Purchasability


Ligand source activities (1 row/activity)

Select all ChEMBL ID Receptor Species Purchasable p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Unit Assay Type Assay Description Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles
CHEMBL1933348 glr_human Human Yes - = Funct
UnclassifiedUnclassified
342 6 1 1 6.7 CCCc1c(cc(c(c1c1ccc(cc1)F)C(O)C)C(C)C)C(C)C
CHEMBL266481 glr_human Human Yes - = Funct
UnclassifiedUnclassified
None None None None
CHEMBL4761047 glr_human Human No 10.9 EC50 = 0.0 nM Funct
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
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
CHEMBL4126027 glr_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL4069307 glr_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL4226451 glr_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL4453136 glr_human Human No 10.8 EC50 = 0.0 nM Funct
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
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
CHEMBL266481 glr_mouse Mouse Yes 10.7 EC50 = 0.0 nM Funct
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
None None None None
CHEMBL266481 glr_human Human Yes 10.7 EC50 = 0.0 nM Funct
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
None None None None
CHEMBL4086979 glr_mouse Mouse No 10.6 EC50 = 0.0 nM Funct
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
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
CHEMBL4098061 glr_human Human No 10.6 EC50 = 0.0 nM Funct
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
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
CHEMBL4469604 glr_human Human No 10.6 EC50 = 0.0 nM Funct
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
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
CHEMBL4126953 glr_human Human No 10.6 EC50 = 0.0 nM Funct
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
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
CHEMBL4226514 glr_human Human No 10.6 EC50 = 0.0 nM Funct
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
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
CHEMBL4098061 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4126738 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4227045 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4466715 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4226613 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4571762 glr_human Human No 10.5 EC50 = 0.0 nM Funct
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
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
CHEMBL4458230 glr_human Human No 10.4 EC50 = 0.0 nM Funct
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
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
CHEMBL4586269 glr_human Human No 10.4 EC50 = 0.0 nM Funct
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
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
CHEMBL4578443 glr_human Human No 10.4 EC50 = 0.0 nM Funct
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
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
CHEMBL4225340 glr_human Human No 10.4 EC50 = 0.0 nM Funct
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
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
CHEMBL1222098 glr_human Human No 10.3 EC50 = 0.0 nM Funct
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
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
CHEMBL1222088 glr_human Human No 10.3 EC50 = 0.0 nM Funct
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
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
CHEMBL1222076 glr_human Human No 10.3 EC50 = 0.0 nM Funct
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
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
CHEMBL1222077 glr_human Human No 10.3 EC50 = 0.1 nM Funct
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
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
CHEMBL1222080 glr_human Human No 10.3 EC50 = 0.1 nM Funct
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
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
CHEMBL4755815 glr_human Human No 10.3 EC50 = 0.1 nM Funct
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
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
CHEMBL1222174 glr_human Human No 10.3 EC50 = 0.1 nM Funct
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
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
CHEMBL1222099 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL4751319 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL266481 glr_human Human Yes 10.2 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL1222082 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1222087 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1222090 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL266481 glr_human Human Yes 10.2 EC50 = 0.1 nM Funct
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
None None None None
CHEMBL1222079 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL4444485 glr_human Human No 10.2 EC50 = 0.1 nM Funct
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
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
CHEMBL1222091 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222101 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222085 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222100 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222092 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL4437733 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222089 glr_human Human No 10.1 EC50 = 0.1 nM Funct
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
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
CHEMBL1222078 glr_human Human No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL1222081 glr_human Human No 10.0 EC50 = 0.1 nM Funct
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
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
CHEMBL4745985 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1222097 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL4098991 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL4745235 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1222083 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1222084 glr_human Human No 9.9 EC50 = 0.1 nM Funct
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
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
CHEMBL1222075 glr_human Human No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL4227861 glr_human Human No 9.8 EC50 = 0.2 nM Funct
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
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
CHEMBL4757675 glr_human Human No 9.4 EC50 = 0.4 nM Funct
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
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
CHEMBL4163714 glr_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL1222086 glr_human Human No 9.3 EC50 = 0.5 nM Funct
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
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
CHEMBL4762061 glr_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL1222102 glr_human Human No 9.2 EC50 = 0.6 nM Funct
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
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
CHEMBL4170727 glr_human Human No 9.1 EC50 = 0.8 nM Funct
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
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
CHEMBL4174154 glr_human Human No 9.1 EC50 = 0.9 nM Funct
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
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
CHEMBL4166241 glr_human Human No 9.1 EC50 = 0.9 nM Funct
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
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
CHEMBL266481 glr_human Human Yes 9.0 EC50 = 1.0 nM Funct
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
None None None None
CHEMBL4076828 glr_human Human No 9.0 EC50 = 1.1 nM Funct
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
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
CHEMBL4098545 glr_human Human No 8.9 EC50 = 1.2 nM Funct
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
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
CHEMBL4072029 glr_human Human No 8.9 EC50 = 1.2 nM Funct
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
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
CHEMBL4167331 glr_human Human No 8.9 EC50 = 1.3 nM Funct
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
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
CHEMBL4162383 glr_human Human No 8.9 EC50 = 1.3 nM Funct
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
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
CHEMBL4159256 glr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL4160347 glr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL4167169 glr_human Human No 8.9 EC50 = 1.4 nM Funct
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
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
CHEMBL4173061 glr_human Human No 8.8 EC50 = 1.6 nM Funct
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
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
CHEMBL4175452 glr_human Human No 8.8 EC50 = 1.7 nM Funct
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
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
CHEMBL4162789 glr_human Human No 6.9 EC50 = 122.6 nM Funct
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
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
CHEMBL4159275 glr_human Human No 7.8 EC50 = 14.6 nM Funct
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
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
CHEMBL4170976 glr_human Human No 7.7 EC50 = 18.6 nM Funct
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
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
CHEMBL4060629 glr_human Human No 8.6 EC50 = 2.3 nM Funct
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
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
CHEMBL4466856 glr_human Human No 8.6 EC50 = 2.3 nM Funct
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
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
CHEMBL1222095 glr_human Human No 8.6 EC50 = 2.4 nM Funct
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
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
CHEMBL4169653 glr_human Human No 8.6 EC50 = 2.4 nM Funct
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
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
CHEMBL4174404 glr_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL4163731 glr_human Human No 8.6 EC50 = 2.8 nM Funct
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
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
CHEMBL4177064 glr_human Human No 8.5 EC50 = 3.0 nM Funct
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
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
CHEMBL4130148 glr_human Human No 8.5 EC50 = 3.1 nM Funct
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
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
CHEMBL4172444 glr_human Human No 8.5 EC50 = 3.4 nM Funct
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
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
CHEMBL1222094 glr_human Human No 8.4 EC50 = 3.7 nM Funct
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
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
CHEMBL4174382 glr_human Human No 8.4 EC50 = 3.9 nM Funct
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
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
CHEMBL4749279 glr_rat Rat No 7.5 EC50 = 30 nM Funct
Agonist activity at rat glucagon receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assayAgonist activity at rat glucagon receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation by FRET assay
5221 175 80 73 -23.1 CC[C@H](C)[C@H](NC(=O)C(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](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)O)[C@@H](C)O)C(C)C
CHEMBL427644 glr_rat Rat No 6.5 EC50 = 320 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCCCN)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)Cc2c[nH]cn2)[C@H](C)O)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@H](CCC(N)=O)C(=O)N1)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL4165144 glr_human Human No 8.4 EC50 = 4.4 nM Funct
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
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
CHEMBL4159003 glr_human Human No 8.4 EC50 = 4.5 nM Funct
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
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
CHEMBL4160365 glr_human Human No 8.3 EC50 = 4.8 nM Funct
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
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
CHEMBL4130044 glr_human Human No 7.4 EC50 = 42.9 nM Funct
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
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
CHEMBL266481 glr_rat Rat Yes 8.3 EC50 = 5 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
None None None None
CHEMBL4225594 glr_human Human No 8.3 EC50 = 5.2 nM Funct
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
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
CHEMBL4159426 glr_human Human No 8.3 EC50 = 5.3 nM Funct
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
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
CHEMBL1222093 glr_human Human No 7.3 EC50 = 50 nM Funct
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
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
CHEMBL4161800 glr_human Human No 8.2 EC50 = 7.0 nM Funct
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
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
CHEMBL266411 glr_rat Rat No 6.1 EC50 = 794 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CC(=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)NC(=O)[C@H](N)Cc2c[nH]cn2)[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)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)N1)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL266481 glr_rat Rat Yes 8.1 EC50 = 8 nM Funct
cAMP accumulation in rat hepatocytes in the presence rolipramcAMP accumulation in rat hepatocytes in the presence rolipram
None None None None
CHEMBL4756489 glr_human Human No 8.1 EC50 = 8.4 nM Funct
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
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
CHEMBL3957356 glr_human Human No 10.0 IC50 = 0.1 nM Bind
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).
