Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
162660600 187963 0 None 1 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4337 106 62 64 -24.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)CSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4761047 187963 0 None 1 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4337 106 62 64 -24.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)CSCc2cccc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
168281065 197790 0 None 2 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3920 140 55 53 -10.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5186705 197790 0 None 2 2 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3920 140 55 53 -10.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL4126027 219787 0 None 74 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.8b00292
137634214 163426 0 None 1 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4121 139 65 62 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4069307 163426 0 None 1 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4121 139 65 62 -27.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4226451 220081 0 None 7 3 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)CN(C)C(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
155523482 177575 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3480 112 54 51 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4453136 177575 0 None - 1 Human 10.8 pEC50 = 10.8 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3480 112 54 51 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168292950 198926 0 None -1 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3881 137 56 53 -12.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5203806 198926 0 None -1 2 Human 10.8 pEC50 = 10.8 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3881 137 56 53 -12.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
168284782 198467 0 None 2 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3907 139 55 53 -10.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5196728 198467 0 None 2 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3907 139 55 53 -10.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5314341 222486 0 None 1 6 Mouse 10.7 pEC50 = 10.7 Functional
Agonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assayAgonist activity at mouse GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay
ChEMBL None None None None 10.1016/j.bmc.2017.10.047
CHEMBL5314341 222486 0 None -8 6 Human 10.7 pEC50 = 10.7 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL None None None None 10.1021/acs.jmedchem.6b00840
137642925 164903 0 None - 1 Mouse 10.6 pEC50 = 10.6 Functional
Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4579 156 66 65 -22.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.7b00174
CHEMBL4086979 164903 0 None - 1 Mouse 10.6 pEC50 = 10.6 Functional
Agonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at mouse glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4579 156 66 65 -22.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1021/acs.jmedchem.7b00174
137659233 165925 0 None -1 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4098061 165925 0 None -1 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
155533592 178669 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4469604 178669 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4126953 219796 0 None 74 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4226514 220082 0 None -1 3 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O 10.1016/j.bmc.2017.10.047
137659233 165925 0 None -1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4098061 165925 0 None -1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4126738 219792 0 None 70 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCC(=O)[C@H](CCN[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC)C(=O)O)C(=O)O 10.1021/acs.jmedchem.8b00292
CHEMBL4227045 220087 0 None -1 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
168283329 197553 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3823 134 55 52 -12.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5183317 197553 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3823 134 55 52 -12.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
168283329 197553 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3823 134 55 52 -12.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5183317 197553 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 3823 134 55 52 -12.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
155532202 178482 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4466715 178482 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4226613 220083 0 None -1 3 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
155562429 182011 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4571762 182011 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168287225 198494 0 None -1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3937 138 57 53 -12.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5197042 198494 0 None -1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3937 138 57 53 -12.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
155526545 177906 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4458230 177906 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3449 112 52 50 -17.1 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
155566739 182660 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4586269 182660 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3464 112 53 50 -16.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
168296994 199100 0 None 1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3839 135 56 53 -13.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5206399 199100 0 None 1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3839 135 56 53 -13.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
168286525 198142 0 None -1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3835 133 54 51 -10.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5192132 198142 0 None -1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3835 133 54 51 -10.5 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
155564592 182316 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3479 112 54 50 -16.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4578443 182316 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3479 112 54 50 -16.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4225340 220074 0 None -1 3 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(=O)O 10.1016/j.bmc.2017.10.047
CHEMBL1222098 215421 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222088 215411 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168285487 198434 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4110 145 58 56 -11.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5196180 198434 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4110 145 58 56 -11.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222076 215400 0 None 3 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168278702 197918 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4151 152 57 57 -10.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)CCCCN=[N+]=[N-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5188299 197918 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4151 152 57 57 -10.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(=O)COCCOCCNC(=O)CCCCN=[N+]=[N-])C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL1222077 215401 0 None 20 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
49864558 22429 0 None 2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
91933345 22429 0 None 2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222080 22429 0 None 2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3537 117 55 51 -16.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
162656099 187509 0 None -3 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCNC(=O)CCCC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4755815 187509 0 None -3 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCNC(=O)CCCC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
49864615 22439 0 None -4 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3362 96 47 47 -11.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)CN[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222174 22439 0 None -4 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3362 96 47 47 -11.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)CN[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222099 215422 0 None -1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
168296031 199065 0 None -1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4091 144 58 55 -12.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5205970 199065 0 None -1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4091 144 58 55 -12.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
162652123 187123 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCCNC(=O)CC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4751319 187123 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4253 123 62 62 -24.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCCCNC(=O)CC[C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC1=O 10.1021/acs.jmedchem.0c01500
168271903 197381 0 None -1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4194 149 61 57 -13.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5180732 197381 0 None -1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 4194 149 61 57 -13.2 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(=O)CC[C@H](N)C(=O)O)C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
102331734 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
1136 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
16132283 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
16133817 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
2994 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
3785 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
44278361 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
77077981 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
CHEMBL266481 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
DB00040 8595 36 None -1 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.7b00174
168274917 197029 0 None 2 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3851 135 55 52 -11.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5175260 197029 0 None 2 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3851 135 55 52 -11.7 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222082 215405 0 None 8 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222087 215410 0 None -2 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222090 215413 0 None 1 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222079 215403 0 None 3 2 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL5314341 222486 0 None -8 6 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None None 10.1038/nchembio.209
155517094 176947 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4444485 176947 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222091 215414 0 None -1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)[C@@H](C)O 10.1038/nchembio.209
168290869 198752 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3837 134 55 52 -12.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5201113 198752 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3837 134 55 52 -12.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL1222101 215424 0 None 2 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)CCC(=O)NCCCC[C@@H](C(=O)N[C@H](C(=O)O)[C@@H](C)O)NC1=O 10.1038/nchembio.209
CHEMBL1222085 215408 0 None -1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222100 215423 0 None 3 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc2cnc[nH]2)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](C(C)C)C(=O)N1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
102331734 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
1136 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
16132283 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
16133817 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
2994 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
3785 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
44278361 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
77077981 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
CHEMBL266481 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
DB00040 8595 36 None -1 6 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2020.113118
CHEMBL1222092 215415 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
155512720 176465 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4437733 176465 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3450 112 52 51 -17.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222089 215412 0 None -3 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168298565 199451 0 None -3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4643 155 67 66 -21.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5218881 199451 0 None -3 2 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4643 155 67 66 -21.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL1222078 215402 0 None 2 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222081 215404 0 None 1 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCS(=O)(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168271945 196878 0 None 1 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3941 140 59 55 -15.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
CHEMBL5172868 196878 0 None 1 2 Human 10.0 pEC50 = 10 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assayAgonist activity at human GCGR expressed in frozen cells assessed as increase in cAMP production measured after 1 hr by HitHunter luminescence assay
ChEMBL 3941 140 59 55 -15.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00217
162648287 186684 0 None -2 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4210 122 64 63 -28.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4745985 186684 0 None -2 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4210 122 64 63 -28.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL1222097 215420 0 None 1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
137662302 166022 0 None 13 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 4314 132 64 64 -25.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00174
CHEMBL4098991 166022 0 None 13 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 5 hrs by luciferase reporter gene assay
ChEMBL 4314 132 64 64 -25.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00174
162648841 186625 0 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4745235 186625 0 None -1 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4215 135 63 63 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL1222083 215406 0 None 4 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222084 215407 0 None 4 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
168299170 199477 0 None -2 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4628 153 66 65 -20.5 CCCCCCCCCCCCCCCC(=O)N[C@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5219454 199477 0 None -2 2 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4628 153 66 65 -20.5 CCCCCCCCCCCCCCCC(=O)N[C@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)CC)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL1222075 215399 0 None 3 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4227861 220093 0 None -1 3 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N[C@@H](CCC(N)=O)C(=O)N1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
168298728 199509 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4261 133 64 63 -25.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220251 199509 0 None -2 2 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4261 133 64 63 -25.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
168284802 198529 0 None 4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4104 144 57 55 -11.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(N)=O)C(=O)O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5197522 198529 0 None 4 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4104 144 57 55 -11.3 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN=[N+]=[N-])C(=O)N[C@@H](CCC(N)=O)C(=O)O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
168299650 199462 0 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4392 150 72 63 -24.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219122 199462 0 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4392 150 72 63 -24.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
168298631 199507 0 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4756 159 68 67 -20.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O)C(=O)O 10.1016/j.ejmech.2020.113118
CHEMBL5220241 199507 0 None -3 2 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4756 159 68 67 -20.9 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O)C(=O)O 10.1016/j.ejmech.2020.113118
162657120 187681 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C/CCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4757675 187681 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C/CCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
168298518 199523 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3474 114 55 51 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL5220666 199523 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3474 114 55 51 -18.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
