C)(C)C1CCC2(CC1)CN(C(C)(C)C)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL194794 70579 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 467 4 2 5 4.5 CC(C)(C)C1CCC2(CC1)CN(C(C)(C)C)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10393857 72116 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 603 8 2 5 6.1 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197754 72116 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 603 8 2 5 6.1 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189572 123409 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616583 123409 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
11421820 68934 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(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
CHEMBL1922710 68934 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(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
16225179 69009 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922926 69009 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57396141 69022 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922938 69022 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11757679 56936 None 0 Human Functional pIC50 = 6.8 6.8 54 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56936 None 0 Human Functional pIC50 = 6.8 6.8 54 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
58352935 110297 None 0 Human Functional pIC50 = 6.8 6.8 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 110297 None 0 Human Functional pIC50 = 6.8 6.8 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
145969316 165226 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227667 165226 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
145969278 165166 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4226770 165166 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
145986774 167137 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 461 12 2 5 5.2 CCCCC(Oc1ncc(-c2ccc(CC)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4288863 167137 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 461 12 2 5 5.2 CCCCC(Oc1ncc(-c2ccc(CC)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
44404222 71991 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197340 71991 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11352811 179106 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
CHEMBL470955 179106 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
122189711 123445 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616690 123445 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
122189712 123446 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616691 123446 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
122189713 123447 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616692 123447 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
122189718 123452 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616697 123452 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
57391489 68991 None 0 Human Functional pIC50 = 7.8 7.8 141 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68991 None 0 Human Functional pIC50 = 7.8 7.8 141 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
11952035 86851 None 0 Human Functional pIC50 = 7.8 7.8 10 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86851 None 0 Human Functional pIC50 = 7.8 7.8 10 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
CHEMBL439289 216295 None 0 Human Functional pIC50 = 7.8 7.8 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL None None None CN[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)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](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2005.01.003
11410772 68709 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1921810 68709 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
51031037 110318 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 110318 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353338 110341 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 110341 None 0 Human Functional pIC50 = 6.8 6.8 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 110342 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 110342 None 0 Human Functional pIC50 = 6.8 6.8 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10099927 136193 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL373234 136193 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10383925 78981 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112991 78981 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
11678966 81415 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
CHEMBL2159332 81415 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
11951681 96909 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL265337 96909 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
44561440 172692 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 584 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(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL448921 172692 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 584 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(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
11478813 68939 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(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
CHEMBL1922715 68939 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(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
11456187 68985 None 1 Human Functional pIC50 = 7.7 7.7 40 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68985 None 1 Human Functional pIC50 = 7.7 7.7 40 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
57393252 68993 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922843 68993 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
91755011 123553 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMPAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMP
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
CHEMBL3617565 123553 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMPAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMP
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
58353464 110291 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 573 8 2 5 5.6 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237891 110291 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 573 8 2 5 5.6 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353408 110292 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237892 110292 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
127046645 139732 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3797757 139732 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
164622383 186047 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4869368 186047 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10370821 72156 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197851 72156 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10008709 141390 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 6 2 7 5.7 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383350 141390 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 6 2 7 5.7 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
9986018 133659 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371235 133659 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189704 123438 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616683 123438 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
57403109 69020 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922936 69020 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
9985625 56941 None 0 Mouse Functional pIC50 = 5.7 5.7 -25 4
Antagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at mouse GCGR 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 56941 None 0 Mouse Functional pIC50 = 5.7 5.7 -25 4
Antagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at mouse GCGR 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
44342725 9971 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibitory concentration against cAMP production in hGR-CHO cellsInhibitory concentration against cAMP production in hGR-CHO cells
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL114761 9971 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Inhibitory concentration against cAMP production in hGR-CHO cellsInhibitory concentration against cAMP production in hGR-CHO cells
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
160115 177129 None 20 Human Functional pIC50 = 4.7 4.7 -1 2
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL 518 1 6 10 4.6 CC1CC(=O)c2c(cc3c(-c4c(O)cc(O)c5c(O)c6c(cc45)OC(C)CC6=O)c(O)cc(O)c3c2O)O1 10.1021/np040093o
CHEMBL463175 177129 None 20 Human Functional pIC50 = 4.7 4.7 -1 2
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL 518 1 6 10 4.6 CC1CC(=O)c2c(cc3c(-c4c(O)cc(O)c5c(O)c6c(cc45)OC(C)CC6=O)c(O)cc(O)c3c2O)O1 10.1021/np040093o
145971123 165171 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226911 165171 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
127046805 139892 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 663 10 2 5 9.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(CC(=O)O)c4ccccc4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798798 139892 None 0 Human Functional pIC50 = 4.7 4.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 663 10 2 5 9.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(CC(=O)O)c4ccccc4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
53377590 123549 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 524 7 2 5 5.0 CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(N2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617561 123549 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 524 7 2 5 5.0 CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(N2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
16100296 72436 None 41 Human Functional pIC50 = 7.7 7.7 -1 4
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
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 10.1016/j.bmcl.2005.06.101
CHEMBL198736 72436 None 41 Human Functional pIC50 = 7.7 7.7 -1 4
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
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 10.1016/j.bmcl.2005.06.101
122189721 123456 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 615 10 2 5 7.9 CCC(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
CHEMBL3616700 123456 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 615 10 2 5 7.9 CCC(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
122189706 123440 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616685 123440 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11238814 68923 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922699 68923 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
127047385 139735 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
CHEMBL3797782 139735 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
44561479 179233 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(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
CHEMBL471979 179233 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(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
11950795 86852 None 0 Human Functional pIC50 = 5.7 5.7 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86852 None 0 Human Functional pIC50 = 5.7 5.7 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
44561439 191310 None 0 Human Functional pIC50 = 7.7 7.7 426 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 191310 None 0 Human Functional pIC50 = 7.7 7.7 426 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
11365464 68931 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(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
CHEMBL1922707 68931 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(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
57403703 68992 None 0 Human Functional pIC50 = 7.7 7.7 41 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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 68992 None 0 Human Functional pIC50 = 7.7 7.7 41 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
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
71472272 123560 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
CHEMBL3617572 123560 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
53467170 123551 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 607 10 2 4 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC12CCC([Si](C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617563 123551 None 0 Human Functional pIC50 = 7.7 7.7 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 607 10 2 4 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC12CCC([Si](C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
44561480 179268 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472154 179268 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
122189696 123430 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616675 123430 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
58353104 110324 None 0 Human Functional pIC50 = 6.7 6.7 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CCC[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
CHEMBL3237923 110324 None 0 Human Functional pIC50 = 6.7 6.7 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CCC[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
145967685 165205 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227364 165205 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
45381268 110327 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 7 2 6 6.4 CC(C)[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
CHEMBL3237926 110327 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 7 2 6 6.4 CC(C)[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
10459436 133665 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371259 133665 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561556 189388 None 0 Human Functional pIC50 = 7.6 7.6 213 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 189388 None 0 Human Functional pIC50 = 7.6 7.6 213 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
11421826 68920 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922696 68920 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
164628536 186571 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876736 186571 None 0 Mouse Functional pIC50 = 7.6 7.6 -2 2
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11592461 81427 None 0 Human Functional pIC50 = 7.6 7.6 64 2
Antagonist activity at human GCGR 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 GCGR 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 81427 None 0 Human Functional pIC50 = 7.6 7.6 64 2
Antagonist activity at human GCGR 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 GCGR 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
11180162 68933 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922709 68933 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10008376 56939 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644181 56939 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
71202743 110343 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3238224 110343 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
145967899 165185 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227099 165185 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
44404243 141356 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383135 141356 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
60170766 81409 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
CHEMBL2159326 81409 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
145970933 165246 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4227967 165246 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
11650288 81416 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
CHEMBL2159333 81416 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR 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 GCGR 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-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
122189716 123450 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616695 123450 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
57401359 69024 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922940 69024 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353323 110340 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238221 110340 None 0 Human Functional pIC50 = 6.6 6.6 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11284982 68987 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(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
CHEMBL1922837 68987 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(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
57393262 68925 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922701 68925 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10072624 72299 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 453 5 2 5 4.1 CC(C)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL198259 72299 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 453 5 2 5 4.1 CC(C)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
122189569 123406 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616580 123406 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
122189719 123453 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616698 123453 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
58352868 110298 None 0 Human Functional pIC50 = 6.6 6.6 6 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237898 110298 None 0 Human Functional pIC50 = 6.6 6.6 6 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
53469058 110350 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 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)CC2 10.1021/jm401858f
CHEMBL3238231 110350 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 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)CC2 10.1021/jm401858f
145989050 165317 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4229115 165317 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
127047256 139858 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798581 139858 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
127047906 139877 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798731 139877 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
164624673 186097 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870133 186097 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
145968206 165287 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228703 165287 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
60171062 81436 None 0 Human Functional pIC50 = 7.6 7.6 104 2
Antagonist activity at human GCGR 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 GCGR 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 81436 None 0 Human Functional pIC50 = 7.6 7.6 104 2
Antagonist activity at human GCGR 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 GCGR 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
58353206 110323 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 7 2 6 6.2 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
CHEMBL3237922 110323 None 0 Human Functional pIC50 = 6.6 6.6 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 7 2 6 6.2 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
122189571 123408 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616582 123408 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
53469820 110359 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 627 8 2 4 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238241 110359 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 627 8 2 4 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
141465337 165183 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4227068 165183 None 0 Human Functional pIC50 = 4.6 4.6 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
164626335 186471 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875380 186471 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44431016 144332 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL390469 144332 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11432140 176233 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459208 176233 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11308245 68986 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(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
CHEMBL1922836 68986 None 0 Human Functional pIC50 = 7.6 7.6 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(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
58352940 110301 None 0 Human Functional pIC50 = 6.6 6.6 4 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237901 110301 None 0 Human Functional pIC50 = 6.6 6.6 4 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10099927 136193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL373234 136193 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10437700 135445 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL372784 135445 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11952035 151559 None 0 Human Functional pIC50 = 5.5 5.5 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 151559 None 0 Human Functional pIC50 = 5.5 5.5 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11353908 68988 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(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
CHEMBL1922838 68988 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(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
58353132 110283 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237884 110283 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
71202253 123550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 589 8 2 6 6.8 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(C2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617562 123550 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 589 8 2 6 6.8 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(C2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
58352762 110317 None 0 Human Functional pIC50 = 5.5 5.5 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237916 110317 None 0 Human Functional pIC50 = 5.5 5.5 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
68860750 114052 None 1 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326188 114052 None 1 Human Functional pIC50 = 6.5 6.5 - 1
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
11527170 81419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR 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 GCGR 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)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159336 81419 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR 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 GCGR 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)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
23550062 71829 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL196800 71829 None 0 Human Functional pIC50 = 8.5 8.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
10416067 71837 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL196844 71837 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
57399593 69002 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922919 69002 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
11657413 81414 None 0 Human Functional pIC50 = 7.5 7.5 44 2
Antagonist activity at human GCGR 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 GCGR 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 81414 None 0 Human Functional pIC50 = 7.5 7.5 44 2
Antagonist activity at human GCGR 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 GCGR 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
58653097 79055 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 605 8 3 5 5.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL2113103 79055 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 605 8 3 5 5.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1 10.1016/j.bmcl.2005.06.101
44372478 51870 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1021/jm050563r
CHEMBL158548 51870 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1021/jm050563r
11585452 81421 None 0 Human Functional pIC50 = 7.5 7.5 47 2
Antagonist activity at human GCGR 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 GCGR 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 81421 None 0 Human Functional pIC50 = 7.5 7.5 47 2
Antagonist activity at human GCGR 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 GCGR 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
CHEMBL524883 218118 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)C[C@@H]2NC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CSSC[C@@H](C(=O)OC)NC(=O)[C@H](C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)CNC(=O)[C@@H]3CCCN3C1=O)NC(=O)CNC(=O)[C@H](Cc1c[nH]c3ccccc13)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)CNC2=O 10.1021/np040093o
58353274 110293 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 489 7 2 4 4.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237893 110293 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 489 7 2 4 4.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
44404243 141356 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383135 141356 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11952211 87985 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 87985 None 0 Human Functional pIC50 = 7.5 7.5 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
10415723 56942 None 0 Human Functional pIC50 = 6.5 6.5 63 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56942 None 0 Human Functional pIC50 = 6.5 6.5 63 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
145969298 165196 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227229 165196 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
10031040 166257 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL426295 166257 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10054055 72344 None 9 Human Functional pIC50 = 7.5 7.5 7 3
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
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 72344 None 9 Human Functional pIC50 = 7.5 7.5 7 3
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
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
57399594 69014 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
CHEMBL1922930 69014 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
11754125 78982 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112992 78982 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
58352925 110302 None 0 Human Functional pIC50 = 6.5 6.5 12 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237902 110302 None 0 Human Functional pIC50 = 6.5 6.5 12 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44431012 150995 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL395760 150995 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
164613898 184828 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4850520 184828 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10053841 56940 None 0 Human Functional pIC50 = 7.5 7.5 85 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56940 None 0 Human Functional pIC50 = 7.5 7.5 85 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
16224591 69003 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922920 69003 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57394374 69021 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922937 69021 None 0 Human Functional pIC50 = 7.5 7.5 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353778 110303 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237903 110303 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469821 110358 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238240 110358 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047121 140051 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
CHEMBL3799820 140051 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
10369580 72236 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198094 72236 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10052441 133699 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371476 133699 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10007881 166012 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL425024 166012 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189580 123417 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616591 123417 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