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
CHEMBL3898076 glr_human Human No 9.7 IC50 = 0.2 nM Bind
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).
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
CHEMBL3918808 glr_human Human No 9.7 IC50 = 0.2 nM Bind
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).
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
CHEMBL428460 glr_rat Rat No 9.7 IC50 = 0.2 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
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]1CCC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2c[nH]cn2)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)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
CHEMBL3617565 glr_human Human No 9.6 IC50 = 0.2 nM Bind
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
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
CHEMBL412488 glr_rat Rat No 9.6 IC50 = 0.2 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
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]1CCC(=O)NCCCC[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)Cc2c[nH]cn2)[C@@H](C)O)[C@@H](C)O)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)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O
CHEMBL3903921 glr_human Human No 9.4 IC50 = 0.4 nM Bind
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).
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
CHEMBL152640 glr_rat Rat No 9.4 IC50 = 0.4 nM Bind
In vitro binding affinity towards rat glucagon receptorIn vitro binding affinity towards rat glucagon receptor
450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C
CHEMBL411831 glr_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL411832 glr_human Human No 9.3 IC50 = 0.5 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL3898694 glr_human Human No 9.2 IC50 = 0.7 nM Bind
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).
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
CHEMBL3616693 glr_human Human No 9.1 IC50 = 0.8 nM Bind
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
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
CHEMBL3974805 glr_human Human No 9.0 IC50 = 1 nM Bind
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).
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
CHEMBL480113 glr_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL499372 glr_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL500315 glr_human Human No 9.0 IC50 = 1 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL3616588 glr_human Human No 9.0 IC50 = 1 nM Bind
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
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
CHEMBL152765 glr_rat Rat No 9.0 IC50 = 1 nM Bind
In vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagon
473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL232239 glr_human Human No 9.0 IC50 = 1.0 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL3939861 glr_human Human No 9.0 IC50 = 1.1 nM Bind
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).
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
CHEMBL3926079 glr_human Human No 8.9 IC50 = 1.3 nM Bind
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).
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
CHEMBL1922834 glr_human Human No 8.9 IC50 = 1.3 nM Bind
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
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
CHEMBL266481 glr_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
None None None None
CHEMBL266481 glr_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
Compound was tested for its ability to displace [125I]glucagon from the glucagon receptorCompound was tested for its ability to displace [125I]glucagon from the glucagon receptor
None None None None
CHEMBL3616689 glr_human Human No 8.8 IC50 = 1.5 nM Bind
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
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
CHEMBL3616692 glr_human Human No 8.8 IC50 = 1.5 nM Bind
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
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
CHEMBL266481 glr_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
None None None None
CHEMBL266481 glr_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
None None None None
CHEMBL429362 glr_rat Rat No 8.8 IC50 = 1.5 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
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](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(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O
CHEMBL266481 glr_rat Rat Yes 8.8 IC50 = 1.5 nM Bind
inhibition of [125]glucagon specific binding.inhibition of [125]glucagon specific binding.
None None None None
CHEMBL3616694 glr_human Human No 8.8 IC50 = 1.6 nM Bind
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
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
CHEMBL3963664 glr_human Human No 8.8 IC50 = 1.7 nM Bind
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).
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
CHEMBL1922708 glr_human Human No 8.8 IC50 = 1.7 nM Bind
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
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
CHEMBL439885 glr_rat Rat No 8.8 IC50 = 1.7 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
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]1CCC(=O)NCCCC[C@H](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)Cc2c[nH]cn2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)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
CHEMBL3943204 glr_human Human No 8.7 IC50 = 1.8 nM Bind
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).
519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1sc2ccccc2c1C
CHEMBL232224 glr_human Human No 8.7 IC50 = 1.8 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL2159349 glr_human Human No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL3616687 glr_human Human No 8.7 IC50 = 1.9 nM Bind
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
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
CHEMBL158676 glr_human Human No 8.0 IC50 = 10 nM Bind
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
402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL323913 glr_human Human Yes 8.0 IC50 = 10 nM Bind
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL486651 glr_human Human No 8.0 IC50 = 10 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL1922933 glr_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL1922936 glr_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL3238216 glr_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL509900 glr_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL3616580 glr_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL3616673 glr_human Human No 8.0 IC50 = 10 nM Bind
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
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
CHEMBL430163 glr_human Human No 8.0 IC50 = 10 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL3037804 glr_rat Rat No 8.0 IC50 = 10 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
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](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](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@H](C)c1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O
CHEMBL153879 glr_human Human No 8.0 IC50 = 10.4 nM Bind
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
533 10 2 6 4.3 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12
CHEMBL2159339 glr_human Human No 8.0 IC50 = 10.7 nM Bind
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
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
CHEMBL3616677 glr_human Human No 7.0 IC50 = 100 nM Funct
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
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
CHEMBL3238215 glr_human Human No 7.0 IC50 = 100 nM Funct
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
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
CHEMBL1922917 glr_human Human No 7.0 IC50 = 100 nM Funct
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
550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1
CHEMBL3799802 glr_human Human Yes 7.0 IC50 = 100 nM Funct
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
587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL3799802 glr_human Human Yes 7.0 IC50 = 100 nM Funct
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
587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL155694 glr_human Human No 7.0 IC50 = 100 nM Bind
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
360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1
CHEMBL160735 glr_human Human No 7.0 IC50 = 100 nM Bind
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
336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1
CHEMBL2369990 glr_rat Rat No 7.0 IC50 = 100 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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
CHEMBL3238219 glr_mouse Mouse No 7.0 IC50 = 100 nM Bind
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
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
CHEMBL4227372 glr_human Human No 7.0 IC50 = 100 nM Bind
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
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
CHEMBL276063 glr_human Human No 7.0 IC50 = 100 nM Bind
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
345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL314181 glr_human Human No 7.0 IC50 = 100 nM Bind
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
441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1
CHEMBL316264 glr_human Human No 7.0 IC50 = 100 nM Bind
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
333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL84373 glr_human Human No 7.0 IC50 = 100 nM Bind
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
390 3 2 2 5.9 Oc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccccc2)cc1
CHEMBL2159334 glr_human Human No 7.0 IC50 = 100.3 nM Bind
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
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
CHEMBL2159327 glr_human Human No 7.0 IC50 = 100.7 nM Funct
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
585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl
CHEMBL436022 glr_human Human No 6.0 IC50 = 1000 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1
CHEMBL114799 glr_human Human Yes 6.0 IC50 = 1000 nM Bind
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL323913 glr_human Human Yes 6.0 IC50 = 1000 nM Bind
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL427744 glr_rat Rat No 6.0 IC50 = 1000 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](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(=O)O)[C@H](C)O
CHEMBL155686 glr_mouse Mouse No 6.0 IC50 = 1000 nM Bind
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
422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL3656296 glr_human Human No 6.0 IC50 = 1000 nM Bind
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.