168299004 199532 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4453 151 73 65 -26.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5221090 199532 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4453 151 73 65 -26.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
168298163 199522 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3488 113 55 51 -18.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL5220630 199522 0 None 1 2 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3488 113 55 51 -18.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)C(C)O 10.1016/j.ejmech.2020.113118
CHEMBL4163714 219997 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222086 215409 0 None -30 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)O)C(C)C 10.1038/nchembio.209
168282938 197524 0 None -1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4117 146 57 55 -10.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5182822 197524 0 None -1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assayAgonist activity at human GCGR expressed in frozen cells assessed as measuring the cAMP level incubated for 1 hr by by HitHunter chemiluminescence based assay
ChEMBL 4117 146 57 55 -10.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN=[N+]=[N-])C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acsmedchemlett.2c00218
CHEMBL5314341 222486 0 None -8 6 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assayAgonist activity at human GCG receptor expressed in CHO cells assessed as increase in cAMP level by TR-FRET assay
ChEMBL None None None None 10.1016/j.bmc.2017.10.047
162659870 188052 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4338 104 61 64 -22.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)CSCc2cc3cc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CSC3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
CHEMBL4762061 188052 0 None -2 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4338 104 61 64 -22.6 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)CSCc2cc3cc(c2)CSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N2CCC[C@H]2C(=O)N[C@@H](CO)C(N)=O)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](CO)NC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CNC(=O)[C@H](CSC3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/acs.jmedchem.0c01500
49864580 22430 0 None -41 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3380 111 48 48 -12.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)CN[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL1222102 22430 0 None -41 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL 3380 111 48 48 -12.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)CN[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4170727 220005 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168298382 199519 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4331 137 64 63 -22.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220497 199519 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4331 137 64 63 -22.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4174154 220010 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4166241 220001 0 None 3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168298376 199514 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4467 150 73 65 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220372 199514 0 None -1 2 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4467 150 73 65 -26.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5314341 222486 0 None -8 6 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None None 10.1016/j.ejmech.2017.07.046
137650720 164059 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4213 135 59 61 -21.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4076828 164059 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4213 135 59 61 -21.8 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
137661599 165974 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 4447 149 73 65 -25.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)O 10.1016/j.ejmech.2017.07.046
CHEMBL4098545 165974 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL 4447 149 73 65 -25.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)O 10.1016/j.ejmech.2017.07.046
137638423 163667 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4486 148 66 64 -22.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00174
CHEMBL4072029 163667 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4486 148 66 64 -22.1 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.7b00174
CHEMBL4167331 220003 0 None 4 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CS)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4162383 219993 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
168299536 199471 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3554 120 56 51 -16.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219263 199471 0 None -9 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3554 120 56 51 -16.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
168299173 199478 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4346 136 64 63 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219458 199478 0 None -2 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4346 136 64 63 -22.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4159256 219987 0 None -1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4160347 219990 0 None 7 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4167169 220002 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CS)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4173061 220009 0 None -1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4175452 220013 0 None 1 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
168299127 199439 0 None -3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3426 114 54 49 -16.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5218509 199439 0 None -3 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3426 114 54 49 -16.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4162789 219994 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CS)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4159275 219988 0 None 3 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4170976 220006 0 None 6 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
137634741 162678 0 None -93 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4185 134 62 62 -26.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
CHEMBL4060629 162678 0 None -93 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL 4185 134 62 62 -26.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.7b00174
155532070 178495 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3451 112 52 52 -18.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL4466856 178495 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation countingActivation of glucagon receptor (unknown origin) transfected in HEK293 cells coinfected with luciferase reporter gene linked CRE element assessed as cAMP accumulation after 5 hrs in presence of luclite substrate by liquid scintillation counting
ChEMBL 3451 112 52 52 -18.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.6b00840
CHEMBL1222095 215418 0 None -85 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4169653 220004 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
168298006 199487 0 None -21 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3569 119 56 51 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5219646 199487 0 None -21 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3569 119 56 51 -16.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
168298501 199515 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3583 120 56 51 -16.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5220384 199515 0 None -16 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 3583 120 56 51 -16.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4174404 220012 0 None 3 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4163731 219998 0 None 1 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4177064 220015 0 None -1 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4130148 219824 0 None 8 3 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.8b00292
CHEMBL4172444 220008 0 None 4 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222094 215417 0 None -33 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4174382 220011 0 None 1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
162651402 186961 0 None -251 5 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.0c01783
CHEMBL4749279 186961 0 None -251 5 Rat 7.5 pEC50 = 7.5 Functional
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
ChEMBL 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 10.1021/acs.jmedchem.0c01783
168299788 199454 0 None -177 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4276 132 64 63 -25.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL5218999 199454 0 None -177 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells incubated for 30 mins and assessed as increase in cAMP accumulation measured by HTRF assay
ChEMBL 4276 132 64 63 -25.4 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1016/j.ejmech.2020.113118
CHEMBL4165144 220000 0 None -1 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CSC1CC(=O)N(CCCCCCCCCCCC(=O)O)C1=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL4159003 219986 0 None 19 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4160365 219991 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CCCCCCCCCCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C1=O 10.1016/j.ejmech.2017.07.046
CHEMBL4130044 219819 0 None -812 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as cAMP accumulation after 30 mins by HTRF assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.8b00292
CHEMBL4225594 220077 0 None -173 3 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assayAgonist activity at human GCG receptor expressed in HEK293 cells assessed as increase in cAMP level after 5 hrs by CRE driven luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.bmc.2017.10.047
CHEMBL4159426 219989 0 None 6 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CS)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL1222093 215416 0 None -275 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assayAgonist activity at GCGR expressed in HEK293 cells assessed as stimulation of cAMP production by luciferase reporter gene assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)N[C@@H](Cc1cnc[nH]1)C(=O)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1038/nchembio.209
CHEMBL4161800 219992 0 None -3 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assayAgonist activity at human GCGR expressed in HEK293 cells assessed as increase in cAMP accumulation after 20 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2017.07.046
CHEMBL5314341 222486 0 None -194 6 Rat 8.1 pEC50 = 8.1 Functional
cAMP accumulation in rat hepatocytes in the presence rolipramcAMP accumulation in rat hepatocytes in the presence rolipram
ChEMBL None None None None 10.1021/jm960800d
162655167 187579 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C\CCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
CHEMBL4756489 187579 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human glucagon receptor expressed in HEK293 cells assessed as induction of cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 4178 120 60 61 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@]1(C)CCC/C=C\CCC[C@](C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O 10.1021/acs.jmedchem.0c01500
164616962 191972 0 None 1 6 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857523 191972 0 None 1 6 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
164616962 191972 0 None -1 6 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857523 191972 0 None -1 6 Mouse 9.3 pIC50 = 9.3 Functional
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3433 123 50 46 -9.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)C(=O)O)C(=O)O 10.1021/acs.jmedchem.0c02069
122189698 130143 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
CHEMBL3616677 130143 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
71243036 117055 0 None 2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 117055 0 None 2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
16225394 75753 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922917 75753 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
57882748 146741 13 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL3799802 146741 13 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
57882748 146741 13 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799802 146741 13 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
60170767 88154 0 None 54 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159327 88154 0 None 54 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
11950971 157683 0 None 2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL395759 157683 0 None 2 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11570626 9328 46 None -6 9 Dog 7.0 pIC50 = 7.0 Functional
Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None -6 9 Dog 7.0 pIC50 = 7.0 Functional
Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None -6 9 Dog 7.0 pIC50 = 7.0 Functional
Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None -6 9 Dog 7.0 pIC50 = 7.0 Functional
Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
10370821 78907 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197851 78907 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11950794 168010 0 None 5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411831 168010 0 None 5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60170969 88174 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159346 88174 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
127047254 146716 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
CHEMBL3799656 146716 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
122189570 130118 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616581 130118 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189579 130127 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616590 130127 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
11950794 168010 0 None 5 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411831 168010 0 None 5 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
44431020 174418 0 None 123 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL430163 174418 0 None 123 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60170970 88175 0 None 199 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159347 88175 0 None 199 4 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
57518490 88164 0 None 56 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159337 88164 0 None 56 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
58353063 117021 0 None 31 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237900 117021 0 None 31 3 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353067 117057 0 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 117057 0 None 2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352821 117037 0 None 28 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237915 117037 0 None 28 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44404227 78906 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197850 78906 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
9985625 63699 0 None 5 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
CHEMBL1644183 63699 0 None 5 5 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
11678967 88157 0 None 29 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
CHEMBL2159330 88157 0 None 29 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
10346647 147132 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL380771 147132 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10007881 172696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL425024 172696 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
145967741 171970 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228690 171970 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
54765285 75770 0 None 128 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922933 75770 0 None 128 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
164628536 193244 0 None 2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876736 193244 0 None 2 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11621378 88181 3 None 131 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159353 88181 3 None 131 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11527207 88168 0 None 81 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
CHEMBL2159340 88168 0 None 81 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
122189693 130138 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616672 130138 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
135819137 99626 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
CHEMBL24388 99626 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
11250000 75681 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
CHEMBL1922704 75681 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
11387112 75688 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922711 75688 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
90655064 117068 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238228 117068 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046968 146681 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