57396140 69018 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 12 2 4 8.0 CC(C)CC[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
CHEMBL1922934 69018 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 12 2 4 8.0 CC(C)CC[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
122189578 123415 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616589 123415 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
68243839 110344 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
CHEMBL3238225 110344 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
71454981 81428 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR 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 GCGR 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 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
CHEMBL2159344 81428 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR 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 GCGR 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 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
122189581 123418 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616592 123418 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
10483611 56937 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644179 56937 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
45381381 110333 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 110333 None 0 Human Functional pIC50 = 6.4 6.4 2 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71202712 110355 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238236 110355 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145969968 165174 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226972 165174 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
56602804 110352 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C 10.1021/jm401858f
CHEMBL3238233 110352 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C 10.1021/jm401858f
44561438 189512 None 0 Human Functional pIC50 = 7.4 7.4 204 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 189512 None 0 Human Functional pIC50 = 7.4 7.4 204 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
45381051 110325 None 0 Human Functional pIC50 = 6.4 6.4 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CCCC[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
CHEMBL3237924 110325 None 0 Human Functional pIC50 = 6.4 6.4 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CCCC[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
122189574 123411 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616585 123411 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
16223791 69008 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922925 69008 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11950972 161326 None 0 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 161326 None 0 Human Functional pIC50 = 7.4 7.4 3 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
164621209 186358 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4873721 186358 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11249762 183947 None 0 Human Functional pIC50 = 8.4 8.4 1122 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 183947 None 0 Human Functional pIC50 = 8.4 8.4 1122 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
122190363 123563 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617575 123563 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
44575544 174102 None 0 Human Functional pIC50 = 8.4 8.4 3 4
Inhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
CHEMBL454246 174102 None 0 Human Functional pIC50 = 8.4 8.4 3 4
Inhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
164617806 184788 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4849980 184788 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
9985625 56941 None 0 Dog Functional pIC50 = 6.4 6.4 -5 4
Antagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at dog GCGR 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 56941 None 0 Dog Functional pIC50 = 6.4 6.4 -5 4
Antagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at dog GCGR 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
71202713 110356 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238237 110356 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22004955 93536 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL24616 93536 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
10325599 141394 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 6 2 7 4.3 CC(C)(C)C1CCC2(CC1)CN(c1ccc(S(C)(=O)=O)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383370 141394 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 6 2 7 4.3 CC(C)(C)C1CCC2(CC1)CN(c1ccc(S(C)(=O)=O)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189701 123435 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616680 123435 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11490393 68936 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(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
CHEMBL1922712 68936 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(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
10435275 123931 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL362657 123931 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
145990090 167097 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCCC(Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4288074 167097 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCCC(Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
58353126 110335 None 0 Human Functional pIC50 = 7.4 7.4 7 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 110335 None 0 Human Functional pIC50 = 7.4 7.4 7 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
57397957 69016 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 598 12 2 4 7.7 CCCC[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
CHEMBL1922932 69016 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 598 12 2 4 7.7 CCCC[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
10007966 72524 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL199013 72524 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
44404234 125018 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 501 5 2 5 5.2 Cc1ccc(N2CC3(CCC(C(C)(C)C)CC3)N(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL364288 125018 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 501 5 2 5 5.2 Cc1ccc(N2CC3(CCC(C(C)(C)C)CC3)N(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.101
10007966 72524 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL199013 72524 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189705 123439 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616684 123439 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11785044 189775 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL515202 189775 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
58352863 110304 None 0 Human Functional pIC50 = 6.4 6.4 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237904 110304 None 0 Human Functional pIC50 = 6.4 6.4 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
122189703 123437 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616682 123437 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
9985625 56941 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56941 None 0 Human Functional pIC50 = 7.4 7.4 5 4
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
57392671 69023 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922939 69023 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11950971 150993 None 0 Human Functional pIC50 = 7.4 7.4 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 150993 None 0 Human Functional pIC50 = 7.4 7.4 2 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
164627630 186446 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875003 186446 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
57400189 68929 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922705 68929 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
58353662 110305 None 0 Human Functional pIC50 = 6.4 6.4 16 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 110305 None 0 Human Functional pIC50 = 6.4 6.4 16 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL526383 218174 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)C[C@@H]2NC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CSSC[C@@H](C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)CNC(=O)[C@@H]3CCCN3C1=O)NC(=O)CNC(=O)[C@H](Cc1c[nH]c3ccccc13)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)CNC2=O 10.1021/np040093o
145968045 165041 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4224961 165041 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10346647 140441 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL380771 140441 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
16223987 69001 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922918 69001 None 0 Human Functional pIC50 = 7.4 7.4 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
145971078 165103 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4225922 165103 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
141465324 165207 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227372 165207 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
53466721 110362 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 665 8 2 6 8.1 C[C@@H](NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1)c1nnn[nH]1 10.1021/jm401858f
CHEMBL3238245 110362 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 665 8 2 6 8.1 C[C@@H](NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1)c1nnn[nH]1 10.1021/jm401858f
127047907 140009 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799556 140009 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10031040 166257 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL426295 166257 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189717 123451 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616696 123451 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
23550062 56874 None 0 Human Functional pIC50 = 7.3 7.3 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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 56874 None 0 Human Functional pIC50 = 7.3 7.3 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR 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
53469443 110363 None 3 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
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 110363 None 3 Human Functional pIC50 = 7.3 7.3 3 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
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
11952211 153830 None 0 Human Functional pIC50 = 7.3 7.3 7 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 153830 None 0 Human Functional pIC50 = 7.3 7.3 7 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11949739 161327 None 0 Human Functional pIC50 = 7.3 7.3 57 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 161327 None 0 Human Functional pIC50 = 7.3 7.3 57 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
23550062 71829 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL196800 71829 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
145970930 165245 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227964 165245 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10326056 56938 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644180 56938 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
60171061 81435 None 0 Human Functional pIC50 = 7.3 7.3 114 2
Antagonist activity at human GCGR 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 GCGR 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 81435 None 0 Human Functional pIC50 = 7.3 7.3 114 2
Antagonist activity at human GCGR 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 GCGR 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
164620673 186124 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870505 186124 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164629129 186583 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876913 186583 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
122189576 123413 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616587 123413 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
53469628 110353 None 0 Human Functional pIC50 = 7.3 7.3 19 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 110353 None 0 Human Functional pIC50 = 7.3 7.3 19 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353156 110306 None 0 Human Functional pIC50 = 6.3 6.3 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 110306 None 0 Human Functional pIC50 = 6.3 6.3 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
45381049 110345 None 0 Human Functional pIC50 = 6.3 6.3 -1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238226 110345 None 0 Human Functional pIC50 = 6.3 6.3 -1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11952211 87985 None 0 Human Functional pIC50 = 6.3 6.3 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 87985 None 0 Human Functional pIC50 = 6.3 6.3 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
57391519 68926 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922702 68926 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
16224781 69011 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
CHEMBL1922928 69011 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
58353369 110307 None 0 Human Functional pIC50 = 6.3 6.3 6 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 110307 None 0 Human Functional pIC50 = 6.3 6.3 6 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
122189573 123410 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(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
CHEMBL3616584 123410 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(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
122189577 123414 None 0 Human Functional pIC50 = 8.3 8.3 588 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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 123414 None 0 Human Functional pIC50 = 8.3 8.3 588 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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
60171059 81433 None 0 Human Functional pIC50 = 8.2 8.2 407 4
Antagonist activity at human GCGR 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 GCGR 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 81433 None 0 Human Functional pIC50 = 8.2 8.2 407 4
Antagonist activity at human GCGR 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 GCGR 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
11952394 87046 None 0 Human Functional pIC50 = 8.2 8.2 660 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 87046 None 0 Human Functional pIC50 = 8.2 8.2 660 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11950075 86848 None 0 Human Functional pIC50 = 6.3 6.3 9 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86848 None 0 Human Functional pIC50 = 6.3 6.3 9 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
58352836 110284 None 0 Human Functional pIC50 = 6.3 6.3 19 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237885 110284 None 0 Human Functional pIC50 = 6.3 6.3 19 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
53469258 110351 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
CHEMBL3238232 110351 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
58352938 110296 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237896 110296 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10257529 71739 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196560 71739 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189695 123429 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616674 123429 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
58352937 110348 None 0 Human Functional pIC50 = 7.3 7.3 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 110348 None 0 Human Functional pIC50 = 7.3 7.3 4 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
57396138 68999 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922916 68999 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
58353839 110357 None 0 Human Functional pIC50 = 6.3 6.3 24 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
CHEMBL3238238 110357 None 0 Human Functional pIC50 = 6.3 6.3 24 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
127047255 140109 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
CHEMBL3800146 140109 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
11950795 86852 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86852 None 0 Human Functional pIC50 = 7.3 7.3 1 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
45381153 110322 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
CHEMBL3237921 110322 None 0 Human Functional pIC50 = 6.3 6.3 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
11785044 176324 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459457 176324 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57397956 69004 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCC[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
CHEMBL1922921 69004 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCC[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
57390854 69019 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922935 69019 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
11570626 2550 None 32 Rhesus macaque Functional pIC50 = 7.3 7.3 -3 8
Antagonist activity at rhesus monkey GCGR 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 rhesus monkey GCGR 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 2550 None 32 Rhesus macaque Functional pIC50 = 7.3 7.3 -3 8
Antagonist activity at rhesus monkey GCGR 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 rhesus monkey GCGR 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 2550 None 32 Rhesus macaque Functional pIC50 = 7.3 7.3 -3 8
Antagonist activity at rhesus monkey GCGR 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 rhesus monkey GCGR 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 2550 None 32 Rhesus macaque Functional pIC50 = 7.3 7.3 -3 8
Antagonist activity at rhesus monkey GCGR 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 rhesus monkey GCGR 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
58352952 110308 None 0 Human Functional pIC50 = 6.3 6.3 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237908 110308 None 0 Human Functional pIC50 = 6.3 6.3 13 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145989480 165304 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228938 165304 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
122189702 123436 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616681 123436 None 0 Human Functional pIC50 = 7.3 7.3 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
10076914 56947 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644189 56947 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
58352858 110309 None 0 Human Functional pIC50 = 6.3 6.3 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 110309 None 0 Human Functional pIC50 = 6.3 6.3 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11699553 81411 None 0 Human Functional pIC50 = 7.2 7.2 72 2
Antagonist activity at human GCGR 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 GCGR 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 81411 None 0 Human Functional pIC50 = 7.2 7.2 72 2
Antagonist activity at human GCGR 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 GCGR 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
10413333 63039 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
CHEMBL178768 63039 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
44389598 64893 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 64893 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
122189709 123443 None 0 Human Functional pIC50 = 8.2 8.2 239 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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 123443 None 0 Human Functional pIC50 = 8.2 8.2 239 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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
164624163 185921 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4867132 185921 None 0 Human Functional pIC50 = 8.2 8.2 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10257529 71739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196560 71739 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
145989947 166890 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 489 11 2 5 6.0 CCCCC(Oc1ncc(-c2ccc(C(C)(C)C)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4284236 166890 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 489 11 2 5 6.0 CCCCC(Oc1ncc(-c2ccc(C(C)(C)C)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10369580 72236 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198094 72236 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
57401963 68922 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922698 68922 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11949740 156817 None 0 Human Functional pIC50 = 7.2 7.2 194 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 156817 None 0 Human Functional pIC50 = 7.2 7.2 194 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
53377591 123552 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 683 11 2 7 8.1 CC(C)(C)CCOc1cccc(C2=NC3(CCC(C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1016/j.bmcl.2015.07.092
CHEMBL3617564 123552 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 683 11 2 7 8.1 CC(C)(C)CCOc1cccc(C2=NC3(CCC(C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1016/j.bmcl.2015.07.092
44404222 71991 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197340 71991 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561519 179293 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472325 179293 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
11599295 183907 None 0 Human Functional pIC50 = 7.2 7.2 229 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 183907 None 0 Human Functional pIC50 = 7.2 7.2 229 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
44389632 63290 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
CHEMBL179181 63290 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
60170968 81429 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR 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 GCGR 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 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159345 81429 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR 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 GCGR 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 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
58352834 110311 None 0 Human Functional pIC50 = 6.2 6.2 10 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237910 110311 None 0 Human Functional pIC50 = 6.2 6.2 10 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353350 110312 None 0 Human Functional pIC50 = 6.2 6.2 6 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237911 110312 None 0 Human Functional pIC50 = 6.2 6.2 6 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047120 139813 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
CHEMBL3798231 139813 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
127046643 139883 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798761 139883 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
9873139 72255 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 7 5.3 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198144 72255 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 7 5.3 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
60170855 81418 None 0 Human Functional pIC50 = 7.2 7.2 15 2
Antagonist activity at human GCGR 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 GCGR 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 81418 None 0 Human Functional pIC50 = 7.2 7.2 15 2
Antagonist activity at human GCGR 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 GCGR 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
11433550 68924 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922700 68924 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
10459436 133665 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371259 133665 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189699 123433 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
CHEMBL3616678 123433 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
9906120 95339 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL25637 95339 None 1 Human Functional pIC50 = 7.2 7.2 - 1
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
10461010 56944 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644186 56944 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11757662 72282 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198214 72282 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
53469056 110349 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238230 110349 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71060230 123562 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617574 123562 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
11952214 86853 None 0 Human Functional pIC50 = 7.2 7.2 6 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86853 None 0 Human Functional pIC50 = 7.2 7.2 6 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
60171060 81434 None 0 Human Functional pIC50 = 7.2 7.2 158 2
Antagonist activity at human GCGR 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 GCGR 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 81434 None 0 Human Functional pIC50 = 7.2 7.2 158 2
Antagonist activity at human GCGR 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 GCGR 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
57403704 68995 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922845 68995 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
58353266 110294 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237894 110294 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
122189720 123454 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616699 123454 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
145981450 166657 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 501 11 2 5 6.0 CCCCC(Oc1ncc(-c2cc(Cl)cc(Cl)c2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4279713 166657 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 501 11 2 5 6.0 CCCCC(Oc1ncc(-c2cc(Cl)cc(Cl)c2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
127047905 139853 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 613 7 1 5 7.8 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798548 139853 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 613 7 1 5 7.8 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
127047122 140001 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
CHEMBL3799499 140001 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
11410779 188338 None 0 Human Functional pIC50 = 8.2 8.2 371 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 188338 None 0 Human Functional pIC50 = 8.2 8.2 371 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
60170856 81425 None 0 Human Functional pIC50 = 8.1 8.1 128 2
Antagonist activity at human GCGR 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 GCGR 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 81425 None 0 Human Functional pIC50 = 8.1 8.1 128 2
Antagonist activity at human GCGR 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 GCGR 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
122189722 123457 None 0 Human Functional pIC50 = 8.1 8.1 295 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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 123457 None 0 Human Functional pIC50 = 8.1 8.1 295 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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
57401986 68932 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(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
CHEMBL1922708 68932 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(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
10323446 133601 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 493 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(C1CCCCC1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL370847 133601 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 493 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(C1CCCCC1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561327 190563 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(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
CHEMBL517861 190563 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(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