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
CHEMBL386030 glr_human Human No 6.0 IC50 = 1000 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL140586 glr_human Human No 6.0 IC50 = 1000 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
357 7 1 2 6.2 CC(C)CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1
CHEMBL143609 glr_human Human No 6.0 IC50 = 1000 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
315 5 1 2 5.2 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1
CHEMBL26238 glr_human Human No 6.0 IC50 = 1000 nM Bind
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
353 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(C)cc1
CHEMBL104137 glr_human Human No 5.0 IC50 = 10000 nM Bind
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
321 4 2 5 2.7 COc1cc(C(=O)N/N=C/c2ccnc3ccccc23)ccc1O
CHEMBL85741 glr_human Human No 5.0 IC50 = 10000 nM Bind
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
391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1
CHEMBL3237885 glr_mouse Mouse No 5.0 IC50 = 10000 nM Bind
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
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
CHEMBL3326180 glr_rat Rat No 4.0 IC50 = 100000 nM Bind
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
381 4 3 6 2.9 Cc1cccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)c1
CHEMBL441011 glr_rat Rat No 7.0 IC50 = 101 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
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](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2c[nH]cn2)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](Cc2ccccc2)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
CHEMBL395759 glr_human Human No 6.0 IC50 = 1013 nM Funct
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
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
CHEMBL1933349 e2r517_canlf Dog Yes 7.0 IC50 = 104.5 nM Funct
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
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
CHEMBL374293 glr_human Human No 6.0 IC50 = 1045 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL197851 glr_human Human No 7.0 IC50 = 105 nM Funct
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
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
CHEMBL411831 glr_human Human No 6.0 IC50 = 1052 nM Funct
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
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
CHEMBL2159346 glr_human Human No 7.0 IC50 = 108 nM Funct
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
499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL3799656 glr_human Human No 5.0 IC50 = 10800 nM Funct
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
509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1
CHEMBL234087 glr_human Human No 6.0 IC50 = 1085 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL374994 glr_human Human No 6.0 IC50 = 1088 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL3616581 glr_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL3616590 glr_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL411831 glr_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL430163 glr_human Human No 8.0 IC50 = 11 nM Funct
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
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
CHEMBL480501 glr_human Human No 8.0 IC50 = 11 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1922707 glr_human Human No 8.0 IC50 = 11 nM Bind
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
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
CHEMBL152184 glr_human Human No 8.0 IC50 = 11.3 nM Bind
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
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
CHEMBL154316 glr_human Human No 7.9 IC50 = 11.4 nM Bind
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
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
CHEMBL2159347 glr_human Human No 7.9 IC50 = 11.5 nM Funct
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
587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL158295 glr_human Human No 7.9 IC50 = 11.6 nM Bind
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
454 5 2 5 4.1 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12
CHEMBL3937819 glr_human Human No 7.9 IC50 = 11.8 nM Bind
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).
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
CHEMBL2159337 glr_human Human No 7.9 IC50 = 11.9 nM Funct
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
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
CHEMBL315613 glr_human Human No 7.0 IC50 = 110 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL315828 glr_human Human No 7.0 IC50 = 110 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1
CHEMBL3237900 glr_human Human No 7.0 IC50 = 110 nM Funct
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
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
CHEMBL3238217 glr_human Human No 7.0 IC50 = 110 nM Funct
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
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
CHEMBL25637 glr_human Human No 7.0 IC50 = 110 nM Bind
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1
CHEMBL158548 glr_human Human No 7.0 IC50 = 110 nM Bind
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
296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL3238214 glr_mouse Mouse No 7.0 IC50 = 110 nM Bind
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
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
CHEMBL3238215 glr_mouse Mouse No 7.0 IC50 = 110 nM Bind
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
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
CHEMBL1922923 glr_human Human No 7.0 IC50 = 110 nM Bind
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
584 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(Cl)cc(Cl)c1
CHEMBL4227229 glr_human Human No 7.0 IC50 = 110 nM Bind
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
571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1
CHEMBL1922711 glr_human Human No 7.0 IC50 = 110 nM Bind
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
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
CHEMBL3616676 glr_human Human No 7.0 IC50 = 110 nM Bind
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
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
CHEMBL159071 glr_human Human No 7.0 IC50 = 110 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
466 9 2 6 5.0 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL25637 glr_human Human No 7.0 IC50 = 110 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1
CHEMBL25637 glr_human Human No 7.0 IC50 = 110 nM Bind
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
343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1
CHEMBL84917 glr_human Human No 7.0 IC50 = 110.2 nM Bind
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
399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1
CHEMBL3237915 glr_human Human No 6.0 IC50 = 1100 nM Funct
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
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
CHEMBL155687 glr_human Human No 6.0 IC50 = 1100 nM Bind
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
376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL116413 glr_human Human No 6.0 IC50 = 1100 nM Bind
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O
CHEMBL84759 glr_human Human No 6.0 IC50 = 1100 nM Bind
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
363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1
CHEMBL3237919 glr_mouse Mouse No 6.0 IC50 = 1100 nM Bind
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
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
CHEMBL3237903 glr_human Human No 6.0 IC50 = 1100 nM Bind
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
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
CHEMBL1644190 glr_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1644201 glr_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1644203 glr_human Human No 6.0 IC50 = 1100 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL3656282 glr_human Human No 6.0 IC50 = 1100 nM Bind
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.
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
CHEMBL286555 glr_human Human No 6.0 IC50 = 1100 nM Bind
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
375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(F)c1
CHEMBL24905 glr_human Human No 5.0 IC50 = 11000 nM Bind
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
375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1F
CHEMBL3799820 glr_human Human No 5.0 IC50 = 11100 nM Bind
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
519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1
CHEMBL412352 glr_rat Rat No 7.0 IC50 = 113 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](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(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL197850 glr_human Human No 7.0 IC50 = 113 nM Funct
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
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
CHEMBL1644183 glr_human Human No 6.9 IC50 = 113.8 nM Funct
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
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
CHEMBL2159330 glr_human Human No 6.9 IC50 = 114.2 nM Funct
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
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
CHEMBL155694 glr_human Human No 5.9 IC50 = 1150.8 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1
CHEMBL380771 glr_human Human No 6.9 IC50 = 116 nM Funct
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
521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1
CHEMBL217901 glr_human Human No 6.9 IC50 = 116 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
582 10 2 4 7.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)c2csc3ccc(Cl)cc23)C(c2ccccc2)c2ccccc2)cc1
CHEMBL425024 glr_human Human No 6.9 IC50 = 116 nM Funct
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
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
CHEMBL17370 glr_human Human Yes 6.9 IC50 = 117.2 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL450411 glr_human Human No 6.9 IC50 = 118 nM Bind
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
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
CHEMBL182148 glr_human Human No 6.9 IC50 = 118 nM Bind
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
435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2
CHEMBL501392 glr_human Human No 6.9 IC50 = 119 nM Bind
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
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
CHEMBL523847 glr_human Human No 6.9 IC50 = 119 nM Bind
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
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
CHEMBL4228690 glr_human Human No 5.9 IC50 = 1190 nM Funct
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
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
CHEMBL1922933 glr_human Human No 7.9 IC50 = 12 nM Funct
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
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
CHEMBL333147 glr_human Human Yes 7.9 IC50 = 12 nM Bind
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL386446 glr_human Human No 7.9 IC50 = 12 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL1922926 glr_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL1922940 glr_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL1922713 glr_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL3616589 glr_human Human No 7.9 IC50 = 12 nM Bind
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
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
CHEMBL2159353 glr_human Human Yes 7.9 IC50 = 12.3 nM Funct