CHEMBL3799439 146681 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
127046098 146861 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3800525 146861 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
11570626 9328 46 None -7 9 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None -7 9 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None -7 9 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None -7 9 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
1148 8705 34 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
619101 8705 34 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
CHEMBL179281 8705 34 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
164628244 193226 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876499 193226 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
145969571 171947 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228281 171947 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
11444850 75742 0 None 54 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922839 75742 0 None 54 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
164616848 191728 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4853767 191728 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170857 88170 0 None 56 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159342 88170 0 None 56 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
122189575 130123 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616586 130123 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
11490222 75683 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922706 75683 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
71243005 117047 0 None 5 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237925 117047 0 None 5 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353046 117058 0 None 3 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 117058 0 None 3 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10077369 63704 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644188 63704 0 None 14 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
127046644 146356 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3797325 146356 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
44404227 78906 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197850 78906 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 5.9 CC(C)(C)C1CCC2(CC1)CN(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189708 130153 0 None 213 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616687 130153 0 None 213 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189715 130160 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616694 130160 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
54765284 75743 0 None 165 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922840 75743 0 None 165 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57393253 75747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922844 75747 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11585375 88166 0 None 30 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159339 88166 0 None 30 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
11273570 75691 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922714 75691 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189694 130139 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616673 130139 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189723 130169 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616702 130169 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
16100296 209618 46 None 1 4 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL62444 209618 46 None 1 4 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
58353013 117016 0 None 10 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237895 117016 0 None 10 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353544 117020 0 None 7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 117020 0 None 7 3 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352803 117059 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 117059 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353232 117009 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237889 117009 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
127045652 146482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798135 146482 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
127047253 146850 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3800473 146850 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
10437700 142152 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL372784 142152 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
16100296 79187 46 None -1 5 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL198736 79187 46 None -1 5 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
11950972 168011 0 None 3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411832 168011 0 None 3 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11952213 93533 0 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232037 93533 0 None 2 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
145967924 171907 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4227634 171907 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
11952035 158249 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL396215 158249 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11570626 9328 46 None 3 9 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None 3 9 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None 3 9 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None 3 9 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
60170971 88176 0 None 186 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159348 88176 0 None 186 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
45381379 117050 0 None 4 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237928 117050 0 None 4 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
16225393 75758 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922922 75758 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
127046099 146688 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799468 146688 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
11757662 79033 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198214 79033 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44389598 71646 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 71646 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
11331120 75737 0 None 81 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922834 75737 0 None 81 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10324097 63636 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643955 63636 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
58353838 117060 0 None 5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238220 117060 0 None 5 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352840 117011 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)c(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237890 117011 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)c(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
90655066 117067 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ncccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238227 117067 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ncccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047904 146607 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799017 146607 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10416067 78588 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL196844 78588 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
10073298 77330 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 467 4 2 5 4.5 CC(C)(C)C1CCC2(CC1)CN(C(C)(C)C)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL194794 77330 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 467 4 2 5 4.5 CC(C)(C)C1CCC2(CC1)CN(C(C)(C)C)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10393857 78867 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 603 8 2 5 6.1 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197754 78867 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 603 8 2 5 6.1 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189572 130120 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616583 130120 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
11421820 75687 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922710 75687 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
16225179 75762 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922926 75762 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57396141 75775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922938 75775 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11757679 63694 0 None 54 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1644178 63694 0 None 54 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
58352935 117018 0 None 8 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 117018 0 None 8 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
145969316 171910 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227667 171910 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
145969278 171850 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4226770 171850 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
145986774 173820 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 461 12 2 5 5.2 CCCCC(Oc1ncc(-c2ccc(CC)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4288863 173820 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 461 12 2 5 5.2 CCCCC(Oc1ncc(-c2ccc(CC)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
44404222 78742 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197340 78742 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11352811 185779 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
CHEMBL470955 185779 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
122189711 130156 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616690 130156 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
122189712 130157 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616691 130157 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
122189713 130158 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616692 130158 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
122189718 130163 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616697 130163 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
57391489 75744 0 None 141 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922841 75744 0 None 141 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11952035 93592 0 None 10 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232239 93592 0 None 10 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL439289 220613 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL None None None CN[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2005.01.003
11410772 75462 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1921810 75462 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
51031037 117039 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 117039 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353338 117062 0 None 3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 117062 0 None 3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 117063 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 117063 0 None 2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10099927 142887 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL373234 142887 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10383925 85725 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112991 85725 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
11678966 88159 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
CHEMBL2159332 88159 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
11951681 103631 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL265337 103631 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
44561440 179368 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 584 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL448921 179368 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 584 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
11478813 75692 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922715 75692 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11456187 75738 2 None 40 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922835 75738 2 None 40 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57393252 75746 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922843 75746 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
91755011 130264 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMPAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMP
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
CHEMBL3617565 130264 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMPAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 30 mins by liquid scintillation counting analysis in presence of [125I]-cAMP
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
58353464 117012 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 573 8 2 5 5.6 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237891 117012 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 573 8 2 5 5.6 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353408 117013 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237892 117013 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
127046645 146423 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3797757 146423 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
164622383 192720 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4869368 192720 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10370821 78907 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197851 78907 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10008709 148081 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 6 2 7 5.7 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383350 148081 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 6 2 7 5.7 CC(C)(C)C1CCC2(CC1)CC(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
9986018 140368 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371235 140368 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189704 130149 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616683 130149 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
57403109 75773 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922936 75773 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
9985625 63699 0 None -25 5 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None -25 5 Mouse 5.7 pIC50 = 5.7 Functional
Antagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at mouse GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
44342725 16741 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibitory concentration against cAMP production in hGR-CHO cellsInhibitory concentration against cAMP production in hGR-CHO cells
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL114761 16741 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Inhibitory concentration against cAMP production in hGR-CHO cellsInhibitory concentration against cAMP production in hGR-CHO cells
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
160115 183803 21 None -1 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL 518 1 6 10 4.6 CC1CC(=O)c2c(cc3c(-c4c(O)cc(O)c5c(O)c6c(cc45)OC(C)CC6=O)c(O)cc(O)c3c2O)O1 10.1021/np040093o
CHEMBL463175 183803 21 None -1 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL 518 1 6 10 4.6 CC1CC(=O)c2c(cc3c(-c4c(O)cc(O)c5c(O)c6c(cc45)OC(C)CC6=O)c(O)cc(O)c3c2O)O1 10.1021/np040093o
145971123 171855 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226911 171855 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
127046805 146583 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 663 10 2 5 9.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(CC(=O)O)c4ccccc4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798798 146583 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 663 10 2 5 9.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(CC(=O)O)c4ccccc4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
53377590 130260 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 524 7 2 5 5.0 CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(N2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617561 130260 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 524 7 2 5 5.0 CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(N2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
16100296 79187 46 None -1 5 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL198736 79187 46 None -1 5 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
122189721 130167 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 615 10 2 5 7.9 CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616700 130167 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 615 10 2 5 7.9 CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189706 130151 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616685 130151 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11238814 75676 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922699 75676 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
127047385 146426 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
CHEMBL3797782 146426 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
44561479 185906 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
CHEMBL471979 185906 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