164626834 186581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876838 186581 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
16224191 69012 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922929 69012 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
11157621 68921 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922697 68921 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11284556 68937 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(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
CHEMBL1922713 68937 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(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
164624086 185809 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865509 185809 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
58353901 110285 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1F)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237886 110285 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1F)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
10481840 72076 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197642 72076 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
145967583 165047 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4225050 165047 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
58353025 110313 None 0 Human Functional pIC50 = 6.1 6.1 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 110313 None 0 Human Functional pIC50 = 6.1 6.1 8 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352954 110319 None 0 Human Functional pIC50 = 6.1 6.1 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237918 110319 None 0 Human Functional pIC50 = 6.1 6.1 1 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145968140 165186 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227111 165186 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
122189697 123431 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616676 123431 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
45381380 110328 None 0 Human Functional pIC50 = 6.1 6.1 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 8 2 6 6.8 CC(C)C[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
CHEMBL3237927 110328 None 0 Human Functional pIC50 = 6.1 6.1 3 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 8 2 6 6.8 CC(C)C[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
122189700 123434 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616679 123434 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
60170854 81417 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR 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 GCGR 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 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
CHEMBL2159334 81417 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR 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 GCGR 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 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
58352961 110286 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237887 110286 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
164616563 185512 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4861024 185512 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11952035 86851 None 0 Human Functional pIC50 = 6.1 6.1 10 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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 86851 None 0 Human Functional pIC50 = 6.1 6.1 10 2
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon 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
11376210 183698 None 0 Human Functional pIC50 = 8.1 8.1 1737 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 183698 None 0 Human Functional pIC50 = 8.1 8.1 1737 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
122189714 123448 None 0 Human Functional pIC50 = 8.1 8.1 301 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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 123448 None 0 Human Functional pIC50 = 8.1 8.1 301 2
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
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
11570626 2550 None 32 Human Functional pIC50 = 7.1 7.1 3 8
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
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 10.1016/j.bmc.2018.02.036
9135 2550 None 32 Human Functional pIC50 = 7.1 7.1 3 8
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
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 10.1016/j.bmc.2018.02.036
CHEMBL1933349 2550 None 32 Human Functional pIC50 = 7.1 7.1 3 8
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
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 10.1016/j.bmc.2018.02.036
DB12044 2550 None 32 Human Functional pIC50 = 7.1 7.1 3 8
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
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 10.1016/j.bmc.2018.02.036
12967031 111635 None 0 Human Functional pIC50 = 6.1 6.1 -2 2
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1021/jm050563r
CHEMBL328126 111635 None 0 Human Functional pIC50 = 6.1 6.1 -2 2
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1021/jm050563r
58353489 110287 None 0 Human Functional pIC50 = 6.1 6.1 12 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237888 110287 None 0 Human Functional pIC50 = 6.1 6.1 12 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
141465320 165260 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4228215 165260 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
164618212 185495 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4860642 185495 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44561390 176140 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459032 176140 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
145982299 166589 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 525 13 2 6 6.5 CCCCC(Oc1ncc(-c2ccc(Oc3ccccc3)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4278513 166589 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 525 13 2 6 6.5 CCCCC(Oc1ncc(-c2ccc(Oc3ccccc3)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
141465346 165275 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4228470 165275 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
122189707 123441 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
CHEMBL3616686 123441 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
58353679 110314 None 0 Human Functional pIC50 = 6.1 6.1 2 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 110314 None 0 Human Functional pIC50 = 6.1 6.1 2 3
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11951857 97040 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL266489 97040 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
71202679 110354 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238235 110354 None 0 Human Functional pIC50 = 6.1 6.1 -5 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53466723 110360 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 677 9 2 5 7.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238242 110360 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 677 9 2 5 7.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145993424 167436 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4294427 167436 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10077102 72102 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 5 5.7 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197718 72102 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 5 5.7 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
141465319 165238 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
CHEMBL4227906 165238 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
90655065 110361 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238243 110361 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10435562 71484 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 487 5 2 5 4.9 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196193 71484 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 487 5 2 5 4.9 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11169089 188403 None 0 Human Functional pIC50 = 8.1 8.1 676 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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 188403 None 0 Human Functional pIC50 = 8.1 8.1 676 2
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
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
122189710 123444 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616689 123444 None 0 Human Functional pIC50 = 8.1 8.1 - 1
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170768 81412 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR 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 GCGR 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 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159329 81412 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR 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 GCGR 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 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
58353695 110315 None 0 Human Functional pIC50 = 6.0 6.0 7 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 110315 None 0 Human Functional pIC50 = 6.0 6.0 7 2
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9986018 133659 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371235 133659 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10054055 72344 None 9 Human Functional pIC50 = 7.0 7.0 7 3
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
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 72344 None 9 Human Functional pIC50 = 7.0 7.0 7 3
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
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
145986381 167194 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4289916 167194 None 0 Human Functional pIC50 = 5.0 5.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10052441 133699 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371476 133699 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
57396139 69010 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922927 69010 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
11238073 68927 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922703 68927 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
134304209 169736 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(cnn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4437105 169736 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(cnn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1Cl 10.1016/j.bmcl.2019.05.036
134304141 174738 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4557989 174738 None 0 Human Functional pKi = 7 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
134304824 174802 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 510 9 2 3 7.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4559572 174802 None 0 Human Functional pKi = 7.0 7.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 510 9 2 3 7.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
155538812 173366 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 455 9 2 4 5.5 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccccc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4524978 173366 None 0 Human Functional pKi = 6.0 6.0 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 455 9 2 4 5.5 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccccc3)ccc21 10.1016/j.bmcl.2019.05.036
134304142 172920 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.8 CC(C)(C)c1ccc(-c2ccc3c(cnn3C(CC3CCCCC3)c3ccc(C(=O)NCCC(=O)O)cc3)c2)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4513964 172920 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.8 CC(C)(C)c1ccc(-c2ccc3c(cnn3C(CC3CCCCC3)c3ccc(C(=O)NCCC(=O)O)cc3)c2)cc1 10.1016/j.bmcl.2019.05.036
134304160 171687 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4465107 171687 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
134304713 175562 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 522 9 2 3 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4576987 175562 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 522 9 2 3 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304136 170824 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4452109 170824 None 0 Human Functional pKi = 6.9 6.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134309610 172159 None 0 Human Functional pKi = 6.9 6.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4471941 172159 None 0 Human Functional pKi = 6.9 6.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
155515237 170039 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 553 10 2 6 5.3 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCN(C)CC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4441433 170039 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 553 10 2 6 5.3 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCN(C)CC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304208 174826 None 0 Human Functional pKi = 5.9 5.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4560114 174826 None 0 Human Functional pKi = 5.9 5.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
155526074 171148 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 9 2 4 7.1 Cc1cc(-c2ccc(C(C)(C)C)cc2)cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc12 10.1016/j.bmcl.2019.05.036
CHEMBL4456905 171148 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 9 2 4 7.1 Cc1cc(-c2ccc(C(C)(C)C)cc2)cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc12 10.1016/j.bmcl.2019.05.036
155539799 172985 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 505 9 2 4 6.7 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cccc4ccccc34)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4515516 172985 None 0 Human Functional pKi = 5.9 5.9 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 505 9 2 4 6.7 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cccc4ccccc34)ccc21 10.1016/j.bmcl.2019.05.036
134304129 172908 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.126668
CHEMBL4513792 172908 None 0 Human Functional pKi = 7.9 7.9 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.126668
134304077 175131 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 10 2 4 7.2 CC(C)CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4567337 175131 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 10 2 4 7.2 CC(C)CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304151 169617 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc2n1 10.1016/j.bmcl.2019.05.036
CHEMBL4434750 169617 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc2n1 10.1016/j.bmcl.2019.05.036
155558364 174841 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.9 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cc(Cl)cc(Cl)c3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4560433 174841 None 0 Human Functional pKi = 5.8 5.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.9 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cc(Cl)cc(Cl)c3)ccc21 10.1016/j.bmcl.2019.05.036
134304194 174773 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 558 9 2 5 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)nc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4558907 174773 None 0 Human Functional pKi = 6.8 6.8 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 558 9 2 5 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)nc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
134304075 170787 None 0 Human Functional pKi = 5.7 5.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4451707 170787 None 0 Human Functional pKi = 5.7 5.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
155515554 170080 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4441980 170080 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1Cl 10.1016/j.bmcl.2019.05.036
155530534 171663 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 12 2 4 7.8 CCCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4464664 171663 None 0 Human Functional pKi = 6.7 6.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 12 2 4 7.8 CCCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304091 172016 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4469925 172016 None 0 Human Functional pKi = 7.7 7.7 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
134304088 171606 None 0 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4463908 171606 None 0 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
134304234 172170 None 0 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1C 10.1016/j.bmcl.2019.126668
CHEMBL4472098 172170 None 0 Human Functional pKi = 7.7 7.7 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1C 10.1016/j.bmcl.2019.126668
134304087 175802 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4582082 175802 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304177 176118 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1C 10.1016/j.bmcl.2019.126668
CHEMBL4589676 176118 None 0 Human Functional pKi = 7.6 7.6 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1C 10.1016/j.bmcl.2019.126668
155517246 170264 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 11 2 4 7.4 CCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4444404 170264 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 11 2 4 7.4 CCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134309610 172159 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4471941 172159 None 0 Human Functional pKi = 6.6 6.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304232 172639 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 469 7 2 4 5.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4483722 172639 None 0 Human Functional pKi = 5.6 5.6 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 469 7 2 4 5.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
155541176 173085 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 10 2 5 6.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(OC(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4517914 173085 None 0 Human Functional pKi = 6.5 6.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 10 2 5 6.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(OC(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304074 170288 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4444819 170288 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
134304171 175128 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4567272 175128 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
155528087 171368 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 540 10 2 6 5.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCOCC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4460356 171368 None 0 Human Functional pKi = 5.5 5.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 540 10 2 6 5.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCOCC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304192 174753 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 552 9 2 5 6.6 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)c2cc1C 10.1016/j.bmcl.2019.05.036
CHEMBL4558340 174753 None 0 Human Functional pKi = 7.5 7.5 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 552 9 2 5 6.6 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)c2cc1C 10.1016/j.bmcl.2019.05.036
134304119 171929 None 10 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1cc2c(cnn2[C@@H](CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1-c1ccc(C(F)(F)F)cc1Cl 10.1016/j.bmcl.2019.126668
CHEMBL4468579 171929 None 10 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1cc2c(cnn2[C@@H](CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1-c1ccc(C(F)(F)F)cc1Cl 10.1016/j.bmcl.2019.126668
134304096 170277 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4444605 170277 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304090 171411 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4460982 171411 None 0 Human Functional pKi = 7.5 7.5 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304131 169685 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.05.036
CHEMBL4436021 169685 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.05.036
134304190 173848 None 0 Human Functional pKi = 7.4 7.4 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4536588 173848 None 0 Human Functional pKi = 7.4 7.4 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
134304219 174004 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4540172 174004 None 0 Human Functional pKi = 7.4 7.4 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1Cl 10.1016/j.bmcl.2019.05.036
155536703 172303 None 0 Human Functional pKi = 6.3 6.3 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4473724 172303 None 0 Human Functional pKi = 6.3 6.3 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
134304173 171120 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 602 11 2 6 7.0 CCOc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4456601 171120 None 0 Human Functional pKi = 7.2 7.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 602 11 2 6 7.0 CCOc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)cc12 10.1016/j.bmcl.2019.05.036
134304191 169938 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 497 9 2 4 6.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4439846 169938 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 497 9 2 4 6.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304793 175921 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 568 9 2 3 7.9 Cc1cc(C(F)(F)F)ccc1-c1cc(F)c2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1C 10.1016/j.bmcl.2019.05.036
CHEMBL4584712 175921 None 0 Human Functional pKi = 6.2 6.2 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 568 9 2 3 7.9 Cc1cc(C(F)(F)F)ccc1-c1cc(F)c2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1C 10.1016/j.bmcl.2019.05.036
155555973 174572 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 506 9 2 5 6.1 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc4ncccc4c3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4554170 174572 None 0 Human Functional pKi = 6.1 6.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 506 9 2 5 6.1 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc4ncccc4c3)ccc21 10.1016/j.bmcl.2019.05.036
134304822 170583 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 536 9 2 3 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.05.036
CHEMBL4449022 170583 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 536 9 2 3 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.05.036
134304145 172523 None 0 Human Functional pKi = 7.1 7.1 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4476825 172523 None 0 Human Functional pKi = 7.1 7.1 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
134304181 170306 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2019.05.036
CHEMBL4445178 170306 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2019.05.036
134304147 172257 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4473209 172257 None 0 Human Functional pKi = 7.1 7.1 - 0
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
155549801 174023 None 0 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4540602 174023 None 0 Human Functional pKi = 7.0 7.0 - 0
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
126961379 220236 None 0 Human Functional pEC50 = 8.0 8.0 - 1
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)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](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
126961379.0 220236 None 0 Human Functional pEC50 = 8.0 8.0 - 1
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)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](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
CHEMBL4297741 220236 None 0 Human Functional pEC50 = 8.0 8.0 - 1
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)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](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
DB15226 220236 None 0 Human Functional pEC50 = 8.0 8.0 - 1
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)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](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
102331734 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
1136 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
16132283 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
16133817 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
16133817.0 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
2994 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
3785 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
44278361 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
77077981 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
CHEMBL266481 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
DB00040 1814 None 28 Human Functional pEC50 = 8.1 8.1 3 3
NoneNone
Drug Central None None None None None
13383 3712 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
168429725 3712 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
168429725.0 3712 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
CHEMBL5314776 3712 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
DB18989 3712 None 0 Human Functional pEC50 = 9.3 9.3 -1 3
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)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](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
102331734 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
1136 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
16132283 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
16133817 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
16133817.0 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
2994 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
3785 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
44278361 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
77077981 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
CHEMBL266481 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
DB00040 1814 None 28 Human Functional pEC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
23549991 2840 None 0 Human Functional pIC50 = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 573 8 3 7 5.1 O=C(N(c1ccc(cc1)C1CCCCC1)Cc1ccc(cc1)C(=O)Nc1n[nH]nn1)Nc1cccc(c1)S(=O)(=O)C 28514451
9574 2840 None 0 Human Functional pIC50 = 7.2 7.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 573 8 3 7 5.1 O=C(N(c1ccc(cc1)C1CCCCC1)Cc1ccc(cc1)C(=O)Nc1n[nH]nn1)Nc1cccc(c1)S(=O)(=O)C 28514451
9760 2844 None 0 Human Functional pIC50 = 7.3 7.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29300013
11570626 2550 None 32 Human Functional pIC50 = 8.2 8.2 3 8
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 2550 None 32 Human Functional pIC50 = 8.2 8.2 3 8
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 2550 None 32 Human Functional pIC50 = 8.2 8.2 3 8
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 2550 None 32 Human Functional pIC50 = 8.2 8.2 3 8
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
3505 2212 None 35 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
5311276 2212 None 35 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
CHEMBL351772 2212 None 35 Human Functional pIC50 = 8.4 8.4 1 2
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
13314 3419 None 0 Human Functional pIC50 = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 702 11 3 4 8.8 CC1=CC(=C(C(=C1)C)C2=CC=C(C=C2)NC(=O)[C@H](CC3=CC=C(C=C3)C(=O)NCCS(=O)(=O)O)C4=CC=C(C=C4)C5=CC=C(C=C5)C(C)(C)C)C None
44625560 3419 None 0 Human Functional pIC50 = 9.3 9.3 - 1
UnclassifiedUnclassified
Guide to Pharmacology 702 11 3 4 8.8 CC1=CC(=C(C(=C1)C)C2=CC=C(C=C2)NC(=O)[C@H](CC3=CC=C(C=C3)C(=O)NCCS(=O)(=O)O)C4=CC=C(C=C4)C5=CC=C(C=C5)C(C)(C)C)C None
1148 1924 None 28 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
619101 1924 None 28 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
CHEMBL179281 1924 None 28 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
1148 1924 None 28 Human Functional pIC50 None 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396
619101 1924 None 28 Human Functional pIC50 None 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396
CHEMBL179281 1924 None 28 Human Functional pIC50 None 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396




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

Species

Assay
Type
Activity
Type
Activity
Relation
Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

CHEMBL5314341 218197 None 0 Mouse Binding pEC50 = 9.5 9.5 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