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
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
CHEMBL346464 glr_human Human No 7.9 IC50 = 12.3 nM Bind
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
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
CHEMBL2159340 glr_human Human No 7.9 IC50 = 12.5 nM Funct
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
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
CHEMBL2111565 glr_human Human No 7.9 IC50 = 12.9 nM Bind
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
514 7 2 5 6.4 O=C(N/N=C/c1cccc2c(OCc3ccc(OC(F)(F)F)cc3)cccc12)c1ccc(O)c(Cl)c1
CHEMBL316361 glr_human Human No 6.9 IC50 = 120 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1
CHEMBL3616672 glr_human Human No 6.9 IC50 = 120 nM Funct
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
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
CHEMBL1922924 glr_human Human No 6.9 IC50 = 120 nM Bind
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
544 11 2 4 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(C)cc(C)c1
CHEMBL3238238 glr_human Human No 6.9 IC50 = 120 nM Bind
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
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
CHEMBL1643955 glr_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1
CHEMBL1644186 glr_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL515045 glr_human Human No 6.9 IC50 = 120 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
540 7 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2C2CCCC2)CC1
CHEMBL421795 glr_human Human No 6.9 IC50 = 120 nM Bind
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
479 8 2 6 4.3 COc1cc(OCCN2CCc3ccccc3C2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1
CHEMBL328942 glr_rat Rat No 6.9 IC50 = 120 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL358250 glr_human Human No 6.9 IC50 = 120 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1
CHEMBL24388 glr_human Human No 6.9 IC50 = 120 nM Funct
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
373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O
CHEMBL87858 glr_human Human No 6.9 IC50 = 120.2 nM Bind
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
343 5 1 2 5.1 Fc1ccc(-c2[nH]c(CCc3ccccc3)nc2-c2ccncc2)cc1
CHEMBL1922704 glr_human Human No 5.9 IC50 = 1200 nM Funct
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
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
CHEMBL1922711 glr_human Human No 5.9 IC50 = 1200 nM Funct
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
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
CHEMBL3238228 glr_human Human No 5.9 IC50 = 1200 nM Funct
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
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
CHEMBL3799439 glr_human Human No 5.9 IC50 = 1200 nM Funct
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
579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1
CHEMBL3800525 glr_human Human No 5.9 IC50 = 1200 nM Funct
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
569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1
CHEMBL107526 glr_human Human No 5.9 IC50 = 1200 nM Bind
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
306 3 3 4 3.0 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1
CHEMBL158676 glr_mouse Mouse No 5.9 IC50 = 1200 nM Bind
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
402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL3237895 glr_mouse Mouse No 5.9 IC50 = 1200 nM Bind
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
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
CHEMBL1644173 glr_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1
CHEMBL1644194 glr_human Human No 5.9 IC50 = 1200 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL160419 glr_human Human No 5.9 IC50 = 1200 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
397 6 3 5 2.8 NC(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12
CHEMBL268534 glr_rat Rat No 5.9 IC50 = 1200 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CC(=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)NC(=O)[C@H](N)Cc2c[nH]cn2)[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)N1)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL105565 glr_human Human No 4.9 IC50 = 12000 nM Bind
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
384 5 2 5 4.4 COc1cc(C(=O)N/N=C/c2ccc(-c3ccc(C)c(Cl)c3)o2)ccc1O
CHEMBL375000 glr_human Human No 5.9 IC50 = 1207 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL2159333 glr_human Human No 6.9 IC50 = 121.5 nM Bind
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
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
CHEMBL1933349 glr_mouse Mouse Yes 6.9 IC50 = 122 nM Funct
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
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
CHEMBL373542 glr_human Human No 6.9 IC50 = 122 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
549 11 3 4 6.2 CCCC1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1
CHEMBL386446 glr_rat Rat No 6.9 IC50 = 122 nM Bind
Inhibition of rat glucagon receptorInhibition of rat glucagon receptor
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
CHEMBL2435137 glr_human Human No 5.9 IC50 = 1230.3 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
360 4 0 3 5.7 CSc1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1
CHEMBL437095 glr_rat Rat No 6.9 IC50 = 126 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](C)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
CHEMBL3798581 glr_human Human No 4.9 IC50 = 12700 nM Bind
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
595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1
CHEMBL429198 glr_rat Rat No 6.9 IC50 = 128 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](CC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](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
CHEMBL179281 glr_human Human Yes 6.9 IC50 = 129 nM Funct
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
346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC
CHEMBL178768 glr_human Human No 6.9 IC50 = 129 nM Bind
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
491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2
CHEMBL4228281 glr_human Human No 5.9 IC50 = 1290 nM Funct
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
561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1
CHEMBL1922839 glr_human Human No 7.9 IC50 = 13 nM Funct
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
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
CHEMBL447684 glr_human Human No 7.9 IC50 = 13 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL316361 glr_human Human No 7.9 IC50 = 13 nM Bind
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
447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1
CHEMBL85807 glr_human Human Yes 7.9 IC50 = 13 nM Bind
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
423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3238221 glr_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL3238222 glr_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL3238223 glr_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL442855 glr_human Human No 7.9 IC50 = 13 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1922702 glr_human Human No 7.9 IC50 = 13 nM Bind
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
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
CHEMBL2159342 glr_human Human No 7.9 IC50 = 13.3 nM Funct
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
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
CHEMBL442135 glr_rat Rat No 7.9 IC50 = 13.6 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
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]1CCC(=O)NCCCC[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)Cc2c[nH]cn2)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccc(O)cc2)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
CHEMBL409654 glr_rat Rat No 7.9 IC50 = 13.7 nM Bind
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
None None None None
CHEMBL156772 glr_human Human No 7.9 IC50 = 13.8 nM Bind
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
513 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC(=O)N2CCc3ccccc3C2)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL3616586 glr_human Human No 6.9 IC50 = 130 nM Funct
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
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
CHEMBL1922706 glr_human Human No 6.9 IC50 = 130 nM Funct
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
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
CHEMBL3237925 glr_human Human No 6.9 IC50 = 130 nM Funct
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
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
CHEMBL3238218 glr_human Human No 6.9 IC50 = 130 nM Funct
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
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
CHEMBL160287 glr_human Human No 6.9 IC50 = 130 nM Bind
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
466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL315311 glr_human Human No 6.9 IC50 = 130 nM Bind
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
457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL315800 glr_human Human No 6.9 IC50 = 130 nM Bind
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
387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1
CHEMBL3238218 glr_mouse Mouse No 6.9 IC50 = 130 nM Bind
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
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
CHEMBL3238246 glr_mouse Mouse No 6.9 IC50 = 130 nM Bind
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
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
CHEMBL3237906 glr_human Human No 6.9 IC50 = 130 nM Bind
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
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
CHEMBL3237917 glr_human Human No 6.9 IC50 = 130 nM Bind
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
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
CHEMBL1644188 glr_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL521650 glr_human Human No 6.9 IC50 = 130 nM Bind
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
537 10 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccccc3)cs2)cc1
CHEMBL390469 glr_human Human No 6.9 IC50 = 130 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL154269 glr_human Human No 6.9 IC50 = 130 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12
CHEMBL429724 glr_rat Rat No 6.9 IC50 = 130 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CCCCNC(=O)C[C@H](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)Cc2c[nH]cn2)[C@H](C)O)[C@H](C)O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CO)C(=O)N1)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL416169 glr_human Human No 6.9 IC50 = 130.0 nM Bind
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
315 3 1 2 4.9 Fc1ccc(-c2[nH]c(-c3ccccc3)nc2-c2ccncc2)cc1
CHEMBL1644188 glr_human Human No 5.9 IC50 = 1300 nM Funct
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
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
CHEMBL351104 glr_human Human No 5.9 IC50 = 1300 nM Bind
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
388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL420232 glr_human Human No 5.9 IC50 = 1300 nM Bind
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
329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237899 glr_mouse Mouse No 5.9 IC50 = 1300 nM Bind
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
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
CHEMBL3656297 glr_human Human No 5.9 IC50 = 1300 nM Bind
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.