11950795 93593 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232241 93593 0 None 1 2 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
44561439 197980 0 None 426 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL518939 197980 0 None 426 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
11365464 75684 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922707 75684 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57403703 75745 0 None 41 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922842 75745 0 None 41 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
71472272 130271 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
CHEMBL3617572 130271 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
53467170 130262 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 607 10 2 4 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC12CCC([Si](C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617563 130262 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 607 10 2 4 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC12CCC([Si](C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
44561480 185941 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472154 185941 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
122189696 130141 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616675 130141 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
58353104 117045 0 None 4 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237923 117045 0 None 4 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145967685 171889 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227364 171889 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
45381268 117048 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 7 2 6 6.4 CC(C)[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237926 117048 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 7 2 6 6.4 CC(C)[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10459436 140374 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371259 140374 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561556 196058 0 None 213 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
CHEMBL511964 196058 0 None 213 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
11421826 75673 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922696 75673 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
164628536 193244 0 None -2 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876736 193244 0 None -2 2 Mouse 7.6 pIC50 = 7.6 Functional
Antagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at mouse GCGR expressed in CHO-K1 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11592461 88171 0 None 64 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159343 88171 0 None 64 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11180162 75686 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922709 75686 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10008376 63697 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644181 63697 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
71202743 117064 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3238224 117064 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
145967899 171869 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227099 171869 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
44404243 148047 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383135 148047 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
60170766 88153 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
CHEMBL2159326 88153 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
145970933 171930 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4227967 171930 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
11650288 88160 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
CHEMBL2159333 88160 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
122189716 130161 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616695 130161 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
57401359 75777 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922940 75777 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353323 117061 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238221 117061 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11284982 75740 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922837 75740 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57393262 75678 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922701 75678 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10072624 79050 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 453 5 2 5 4.1 CC(C)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL198259 79050 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 453 5 2 5 4.1 CC(C)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
122189569 130117 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616580 130117 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
122189719 130164 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616698 130164 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
58352868 117019 0 None 6 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237898 117019 0 None 6 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
53469058 117071 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C)CC2 10.1021/jm401858f
CHEMBL3238231 117071 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 609 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C)CC2 10.1021/jm401858f
145989050 172001 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4229115 172001 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
9985625 63699 0 None -33 5 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at rat GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None -33 5 Rat 5.6 pIC50 = 5.6 Functional
Antagonist activity at rat GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at rat GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
127047256 146549 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798581 146549 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
127047906 146568 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798731 146568 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
164624673 192770 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870133 192770 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
145968206 171971 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228703 171971 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
60171062 88180 0 None 104 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159352 88180 0 None 104 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
58353206 117044 0 None 2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237922 117044 0 None 2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
122189571 130119 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616582 130119 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
53469820 117080 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 627 8 2 4 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238241 117080 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 627 8 2 4 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
141465337 171867 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4227068 171867 0 None - 1 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
164626335 193144 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875380 193144 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44431016 151022 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL390469 151022 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11432140 182908 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459208 182908 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11308245 75739 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922836 75739 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
58352940 117022 0 None 4 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237901 117022 0 None 4 3 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10099927 142887 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL373234 142887 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 589 8 2 4 6.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10437700 142152 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL372784 142152 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11952035 158249 0 None 3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL396215 158249 0 None 3 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11353908 75741 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922838 75741 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
58353132 117004 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237884 117004 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
71202253 130261 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 589 8 2 6 6.8 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(C2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
CHEMBL3617562 130261 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 589 8 2 6 6.8 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(C2CCCCC2)=NC12CCC(C(C)(C)C)CC2 10.1016/j.bmcl.2015.07.092
58352762 117038 0 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237916 117038 0 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
68860750 120765 1 None -1 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326188 120765 1 None -1 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in human hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
11527170 88163 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159336 88163 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
23550062 78580 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL196800 78580 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
10416067 78588 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
CHEMBL196844 78588 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 593 6 2 5 6.2 CC(c1ccc(Br)cc1)N1CC2(CCC(C(C)(C)C)CC2)N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C1=O 10.1016/j.bmcl.2005.06.101
57399593 75755 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922919 75755 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
11657413 88158 0 None 44 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
CHEMBL2159331 88158 0 None 44 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
58653097 85799 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 605 8 3 5 5.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL2113103 85799 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 605 8 3 5 5.6 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1 10.1016/j.bmcl.2005.06.101
44372478 58629 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1021/jm050563r
CHEMBL158548 58629 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1021/jm050563r
11585452 88165 0 None 47 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159338 88165 0 None 47 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL524883 222407 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)C[C@@H]2NC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CSSC[C@@H](C(=O)OC)NC(=O)[C@H](C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)CNC(=O)[C@@H]3CCCN3C1=O)NC(=O)CNC(=O)[C@H](Cc1c[nH]c3ccccc13)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)CNC2=O 10.1021/np040093o
58353274 117014 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 489 7 2 4 4.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237893 117014 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 489 7 2 4 4.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
44404243 148047 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383135 148047 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 571 6 2 6 5.8 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11952211 94726 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL234087 94726 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10415723 63700 0 None 63 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644184 63700 0 None 63 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
145969298 171880 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227229 171880 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
10031040 172941 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL426295 172941 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10054055 79095 12 None 7 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198387 79095 12 None 7 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
57399594 75767 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
CHEMBL1922930 75767 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
11754125 85726 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112992 85726 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
58352925 117023 0 None 12 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237902 117023 0 None 12 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44431012 157685 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL395760 157685 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
164613898 191501 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4850520 191501 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10053841 63698 0 None 85 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644182 63698 0 None 85 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
16224591 75756 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922920 75756 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57394374 75774 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922937 75774 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353778 117024 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237903 117024 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469821 117079 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238240 117079 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047121 146742 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
CHEMBL3799820 146742 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
10369580 78987 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198094 78987 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
10052441 140408 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371476 140408 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10007881 172696 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL425024 172696 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 555 5 2 5 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189580 130128 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616591 130128 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
57396140 75771 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 12 2 4 8.0 CC(C)CC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922934 75771 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 612 12 2 4 8.0 CC(C)CC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
122189578 130126 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616589 130126 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
68243839 117065 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
CHEMBL3238225 117065 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
71454981 88172 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
CHEMBL2159344 88172 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
122189581 130129 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616592 130129 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
10483611 63695 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644179 63695 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
45381381 117054 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 117054 0 None 2 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71202712 117076 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238236 117076 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145969968 171858 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226972 171858 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
56602804 117073 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C 10.1021/jm401858f
CHEMBL3238233 117073 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C 10.1021/jm401858f
44561438 196182 0 None 204 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL513067 196182 0 None 204 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
45381051 117046 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237924 117046 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
122189574 130122 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616585 130122 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
16223791 75761 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922925 75761 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11950972 168011 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411832 168011 0 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
164621209 193031 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4873721 193031 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11249762 190620 0 None 1122 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL480692 190620 0 None 1122 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
122190363 130274 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617575 130274 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
44575544 180777 0 None 3 4 Human 8.4 pIC50 = 8.4 Functional
Inhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
CHEMBL454246 180777 0 None 3 4 Human 8.4 pIC50 = 8.4 Functional
Inhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of GCGR expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