171351361 194515 None 0 Mouse Binding pEC50 = 9.3 9.3 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4146 133 61 61 -21.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5288119 194515 None 0 Mouse Binding pEC50 = 9.3 9.3 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4146 133 61 61 -21.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
171342584 193657 None 0 Mouse Binding pEC50 = 9.2 9.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4249 136 63 63 -21.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(=O)N[C@@H](CS)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5268054 193657 None 0 Mouse Binding pEC50 = 9.2 9.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4249 136 63 63 -21.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(=O)N[C@@H](CS)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
171357544 194269 None 0 Mouse Binding pEC50 = 9.2 9.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4107 132 61 61 -19.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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)NCC(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5282576 194269 None 0 Mouse Binding pEC50 = 9.2 9.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4107 132 61 61 -19.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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)NCC(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=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)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
171351626 193598 None 0 Mouse Binding pEC50 = 9.0 9.0 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4472 152 70 64 -21.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5266722 193598 None 0 Mouse Binding pEC50 = 9.0 9.0 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4472 152 70 64 -21.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
171352614 193971 None 0 Mouse Binding pEC50 = 8.8 8.8 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4473 152 70 64 -21.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5275572 193971 None 0 Mouse Binding pEC50 = 8.8 8.8 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4473 152 70 64 -21.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
171345730 194482 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 151 72 64 -23.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5287118 194482 None 0 Mouse Binding pEC50 = 8.5 8.5 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 151 72 64 -23.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
171345909 194404 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4444 148 72 64 -24.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5285379 194404 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4444 148 72 64 -24.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
168299178 192815 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4446 149 73 65 -26.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5219598 192815 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4446 149 73 65 -26.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
171354015 194040 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 150 72 64 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5277323 194040 None 0 Mouse Binding pEC50 = 8.2 8.2 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 150 72 64 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)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(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
171348496 193823 None 0 Mouse Binding pEC50 = 8.0 8.0 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4514 154 70 64 -21.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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](CCC(=O)O)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)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5272283 193823 None 0 Mouse Binding pEC50 = 8.0 8.0 - 0
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4514 154 70 64 -21.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[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](CCCNC(=N)N)NC(=O)[C@H](CCCCN)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](CCC(=O)O)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)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
129010858 150963 None 0 Human Binding pIC50 = 10 10.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 614 11 2 5 8.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3957356 150963 None 0 Human Binding pIC50 = 10 10.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 614 11 2 5 8.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
129010857 143500 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 594 11 2 5 7.9 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(C)cc12 nan
CHEMBL3898076 143500 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 594 11 2 5 7.9 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(C)cc12 nan
129010859 146130 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 618 10 2 4 8.5 N#Cc1cc(Cl)cc2c(C(c3ccc(Cl)cc3)[C@H](CCC(F)(F)F)c3ccc(C(=O)NCCC(=O)O)cc3)csc12 nan
CHEMBL3918808 146130 None 0 Human Binding pIC50 = 9.7 9.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 618 10 2 4 8.5 N#Cc1cc(Cl)cc2c(C(c3ccc(Cl)cc3)[C@H](CCC(F)(F)F)c3ccc(C(=O)NCCC(=O)O)cc3)csc12 nan
91755011 123553 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysisDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
CHEMBL3617565 123553 None 0 Human Binding pIC50 = 9.6 9.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysisDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
129010860 144239 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 11 2 4 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3903921 144239 None 0 Human Binding pIC50 = 9.4 9.4 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 11 2 4 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
11950794 161325 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 161325 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11950972 161326 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 161326 None 0 Human Binding pIC50 = 9.3 9.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
129010856 143580 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)c(Cl)c1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3898694 143580 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)c(Cl)c1)c1csc2c(C#N)cc(Cl)cc12 nan
122189714 123448 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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 123448 None 0 Human Binding pIC50 = 9.1 9.1 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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
129010861 153009 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3974805 153009 None 0 Human Binding pIC50 = 9 9.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
11376210 183698 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 183698 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
11410779 188338 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 188338 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
11169089 188403 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 188403 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
122189577 123414 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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 123414 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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
11952035 86851 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86851 None 0 Human Binding pIC50 = 9 9.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
129010853 148774 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 548 10 2 4 7.5 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(F)cc12 nan
CHEMBL3939861 148774 None 0 Human Binding pIC50 = 9.0 9.0 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 548 10 2 4 7.5 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(F)cc12 nan
129010854 147045 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 544 10 2 4 7.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C)cc12 nan
CHEMBL3926079 147045 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 544 10 2 4 7.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C)cc12 nan
11331120 68984 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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 68984 None 0 Human Binding pIC50 = 8.9 8.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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
122189710 123444 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616689 123444 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189713 123447 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616692 123447 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
122189715 123449 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616694 123449 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
129010855 151708 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C(F)(F)F)cc12 nan
CHEMBL3963664 151708 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C(F)(F)F)cc12 nan
57401986 68932 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(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
CHEMBL1922708 68932 None 0 Human Binding pIC50 = 8.8 8.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(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
129010864 149197 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1sc2ccccc2c1C nan
CHEMBL3943204 149197 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1sc2ccccc2c1C nan
11950075 86848 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86848 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
60171059 81433 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81433 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
122189708 123442 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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 123442 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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
44372948 52021 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 52021 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819146 110382 None 6 Human Binding pIC50 = 8 8.0 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 110382 None 6 Human Binding pIC50 = 8 8.0 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10483282 185879 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 185879 None 0 Human Binding pIC50 = 8 8.0 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
54765285 69017 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
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 69017 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
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
57403109 69020 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922936 69020 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353126 110335 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 110335 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11329242 189191 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 3 6 5.2 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2008.05.072
CHEMBL509900 189191 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 3 6 5.2 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2008.05.072
122189569 123406 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616580 123406 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
122189694 123428 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616673 123428 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
44431020 167739 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 167739 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11027864 46669 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 533 10 2 6 4.3 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL153879 46669 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 533 10 2 6 4.3 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
11585375 81422 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81422 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
44372720 48589 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 48589 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372477 54219 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160735 54219 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58352803 110338 None 0 Mouse Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 110338 None 0 Mouse Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
141465324 165207 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227372 165207 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
10215420 98553 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL276063 98553 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319617 106614 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL314181 106614 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
10592750 107209 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL316264 107209 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319245 208410 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 390 3 2 2 5.9 Oc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccccc2)cc1 10.1007/s00044-013-0869-9
CHEMBL84373 208410 None 0 Human Binding pIC50 = 7 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 390 3 2 2 5.9 Oc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccccc2)cc1 10.1007/s00044-013-0869-9
60170854 81417 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
CHEMBL2159334 81417 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
44372700 168713 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL436022 168713 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
135819143 9980 None 6 Human Binding pIC50 = 6 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114799 9980 None 6 Human Binding pIC50 = 6 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
135819146 110382 None 6 Human Binding pIC50 = 6 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 110382 None 6 Human Binding pIC50 = 6 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
44372471 48575 None 0 Mouse Binding pIC50 = 6 6.0 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 48575 None 0 Mouse Binding pIC50 = 6 6.0 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
56602994 127147 None 0 Human Binding pIC50 = 6 6.0 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 593 11 2 4 7.2 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)=NC1(C)C nan
CHEMBL3656296 127147 None 0 Human Binding pIC50 = 6 6.0 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 593 11 2 4 7.2 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)=NC1(C)C nan
16100338 141849 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 603 7 2 4 7.2 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)N3CCCC(C(=O)O)C3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL386030 141849 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 603 7 2 4 7.2 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)N3CCCC(C(=O)O)C3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
22005339 31750 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.2 CC(C)CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140586 31750 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.2 CC(C)CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004918 35279 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 315 5 1 2 5.2 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL143609 35279 None 0 Human Binding pIC50 = 6 6.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 315 5 1 2 5.2 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004877 96529 None 0 Human Binding pIC50 = 6 6.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 353 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(C)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL26238 96529 None 0 Human Binding pIC50 = 6 6.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 353 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(C)cc1 10.1016/s0960-894x(02)00143-9
10980170 4806 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 4 2 5 2.7 COc1cc(C(=O)N/N=C/c2ccnc3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104137 4806 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 4 2 5 2.7 COc1cc(C(=O)N/N=C/c2ccnc3ccccc23)ccc1O 10.1021/jm000547o
44319276 208567 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85741 208567 None 0 Human Binding pIC50 = 5 5.0 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL437471 216185 None 0 Human Binding pIC50 = 5 5.0 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
58352836 110284 None 0 Mouse Binding pIC50 = 5 5.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237885 110284 None 0 Mouse Binding pIC50 = 5 5.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
16100297 137026 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 504 8 3 4 5.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2)CC1 10.1021/jm058026u
CHEMBL374293 137026 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 504 8 3 4 5.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2)CC1 10.1021/jm058026u
164626834 186581 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876838 186581 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11952211 87985 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 87985 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
16100327 137296 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 479 8 3 3 5.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccccc2)CC1 10.1021/jm058026u
CHEMBL374994 137296 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 479 8 3 3 5.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccccc2)CC1 10.1021/jm058026u
11599295 183907 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 183907 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
11365464 68931 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(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
CHEMBL1922707 68931 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(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
10951864 44804 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 560 6 2 5 5.6 O=C(N/N=C/c1ccc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152184 44804 None 0 Human Binding pIC50 = 8.0 8.0 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 560 6 2 5 5.6 O=C(N/N=C/c1ccc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10974243 47186 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 635 7 3 6 5.6 O=C(N/N=C/c1ccc(OCC(=O)N2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154316 47186 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 635 7 3 6 5.6 O=C(N/N=C/c1ccc(OCC(=O)N2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10434112 51547 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 454 5 2 5 4.1 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL158295 51547 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 454 5 2 5 4.1 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
129010862 148522 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 3 8.8 CCC[C@H](c1ccc(C(=O)NCC(F)(F)C(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL3937819 148522 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 3 8.8 CCC[C@H](c1ccc(C(=O)NCC(F)(F)C(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
44319474 107109 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315613 107109 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10363819 107133 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
CHEMBL315828 107133 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
9906120 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
CHEMBL25637 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
44372478 51870 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 51870 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
45381381 110333 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 110333 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71243036 110334 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 110334 None 0 Mouse Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
16225177 69006 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922923 69006 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2011.09.105
145969298 165196 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227229 165196 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
11387112 68935 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922711 68935 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189697 123431 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616676 123431 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
44373547 52449 None 0 Human Binding pIC50 = 7.0 7.0 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 466 9 2 6 5.0 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL159071 52449 None 0 Human Binding pIC50 = 7.0 7.0 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 466 9 2 6 5.0 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
9906120 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL25637 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
9906120 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL25637 95339 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
44318988 208465 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL84917 208465 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
19072340 48577 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155687 48577 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
135819149 10454 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 10454 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
44319258 208447 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84759 208447 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1016/s0960-894x(01)00498-x
71203427 110320 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237919 110320 None 0 Mouse Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353778 110303 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237903 110303 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10416258 56948 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644190 56948 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
53321835 56959 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644201 56959 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
53319214 56961 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644203 56961 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
56602866 127133 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 597 10 2 6 6.4 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
CHEMBL3656282 127133 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 597 10 2 6 6.4 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
22005341 100028 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(F)c1 10.1016/s0960-894x(02)00143-9
CHEMBL286555 100028 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(F)c1 10.1016/s0960-894x(02)00143-9
20647512 94134 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1F 10.1016/s0960-894x(02)00143-9
CHEMBL24905 94134 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1F 10.1016/s0960-894x(02)00143-9
127047121 140051 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
CHEMBL3799820 140051 None 0 Human Binding pIC50 = 5.0 5.0 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
164620673 186124 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870505 186124 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372720 48589 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL155694 48589 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
44418929 82628 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 582 10 2 4 7.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)c2csc3ccc(Cl)cc23)C(c2ccccc2)c2ccccc2)cc1 10.1021/jm058026u
CHEMBL217901 82628 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 582 10 2 4 7.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)c2csc3ccc(Cl)cc23)C(c2ccccc2)c2ccccc2)cc1 10.1021/jm058026u
9841863 60078 None 21 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL17370 60078 None 21 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
22496412 172807 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 172807 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
44389598 64893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 64893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
42617999 188482 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 188482 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
22496557 193370 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 193370 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
135819133 114478 None 1 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 114478 None 1 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10257357 141925 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 141925 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
16225179 69009 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922926 69009 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57401359 69024 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922940 69024 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11284556 68937 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(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
CHEMBL1922713 68937 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(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
122189578 123415 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616589 123415 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
11082135 119675 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccc(F)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346464 119675 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccc(F)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164617806 184788 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4849980 184788 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164625627 185891 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3389 111 53 50 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4866685 185891 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3389 111 53 50 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
71456151 78470 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1cccc2c(OCc3ccc(OC(F)(F)F)cc3)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111565 78470 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1cccc2c(OCc3ccc(OC(F)(F)F)cc3)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44319713 107224 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL316361 107224 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
16224190 69007 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 544 11 2 4 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(C)cc(C)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922924 69007 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 544 11 2 4 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(C)cc(C)c1 10.1016/j.bmcl.2011.09.105
58353839 110357 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
CHEMBL3238238 110357 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
10324097 56878 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56878 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
10461010 56944 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644186 56944 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11786041 189749 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 540 7 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2C2CCCC2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL515045 189749 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 540 7 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2C2CCCC2)CC1 10.1016/j.bmcl.2008.05.072
11145271 164859 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 479 8 2 6 4.3 COc1cc(OCCN2CCc3ccccc3C2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL421795 164859 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 479 8 2 6 4.3 COc1cc(OCCN2CCc3ccccc3C2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44361298 121555 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL358250 121555 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
11024350 208874 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 343 5 1 2 5.1 Fc1ccc(-c2[nH]c(CCc3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87858 208874 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 343 5 1 2 5.1 Fc1ccc(-c2[nH]c(CCc3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
135542439 5474 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 306 3 3 4 3.0 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
CHEMBL107526 5474 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 306 3 3 4 3.0 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