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
CHEMBL160138 glr_human Human No 5.9 IC50 = 1300 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
452 8 2 5 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1OCc1ccc(C(C)C)cc1
CHEMBL3797325 glr_human Human No 4.9 IC50 = 13000 nM Funct
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
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
CHEMBL276063 glr_human Human No 4.9 IC50 = 13000 nM Bind
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
345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL502694 glr_human Human No 6.9 IC50 = 131 nM Bind
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
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
CHEMBL439690 glr_rat Rat No 6.9 IC50 = 131 nM Bind
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
2693 89 37 35 -7.7 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](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)CCCCCc1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O
CHEMBL157226 glr_human Human No 6.9 IC50 = 133 nM Bind
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
521 10 3 6 5.0 COc1cc(OCCNCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1
CHEMBL197850 glr_human Human No 6.9 IC50 = 135 nM Funct
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
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
CHEMBL160238 glr_human Human No 5.9 IC50 = 1361.4 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL218740 glr_human Human No 6.9 IC50 = 137 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL182148 glr_human Human No 6.9 IC50 = 139 nM Bind
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
435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2
CHEMBL3616687 glr_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL3616694 glr_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL1922840 glr_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL1922844 glr_human Human No 7.9 IC50 = 14 nM Funct
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
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
CHEMBL486634 glr_human Human No 7.9 IC50 = 14 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL509710 glr_human Human No 7.9 IC50 = 14 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL520893 glr_human Human No 7.9 IC50 = 14 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL3238218 glr_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL488682 glr_human Human No 7.9 IC50 = 14 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1922698 glr_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL1922843 glr_human Human No 7.9 IC50 = 14 nM Bind
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
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
CHEMBL2159339 glr_human Human No 7.9 IC50 = 14.1 nM Funct
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
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
CHEMBL1922714 glr_human Human No 7.8 IC50 = 14.4 nM Funct
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
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
CHEMBL346694 glr_human Human No 7.8 IC50 = 14.5 nM Bind
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
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
CHEMBL153950 glr_human Human No 7.8 IC50 = 14.7 nM Bind
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
541 9 3 5 6.4 O=C(N/N=C/c1ccc(OCCNCc2ccc(Cl)c(Cl)c2)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL2159350 glr_human Human No 7.8 IC50 = 14.8 nM Bind
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
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
CHEMBL3616673 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL3616702 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL62444 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL3237895 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL3237899 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL3238219 glr_human Human No 6.9 IC50 = 140 nM Funct
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
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
CHEMBL158989 glr_human Human No 6.9 IC50 = 140 nM Bind
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
339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL159198 glr_human Human No 6.9 IC50 = 140 nM Bind
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
408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL160372 glr_human Human No 6.9 IC50 = 140 nM Bind
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
254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1
CHEMBL156458 glr_human Human No 6.9 IC50 = 140 nM Bind
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
388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL85102 glr_human Human No 6.9 IC50 = 140 nM Bind
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
407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3238217 glr_mouse Mouse No 6.9 IC50 = 140 nM Bind
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
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
CHEMBL3238223 glr_mouse Mouse No 6.9 IC50 = 140 nM Bind
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
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
CHEMBL351724 glr_human Human No 6.9 IC50 = 140 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
438 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC2CCCCO2)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL373541 glr_human Human No 6.9 IC50 = 140 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL315311 glr_human Human No 6.9 IC50 = 140.3 nM Bind
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
457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237889 glr_human Human No 5.9 IC50 = 1400 nM Funct
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
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
CHEMBL3798135 glr_human Human No 5.9 IC50 = 1400 nM Funct
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
537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1
CHEMBL3800473 glr_human Human No 5.9 IC50 = 1400 nM Funct
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
553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1
CHEMBL159163 glr_human Human No 5.9 IC50 = 1400 nM Bind
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
329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL471580 glr_rat Rat No 5.9 IC50 = 1400 nM Bind
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
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
CHEMBL85534 glr_human Human No 5.9 IC50 = 1400 nM Bind
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
393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1
CHEMBL3326171 glr_rat Rat No 5.9 IC50 = 1400 nM Bind
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
416 4 3 4 4.5 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(F)c1
CHEMBL25115 glr_human Human No 5.9 IC50 = 1400 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1
CHEMBL25115 glr_human Human No 5.9 IC50 = 1400 nM Bind
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
339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1
CHEMBL328126 glr_human Human No 5.9 IC50 = 1402.8 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1
CHEMBL219308 glr_human Human No 6.9 IC50 = 141 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
523 13 3 4 5.8 CCCCC(CC)N(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(OC(F)(F)F)cc1
CHEMBL372784 glr_human Human No 5.9 IC50 = 1416 nM Funct
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
555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1
CHEMBL346698 glr_human Human No 4.9 IC50 = 14223.3 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL198736 glr_human Human Yes 6.8 IC50 = 144 nM Funct
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
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
CHEMBL351772 glr_human Human Yes 5.8 IC50 = 1442.1 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br
CHEMBL3799499 glr_human Human No 4.8 IC50 = 14500 nM Bind
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
533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21
CHEMBL3800146 glr_human Human No 4.8 IC50 = 14500 nM Bind
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
525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1
CHEMBL411832 glr_human Human No 5.8 IC50 = 1454 nM Funct
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
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
CHEMBL232037 glr_human Human No 5.8 IC50 = 1467 nM Funct
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
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
CHEMBL411831 glr_human Human No 6.8 IC50 = 148 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL3238237 glr_human Human No 6.8 IC50 = 149 nM Bind
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
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
CHEMBL4227634 glr_human Human No 5.8 IC50 = 1490 nM Funct
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
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
CHEMBL396215 glr_human Human No 7.8 IC50 = 15 nM Funct
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
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
CHEMBL267876 glr_rat Rat No 7.8 IC50 = 15 nM Bind
Compound was evaluated for its ability to displace radiolabeled glucagon (inactive up to 100 uM)Compound was evaluated for its ability to displace radiolabeled glucagon (inactive up to 100 uM)
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=C(N)N)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](Cc1c[nH]cn1)Nc1c([N+](=O)[O-])cc([N+](=O)[O-])cc1[N+](=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
CHEMBL3237927 glr_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL3238224 glr_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL517861 glr_human Human No 7.8 IC50 = 15 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL3616684 glr_human Human No 7.8 IC50 = 15 nM Bind
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
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
CHEMBL2159345 glr_human Human No 7.8 IC50 = 15.3 nM Bind
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
511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL2159329 glr_human Human No 7.8 IC50 = 15.6 nM Bind
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
573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL1933349 glr_human Human Yes 7.8 IC50 = 15.7 nM Funct
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
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
CHEMBL413964 glr_human Human No 7.8 IC50 = 15.7 nM Bind
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
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
CHEMBL2159348 glr_human Human No 7.8 IC50 = 15.8 nM Funct
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
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
CHEMBL84840 glr_human Human No 6.8 IC50 = 150 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1
CHEMBL85807 glr_human Human Yes 6.8 IC50 = 150 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237928 glr_human Human No 6.8 IC50 = 150 nM Funct
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
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
CHEMBL1922922 glr_human Human No 6.8 IC50 = 150 nM Funct
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
534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1
CHEMBL350255 glr_human Human No 6.8 IC50 = 150 nM Bind
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
408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1
CHEMBL347663 glr_mouse Mouse No 6.8 IC50 = 150 nM Bind
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
402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL3237907 glr_human Human No 6.8 IC50 = 150 nM Bind
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
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
CHEMBL161431 glr_human Human No 6.8 IC50 = 150 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
476 8 2 6 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(F)c(F)c1
CHEMBL356089 glr_human Human No 6.8 IC50 = 150 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1
CHEMBL314701 glr_human Human Yes 6.8 IC50 = 150.3 nM Bind
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
423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL85534 glr_human Human No 6.8 IC50 = 150.3 nM Bind
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
393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1
CHEMBL3799468 glr_human Human No 5.8 IC50 = 1500 nM Funct
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
599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1
CHEMBL314652 glr_human Human Yes 5.8 IC50 = 1500 nM Bind
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
365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1
CHEMBL3237897 glr_mouse Mouse No 5.8 IC50 = 1500 nM Bind
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
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
CHEMBL3237913 glr_mouse Mouse No 5.8 IC50 = 1500 nM Bind
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
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
CHEMBL3237920 glr_mouse Mouse No 5.8 IC50 = 1500 nM Bind
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
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
CHEMBL160652 glr_human Human No 5.8 IC50 = 1500 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
422 7 2 4 5.5 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cc2)cc1
CHEMBL2372773 glr_rat Rat No 5.8 IC50 = 1500 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CCCCNC(=O)C[C@H](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)Cc2c[nH]cn2)[C@H](C)O)[C@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O