164617806 191461 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4849980 191461 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
9985625 63699 0 None -5 5 Dog 6.4 pIC50 = 6.4 Functional
Antagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None -5 5 Dog 6.4 pIC50 = 6.4 Functional
Antagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at dog GCGR assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
71202713 117077 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238237 117077 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22004955 100258 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL24616 100258 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
10325599 148085 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 6 2 7 4.3 CC(C)(C)C1CCC2(CC1)CN(c1ccc(S(C)(=O)=O)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL383370 148085 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 565 6 2 7 4.3 CC(C)(C)C1CCC2(CC1)CN(c1ccc(S(C)(=O)=O)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189701 130146 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616680 130146 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11490393 75689 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922712 75689 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10435275 130642 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL362657 130642 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
145990090 173780 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCCC(Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4288074 173780 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCCC(Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
58353126 117056 0 None 7 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 117056 0 None 7 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
57397957 75769 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 598 12 2 4 7.7 CCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922932 75769 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 598 12 2 4 7.7 CCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
10007966 79274 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL199013 79274 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
44404234 131729 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 501 5 2 5 5.2 Cc1ccc(N2CC3(CCC(C(C)(C)C)CC3)N(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL364288 131729 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 501 5 2 5 5.2 Cc1ccc(N2CC3(CCC(C(C)(C)C)CC3)N(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)C2=O)cc1 10.1016/j.bmcl.2005.06.101
10007966 79274 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL199013 79274 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 559 7 2 3 6.6 CC(C)(C)C1CCC2(CC1)CN(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189705 130150 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616684 130150 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11785044 196445 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL515202 196445 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
58352863 117025 0 None 13 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237904 117025 0 None 13 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
122189703 130148 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616682 130148 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
9985625 63699 0 None 5 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None 5 5 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
57392671 75776 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922939 75776 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11950971 157683 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL395759 157683 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
164627630 193119 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875003 193119 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
57400189 75682 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922705 75682 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
58353662 117026 0 None 16 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 117026 0 None 16 3 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL526383 222463 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIAAntagonist activity at human glucagon receptor expressed in BHK21 cells assessed as inhibition of glucagon-induced cAMP elevation by RIA
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)C[C@@H]2NC(=O)[C@H](CO)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CSSC[C@@H](C(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@@H]3CCCN3C(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)CNC(=O)[C@@H]3CCCN3C1=O)NC(=O)CNC(=O)[C@H](Cc1c[nH]c3ccccc13)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)CNC2=O 10.1021/np040093o
145968045 171725 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4224961 171725 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10346647 147132 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL380771 147132 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
16223987 75754 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922918 75754 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
145971078 171787 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4225922 171787 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
141465324 171891 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227372 171891 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
53466721 117083 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 665 8 2 6 8.1 C[C@@H](NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1)c1nnn[nH]1 10.1021/jm401858f
CHEMBL3238245 117083 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 665 8 2 6 8.1 C[C@@H](NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1)c1nnn[nH]1 10.1021/jm401858f
127047907 146700 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799556 146700 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10031040 172941 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL426295 172941 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189717 130162 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616696 130162 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
23550062 63632 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1643951 63632 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
53469443 117084 1 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238246 117084 1 None 3 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11952211 160520 0 None 7 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL398180 160520 0 None 7 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11949739 168012 0 None 57 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411833 168012 0 None 57 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
23550062 78580 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
CHEMBL196800 78580 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2005.06.101
145970930 171929 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227964 171929 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10326056 63696 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644180 63696 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
60171061 88179 0 None 114 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159351 88179 0 None 114 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
164620673 192797 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870505 192797 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164629129 193256 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876913 193256 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
122189576 130124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616587 130124 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
53469628 117074 0 None 19 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 117074 0 None 19 3 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353156 117027 0 None 13 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 117027 0 None 13 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
45381049 117066 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238226 117066 0 None -1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11952211 94726 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL234087 94726 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
57391519 75679 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922702 75679 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
16224781 75764 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
CHEMBL1922928 75764 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
58353369 117028 0 None 6 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 117028 0 None 6 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
122189573 130121 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616584 130121 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
68860750 120765 1 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in rat hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in rat hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326188 120765 1 None 1 2 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of glucagon-induced glucagon receptor-mediated cAMP production in rat hepatocytes after 15 mins by cAMP dynamic2 assayInhibition of glucagon-induced glucagon receptor-mediated cAMP production in rat hepatocytes after 15 mins by cAMP dynamic2 assay
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
122189577 130125 0 None 588 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616588 130125 0 None 588 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
60171059 88177 0 None 407 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159349 88177 0 None 407 4 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11952394 93787 0 None 660 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232448 93787 0 None 660 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11950075 93589 0 None 9 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232224 93589 0 None 9 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
58352836 117005 0 None 19 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237885 117005 0 None 19 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
53469258 117072 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
CHEMBL3238232 117072 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
58352938 117017 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237896 117017 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10257529 78490 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196560 78490 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
122189695 130140 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616674 130140 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
58352937 117069 0 None 4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 117069 0 None 4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
57396138 75752 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922916 75752 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
58353839 117078 0 None 24 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
CHEMBL3238238 117078 0 None 24 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
127047255 146800 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
CHEMBL3800146 146800 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
11950795 93593 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232241 93593 0 None 1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
45381153 117043 0 None 3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
CHEMBL3237921 117043 0 None 3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
11785044 182998 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459457 182998 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57397956 75757 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922921 75757 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 584 11 2 4 7.3 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57390854 75772 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922935 75772 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
11570626 9328 46 None -3 9 Rhesus macaque 7.3 pIC50 = 7.3 Functional
Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None -3 9 Rhesus macaque 7.3 pIC50 = 7.3 Functional
Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None -3 9 Rhesus macaque 7.3 pIC50 = 7.3 Functional
Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None -3 9 Rhesus macaque 7.3 pIC50 = 7.3 Functional
Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
58352952 117029 0 None 13 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237908 117029 0 None 13 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145989480 171988 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228938 171988 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
122189702 130147 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616681 130147 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
10076914 63705 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644189 63705 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
58352858 117030 0 None 8 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 117030 0 None 8 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11699553 88155 0 None 72 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
CHEMBL2159328 88155 0 None 72 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
10413333 69793 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
CHEMBL178768 69793 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
44389598 71646 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 71646 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
122189709 130154 0 None 239 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616688 130154 0 None 239 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
164624163 192594 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4867132 192594 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10257529 78490 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196560 78490 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 575 8 2 4 6.2 CC(C)(C)C1CCC2(CC1)CN(c1cccc(OC(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
145989947 173573 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 489 11 2 5 6.0 CCCCC(Oc1ncc(-c2ccc(C(C)(C)C)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4284236 173573 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 489 11 2 5 6.0 CCCCC(Oc1ncc(-c2ccc(C(C)(C)C)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10369580 78987 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198094 78987 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 525 7 2 3 6.0 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
57401963 75675 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922698 75675 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11949740 163504 0 None 194 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL407028 163504 0 None 194 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
53377591 130263 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 683 11 2 7 8.1 CC(C)(C)CCOc1cccc(C2=NC3(CCC(C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1016/j.bmcl.2015.07.092
CHEMBL3617564 130263 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assayAntagonist activity at recombinant human glucagon receptor expressed in CHO cells assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 45 mins by LANCE assay
ChEMBL 683 11 2 7 8.1 CC(C)(C)CCOc1cccc(C2=NC3(CCC(C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1016/j.bmcl.2015.07.092
44404222 78742 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197340 78742 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 505 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561519 185966 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472325 185966 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
11599295 190580 0 None 229 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL480501 190580 0 None 229 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
44389632 70044 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
CHEMBL179181 70044 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibition of glucagon induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
60170968 88173 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159345 88173 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
58352834 117032 0 None 10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237910 117032 0 None 10 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353350 117033 0 None 6 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237911 117033 0 None 6 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127047120 146504 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
CHEMBL3798231 146504 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
127046643 146574 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798761 146574 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
9873139 79006 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 7 5.3 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198144 79006 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 585 6 2 7 5.3 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
60170855 88162 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159335 88162 0 None 15 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
11433550 75677 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922700 75677 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