44372948 52021 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 52021 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353013 110295 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237895 110295 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11756248 56931 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56931 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
10415955 56952 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644194 56952 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
22999282 53826 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 6 3 5 2.8 NC(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL160419 53826 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 6 3 5 2.8 NC(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
11760806 5098 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 5 2 5 4.4 COc1cc(C(=O)N/N=C/c2ccc(-c3ccc(C)c(Cl)c3)o2)ccc1O 10.1021/jm000547o
CHEMBL105565 5098 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 5 2 5 4.4 COc1cc(C(=O)N/N=C/c2ccc(-c3ccc(C)c(Cl)c3)o2)ccc1O 10.1021/jm000547o
16100312 137297 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 6 4.5 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC3(CC2)OCCO3)cc1 10.1021/jm058026u
CHEMBL375000 137297 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 6 4.5 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC3(CC2)OCCO3)cc1 10.1021/jm058026u
11650288 81416 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
CHEMBL2159333 81416 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
16100311 136506 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.2 CCCC1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL373542 136506 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.2 CCCC1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
73355439 92636 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 0 3 5.7 CSc1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
CHEMBL2435137 92636 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 0 3 5.7 CSc1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
127047256 139858 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798581 139858 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
10413333 63039 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
CHEMBL178768 63039 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
10282162 172524 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 172524 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
44319713 107224 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL316361 107224 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
44319495 208571 None 2 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85807 208571 None 2 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353323 110340 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238221 110340 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353338 110341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 110341 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 110342 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 110342 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11456034 169562 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 8 3 7 7.1 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)c3ccc(Oc4ccc(Cl)cc4)c(Cl)c3)nc2c1 10.1016/j.bmcl.2008.05.072
CHEMBL442855 169562 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 8 3 7 7.1 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)c3ccc(Oc4ccc(Cl)cc4)c(Cl)c3)nc2c1 10.1016/j.bmcl.2008.05.072
57391519 68926 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922702 68926 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
164620899 185799 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3403 112 53 50 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865371 185799 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3403 112 53 50 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10864173 49845 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC(=O)N2CCc3ccccc3C2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156772 49845 None 0 Human Binding pIC50 = 7.9 7.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC(=O)N2CCc3ccccc3C2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164624163 185921 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4867132 185921 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372870 53659 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 53659 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44318950 107062 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315311 107062 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
9843239 107129 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315800 107129 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58353046 110337 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 110337 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469443 110363 None 3 Mouse Binding pIC50 = 6.9 6.9 - 1
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
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 110363 None 3 Mouse Binding pIC50 = 6.9 6.9 - 1
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
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
58353156 110306 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 110306 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
51031037 110318 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 110318 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10077369 56946 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56946 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
9871912 192733 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 192733 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
44431016 144332 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL390469 144332 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11102467 47127 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL154269 47127 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
9836535 162233 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 315 3 1 2 4.9 Fc1ccc(-c2[nH]c(-c3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL416169 162233 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 315 3 1 2 4.9 Fc1ccc(-c2[nH]c(-c3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372671 120181 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL351104 120181 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10246001 163601 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL420232 163601 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353544 110299 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 110299 None 0 Mouse Binding pIC50 = 5.9 5.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
56602934 127148 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 503 8 2 4 5.0 CC(C)[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656297 127148 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 503 8 2 4 5.0 CC(C)[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
44373635 53514 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 452 8 2 5 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160138 53514 None 0 Human Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 452 8 2 5 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10215420 98553 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL276063 98553 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
22496546 188559 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 188559 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
10962393 50366 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 521 10 3 6 5.0 COc1cc(OCCNCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL157226 50366 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 521 10 3 6 5.0 COc1cc(OCCNCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164626335 186471 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875380 186471 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372846 53605 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160238 53605 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
16100313 83285 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 591 13 3 4 7.4 CCCC1(CCC)CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL218740 83285 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 591 13 3 4 7.4 CCCC1(CCC)CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44389598 64893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 64893 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
10231964 185862 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 185862 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
10145603 189179 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 189179 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
10280734 192591 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 192591 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
58353046 110337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 110337 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44561584 186832 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 8 3 6 4.4 Cn1c(N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL488682 186832 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 8 3 6 4.4 Cn1c(N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57401963 68922 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922698 68922 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
57393252 68993 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922843 68993 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL413890 215557 None 21 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)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](CCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10907780 119698 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 553 9 3 7 5.4 COc1cc(NC(=O)CSc2ccc(OC(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346694 119698 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 553 9 3 7 5.4 COc1cc(NC(=O)CSc2ccc(OC(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10951675 46747 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 541 9 3 5 6.4 O=C(N/N=C/c1ccc(OCCNCc2ccc(Cl)c(Cl)c2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL153950 46747 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 541 9 3 5 6.4 O=C(N/N=C/c1ccc(OCCNCc2ccc(Cl)c(Cl)c2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
60171060 81434 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81434 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
44373083 52386 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 52386 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372701 52553 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159198 52553 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372397 53763 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160372 53763 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372688 49442 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 49442 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44318935 208489 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85102 208489 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353067 110336 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 110336 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 110342 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 110342 None 0 Mouse Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44373783 120249 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 438 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC2CCCCO2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
CHEMBL351724 120249 None 0 Human Binding pIC50 = 6.9 6.9 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 438 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC2CCCCO2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
16100302 136504 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2)CC1 10.1021/jm058026u
CHEMBL373541 136504 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2)CC1 10.1021/jm058026u
44318950 107062 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL315311 107062 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
19072347 52527 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159163 52527 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10318451 208534 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85534 208534 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
22005335 94484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL25115 94484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
22005335 94484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(02)00143-9
CHEMBL25115 94484 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(02)00143-9
12967031 111635 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL328126 111635 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
44418928 83388 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 523 13 3 4 5.8 CCCCC(CC)N(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm058026u
CHEMBL219308 83388 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 523 13 3 4 5.8 CCCCC(CC)N(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm058026u
44372676 119700 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL346698 119700 None 0 Human Binding pIC50 = 4.9 4.9 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
3505 2212 None 35 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
5311276 2212 None 35 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
CHEMBL351772 2212 None 35 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
127047122 140001 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
CHEMBL3799499 140001 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
127047255 140109 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
CHEMBL3800146 140109 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
164618212 185495 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4860642 185495 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11950794 161325 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 161325 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
71202713 110356 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238237 110356 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
45381380 110328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[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
CHEMBL3237927 110328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[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
71202743 110343 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3238224 110343 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
44561327 190563 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(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
CHEMBL517861 190563 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(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
122189705 123439 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616684 123439 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170968 81429 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159345 81429 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
164616848 185055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4853767 185055 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170768 81412 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159329 81412 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11733947 161859 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 510 8 3 6 4.6 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL413964 161859 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 510 8 3 6 4.6 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
44318934 208454 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84840 208454 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
44319495 208571 None 2 Human Binding pIC50 = 6.8 6.8 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85807 208571 None 2 Human Binding pIC50 = 6.8 6.8 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
12967034 120088 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 120088 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373192 119800 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 119800 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353369 110307 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 110307 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
44373781 54957 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 476 8 2 6 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(F)c(F)c1 10.1016/s0960-894x(01)00819-8
CHEMBL161431 54957 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 476 8 2 6 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(F)c(F)c1 10.1016/s0960-894x(01)00819-8
44361158 121002 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL356089 121002 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
10093802 106970 None 3 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL314701 106970 None 3 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
10318451 208534 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL85534 208534 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
9998923 106962 None 2 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314652 106962 None 2 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352935 110297 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 110297 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353679 110314 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 110314 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
70900317 110321 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237920 110321 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44373553 54104 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 422 7 2 4 5.5 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cc2)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160652 54104 None 0 Human Binding pIC50 = 5.8 5.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 422 7 2 4 5.5 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cc2)cc1 10.1016/s0960-894x(01)00819-8
22496358 187425 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 187425 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
16100304 83377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 641 9 3 4 7.2 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2Br)CC1 10.1021/jm058026u
CHEMBL219252 83377 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 641 9 3 4 7.2 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2Br)CC1 10.1021/jm058026u
10435275 123931 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL362657 123931 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
135819157 9972 None 1 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 9972 None 1 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
16100300 137326 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 137326 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
16225178 68998 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 586 12 2 4 7.7 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1Cc1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922915 68998 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 586 12 2 4 7.7 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1Cc1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
57397957 69016 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 598 12 2 4 7.7 CCCC[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
CHEMBL1922932 69016 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 598 12 2 4 7.7 CCCC[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
57392671 69023 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922939 69023 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
53469628 110353 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 110353 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11260553 176325 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 5.4 CCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459458 176325 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 5.4 CCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11261540 188942 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 562 8 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL506520 188942 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 562 8 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
60170855 81418 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81418 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
11048232 50420 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 428 7 2 5 3.6 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL157280 50420 None 0 Human Binding pIC50 = 7.8 7.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 428 7 2 5 3.6 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
11585452 81421 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81421 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
58353126 110335 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 110335 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
70900317 110321 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237920 110321 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44561557 179005 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 4.6 Cn1c(N(Cc2ccc(C(=O)NCc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL469904 179005 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 4.6 Cn1c(N(Cc2ccc(C(=O)NCc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11433550 68924 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922700 68924 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
44373923 54967 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 478 6 2 7 5.2 CC(C)(C)c1nc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)no1 10.1016/s0960-894x(01)00819-8
CHEMBL161505 54967 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 478 6 2 7 5.2 CC(C)(C)c1nc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)no1 10.1016/s0960-894x(01)00819-8
9952509 208836 None 13 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87588 208836 None 13 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372577 53688 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 238 2 1 1 3.9 Fc1ccc(-c2cc[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160314 53688 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 238 2 1 1 3.9 Fc1ccc(-c2cc[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
9929037 53900 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160490 53900 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44372720 48589 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 48589 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
10255803 56934 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644176 56934 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
164629129 186583 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876913 186583 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
71452715 78912 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 6 2 6 3.5 CC(C)S(=O)(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL2112904 78912 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 6 2 6 3.5 CC(C)S(=O)(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
9914410 186563 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 186563 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
16100314 83489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 544 10 3 5 6.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cccc([N+](=O)[O-])c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
CHEMBL219968 83489 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 544 10 3 5 6.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cccc([N+](=O)[O-])c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
44372847 53661 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160289 53661 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
12967035 51852 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 51852 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
57397956 69004 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCC[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
CHEMBL1922921 69004 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCC[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
57396140 69018 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 12 2 4 8.0 CC(C)CC[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
CHEMBL1922934 69018 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 12 2 4 8.0 CC(C)CC[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
71243036 110334 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 110334 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
3505 2212 None 35 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 2212 None 35 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 2212 None 35 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
44372471 48575 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 48575 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353338 110341 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 110341 None 0 Mouse Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352935 110297 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 110297 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353695 110315 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 110315 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11785044 189775 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL515202 189775 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
12967034 120088 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 120088 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58352925 110302 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237902 110302 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353369 110307 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 110307 None 0 Mouse Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
10436554 56881 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643958 56881 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
122189571 123408 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616582 123408 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
56602932 127140 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 543 9 2 4 5.4 CC1(C2CCCCC2)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656289 127140 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 543 9 2 4 5.4 CC1(C2CCCCC2)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
56602931 127141 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 475 8 2 4 3.8 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656290 127141 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 475 8 2 4 3.8 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
56602995 127146 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 501 8 2 4 4.7 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)C1CC1 nan
CHEMBL3656295 127146 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 501 8 2 4 4.7 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)C1CC1 nan
16100319 83371 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 8 3 4 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL219191 83371 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 8 3 4 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
11559533 140261 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 359 7 0 3 4.9 O=C(c1ccc(OCCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
CHEMBL380387 140261 None 0 Human Binding pIC50 = 4.8 4.8 - 0
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 359 7 0 3 4.9 O=C(c1ccc(OCCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
16100336 83423 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 513 11 3 3 5.4 CCCCc1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
CHEMBL219446 83423 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 513 11 3 3 5.4 CCCCc1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
135819146 110382 None 6 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 110382 None 6 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10144633 172530 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 172530 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