CHEMBL493019 glr_human Human No 6.8 IC50 = 153 nM Bind
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
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
CHEMBL219252 glr_human Human No 6.8 IC50 = 153 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL362657 glr_human Human No 6.8 IC50 = 153 nM Bind
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
479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N
CHEMBL198214 glr_human Human No 6.8 IC50 = 156 nM Funct
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
565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1
CHEMBL182148 glr_human Human No 6.8 IC50 = 158 nM Funct
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
435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2
CHEMBL114762 glr_human Human Yes 7.8 IC50 = 16 nM Bind
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL375167 glr_human Human No 7.8 IC50 = 16 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL1922915 glr_human Human No 7.8 IC50 = 16 nM Bind
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
586 12 2 4 7.7 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1Cc1ccc(C(C)(C)C)cc1
CHEMBL1922932 glr_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL1922939 glr_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL3238234 glr_human Human No 7.8 IC50 = 16 nM Bind
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
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
CHEMBL459458 glr_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL506520 glr_human Human No 7.8 IC50 = 16 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
562 8 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2Cc2ccccc2)CC1
CHEMBL2159335 glr_human Human No 7.8 IC50 = 16 nM Bind
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
599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl
CHEMBL1922834 glr_human Human No 7.8 IC50 = 16.3 nM Funct
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
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
CHEMBL157280 glr_human Human No 7.8 IC50 = 16.5 nM Bind
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
428 7 2 5 3.6 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12
CHEMBL2159338 glr_human Human No 7.8 IC50 = 16.6 nM Bind
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
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
CHEMBL1643955 glr_human Human No 6.8 IC50 = 160 nM Funct
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
511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1
CHEMBL3238220 glr_human Human No 6.8 IC50 = 160 nM Funct
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
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
CHEMBL3238216 glr_mouse Mouse No 6.8 IC50 = 160 nM Bind
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
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
CHEMBL3237920 glr_human Human No 6.8 IC50 = 160 nM Bind
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
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
CHEMBL3326174 glr_rat Rat No 6.8 IC50 = 160 nM Bind
Displacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-countingDisplacement of [125I]glucagon from glucagon receptor in rat hepatocyte membranes after 30 mins by gamma-counting
466 4 3 4 5.4 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(C(F)(F)F)c1
CHEMBL469904 glr_human Human No 6.8 IC50 = 160 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL1922700 glr_human Human No 6.8 IC50 = 160 nM Bind
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
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
CHEMBL161505 glr_human Human No 6.8 IC50 = 160 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
478 6 2 7 5.2 CC(C)(C)c1nc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)no1
CHEMBL87588 glr_human Human Yes 6.8 IC50 = 160.0 nM Bind
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
393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1
CHEMBL160314 glr_human Human No 6.8 IC50 = 160.3 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
238 2 1 1 3.9 Fc1ccc(-c2cc[nH]c2-c2ccncc2)cc1
CHEMBL160490 glr_human Human No 6.8 IC50 = 160.3 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237890 glr_human Human No 5.8 IC50 = 1600 nM Funct
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
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
CHEMBL3238227 glr_human Human No 5.8 IC50 = 1600 nM Funct
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
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
CHEMBL3799017 glr_human Human No 5.8 IC50 = 1600 nM Funct
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
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
CHEMBL492813 glr_rat Rat No 5.8 IC50 = 1600 nM Bind
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1
CHEMBL155694 glr_human Human No 5.8 IC50 = 1600 nM Bind
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
360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1
CHEMBL1644176 glr_human Human No 4.8 IC50 = 16000 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1
CHEMBL2112904 glr_human Human No 6.8 IC50 = 163 nM Bind
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
435 6 2 6 3.5 CC(C)S(=O)(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12
CHEMBL196844 glr_human Human No 6.8 IC50 = 164 nM Funct
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
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
CHEMBL487662 glr_human Human No 6.8 IC50 = 166 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL194794 glr_human Human No 5.8 IC50 = 1663 nM Funct
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
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
CHEMBL219968 glr_human Human No 6.8 IC50 = 167 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
544 10 3 5 6.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cccc([N+](=O)[O-])c2)c2ccc(C3CCCCC3)cc2)cc1
CHEMBL160289 glr_human Human No 5.8 IC50 = 1690.4 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL197754 glr_human Human No 5.8 IC50 = 1691 nM Funct
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
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
CHEMBL3616583 glr_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL1922710 glr_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL1922926 glr_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL1922938 glr_human Human No 7.8 IC50 = 17 nM Funct
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
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
CHEMBL158535 glr_human Human No 7.8 IC50 = 17 nM Bind
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
386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL1922921 glr_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL1922934 glr_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL3238215 glr_human Human No 7.8 IC50 = 17 nM Bind
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
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
CHEMBL1644178 glr_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL3237897 glr_human Human No 6.8 IC50 = 170 nM Funct
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
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
CHEMBL351772 glr_human Human Yes 6.8 IC50 = 170 nM Bind
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
466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br
CHEMBL155686 glr_human Human No 6.8 IC50 = 170 nM Bind
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
422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL3238222 glr_mouse Mouse No 6.8 IC50 = 170 nM Bind
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
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
CHEMBL3237897 glr_human Human No 6.8 IC50 = 170 nM Bind
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
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
CHEMBL3237914 glr_human Human No 6.8 IC50 = 170 nM Bind
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
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
CHEMBL515202 glr_human Human No 6.8 IC50 = 170 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL328942 glr_rat Rat No 6.8 IC50 = 170 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL4227667 glr_human Human No 5.8 IC50 = 1700 nM Funct
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
601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL519776 glr_rat Rat No 5.8 IC50 = 1700 nM Bind
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
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
CHEMBL350255 glr_human Human No 5.8 IC50 = 1700 nM Bind
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
408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237902 glr_mouse Mouse No 5.8 IC50 = 1700 nM Bind
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
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
CHEMBL3237907 glr_mouse Mouse No 5.8 IC50 = 1700 nM Bind
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
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
CHEMBL1643958 glr_human Human No 5.8 IC50 = 1700 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1
CHEMBL3616582 glr_human Human No 5.8 IC50 = 1700 nM Bind
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
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
CHEMBL3656289 glr_human Human No 5.8 IC50 = 1700 nM Bind
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.
543 9 2 4 5.4 CC1(C2CCCCC2)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1
CHEMBL3656290 glr_human Human No 5.8 IC50 = 1700 nM Bind
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.
475 8 2 4 3.8 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1
CHEMBL3656295 glr_human Human No 5.8 IC50 = 1700 nM Bind
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.
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
CHEMBL219191 glr_human Human No 5.8 IC50 = 1700 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL380387 glr_human Human No 4.8 IC50 = 17000 nM Bind
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
359 7 0 3 4.9 O=C(c1ccc(OCCCN2CCCC2)cc1)c1cccc2ccccc12
CHEMBL4226770 glr_human Human No 4.8 IC50 = 17060 nM Funct
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
571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12
CHEMBL4288863 glr_human Human No 4.8 IC50 = 17700 nM Funct
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
461 12 2 5 5.2 CCCCC(Oc1ncc(-c2ccc(CC)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1
CHEMBL197340 glr_human Human No 6.8 IC50 = 178 nM Funct
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
505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1
CHEMBL219446 glr_human Human No 6.8 IC50 = 179 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
513 11 3 3 5.4 CCCCc1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C2Cc3ccccc3C2)cc1
CHEMBL470955 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL3616690 glr_human Human No 7.8 IC50 = 18 nM Funct
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
629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21
CHEMBL3616691 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL3616692 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL3616697 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL1922841 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL232239 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL323913 glr_human Human Yes 7.8 IC50 = 18 nM Bind
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL447742 glr_human Human No 7.8 IC50 = 18 nM Bind
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
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
CHEMBL1922697 glr_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1922703 glr_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL439289 glr_human Human No 7.8 IC50 = 18 nM Funct
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
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
CHEMBL439289 glr_human Human No 7.8 IC50 = 18 nM Bind
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
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
CHEMBL1921810 glr_human Human No 6.8 IC50 = 180 nM Funct
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
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
CHEMBL3237917 glr_human Human No 6.8 IC50 = 180 nM Funct
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
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
CHEMBL3238222 glr_human Human No 6.8 IC50 = 180 nM Funct
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
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
CHEMBL3238223 glr_human Human No 6.8 IC50 = 180 nM Funct
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
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
CHEMBL158676 glr_human Human No 6.8 IC50 = 180 nM Bind
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
402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL4226972 glr_human Human No 6.8 IC50 = 180 nM Bind
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
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
CHEMBL159093 glr_human Human No 6.8 IC50 = 180 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
524 9 2 7 5.3 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(OC(F)(F)F)cc1
CHEMBL328942 glr_rat Rat No 6.8 IC50 = 180 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(C)=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC
CHEMBL348401 glr_human Human No 6.7 IC50 = 180.3 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1
CHEMBL447535 glr_human Human Yes 5.8 IC50 = 1800 nM Bind
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
290 3 2 3 3.3 O=C(N/N=C/c1cccc2ccccc12)c1ccc(O)cc1
CHEMBL455323 glr_rat Rat No 5.8 IC50 = 1800 nM Bind
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