10459436 140374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371259 140374 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 523 5 2 5 5.1 CC(C)(C)C1CCC2(CC1)CN(c1ccc(F)c(F)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
122189699 130144 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
CHEMBL3616678 130144 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
9906120 102061 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL25637 102061 1 None - 1 Human 7.2 pIC50 = 7.2 Functional
Tested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cellsTested for its ability to inhibit cAMP production in human glucagon receptor expressed CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
10461010 63702 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644186 63702 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11757662 79033 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198214 79033 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 565 5 2 5 5.6 CC(C)(C)C1CCC2(CC1)CN(c1ccc(Br)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
53469056 117070 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238230 117070 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71060230 130273 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617574 130273 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysisAntagonist activity at human glucagon receptor expressed in HEK293 cell membranes assessed as inhibition of glucagon-stimulated intracellular cAMP formation preincubated for 30 mins followed by glucagon stimulation measured after 5 mins by TR-FRET analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
11952214 93594 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232242 93594 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60171060 88178 0 None 158 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159350 88178 0 None 158 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
57403704 75748 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922845 75748 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
58353266 117015 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237894 117015 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
122189720 130165 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616699 130165 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
145981450 173341 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 501 11 2 5 6.0 CCCCC(Oc1ncc(-c2cc(Cl)cc(Cl)c2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4279713 173341 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 501 11 2 5 6.0 CCCCC(Oc1ncc(-c2cc(Cl)cc(Cl)c2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
127047905 146544 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 613 7 1 5 7.8 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3798548 146544 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 613 7 1 5 7.8 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)C4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
127047122 146692 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
CHEMBL3799499 146692 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assayAntagonist activity at wild type human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation incubated for 30 mins by TR-FRET assay
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
11410779 195010 0 None 371 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL499372 195010 0 None 371 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
60170856 88169 0 None 128 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159341 88169 0 None 128 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
122189722 130168 0 None 295 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616701 130168 0 None 295 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
57401986 75685 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922708 75685 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10323446 140310 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 493 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(C1CCCCC1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL370847 140310 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 493 5 2 5 5.0 CC(C)(C)C1CCC2(CC1)CN(C1CCCCC1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
44561327 197233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL517861 197233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
164626834 193254 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876838 193254 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
16224191 75765 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922929 75765 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
11570626 9328 46 None -44 9 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat 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 rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None -44 9 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat 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 rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None -44 9 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat 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 rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None -44 9 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat 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 rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
11157621 75674 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922697 75674 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11284556 75690 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922713 75690 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
164624086 192482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865509 192482 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
58353901 117006 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1F)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237886 117006 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 507 7 2 4 4.8 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccccc1F)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
10481840 78827 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197642 78827 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1Cl)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
145967583 171731 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4225050 171731 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
58353025 117034 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 117034 0 None 8 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352954 117040 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237918 117040 0 None 1 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145968140 171870 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227111 171870 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
122189697 130142 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616676 130142 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
45381380 117049 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237927 117049 0 None 3 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
122189700 130145 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616679 130145 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
60170854 88161 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
CHEMBL2159334 88161 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
58352961 117007 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237887 117007 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
164616563 192185 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4861024 192185 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11952035 93592 0 None 10 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232239 93592 0 None 10 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11376210 190371 0 None 1737 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
CHEMBL480113 190371 0 None 1737 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
122189714 130159 0 None 301 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616693 130159 0 None 301 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
11570626 9328 46 None 3 9 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
9135 9328 46 None 3 9 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
CHEMBL1933349 9328 46 None 3 9 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
DB12044 9328 46 None 3 9 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
12967031 118349 0 None -2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1021/jm050563r
CHEMBL328126 118349 0 None -2 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against glucagon receptorAntagonist activity against glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1021/jm050563r
58353489 117008 0 None 12 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237888 117008 0 None 12 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
141465320 171944 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4228215 171944 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
164618212 192168 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4860642 192168 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP productionAntagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44561390 182815 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459032 182815 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
145982299 173273 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 525 13 2 6 6.5 CCCCC(Oc1ncc(-c2ccc(Oc3ccccc3)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4278513 173273 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 525 13 2 6 6.5 CCCCC(Oc1ncc(-c2ccc(Oc3ccccc3)cc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
141465346 171959 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4228470 171959 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
122189707 130152 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
CHEMBL3616686 130152 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
58353679 117035 0 None 2 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 117035 0 None 2 3 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11951857 103762 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL266489 103762 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulationAntagonist activity at human glucagon receptor transfected in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
71202679 117075 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238235 117075 0 None -5 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53466723 117081 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 677 9 2 5 7.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238242 117081 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 677 9 2 5 7.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145993424 174119 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4294427 174119 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10077102 78853 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 5 5.7 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL197718 78853 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 589 8 2 5 5.7 CC(C)(C)C1CCC2(CC1)C(=O)N(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2005.06.101
141465319 171922 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
CHEMBL4227906 171922 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assayAntagonist activity at human glucagon receptor expressed in HEK293T cells assessed as inhibition of glucagon-induced cAMP accumulation after 30 mins by HTRF assay
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
90655065 117082 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238243 117082 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10435562 78235 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 487 5 2 5 4.9 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL196193 78235 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 487 5 2 5 4.9 CC(C)(C)C1CCC2(CC1)CN(c1ccccc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
11169089 195075 0 None 676 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL500315 195075 0 None 676 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulationAntagonist activity against human GCGR expressed in CHO cells assessed as glucagon-induced cAMP accumulation
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
122189710 130155 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616689 130155 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP productionAntagonist activity against human glucagon receptor expressed in CHO cells assessed as reduction in glucagon-induced cAMP production
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170768 88156 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159329 88156 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counterAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
58353695 117036 0 None 7 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 117036 0 None 7 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assayAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-stimulated cAMP production preincubated for 30 mins followed by glucagon induction measured after 45 mins by LANCE assay
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9986018 140368 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371235 140368 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 599 7 2 6 5.8 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
10054055 79095 12 None 7 3 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL198387 79095 12 None 7 3 Human 7.0 pIC50 = 7.0 Functional
Inhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cellsInhibitory concentration against glucagon-induced cAMP accumulation in human glucagon receptor transfected CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)C1CCC2(CC1)CCN(c1ccc(OC(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
145986381 173877 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
CHEMBL4289916 173877 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assayAntagonist activity at human glucagon receptor expressed in CHO-K1 GCGR Gs cells assessed as inhibition of glucagon-induced cAMP accumulation pre-incubated for 10 mins before glucagon and forskolin addition and further incubated for 30 mins by luminescence-based assay
ChEMBL 433 11 2 5 4.7 CCCC[C@@H](Oc1ncc(-c2ccccc2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmc.2018.10.013
10052441 140408 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
CHEMBL371476 140408 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagonAntagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon
ChEMBL 521 5 2 5 5.5 CC(C)(C)C1CCC2(CC1)CN(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)Nc2nn[nH]n2)cc1 10.1016/j.bmcl.2005.06.101
57396139 75763 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922927 75763 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation countingAntagonist activity at human glucagon receptor expressed in CHO cells assessed as inhibition of forskolin/glucagon-induced cAMP production preincubated for 30 mins before glucagon challenge measured after 30 mins using [125I]-cAMP by liquid scintillation counting
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
11238073 75680 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922703 75680 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation countingAntagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced [125I]cAMP accumulation after 30 mins by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
134304209 176412 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(cnn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4437105 176412 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(cnn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1Cl 10.1016/j.bmcl.2019.05.036
134304141 181413 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4557989 181413 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
134304824 181477 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 510 9 2 3 7.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4559572 181477 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 510 9 2 3 7.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
155538812 180041 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 455 9 2 4 5.5 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccccc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4524978 180041 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 455 9 2 4 5.5 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccccc3)ccc21 10.1016/j.bmcl.2019.05.036
134304142 179596 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.8 CC(C)(C)c1ccc(-c2ccc3c(cnn3C(CC3CCCCC3)c3ccc(C(=O)NCCC(=O)O)cc3)c2)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4513964 179596 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.8 CC(C)(C)c1ccc(-c2ccc3c(cnn3C(CC3CCCCC3)c3ccc(C(=O)NCCC(=O)O)cc3)c2)cc1 10.1016/j.bmcl.2019.05.036
134304160 178363 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
CHEMBL4465107 178363 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2C(CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.05.036
134304713 182237 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 522 9 2 3 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4576987 182237 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 522 9 2 3 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ccc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304136 177500 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4452109 177500 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134309610 178835 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4471941 178835 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