11157621 68921 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922697 68921 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11238073 68927 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922703 68927 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL439289 216295 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL None None None CN[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)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](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(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(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2005.01.003
44372948 52021 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 52021 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
145969968 165174 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226972 165174 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
44373676 52472 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 524 9 2 7 5.3 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL159093 52472 None 0 Human Binding pIC50 = 6.8 6.8 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 524 9 2 7 5.3 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00819-8
44372406 119880 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL348401 119880 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
6862006 172423 None 6 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 290 3 2 3 3.3 O=C(N/N=C/c1cccc2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
CHEMBL447535 172423 None 6 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 290 3 2 3 3.3 O=C(N/N=C/c1cccc2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
22005118 31810 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 399 11 1 2 7.5 CCCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140636 31810 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 399 11 1 2 7.5 CCCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22005111 119497 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 297 5 1 2 5.1 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL344911 119497 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 297 5 1 2 5.1 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
44369318 45096 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 444 6 2 5 4.4 CC(C)CS(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL152461 45096 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 444 6 2 5 4.4 CC(C)CS(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
1148 1924 None 28 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
619101 1924 None 28 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
CHEMBL179281 1924 None 28 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
127046644 139665 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3797325 139665 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
16100305 83360 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 617 11 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2C(F)(F)F)CC1 10.1021/jm058026u
CHEMBL219138 83360 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 617 11 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2C(F)(F)F)CC1 10.1021/jm058026u
164613898 184828 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4850520 184828 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
57403704 68995 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922845 68995 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11812426 78914 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 451 5 2 7 3.7 CN(C)c1ccc(C(=O)n2cc(/C=N/NC(=O)c3ccc(O)c(C#N)c3)c3ccccc32)cc1 10.1021/jm0208572
CHEMBL2112907 78914 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 451 5 2 7 3.7 CN(C)c1ccc(C(=O)n2cc(/C=N/NC(=O)c3ccc(O)c(C#N)c3)c3ccccc32)cc1 10.1021/jm0208572
10995358 45048 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 565 10 3 5 5.9 O=C(N/N=C/c1ccc(OCCNCCc2ccc(Br)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152409 45048 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 565 10 3 5 5.9 O=C(N/N=C/c1ccc(OCCNCCc2ccc(Br)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
135819137 92904 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL24388 92904 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
9929037 53900 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 53900 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
135819149 10454 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 10454 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
10338890 208480 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85009 208480 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353838 110339 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238220 110339 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353544 110299 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 110299 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71203427 110320 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237919 110320 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
135819137 92904 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
CHEMBL24388 92904 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
19072347 52527 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL159163 52527 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44319442 208783 None 1 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 383 3 1 3 5.3 Fc1ccc(-c2[nH]c(-c3ccc(Br)o3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87248 208783 None 1 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 383 3 1 3 5.3 Fc1ccc(-c2[nH]c(-c3ccc(Br)o3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44373707 54966 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 483 10 2 5 5.7 COc1cc(CCNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL161494 54966 None 0 Human Binding pIC50 = 5.7 5.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 483 10 2 5 5.7 COc1cc(CCNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
22004948 93374 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 387 9 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(CO)c1 10.1016/s0960-894x(02)00143-9
CHEMBL24527 93374 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 387 9 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(CO)c1 10.1016/s0960-894x(02)00143-9
145968206 165287 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228703 165287 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
53469258 110351 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
CHEMBL3238232 110351 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
16100310 79136 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 576 10 3 5 4.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCN(C(=O)C3CC3)CC2)cc1 10.1021/jm058026u
CHEMBL2113259 79136 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 576 10 3 5 4.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCN(C(=O)C3CC3)CC2)cc1 10.1021/jm058026u
44561440 172692 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 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(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL448921 172692 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 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(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
44561391 175766 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 502 6 3 8 4.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(O)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL458145 175766 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 502 6 3 8 4.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(O)ccc21 10.1016/j.bmcl.2008.05.072
11249762 183947 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 183947 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
44561439 191310 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 191310 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
122189573 123410 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(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
CHEMBL3616584 123410 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(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
122189696 123430 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616675 123430 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
129010852 142872 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2ccccc12 nan
CHEMBL3892787 142872 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2ccccc12 nan
11444850 68989 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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 68989 None 0 Human Binding pIC50 = 8.7 8.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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
9955419 45302 None 8 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity against human glucagon receptorAntagonist activity against human glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1016/j.bmcl.2014.07.025
CHEMBL152640 45302 None 8 Human Binding pIC50 = 8.6 8.6 - 1
Antagonist activity against human glucagon receptorAntagonist activity against human glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1016/j.bmcl.2014.07.025
46853083 160416 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 593 8 2 5 8.1 CCC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL4110618 160416 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 593 8 2 5 8.1 CCC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
9955419 45302 None 8 Human Binding pIC50 = 8.6 8.6 - 1
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL152640 45302 None 8 Human Binding pIC50 = 8.6 8.6 - 1
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
11952035 151559 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 151559 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
46853084 159950 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 607 9 2 5 7.8 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL4106672 159950 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 607 9 2 5 7.8 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
57518490 81420 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81420 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
122189709 123443 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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 123443 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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
122189722 123457 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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 123457 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
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
11273570 68938 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(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
CHEMBL1922714 68938 None 0 Human Binding pIC50 = 8.6 8.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(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
11038653 45114 None 0 Human Binding pIC50 = 8.6 8.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 522 6 2 6 5.4 N#Cc1cc(C(=O)N/N=C/c2ccc(N(C(=O)C3CCCC3)C(=O)C3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL152477 45114 None 0 Human Binding pIC50 = 8.6 8.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 522 6 2 6 5.4 N#Cc1cc(C(=O)N/N=C/c2ccc(N(C(=O)C3CCCC3)C(=O)C3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
44373213 119901 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 119901 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819157 9972 None 1 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 9972 None 1 Human Binding pIC50 = 7.7 7.7 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
11570626 2550 None 32 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
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 10.1016/j.bmc.2018.02.036
9135 2550 None 32 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
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 10.1016/j.bmc.2018.02.036
CHEMBL1933349 2550 None 32 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
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 10.1016/j.bmc.2018.02.036
DB12044 2550 None 32 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
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 10.1016/j.bmc.2018.02.036
10073574 45441 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1021/jm0208572
CHEMBL152765 45441 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1021/jm0208572
10073574 45441 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL152765 45441 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44319258 208447 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1007/s00044-013-0869-9
CHEMBL84759 208447 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1007/s00044-013-0869-9
44373192 119800 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 119800 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
12967031 111635 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL328126 111635 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
135503676 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
CHEMBL107070 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
58352937 110348 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 110348 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
141465320 165260 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4228215 165260 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
11068219 49693 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1cccc2c(CO)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156654 49693 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1cccc2c(CO)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
135503676 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
CHEMBL107070 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
135538098 163473 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 3 4 5 2.6 Nc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL419364 163473 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 3 4 5 2.6 Nc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
135819157 9972 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 9972 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
9902041 61861 None 16 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17736 61861 None 16 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10592750 107209 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL316264 107209 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
53323247 56875 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56875 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
56602933 127149 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 5.5 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656298 127149 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 5.5 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
11383934 51800 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 8 2 7 3.3 COc1cc(CO/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1C(C)C 10.1016/s0960-894x(01)00819-8
CHEMBL158497 51800 None 0 Human Binding pIC50 = 4.7 4.7 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 8 2 7 3.3 COc1cc(CO/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1C(C)C 10.1016/s0960-894x(01)00819-8
22005295 34160 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 311 8 1 2 5.1 CCCCCc1c(CC)nc(CC)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL142589 34160 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 311 8 1 2 5.1 CCCCCc1c(CC)nc(CC)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
127046645 139732 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3797757 139732 None 0 Human Binding pIC50 = 4.7 4.7 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
135503676 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL107070 5387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
58352803 110338 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 110338 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
16100296 205297 None 41 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 205297 None 41 Human Binding pIC50 = 7.7 7.7 - 1
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
11114038 44711 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152103 44711 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111214 44711 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372888 53979 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160550 53979 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
15407872 60154 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL17396 60154 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0869-9
16100303 83312 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2OC(F)(F)F)CC1 10.1021/jm058026u
CHEMBL218871 83312 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2OC(F)(F)F)CC1 10.1021/jm058026u
11952035 86851 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86851 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
22496449 174541 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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 174541 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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
11950971 150993 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 150993 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
45381379 110329 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(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
CHEMBL3237928 110329 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(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
90655064 110347 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238228 110347 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11951857 97040 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL266489 97040 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
11826682 119593 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 5 2 5 5.1 N#Cc1cc(C(=O)N/N=C/c2cccc3c2ccn3Cc2ccc(C(F)(F)F)cc2)ccc1O 10.1021/jm0208572
CHEMBL345713 119593 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 5 2 5 5.1 N#Cc1cc(C(=O)N/N=C/c2cccc3c2ccn3Cc2ccc(C(F)(F)F)cc2)ccc1O 10.1021/jm0208572
10982999 165048 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 437 7 2 4 4.4 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL422506 165048 None 0 Human Binding pIC50 = 7.7 7.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 437 7 2 4 4.4 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
9957123 120002 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(OC(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL349552 120002 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(OC(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
9929037 53900 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 53900 None 0 Mouse Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10076995 56953 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644195 56953 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
11186974 33968 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142414 33968 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44319495 208571 None 2 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85807 208571 None 2 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
10338890 208480 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85009 208480 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
135819133 114478 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 114478 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
44372847 53661 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160289 53661 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44318988 208465 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84917 208465 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352940 110301 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237901 110301 None 0 Mouse Binding pIC50 = 5.7 5.7 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
1714260 208470 None 10 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 374 3 1 1 6.2 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL84952 208470 None 10 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 374 3 1 1 6.2 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)cc1 10.1007/s00044-013-0869-9
59092268 78916 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 470 6 2 5 4.8 O=C(N/N=C/c1ccc(CS(=O)(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2112909 78916 None 0 Human Binding pIC50 = 6.7 6.7 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 470 6 2 5 4.8 O=C(N/N=C/c1ccc(CS(=O)(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
20775791 188806 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 597 10 3 7 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL504260 188806 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 597 10 3 7 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100298 83387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm058026u
CHEMBL219307 83387 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm058026u
16223791 69008 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922925 69008 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
45381051 110325 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[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
CHEMBL3237924 110325 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[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
58353067 110336 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 110336 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9824797 45740 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1021/jm0208572
CHEMBL153038 45740 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1021/jm0208572
44373782 119925 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 9 2 6 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL348785 119925 None 0 Human Binding pIC50 = 7.6 7.6 - 1
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 9 2 6 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10338890 208480 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85009 208480 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
16100296 72436 None 41 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 72436 None 41 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
12967034 120088 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of MgBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of Mg
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 120088 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of MgBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of Mg
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373083 52386 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 52386 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
145969316 165226 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227667 165226 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
11352330 186679 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 490 8 2 5 5.4 Cn1c(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL487828 186679 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 490 8 2 5 5.4 Cn1c(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44372701 52553 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159198 52553 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372700 168713 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL436022 168713 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58353662 110305 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 110305 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44275043 98754 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 354 8 2 3 5.8 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1N 10.1016/s0960-894x(02)00143-9
CHEMBL277627 98754 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 354 8 2 3 5.8 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1N 10.1016/s0960-894x(02)00143-9
135504174 5422 None 2 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 309 4 3 4 2.6 COc1cc(C(=O)N/N=C/c2c[nH]c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL107258 5422 None 2 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 309 4 3 4 2.6 COc1cc(C(=O)N/N=C/c2c[nH]c3ccccc23)ccc1O 10.1021/jm000547o
60170766 81409 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
CHEMBL2159326 81409 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
164617749 184675 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 52 49 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)CN(CCCC(=O)O)C(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4848485 184675 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 52 49 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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)CN(CCCC(=O)O)C(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
16224591 69003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922920 69003 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
71243005 110326 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[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
CHEMBL3237925 110326 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[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
53469443 110363 None 3 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
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 110363 None 3 Human Binding pIC50 = 7.6 7.6 - 1
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
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
11283703 175199 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 8 2 7 5.8 CCCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL456877 175199 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 8 2 7 5.8 CCCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11410772 68709 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1921810 68709 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
44372720 48589 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 48589 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
22004988 165266 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL422833 165266 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
10076778 56954 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 10 2 5 6.5 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)NCCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.11.074
CHEMBL1644196 56954 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 10 2 5 6.5 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)NCCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.11.074
44319713 107224 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1007/s00044-013-0869-9
CHEMBL316361 107224 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1007/s00044-013-0869-9
16100301 169359 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 578 11 3 4 6.0 CCN(CC)C(=O)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
CHEMBL441160 169359 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 578 11 3 4 6.0 CCN(CC)C(=O)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
135819149 10454 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 10454 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
22496358 187425 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter 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 187425 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter 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
44372847 53661 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160289 53661 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
3505 2212 None 35 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 2212 None 35 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 2212 None 35 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
10461326 56945 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 2 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644187 56945 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 2 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
22005250 34587 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.5 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142944 34587 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.5 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44319474 107109 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL315613 107109 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
58352863 110304 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237904 110304 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10873618 51107 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 426 7 2 5 3.6 CCN(CC)C(=O)Cn1ccc2c(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cccc21 10.1021/jm0208572
CHEMBL157913 51107 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 426 7 2 5 3.6 CCN(CC)C(=O)Cn1ccc2c(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cccc21 10.1021/jm0208572
44372700 168713 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL436022 168713 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