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
CHEMBL140636 glr_human Human No 5.8 IC50 = 1800 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
399 11 1 2 7.5 CCCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1
CHEMBL344911 glr_human Human No 5.8 IC50 = 1800 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
297 5 1 2 5.1 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1
CHEMBL152461 glr_human Human No 6.7 IC50 = 181 nM Bind
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
444 6 2 5 4.4 CC(C)CS(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12
CHEMBL179281 glr_human Human Yes 6.7 IC50 = 181 nM Bind
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
346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC
CHEMBL3797325 glr_human Human No 4.7 IC50 = 18100 nM Bind
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
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
CHEMBL373234 glr_human Human No 6.7 IC50 = 182 nM Funct
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
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
CHEMBL219138 glr_human Human No 6.7 IC50 = 182 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL2112991 glr_human Human No 6.7 IC50 = 185 nM Funct
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
360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N
CHEMBL2159332 glr_human Human No 6.7 IC50 = 189 nM Funct
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
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
CHEMBL265337 glr_human Human No 6.7 IC50 = 189 nM Funct
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
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
CHEMBL448921 glr_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL1922715 glr_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL1922835 glr_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL1922843 glr_human Human No 7.7 IC50 = 19 nM Funct
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
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
CHEMBL442499 glr_rat Rat No 7.7 IC50 = 19 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](Cc1c[nH]c2ccccc12)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
CHEMBL1922845 glr_human Human No 7.7 IC50 = 19 nM Bind
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
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
CHEMBL2112907 glr_human Human No 7.7 IC50 = 19.1 nM Bind
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
451 5 2 7 3.7 CN(C)c1ccc(C(=O)n2cc(/C=N/NC(=O)c3ccc(O)c(C#N)c3)c3ccccc32)cc1
CHEMBL3617565 glr_human Human No 7.7 IC50 = 19.2 nM Funct
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
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
CHEMBL152409 glr_human Human No 7.7 IC50 = 19.7 nM Bind
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
565 10 3 5 5.9 O=C(N/N=C/c1ccc(OCCNCCc2ccc(Br)cc2)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL24388 glr_human Human No 6.7 IC50 = 190 nM Bind
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O
CHEMBL160490 glr_human Human No 6.7 IC50 = 190 nM Bind
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
364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL116413 glr_human Human No 6.7 IC50 = 190 nM Bind
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O
CHEMBL85009 glr_human Human No 6.7 IC50 = 190 nM Bind
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
365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3238220 glr_mouse Mouse No 6.7 IC50 = 190 nM Bind
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
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
CHEMBL3237899 glr_human Human No 6.7 IC50 = 190 nM Bind
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
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
CHEMBL3237919 glr_human Human No 6.7 IC50 = 190 nM Bind
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
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
CHEMBL266411 glr_rat Rat No 6.7 IC50 = 190 nM Bind
In vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassayIn vitro receptor binding affinity (95% CL) using rat liver plasma membrane bioassay
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]1CC(=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)NC(=O)[C@H](N)Cc2c[nH]cn2)[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)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)N1)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O
CHEMBL24388 glr_human Human No 6.7 IC50 = 190 nM Bind
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
373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O
CHEMBL159163 glr_human Human No 6.7 IC50 = 190.1 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL87248 glr_human Human No 6.7 IC50 = 190.1 nM Bind
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
383 3 1 3 5.3 Fc1ccc(-c2[nH]c(-c3ccc(Br)o3)nc2-c2ccncc2)cc1
CHEMBL3237891 glr_human Human No 5.7 IC50 = 1900 nM Funct
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
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
CHEMBL3237892 glr_human Human No 5.7 IC50 = 1900 nM Funct
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
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
CHEMBL3797757 glr_human Human No 5.7 IC50 = 1900 nM Funct
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
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
CHEMBL161494 glr_human Human No 5.7 IC50 = 1900 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
483 10 2 5 5.7 COc1cc(CCNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL24527 glr_human Human No 4.7 IC50 = 19000 nM Bind
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
387 9 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(CO)c1
CHEMBL4228703 glr_human Human No 5.7 IC50 = 1920 nM Bind
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
533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1
CHEMBL197851 glr_human Human No 6.7 IC50 = 193 nM Funct
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
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
CHEMBL3238232 glr_human Human No 6.7 IC50 = 195 nM Bind
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
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
CHEMBL383350 glr_human Human No 5.7 IC50 = 1965 nM Funct
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
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
CHEMBL371235 glr_human Human No 5.7 IC50 = 1975 nM Funct
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
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
CHEMBL2113259 glr_human Human No 5.7 IC50 = 1984 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL448921 glr_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL458145 glr_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL480692 glr_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL518939 glr_human Human No 8.7 IC50 = 2 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL3616584 glr_human Human No 8.7 IC50 = 2 nM Bind
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
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
CHEMBL3616675 glr_human Human No 8.7 IC50 = 2 nM Bind
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
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
CHEMBL3892787 glr_human Human No 8.7 IC50 = 2.2 nM Bind
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).
519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2ccccc12
CHEMBL1922839 glr_human Human No 8.7 IC50 = 2.2 nM Bind
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
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
CHEMBL152640 glr_human Human No 8.6 IC50 = 2.3 nM Bind
Antagonist activity against human glucagon receptorAntagonist activity against human glucagon receptor
450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C
CHEMBL4110618 glr_human Human No 8.6 IC50 = 2.3 nM Bind
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).
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
CHEMBL152640 glr_human Human No 8.6 IC50 = 2.3 nM Bind
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
450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C
CHEMBL413666 glr_rat Rat No 8.6 IC50 = 2.3 nM Bind
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
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](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[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
CHEMBL396215 glr_human Human No 8.6 IC50 = 2.3 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL4106672 glr_human Human No 8.6 IC50 = 2.5 nM Bind
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).
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
CHEMBL2159337 glr_human Human No 8.6 IC50 = 2.5 nM Bind
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
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
CHEMBL3616688 glr_human Human No 8.6 IC50 = 2.6 nM Bind
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
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
CHEMBL3616701 glr_human Human No 8.6 IC50 = 2.6 nM Bind
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
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
CHEMBL1922714 glr_human Human No 8.6 IC50 = 2.8 nM Bind
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
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
CHEMBL152477 glr_human Human No 8.6 IC50 = 2.8 nM Bind
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
522 6 2 6 5.4 N#Cc1cc(C(=O)N/N=C/c2ccc(N(C(=O)C3CCCC3)C(=O)C3CCCC3)c3ccccc23)ccc1O
CHEMBL3616683 glr_human Human No 7.7 IC50 = 20 nM Funct
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
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
CHEMBL1922936 glr_human Human No 7.7 IC50 = 20 nM Funct
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
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
CHEMBL348555 glr_human Human No 7.7 IC50 = 20 nM Bind
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
387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL114762 glr_human Human Yes 7.7 IC50 = 20 nM Bind
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL1933349 glr_human Human Yes 7.7 IC50 = 20 nM Bind
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
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
CHEMBL152765 glr_human Human No 7.7 IC50 = 20 nM Bind
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
473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL152765 glr_human Human No 7.7 IC50 = 20 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL84759 glr_human Human No 7.7 IC50 = 20.0 nM Bind
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
363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1
CHEMBL439271 glr_rat Rat No 6.7 IC50 = 200 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](CC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](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(=O)O)[C@H](C)O
CHEMBL347663 glr_human Human No 6.7 IC50 = 200 nM Bind
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
402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1
CHEMBL328126 glr_mouse Mouse No 6.7 IC50 = 200 nM Bind
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
348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1
CHEMBL107070 glr_human Human No 6.7 IC50 = 200 nM Bind
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL3238229 glr_mouse Mouse No 6.7 IC50 = 200 nM Bind
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
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
CHEMBL4228215 glr_human Human No 6.7 IC50 = 200 nM Bind
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
521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1
CHEMBL156654 glr_human Human No 6.7 IC50 = 200 nM Bind
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
354 4 3 4 3.5 O=C(N/N=C/c1cccc2c(CO)cccc12)c1ccc(O)c(Cl)c1
CHEMBL107070 glr_human Human No 6.7 IC50 = 200 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL1644183 glr_mouse Mouse No 5.7 IC50 = 2000 nM Funct
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
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
CHEMBL419364 glr_human Human No 5.7 IC50 = 2000 nM Bind
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
321 3 4 5 2.6 Nc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O
CHEMBL114762 glr_human Human Yes 5.7 IC50 = 2000 nM Bind
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL501628 glr_rat Rat No 5.7 IC50 = 2000 nM Bind
Binding affinity to glucagon receptor in rat liver membrane by membrane filter assayBinding affinity to glucagon receptor in rat liver membrane by membrane filter assay
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
CHEMBL427744 glr_rat Rat No 5.7 IC50 = 2000 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](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(=O)O)[C@H](C)O
CHEMBL438218 glr_rat Rat No 5.7 IC50 = 2000 nM Bind
Binding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagonBinding affinity towards Glucagon receptor in rat liver plasma membranes by displacement of 125 I-labelled glucagon
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](CC(=O)O)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
CHEMBL17736 glr_human Human Yes 5.7 IC50 = 2000 nM Bind
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
330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL316264 glr_human Human No 5.7 IC50 = 2000 nM Bind
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
333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL1643952 glr_human Human No 5.7 IC50 = 2000 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
444 6 1 4 6.2 O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1
CHEMBL3656298 glr_human Human No 5.7 IC50 = 2000 nM Bind
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.