155515237 176715 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 553 10 2 6 5.3 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCN(C)CC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4441433 176715 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 553 10 2 6 5.3 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCN(C)CC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304208 181501 0 None - 0 Human 5.9 pKi = 5.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4560114 181501 0 None - 0 Human 5.9 pKi = 5.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
155526074 177824 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 9 2 4 7.1 Cc1cc(-c2ccc(C(C)(C)C)cc2)cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc12 10.1016/j.bmcl.2019.05.036
CHEMBL4456905 177824 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 9 2 4 7.1 Cc1cc(-c2ccc(C(C)(C)C)cc2)cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc12 10.1016/j.bmcl.2019.05.036
155539799 179661 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 505 9 2 4 6.7 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cccc4ccccc34)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4515516 179661 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 505 9 2 4 6.7 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cccc4ccccc34)ccc21 10.1016/j.bmcl.2019.05.036
134304129 179584 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.126668
CHEMBL4513792 179584 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.126668
134304077 181806 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 10 2 4 7.2 CC(C)CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4567337 181806 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 10 2 4 7.2 CC(C)CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304151 176293 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc2n1 10.1016/j.bmcl.2019.05.036
CHEMBL4434750 176293 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc2n1 10.1016/j.bmcl.2019.05.036
155558364 181516 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.9 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cc(Cl)cc(Cl)c3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4560433 181516 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.9 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3cc(Cl)cc(Cl)c3)ccc21 10.1016/j.bmcl.2019.05.036
134304194 181448 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 558 9 2 5 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)nc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4558907 181448 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 558 9 2 5 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)nc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
134304075 177463 0 None - 0 Human 5.7 pKi = 5.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4451707 177463 0 None - 0 Human 5.7 pKi = 5.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
155515554 176756 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4441980 176756 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1Cl 10.1016/j.bmcl.2019.05.036
155530534 178339 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 12 2 4 7.8 CCCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4464664 178339 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 12 2 4 7.8 CCCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304091 178692 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4469925 178692 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
134304088 178282 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4463908 178282 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 567 10 2 5 6.9 COc1c(-c2ccc(C(F)(F)F)cc2C)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
134304234 178846 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1C 10.1016/j.bmcl.2019.126668
CHEMBL4472098 178846 0 None - 0 Human 7.7 pKi = 7.7 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc2c1C 10.1016/j.bmcl.2019.126668
134304087 182477 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4582082 182477 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304177 182793 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1C 10.1016/j.bmcl.2019.126668
CHEMBL4589676 182793 0 None - 0 Human 7.6 pKi = 7.6 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1C 10.1016/j.bmcl.2019.126668
155517246 176940 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 11 2 4 7.4 CCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4444404 176940 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 525 11 2 4 7.4 CCCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134309610 178835 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4471941 178835 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 523 9 2 4 6.6 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304232 179315 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 469 7 2 4 5.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4483722 179315 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 469 7 2 4 5.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
155541176 179761 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 10 2 5 6.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(OC(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4517914 179761 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 539 10 2 5 6.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(OC(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304074 176964 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4444819 176964 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.05.036
134304171 181803 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4567272 181803 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
155528087 178044 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 540 10 2 6 5.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCOCC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4460356 178044 0 None - 0 Human 5.5 pKi = 5.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 540 10 2 6 5.4 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(N4CCOCC4)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304192 181428 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 552 9 2 5 6.6 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)c2cc1C 10.1016/j.bmcl.2019.05.036
CHEMBL4558340 181428 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 552 9 2 5 6.6 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)c2cc1C 10.1016/j.bmcl.2019.05.036
134304119 178605 9 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1cc2c(cnn2[C@@H](CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1-c1ccc(C(F)(F)F)cc1Cl 10.1016/j.bmcl.2019.126668
CHEMBL4468579 178605 9 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1cc2c(cnn2[C@@H](CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1-c1ccc(C(F)(F)F)cc1Cl 10.1016/j.bmcl.2019.126668
134304096 176953 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4444605 176953 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304090 178087 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
CHEMBL4460982 178087 0 None - 0 Human 7.5 pKi = 7.5 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 587 10 2 5 7.2 COc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn([C@H](CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)cc12 10.1016/j.bmcl.2019.126668
134304131 176361 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.05.036
CHEMBL4436021 176361 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 551 9 2 4 7.2 Cc1cc(C(F)(F)F)ccc1-c1cc2cnn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)c2cc1C 10.1016/j.bmcl.2019.05.036
134304190 180523 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
CHEMBL4536588 180523 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 571 9 2 4 7.5 Cc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2c1cnn2[C@@H](CC(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2019.126668
134304219 180679 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1Cl 10.1016/j.bmcl.2019.05.036
CHEMBL4540172 180679 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 571 9 2 4 7.5 Cc1cc(C(F)(F)F)ccc1-c1cc2cn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)cc3)nc2cc1Cl 10.1016/j.bmcl.2019.05.036
155536703 178979 0 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4473724 178979 0 None - 0 Human 6.3 pKi = 6.3 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
134304173 177796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 602 11 2 6 7.0 CCOc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)cc12 10.1016/j.bmcl.2019.05.036
CHEMBL4456601 177796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 602 11 2 6 7.0 CCOc1c(-c2ccc(C(F)(F)F)cc2Cl)ccc2nn(C(CC(C)C)c3ccc(C(=O)NCCC(=O)O)nc3)cc12 10.1016/j.bmcl.2019.05.036
134304191 176614 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 497 9 2 4 6.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4439846 176614 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 497 9 2 4 6.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(C)(C)C)cc3)ccc21 10.1016/j.bmcl.2019.05.036
134304793 182596 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 568 9 2 3 7.9 Cc1cc(C(F)(F)F)ccc1-c1cc(F)c2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1C 10.1016/j.bmcl.2019.05.036
CHEMBL4584712 182596 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 568 9 2 3 7.9 Cc1cc(C(F)(F)F)ccc1-c1cc(F)c2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1C 10.1016/j.bmcl.2019.05.036
155555973 181247 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 506 9 2 5 6.1 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc4ncccc4c3)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4554170 181247 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 506 9 2 5 6.1 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc4ncccc4c3)ccc21 10.1016/j.bmcl.2019.05.036
134304822 177259 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 536 9 2 3 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.05.036
CHEMBL4449022 177259 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 536 9 2 3 7.5 Cc1cc(C(F)(F)F)ccc1-c1ccc2c(ccn2C(CC(C)C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmcl.2019.05.036
134304145 179199 0 None - 0 Human 7.1 pKi = 7.1 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4476825 179199 0 None - 0 Human 7.1 pKi = 7.1 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 557 9 2 4 7.2 CC(C)C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.126668
134304181 176982 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2019.05.036
CHEMBL4445178 176982 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 511 9 2 4 6.8 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc2cc(-c3ccc(C(C)(C)C)cc3)ccc2n1 10.1016/j.bmcl.2019.05.036
134304147 178933 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
CHEMBL4473209 178933 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assayAntagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE assay
ChEMBL 557 9 2 4 7.2 CC(C)CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3Cl)ccc21 10.1016/j.bmcl.2019.05.036
155549801 180698 0 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
CHEMBL4540602 180698 0 None - 0 Human 7.0 pKi = 7.0 Functional
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assayInhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay
ChEMBL 523 9 2 4 6.6 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1ncc2cc(-c3ccc(C(F)(F)F)cc3)ccc21 10.1016/j.bmcl.2019.126668
1150 8169 0 None - 1 Rat 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 2560175
1150 8169 0 None - 1 Rat 7.2 pA2 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 3035568
126961379 224531 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
CHEMBL4297741 224531 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
DB15226 224531 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central 3380 109 52 49 -14.7 C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC3=CC=C(C=C3)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC5=CNC6=CC=CC=C65)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H]([C@@H](C)O)C(=O)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC7=CNC=N7)N)O None
102331734 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
1136 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16132283 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
16133817 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
2994 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
3785 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
44278361 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
77077981 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
CHEMBL266481 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
DB00040 8595 36 None -1 6 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central None None None None None
13383 10484 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
168429725 10484 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
CHEMBL5314776 10484 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
DB18989 10484 0 None -1 3 Human 9.3 pEC50 = 9.3 Functional
Determined using a cAMP assay in CHO-K1 cells expressing hGCGRDetermined using a cAMP assay in CHO-K1 cells expressing hGCGR
Guide to Pharmacology None None None CC[C@H](C)[C@@H](C(=O)N[C@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)[C@@H](CO)NC(=O)CNC(=O)CCC(C(=O)O)NC(=O)CCCCCCCCCCCCCCCCC(=O)O)C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CO)C(=O)N[C@H](C)C(=O)N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CC=C(C=C5)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)[C@H]([C@@H](C)O)NC(=O)CNC(=O)[C@H](CCC(=O)N)NC(=O)C7(CCC7)NC(=O)[C@H](CC8=CNC=N8)N 36356832
102331734 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
1136 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
16132283 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
16133817 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
2994 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
3785 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
44278361 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
77077981 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
CHEMBL266481 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
DB00040 8595 36 None -1 6 Human 9.0 pEC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 4305077
1147 8597 0 None - 1 Rat 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 216670
194323 8597 0 None - 1 Rat 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 216670
CHEMBL749 8597 0 None - 1 Rat 4.0 pEC50 None 4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 216670
1146 8596 0 None - 1 Rat 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 210180
155817398 8596 0 None - 1 Rat 6.0 pEC50 None 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 210180
102331734 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
1136 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
16132283 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
16133817 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
2994 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
3785 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
44278361 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
77077981 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
CHEMBL266481 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
DB00040 8595 36 None -26 6 Rat 8.1 pIC50 = 8.1 Functional
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
Drug Central None None None None None
23549991 9615 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 573 8 3 7 5.1 O=C(N(c1ccc(cc1)C1CCCCC1)Cc1ccc(cc1)C(=O)Nc1n[nH]nn1)Nc1cccc(c1)S(=O)(=O)C 28514451
9574 9615 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 573 8 3 7 5.1 O=C(N(c1ccc(cc1)C1CCCCC1)Cc1ccc(cc1)C(=O)Nc1n[nH]nn1)Nc1cccc(c1)S(=O)(=O)C 28514451
9760 9619 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29300013
11570626 9328 46 None 3 9 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
9135 9328 46 None 3 9 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
CHEMBL1933349 9328 46 None 3 9 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
DB12044 9328 46 None 3 9 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 22708876
3505 8993 45 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
5311276 8993 45 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
CHEMBL351772 8993 45 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10085108
13314 10192 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 702 11 3 4 8.8 CC1=CC(=C(C(=C1)C)C2=CC=C(C=C2)NC(=O)[C@H](CC3=CC=C(C=C3)C(=O)NCCS(=O)(=O)O)C4=CC=C(C=C4)C5=CC=C(C=C5)C(C)(C)C)C None
1148 8705 34 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
619101 8705 34 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
CHEMBL179281 8705 34 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15561959
1148 8705 34 None - 1 Human 7.5 pIC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396
619101 8705 34 None - 1 Human 7.5 pIC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396
CHEMBL179281 8705 34 None - 1 Human 7.5 pIC50 None 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 15713396
1151 8170 0 None - 1 Rat 8.7 pIC50 None 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11532074




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
102331734 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
1136 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
16132283 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
16133817 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
2994 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