57394374 69021 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922937 69021 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
68243839 110344 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
CHEMBL3238225 110344 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
122189699 123433 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
CHEMBL3616678 123433 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
12967035 51852 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 51852 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44373103 54159 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160690 54159 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
11142525 5699 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 346 5 2 4 3.8 COc1cc(C(=O)N/N=C/c2ccc(-c3ccccc3)cc2)ccc1O 10.1021/jm000547o
CHEMBL107802 5699 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 346 5 2 4 3.8 COc1cc(C(=O)N/N=C/c2ccc(-c3ccccc3)cc2)ccc1O 10.1021/jm000547o
20775792 188889 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 9 3 6 5.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL505685 188889 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 9 3 6 5.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100315 83334 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 5.7 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
CHEMBL219010 83334 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 5.7 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
44372677 53774 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL160380 53774 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
11048896 48370 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 464 5 2 5 3.3 CN1CCN(C(=O)Cc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)CC1 10.1021/jm0208572
CHEMBL155449 48370 None 0 Human Binding pIC50 = 6.6 6.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 464 5 2 5 3.3 CN1CCN(C(=O)Cc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)CC1 10.1021/jm0208572
10369510 173221 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 173221 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
44319474 107109 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315613 107109 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10257357 141925 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor 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/jm058026u
CHEMBL386446 141925 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor 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/jm058026u
9869430 122033 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 6.1 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(Cl)c(Cl)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL359126 122033 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 6.1 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(Cl)c(Cl)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
11049977 119711 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346801 119711 None 0 Human Binding pIC50 = 7.6 7.6 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44373213 119901 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 119901 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
12967035 51852 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 51852 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
9952509 208836 None 13 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL87588 208836 None 13 Human Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
53469821 110358 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238240 110358 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44372405 52015 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158671 52015 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
10077065 56950 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)NCCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644192 56950 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)NCCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
44373585 51884 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 464 9 3 7 4.6 COc1cc(/C=N/NC(=O)c2ccc(O)c(O)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158556 51884 None 0 Human Binding pIC50 = 5.6 5.6 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 464 9 3 7 4.6 COc1cc(/C=N/NC(=O)c2ccc(O)c(O)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
145967583 165047 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4225050 165047 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
145970933 165246 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4227967 165246 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
129010851 151073 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 553 10 2 3 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C)cc(Cl)cc12 nan
CHEMBL3958315 151073 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 553 10 2 3 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C)cc(Cl)cc12 nan
135819143 9980 None 6 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114799 9980 None 6 Human Binding pIC50 = 7.6 7.6 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
16223987 69001 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922918 69001 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
16224781 69011 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
CHEMBL1922928 69011 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
53325824 56943 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 9 3 6 5.6 O=C(NC[C@@H](O)C(=O)O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644185 56943 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 9 3 6 5.6 O=C(NC[C@@H](O)C(=O)O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11949739 161327 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 161327 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11037917 50109 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 7 3 6 3.9 COc1cc(NC(=O)Cc2ccc(Cl)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL157000 50109 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 7 3 6 3.9 COc1cc(NC(=O)Cc2ccc(Cl)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
45381379 110329 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(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
CHEMBL3237928 110329 None 0 Mouse Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(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
145967899 165185 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227099 165185 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
10066912 208620 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL86250 208620 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319712 105988 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3cc(Br)cs3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL312825 105988 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3cc(Br)cs3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58353695 110315 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 110315 None 0 Mouse Binding pIC50 = 5.6 5.6 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
135501650 5688 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1O 10.1021/jm000547o
CHEMBL107795 5688 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1O 10.1021/jm000547o
44372650 53810 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160401 53810 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44372688 49442 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL156458 49442 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
11113699 47349 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1ccc2c(ccn2Cc2ccc(OC(F)(F)F)cc2)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154437 47349 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1ccc2c(ccn2Cc2ccc(OC(F)(F)F)cc2)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
11024220 46697 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 338 4 3 4 2.9 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm0208572
CHEMBL153905 46697 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 338 4 3 4 2.9 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm0208572
11782911 119579 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 345 4 3 5 2.7 N#Cc1cc(C(=O)N/N=C/c2ccc(CO)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL345589 119579 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 345 4 3 5 2.7 N#Cc1cc(C(=O)N/N=C/c2ccc(CO)c3ccccc23)ccc1O 10.1021/jm0208572
10093802 106970 None 3 Human Binding pIC50 = 6.5 6.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314701 106970 None 3 Human Binding pIC50 = 6.5 6.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
44372556 49164 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL156207 49164 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373191 119778 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347462 119778 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
9952509 208836 None 13 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL87588 208836 None 13 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
10882636 4864 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 350 5 2 5 3.3 COc1cc(C(=O)N/N=C/c2ccc(OC)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104338 4864 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 350 5 2 5 3.3 COc1cc(C(=O)N/N=C/c2ccc(OC)c3ccccc23)ccc1O 10.1021/jm000547o
10481623 56879 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643956 56879 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
9983854 56930 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644172 56930 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
53325825 56960 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644202 56960 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
11034750 169514 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 326 4 2 4 3.5 COc1cc(C(=O)N/N=C/c2ccc(C(C)(C)C)cc2)ccc1O 10.1021/jm000547o
CHEMBL442389 169514 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 326 4 2 4 3.5 COc1cc(C(=O)N/N=C/c2ccc(C(C)(C)C)cc2)ccc1O 10.1021/jm000547o
16100321 137980 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 564 8 4 5 5.5 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)NO)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL376322 137980 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 564 8 4 5 5.5 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)NO)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44373192 119800 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 119800 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
122189580 123417 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616591 123417 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189702 123436 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616681 123436 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189711 123445 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616690 123445 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
11308245 68986 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(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
CHEMBL1922836 68986 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(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
23550062 56874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56874 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
129010863 152160 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL3967446 152160 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
122189716 123450 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616695 123450 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
11950795 86852 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86852 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11145871 49792 None 0 Human Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 531 6 2 5 6.2 O=C(N/N=C/c1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156724 49792 None 0 Human Binding pIC50 = 8.5 8.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 531 6 2 5 6.2 O=C(N/N=C/c1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
122189719 123453 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616698 123453 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
11952211 153830 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 153830 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
10032265 186428 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 186428 None 1 Human Binding pIC50 = 8.4 8.4 - 1
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
44372904 53989 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160561 53989 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819133 114478 None 1 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 114478 None 1 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
44372688 49442 None 0 Mouse Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 49442 None 0 Mouse Binding pIC50 = 7.5 7.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
11490222 68930 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(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
CHEMBL1922706 68930 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(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
145969571 165263 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228281 165263 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
22004872 34513 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142886 34513 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44372701 52553 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL159198 52553 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
10133915 61789 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL17722 61789 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319276 208567 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL85741 208567 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372478 51870 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 51870 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10076914 56947 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644189 56947 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
22005388 94526 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(F)c1 10.1016/s0960-894x(02)00143-9
CHEMBL25137 94526 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(F)c1 10.1016/s0960-894x(02)00143-9
44373464 119766 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 496 9 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C(=O)O)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL347370 119766 None 0 Human Binding pIC50 = 4.5 4.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 496 9 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C(=O)O)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44372478 51870 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 51870 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44369291 45167 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 469 7 2 5 5.4 O=C(N/N=C/c1cn(Cc2ccc(OC(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152537 45167 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 469 7 2 5 5.4 O=C(N/N=C/c1cn(Cc2ccc(OC(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
57399593 69002 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922919 69002 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
58352937 110348 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 110348 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
44561390 176140 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459032 176140 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57403703 68992 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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 68992 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
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
44373486 52111 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 516 9 2 6 6.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2Cl)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158753 52111 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 516 9 2 6 6.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2Cl)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
71243005 110326 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[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
CHEMBL3237925 110326 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[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
145967924 165223 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4227634 165223 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
22496395 187454 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 187454 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
127047120 139813 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
CHEMBL3798231 139813 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
16225394 69000 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922917 69000 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
10054055 188533 None 9 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)[C@H]1CC[C@@]2(CCN(c3ccc(OC(F)(F)F)cc3)C(=O)N2Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL502203 188533 None 9 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)[C@H]1CC[C@@]2(CCN(c3ccc(OC(F)(F)F)cc3)C(=O)N2Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)CC1 10.1016/j.bmcl.2008.05.072
44372396 54071 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 252 2 1 1 4.2 Cc1cc(-c2ccc(F)cc2)c(-c2ccncc2)[nH]1 10.1007/s00044-013-0801-3
CHEMBL160627 54071 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 252 2 1 1 4.2 Cc1cc(-c2ccc(F)cc2)c(-c2ccncc2)[nH]1 10.1007/s00044-013-0801-3
44319591 106636 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314238 106636 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352952 110308 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237908 110308 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10044081 62623 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nnc(CC(C)C)o2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL178302 62623 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nnc(CC(C)C)o2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
145968140 165186 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227111 165186 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10928006 120272 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 4 3 4 4.9 CC(C)(C)C(=O)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL352005 120272 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 4 3 4 4.9 CC(C)(C)C(=O)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
11114038 44711 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152103 44711 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111214 44711 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
9956429 49708 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 5.8 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(C(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156666 49708 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 5.8 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(C(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
58353679 110314 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 110314 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53316573 56958 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644200 56958 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
44373586 54192 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160715 54192 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
58352868 110298 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237898 110298 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353156 110306 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 110306 None 0 Mouse Binding pIC50 = 5.5 5.5 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44318935 208489 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85102 208489 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
71454981 81428 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
CHEMBL2159344 81428 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
11952211 153830 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 153830 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
22496457 172661 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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 172661 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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
57396139 69010 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922927 69010 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
22496451 178123 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 178123 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
12967033 54085 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160638 54085 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372923 119606 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 119606 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 119700 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 119700 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353025 110313 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 110313 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11950795 86852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86852 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
44372638 50661 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL157529 50661 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
9998923 106962 None 2 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL314652 106962 None 2 Human Binding pIC50 = 6.5 6.5 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
9843239 107129 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315800 107129 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
135442286 5444 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(O)c1 10.1021/jm000547o
CHEMBL107388 5444 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(O)c1 10.1021/jm000547o
56602867 127135 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 547 10 2 6 5.2 CC(C)CC1(C)N=C(c2cccc(F)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
CHEMBL3656284 127135 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 547 10 2 6 5.2 CC(C)CC1(C)N=C(c2cccc(F)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
135542465 5460 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 374 3 3 4 4.3 O=C(N/N=C/c1ccc(O)c2ccccc12)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm000547o
CHEMBL107473 5460 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 374 3 3 4 4.3 O=C(N/N=C/c1ccc(O)c2ccccc12)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm000547o
122189707 123441 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
CHEMBL3616686 123441 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
16100299 83338 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 521 9 3 3 6.7 CC(C)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
CHEMBL219030 83338 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 521 9 3 3 6.7 CC(C)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
11048133 47374 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 6 2 4 4.4 CCN(CC)C(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154460 47374 None 0 Human Binding pIC50 = 7.5 7.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 6 2 4 4.4 CCN(CC)C(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44372638 50661 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 50661 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
22005015 35315 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 9 1 2 6.8 CCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL143664 35315 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 9 1 2 6.8 CCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
89568983 127144 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 3 4 4.9 CC1(C2CCCCC2)NC(c2cccc(C(F)(F)F)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656293 127144 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 3 4 4.9 CC1(C2CCCCC2)NC(c2cccc(C(F)(F)F)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
44411371 139628 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 411 9 1 4 6.0 COc1ccc(NCCCOc2ccc(C(=O)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2006.02.013
CHEMBL379600 139628 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 411 9 1 4 6.0 COc1ccc(NCCCOc2ccc(C(=O)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2006.02.013
44369018 48028 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 430 5 2 5 4.1 CC(C)S(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL155021 48028 None 0 Human Binding pIC50 = 6.5 6.5 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 430 5 2 5 4.1 CC(C)S(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
11952035 151559 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 151559 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
16100334 83406 None 2 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 83406 None 2 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
53469058 110350 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 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)CC2 10.1021/jm401858f
CHEMBL3238231 110350 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 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)CC2 10.1021/jm401858f
10053841 56940 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56940 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
22496365 188961 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 188961 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
164616563 185512 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4861024 185512 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164612071 184662 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3198 104 49 45 -13.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4848344 184662 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3198 104 49 45 -13.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164622383 186047 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4869368 186047 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
9946911 53937 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160525 53937 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58352834 110311 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237910 110311 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046098 140170 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3800525 140170 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
10383925 78981 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112991 78981 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
3505 2212 None 35 Mouse Binding pIC50 = 7.4 7.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 2212 None 35 Mouse Binding pIC50 = 7.4 7.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 2212 None 35 Mouse Binding pIC50 = 7.4 7.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
57390854 69019 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922935 69019 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
176155 4165 None 0 Human Binding pIC50 = 7.4 7.4 - 3
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL10 4165 None 0 Human Binding pIC50 = 7.4 7.4 - 3
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
164628244 186553 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876499 186553 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164609866 185333 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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[C@H](CCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857992 185333 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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[C@H](CCC(=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](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164624086 185809 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865509 185809 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)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](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170767 81410 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81410 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
44372846 53605 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160238 53605 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58353206 110323 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 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
CHEMBL3237922 110323 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 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