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
CHEMBL114761 glr_human Human No 5.7 IC50 = 2000 nM Funct
Inhibitory concentration against cAMP production in hGR-CHO cellsInhibitory concentration against cAMP production in hGR-CHO cells
341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1
CHEMBL463175 glr_human Human Yes 4.7 IC50 = 20000 nM Funct
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
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
CHEMBL158497 glr_human Human No 4.7 IC50 = 20000 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
397 8 2 7 3.3 COc1cc(CO/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1C(C)C
CHEMBL142589 glr_human Human No 4.7 IC50 = 20000 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
311 8 1 2 5.1 CCCCCc1c(CC)nc(CC)c(CO)c1-c1ccccc1
CHEMBL3797757 glr_human Human No 4.7 IC50 = 20200 nM Bind
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
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
CHEMBL107070 glr_human Human No 6.7 IC50 = 203 nM Bind
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
340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL4226911 glr_human Human No 5.7 IC50 = 2030 nM Funct
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
572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1
CHEMBL3798798 glr_human Human No 4.7 IC50 = 20800 nM Funct
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
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
CHEMBL3617561 glr_human Human No 6.7 IC50 = 209 nM Funct
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
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
CHEMBL198736 glr_human Human Yes 7.7 IC50 = 21 nM Funct
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
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
CHEMBL3616700 glr_human Human No 7.7 IC50 = 21 nM Funct
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
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
CHEMBL3238219 glr_human Human No 7.7 IC50 = 21 nM Bind
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
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
CHEMBL62444 glr_human Human No 7.7 IC50 = 21 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL413208 glr_rat Rat No 7.7 IC50 = 21.2 nM Bind
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
2665 87 37 35 -8.5 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](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)CCCc1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O
CHEMBL152103 glr_human Human No 7.7 IC50 = 21.2 nM Bind
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
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
CHEMBL2111214 glr_human Human No 7.7 IC50 = 21.2 nM Bind
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
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
CHEMBL3616685 glr_human Human No 6.7 IC50 = 210 nM Funct
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
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
CHEMBL1922699 glr_human Human No 6.7 IC50 = 210 nM Funct
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
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
CHEMBL160550 glr_human Human No 6.7 IC50 = 210.4 nM Bind
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL17396 glr_human Human No 6.7 IC50 = 210.4 nM Bind
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
340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1
CHEMBL3797782 glr_human Human No 5.7 IC50 = 2100 nM Funct
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
569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12
CHEMBL471979 glr_human Human No 6.7 IC50 = 213 nM Funct
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
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
CHEMBL218871 glr_human Human No 6.7 IC50 = 215 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL232239 glr_human Human No 6.7 IC50 = 216 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL232241 glr_human Human No 5.7 IC50 = 2173 nM Funct
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
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
CHEMBL455323 glr_mouse Mouse No 6.7 IC50 = 218 nM Bind
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
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
CHEMBL395759 glr_human Human No 6.7 IC50 = 218 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL518939 glr_human Human No 7.7 IC50 = 22 nM Funct
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
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
CHEMBL1922707 glr_human Human No 7.7 IC50 = 22 nM Funct
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
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
CHEMBL1922842 glr_human Human No 7.7 IC50 = 22 nM Funct
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
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
CHEMBL3617572 glr_human Human No 7.7 IC50 = 22 nM Funct
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
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
CHEMBL3617563 glr_human Human No 7.7 IC50 = 22 nM Funct
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
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
CHEMBL3237928 glr_human Human No 7.7 IC50 = 22 nM Bind
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
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
CHEMBL3238228 glr_human Human No 7.7 IC50 = 22 nM Bind
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
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
CHEMBL266489 glr_human Human No 7.7 IC50 = 22 nM Bind
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
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
CHEMBL345713 glr_human Human No 7.7 IC50 = 22.3 nM Bind
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
462 5 2 5 5.1 N#Cc1cc(C(=O)N/N=C/c2cccc3c2ccn3Cc2ccc(C(F)(F)F)cc2)ccc1O
CHEMBL422506 glr_human Human No 7.7 IC50 = 22.6 nM Bind
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
437 7 2 4 4.4 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12
CHEMBL349552 glr_human Human No 7.6 IC50 = 22.9 nM Bind
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
487 6 2 5 5.7 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(OC(F)(F)F)cc1)c1ccc(O)c(Cl)c1
CHEMBL472154 glr_human Human No 6.7 IC50 = 220 nM Funct
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
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
CHEMBL3616675 glr_human Human No 6.7 IC50 = 220 nM Funct
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
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
CHEMBL3237923 glr_human Human No 6.7 IC50 = 220 nM Funct
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
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
CHEMBL4227364 glr_human Human No 6.7 IC50 = 220 nM Funct
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
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
CHEMBL160490 glr_mouse Mouse No 6.7 IC50 = 220 nM Bind
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
364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL1644195 glr_human Human No 6.7 IC50 = 220 nM Bind
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
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
CHEMBL142414 glr_human Human No 6.7 IC50 = 220 nM Bind
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1
CHEMBL85807 glr_human Human Yes 6.7 IC50 = 220.3 nM Bind
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
423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1
CHEMBL85009 glr_human Human No 5.7 IC50 = 2200 nM Bind
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL3237926 glr_human Human No 5.7 IC50 = 2200 nM Funct
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
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
CHEMBL333147 glr_human Human Yes 5.7 IC50 = 2200 nM Bind
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O
CHEMBL160289 glr_human Human No 5.7 IC50 = 2200 nM Bind
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
328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1
CHEMBL84917 glr_human Human No 5.7 IC50 = 2200 nM Bind
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
399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1
CHEMBL3237901 glr_mouse Mouse No 5.7 IC50 = 2200 nM Bind
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
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
CHEMBL84952 glr_human Human Yes 5.7 IC50 = 2200 nM Bind
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
374 3 1 1 6.2 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)cc1
CHEMBL2112909 glr_human Human No 6.7 IC50 = 221 nM Bind
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
470 6 2 5 4.8 O=C(N/N=C/c1ccc(CS(=O)(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1
CHEMBL504260 glr_human Human No 6.7 IC50 = 225 nM Bind
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
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
CHEMBL219307 glr_human Human No 6.7 IC50 = 226 nM Bind
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
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
CHEMBL371259 glr_human Human No 6.6 IC50 = 227 nM Funct
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
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
CHEMBL511964 glr_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL1922696 glr_human Human No 7.6 IC50 = 23 nM Funct
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
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
CHEMBL198736 glr_rat Rat Yes 7.6 IC50 = 23 nM Bind
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
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
CHEMBL1922925 glr_human Human No 7.6 IC50 = 23 nM Bind
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
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
CHEMBL3237924 glr_human Human No 7.6 IC50 = 23 nM Bind
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
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
CHEMBL3238217 glr_human Human No 7.6 IC50 = 23 nM Bind
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
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
CHEMBL153038 glr_human Human No 7.6 IC50 = 23 nM Bind
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
445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1
CHEMBL348785 glr_human Human No 7.6 IC50 = 23 nM Bind
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
482 9 2 6 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1
CHEMBL85009 glr_human Human No 7.6 IC50 = 23.0 nM Bind
Inhibition of