145971078 165103 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4225922 165103 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
56602804 110352 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3238233 110352 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
10030697 179180 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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 179180 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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
44373192 119800 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL347663 119800 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
22496384 187253 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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 187253 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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
45381049 110345 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238226 110345 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
57400189 68929 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922705 68929 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
11102152 49926 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 5 3 4 5.1 O=C(N/N=C/c1ccc(NC(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156837 49926 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 5 3 4 5.1 O=C(N/N=C/c1ccc(NC(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372888 53979 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160550 53979 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44318935 208489 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85102 208489 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10436553 56876 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56876 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
44389584 64614 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 395 7 1 4 5.0 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccccc1)C2 10.1016/j.bmcl.2005.01.003
CHEMBL181669 64614 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 395 7 1 4 5.0 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccccc1)C2 10.1016/j.bmcl.2005.01.003
10415723 56942 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 56942 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
122189723 123458 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616702 123458 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
44372405 52015 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158671 52015 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
135533241 5386 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 324 3 3 4 3.2 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm000547o
CHEMBL107069 5386 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 324 3 3 4 3.2 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm000547o
141465346 165275 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4228470 165275 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
44373462 164889 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2cc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL421833 164889 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2cc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00819-8
127047253 140159 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3800473 140159 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
145989480 165304 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228938 165304 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
44372870 53659 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 53659 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10232009 186567 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 186567 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
45381381 110333 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 110333 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
11785044 176324 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459457 176324 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44561479 179233 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(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
CHEMBL471979 179233 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(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
44561438 189512 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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 189512 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
11421826 68920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922696 68920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
122189570 123407 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(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
CHEMBL3616581 123407 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(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
122189576 123413 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616587 123413 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189581 123418 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616592 123418 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189703 123437 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616682 123437 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189712 123446 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616691 123446 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
122189718 123452 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616697 123452 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
122189720 123454 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616699 123454 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189721 123456 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 615 10 2 5 7.9 CCC(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
CHEMBL3616700 123456 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 615 10 2 5 7.9 CCC(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
11621378 81437 None 3 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81437 None 3 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
11952211 87985 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 87985 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
60170857 81426 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81426 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
44368911 119920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1021/jm0208572
CHEMBL348702 119920 None 0 Human Binding pIC50 = 8.4 8.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1021/jm0208572
11421820 68934 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(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
CHEMBL1922710 68934 None 0 Human Binding pIC50 = 8.4 8.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(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
60170856 81425 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81425 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
10053876 47011 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 574 7 2 5 5.5 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154159 47011 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 574 7 2 5 5.5 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
46853082 160852 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 617 12 2 5 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(-c3ccnn3C)cc(F)cc12 nan
CHEMBL4114029 160852 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 617 12 2 5 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(-c3ccnn3C)cc(F)cc12 nan
11952214 86853 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86853 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11950971 150993 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 150993 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11952394 87046 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 87046 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
10864579 46994 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 551 6 2 6 4.8 N#Cc1cc(C(=O)N/N=C/c2ccc(C(=O)N3CCN(Cc4ccc(Cl)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL154149 46994 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 551 6 2 6 4.8 N#Cc1cc(C(=O)N/N=C/c2ccc(C(=O)N3CCN(Cc4ccc(Cl)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
12967032 53653 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160281 53653 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
12967033 54085 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160638 54085 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372923 119606 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 119606 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 119700 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 119700 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44373191 119778 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347462 119778 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819149 10454 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 10454 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
122189706 123440 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616685 123440 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
10474631 106008 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL312928 106008 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
11678967 81413 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81413 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
44372454 119610 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345863 119610 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372677 53774 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160380 53774 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44319591 106636 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314238 106636 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
51031037 110318 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 110318 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22005204 31676 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 329 6 1 2 5.6 CCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140514 31676 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 329 6 1 2 5.6 CCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
58353350 110312 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237911 110312 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10970292 46195 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL153438 46195 None 0 Human Binding pIC50 = 7.4 7.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
127046643 139883 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798761 139883 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
127047907 140009 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799556 140009 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10053886 191873 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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 191873 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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
57393262 68925 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922701 68925 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
45381051 110325 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[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
CHEMBL3237924 110325 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[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
45381380 110328 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[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
CHEMBL3237927 110328 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[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
22496441 179323 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 587 11 2 7 7.0 COc1ccccc1-c1csc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(SC(F)(F)F)cc2)n1 10.1021/jm8016249
CHEMBL472586 179323 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 587 11 2 7 7.0 COc1ccccc1-c1csc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(SC(F)(F)F)cc2)n1 10.1021/jm8016249
44372946 51771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1007/s00044-013-0801-3
CHEMBL158477 51771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1007/s00044-013-0801-3
12967032 53653 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160281 53653 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
12967033 54085 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160638 54085 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
10324098 56880 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643957 56880 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
56602930 127142 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 4.8 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656291 127142 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 4.8 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
9929037 53900 None 0 Mouse Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 53900 None 0 Mouse Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10326056 56938 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644180 56938 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
44372638 50661 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 50661 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
53323150 56955 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 8 2 7 6.1 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)n1 10.1016/j.bmcl.2010.11.074
CHEMBL1644197 56955 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 8 2 7 6.1 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)n1 10.1016/j.bmcl.2010.11.074
11045195 5243 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 312 5 2 4 3.3 COc1cc(C(=O)N/N=C/c2ccc(C(C)C)cc2)ccc1O 10.1021/jm000547o
CHEMBL106320 5243 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 312 5 2 4 3.3 COc1cc(C(=O)N/N=C/c2ccc(C(C)C)cc2)ccc1O 10.1021/jm000547o
11078726 5330 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 354 5 2 5 3.1 COc1cc(C(=O)N/N=C/c2ccc(OC(F)(F)F)cc2)ccc1O 10.1021/jm000547o
CHEMBL106795 5330 None 0 Human Binding pIC50 = 4.4 4.4 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 354 5 2 5 3.1 COc1cc(C(=O)N/N=C/c2ccc(OC(F)(F)F)cc2)ccc1O 10.1021/jm000547o
58353662 110305 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 110305 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469056 110349 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238230 110349 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
44324149 209501 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL91652 209501 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44373213 119901 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 119901 None 0 Mouse Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58352858 110309 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 110309 None 0 Mouse Binding pIC50 = 5.4 5.4 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11113396 47423 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 466 8 2 5 3.5 CN(C)CCN(C)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154498 47423 None 0 Human Binding pIC50 = 6.4 6.4 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 466 8 2 5 3.5 CN(C)CCN(C)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44372946 51771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
CHEMBL158477 51771 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
57390853 69015 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
CHEMBL1922931 69015 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
10257629 187381 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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 187381 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane 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
12967032 53653 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160281 53653 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
58353025 110313 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 110313 None 0 Mouse Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
16225393 69005 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922922 69005 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
16100296 83376 None 41 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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 10.1021/jm058026u
CHEMBL219244 83376 None 41 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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 10.1021/jm058026u
11081564 47409 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 496 7 3 6 4.2 COc1cc(NC(=O)Cc2cccc(C(F)(F)F)c2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL154485 47409 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 496 7 3 6 4.2 COc1cc(NC(=O)Cc2cccc(C(F)(F)F)c2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
58352954 110319 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237918 110319 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046099 139997 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799468 139997 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
12967035 51852 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL158535 51852 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
22496477 172880 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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 172880 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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
22496371 170029 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 170029 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
44373730 54965 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 9 2 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2F)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL161483 54965 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 9 2 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2F)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10030948 56935 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 9 2 5 7.0 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1644177 56935 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 9 2 5 7.0 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)CC1 10.1016/j.bmcl.2010.11.074
9555433 4951 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1cc(C(=O)N/N=C/c2cccc3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104761 4951 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1cc(C(=O)N/N=C/c2cccc3ccccc23)ccc1O 10.1021/jm000547o
22005048 99760 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 369 9 1 3 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(OC)c1 10.1016/s0960-894x(02)00143-9
CHEMBL284699 99760 None 0 Human Binding pIC50 = 4.3 4.3 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 369 9 1 3 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(OC)c1 10.1016/s0960-894x(02)00143-9
44561285 173208 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 434 4 2 3 6.4 O=C(NC(=O)c1ccccc1Cl)Nc1ccc(Oc2ccc(Cl)cc2)c(Cl)c1 10.1016/j.bmcl.2008.05.072
CHEMBL452040 173208 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 434 4 2 3 6.4 O=C(NC(=O)c1ccccc1Cl)Nc1ccc(Oc2ccc(Cl)cc2)c(Cl)c1 10.1016/j.bmcl.2008.05.072
11813262 49848 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 8 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(Cl)c1OCCN1CCc2ccccc2C1 10.1021/jm0208572
CHEMBL156777 49848 None 0 Human Binding pIC50 = 6.3 6.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 8 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(Cl)c1OCCN1CCc2ccccc2C1 10.1021/jm0208572
44372870 53659 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 53659 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
11952213 86792 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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 86792 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
11102467 47127 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154269 47127 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
9841863 60078 None 21 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL17370 60078 None 21 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372406 119880 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL348401 119880 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
9841863 60078 None 21 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17370 60078 None 21 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58352858 110309 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 110309 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10483611 56937 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644179 56937 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
6875509 5209 None 7 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1ccc(/C=N/NC(=O)c2ccc(O)cc2)c2ccccc12 10.1021/jm000547o
CHEMBL106134 5209 None 7 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1ccc(/C=N/NC(=O)c2ccc(O)cc2)c2ccccc12 10.1021/jm000547o
10960967 163635 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 430 6 2 5 5.0 COc1cc(C(=O)N/N=C/c2cccc(Oc3cccc(C(F)(F)F)c3)c2)ccc1O 10.1021/jm000547o
CHEMBL420290 163635 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 430 6 2 5 5.0 COc1cc(C(=O)N/N=C/c2cccc(Oc3cccc(C(F)(F)F)c3)c2)ccc1O 10.1021/jm000547o
44373083 52386 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 52386 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
56602803 127137 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 495 9 2 4 5.0 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
CHEMBL3656286 127137 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 495 9 2 4 5.0 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
141465337 165183 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4227068 165183 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
10211943 173346 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 173346 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
122189693 123427 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616672 123427 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170971 81432 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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 81432 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
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
9825482 45883 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 459 5 2 4 6.0 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL153157 45883 None 0 Human Binding pIC50 = 8.3 8.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 459 5 2 4 6.0 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c1C 10.1021/jm0208572
9885993 208979 None 12 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL88486 208979 None 12 Human Binding pIC50 = 8.3 8.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
57396141 69022 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922938 69022 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11102344 44923 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 5 2 4 5.7 Cc1cc(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c(C)c1 10.1021/jm0208572
CHEMBL152293 44923 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 5 2 4 5.7 Cc1cc(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c(C)c1 10.1021/jm0208572
10907299 45099 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 505 7 3 4 5.6 O=C(N/N=C/c1ccc(C(=O)NCCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152464 45099 None 0 Human Binding pIC50 = 8.2 8.2 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 505 7 3 4 5.6 O=C(N/N=C/c1ccc(C(=O)NCCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44373083 52386 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL158989 52386 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
9946911 53937 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160525 53937 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44372471 48575 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 48575 None 0 Mouse Binding pIC50 = 7.3 7.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
57882748 140050 None 12 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL3799802 140050 None 12 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
122189698 123432 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
CHEMBL3616677 123432 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
22496449 174541 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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 174541 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon 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
44373527 51595 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 493 10 2 8 4.8 COc1cc(/C=N/NC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158330 51595 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 493 10 2 8 4.8 COc1cc(/C=N/NC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44319257 107136 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccc(F)cc2)ccn1 10.1007/s00044-013-0869-9
CHEMBL315836 107136 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccc(F)cc2)ccn1 10.1007/s00044-013-0869-9
44372677 53774 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160380 53774 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372923 119606 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 119606 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 119700 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 119700 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372454 119610 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345863 119610 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353104 110324 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[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
CHEMBL3237923 110324 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[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
145971123 165171 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226911 165171 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
135819135 94392 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1O 10.1016/s0960-894x(02)00143-9
CHEMBL25066 94392 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1O 10.1016/s0960-894x(02)00143-9
135819157 9972 None 1 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 9972 None 1 Human Binding pIC50 = 5.3 5.3 - 0
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10144925 191955 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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 191955 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR 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
10393937 188495 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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 188495 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor 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
57401358 68997 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 7 2 7 5.6 O=C(Nc1nnn[nH]1)c1ccc(Cn2c(C(=O)c3ccc(OC(F)(F)F)cc3)cc3ccc(C(F)(F)F)cc32)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922914 68997 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 7 2 7 5.6 O=C(Nc1nnn[nH]1)c1ccc(Cn2c(C(=O)c3ccc(OC(F)(F)F)cc3)cc3ccc(C(F)(F)F)cc32)cc1 10.1016/j.bmcl.2011.09.105
10962252 45422 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 507 7 3 5 5.6 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)Nc1ccc(Cl)cc1 10.1021/jm0208572
CHEMBL152747 45422 None 0 Human Binding pIC50 = 7.3 7.3 - 0
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 507 7 3 5 5.6 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)Nc1ccc(Cl)cc1 10.1021/jm0208572
44319617 106614 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314181 106614 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
56602869 127134 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 583 9 2 6 6.7 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)Nc2nnn[nH]2)cc1 nan
CHEMBL3656283 127134 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 583 9 2 6 6.7 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)Nc2nnn[nH]2)cc1 nan
56602870 127143 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 559 10 2 5 5.0 CC1(C2CCCCC2)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656292 127143 None 0 Human Binding pIC50 = 5.3 5.3 - 0
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 559 10 2 5 5.0 CC1(C2CCCCC2)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
57396138 68999 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922916 68999 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
53469628 110353 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 110353 None 0 Mouse Binding pIC50 = 6.3 6.3 - 0
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353132 110283 None 0 Human Binding pIC50 = 6.3 6.3