3785 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
44278361 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
77077981 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
CHEMBL266481 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
DB00040 8595 36 None - 1 Mouse 9.5 pEC50 = 9.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL None None None None 10.1016/j.ejmech.2020.112496
CHEMBL5288119 201186 0 None - 0 Mouse 9.3 pEC50 = 9.3 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4146 133 61 61 -21.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5268054 200327 0 None - 0 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4249 136 63 63 -21.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5282576 200940 0 None - 0 Mouse 9.2 pEC50 = 9.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4107 132 61 61 -19.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NCC(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(N)=O)[C@@H](C)O 10.1016/j.ejmech.2020.112496
CHEMBL5266722 200268 0 None - 0 Mouse 9.0 pEC50 = 9.0 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4472 152 70 64 -21.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5275572 200641 0 None - 0 Mouse 8.8 pEC50 = 8.8 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4473 152 70 64 -21.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5287118 201153 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 151 72 64 -23.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL427644 220139 0 None - 0 Rat 6.5 pEC50 = 6.5 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]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 10.1021/jm990559d
CHEMBL5314341 222486 0 None - 0 Rat 8.3 pEC50 = 8.3 Binding
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
ChEMBL None None None None 10.1021/jm990559d
CHEMBL5285379 201075 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4444 148 72 64 -24.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
168299178 199485 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4446 149 73 65 -26.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5219598 199485 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4446 149 73 65 -26.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL5277323 200710 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4486 150 72 64 -24.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
CHEMBL266411 217461 0 None - 0 Rat 6.1 pEC50 = 6.1 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]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 10.1021/jm990559d
CHEMBL5272283 200494 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulationAgonist activity at mouse GCGR expressed in CHO cells assessed as increase in cAMP accumulation
ChEMBL 4514 154 70 64 -21.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)Cc1c[nH]cn1)[C@@H](C)O)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.ejmech.2020.112496
129010858 157653 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 614 11 2 5 8.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3957356 157653 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 614 11 2 5 8.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
129010857 150191 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 594 11 2 5 7.9 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(C)cc12 nan
CHEMBL3898076 150191 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 594 11 2 5 7.9 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(OC(F)(F)F)cc1)c1csc2c(C#N)cc(C)cc12 nan
129010859 152820 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 618 10 2 4 8.5 N#Cc1cc(Cl)cc2c(C(c3ccc(Cl)cc3)[C@H](CCC(F)(F)F)c3ccc(C(=O)NCCC(=O)O)cc3)csc12 nan
CHEMBL3918808 152820 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 618 10 2 4 8.5 N#Cc1cc(Cl)cc2c(C(c3ccc(Cl)cc3)[C@H](CCC(F)(F)F)c3ccc(C(=O)NCCC(=O)O)cc3)csc12 nan
CHEMBL428460 220225 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]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 10.1021/jm010091q
91755011 130264 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysisDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
CHEMBL3617565 130264 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysisDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis
ChEMBL 590 11 3 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(OC(F)(F)F)cc1)c1c[nH]c2c(F)cc(Cl)cc12 10.1016/j.bmcl.2015.07.092
CHEMBL412488 219775 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]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 10.1021/jm010091q
129010860 150929 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 11 2 4 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3903921 150929 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 11 2 4 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
9955419 52062 5 None - 1 Rat 9.4 pIC50 = 9.4 Binding
In vitro binding affinity towards rat glucagon receptorIn vitro binding affinity towards rat glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL152640 52062 5 None - 1 Rat 9.4 pIC50 = 9.4 Binding
In vitro binding affinity towards rat glucagon receptorIn vitro binding affinity towards rat glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
11950794 168010 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411831 168010 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11950972 168011 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411832 168011 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
129010856 150271 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)c(Cl)c1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3898694 150271 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)c(Cl)c1)c1csc2c(C#N)cc(Cl)cc12 nan
122189714 130159 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616693 130159 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 713 13 2 6 9.3 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
129010861 159699 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL3974805 159699 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.2 CC(C)C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
11376210 190371 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
CHEMBL480113 190371 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
11410779 195010 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL499372 195010 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 592 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCc3ccccc3)ccc21 10.1016/j.bmcl.2008.05.072
11169089 195075 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL500315 195075 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 570 8 2 8 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
122189577 130125 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616588 130125 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
10073574 52201 0 None - 0 Rat 9.0 pIC50 = 9 Binding
In vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL152765 52201 0 None - 0 Rat 9.0 pIC50 = 9 Binding
In vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against rat glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
11952035 93592 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232239 93592 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
129010853 155465 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 548 10 2 4 7.5 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(F)cc12 nan
CHEMBL3939861 155465 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 548 10 2 4 7.5 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(F)cc12 nan
129010854 153735 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 544 10 2 4 7.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C)cc12 nan
CHEMBL3926079 153735 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 544 10 2 4 7.7 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C)cc12 nan
11331120 75737 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922834 75737 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL5314341 222486 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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
ChEMBL None None None None 10.1021/jm960800d
CHEMBL5314341 222486 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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
ChEMBL None None None None 10.1016/0960-894X(95)00307-F
122189710 130155 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616689 130155 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 13 2 6 9.1 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(SC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189713 130158 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616692 130158 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 677 13 2 6 8.5 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL5314341 222486 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None None 10.1021/jm010091q
CHEMBL5314341 222486 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
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
ChEMBL None None None None 10.1021/jm990559d
CHEMBL429362 220304 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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 10.1021/jm960130b
CHEMBL5314341 222486 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
inhibition of [125]glucagon specific binding.inhibition of [125]glucagon specific binding.
ChEMBL None None None None 10.1021/jm000453e
122189715 130160 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616694 130160 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 697 12 2 5 9.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
129010855 158398 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C(F)(F)F)cc12 nan
CHEMBL3963664 158398 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 598 10 2 4 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(C(F)(F)F)cc12 nan
57401986 75685 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922708 75685 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 9 2 8 6.3 CCCCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL439885 220629 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H]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 10.1021/jm010091q
129010864 155888 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1sc2ccccc2c1C nan
CHEMBL3943204 155888 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1sc2ccccc2c1C nan
11950075 93589 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232224 93589 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 588 9 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
60171059 88177 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159349 88177 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 621 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(C(F)(F)F)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
122189708 130153 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616687 130153 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 13 2 6 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
44372948 58780 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 58780 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819146 117103 9 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 117103 9 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10483282 192552 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 577 8 4 4 5.8 Cc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL486651 192552 0 None - 0 Human 8.0 pIC50 = 8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 577 8 4 4 5.8 Cc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc(C(F)(F)F)c1 10.1021/jm7015599
54765285 75770 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922933 75770 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 13 2 4 8.1 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57403109 75773 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922936 75773 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 13 2 4 7.6 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
58353126 117056 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 117056 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11329242 195861 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 3 6 5.2 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2008.05.072
CHEMBL509900 195861 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 3 6 5.2 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)nc2c1 10.1016/j.bmcl.2008.05.072
122189569 130117 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616580 130117 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(OC)cc3)ccc21 10.1016/j.bmcl.2015.08.015
122189694 130139 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616673 130139 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)ccc2Cl)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
44431020 174418 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL430163 174418 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 573 7 3 3 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL3037804 217700 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](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 10.1021/jm960130b
11027864 53429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 533 10 2 6 4.3 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL153879 53429 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 533 10 2 6 4.3 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
11585375 88166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159339 88166 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 625 8 2 4 8.5 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(C(F)(F)F)ccc2c1 10.1021/jm300579z
44372720 55349 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 55349 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372477 60977 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160735 60977 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL2369990 216545 0 None - 1 Rat 7.0 pIC50 = 7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
58352803 117059 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 117059 0 None - 0 Mouse 7.0 pIC50 = 7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
141465324 171891 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227372 171891 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1cccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1 10.1016/j.bmc.2018.02.036
10215420 105276 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL276063 105276 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319617 113335 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL314181 113335 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
10592750 113930 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL316264 113930 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319245 212731 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 390 3 2 2 5.9 Oc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccccc2)cc1 10.1007/s00044-013-0869-9
CHEMBL84373 212731 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 390 3 2 2 5.9 Oc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccccc2)cc1 10.1007/s00044-013-0869-9
60170854 88161 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
CHEMBL2159334 88161 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 9 2 5 7.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(OC(F)(F)F)cc1 10.1021/jm300579z
44372700 175389 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL436022 175389 0 None - 0 Human 6.0 pIC50 = 6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
135819143 16750 7 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114799 16750 7 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
135819146 117103 9 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 117103 9 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL427744 220149 0 None - 1 Rat 6.0 pIC50 = 6 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
44372471 55335 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 55335 0 None - 0 Mouse 6.0 pIC50 = 6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
56602994 133857 0 None - 0 Human 6.0 pIC50 = 6 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 593 11 2 4 7.2 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)=NC1(C)C nan
CHEMBL3656296 133857 0 None - 0 Human 6.0 pIC50 = 6 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 593 11 2 4 7.2 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(-c3cc(Cl)cc(Cl)c3)cc2)=NC1(C)C nan
16100338 148540 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 603 7 2 4 7.2 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)N3CCCC(C(=O)O)C3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL386030 148540 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 603 7 2 4 7.2 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)N3CCCC(C(=O)O)C3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
22005339 38516 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.2 CC(C)CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140586 38516 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.2 CC(C)CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004918 42044 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 315 5 1 2 5.2 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL143609 42044 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 315 5 1 2 5.2 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004877 103251 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 353 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(C)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL26238 103251 0 None - 0 Human 6.0 pIC50 = 6 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 353 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(C)cc1 10.1016/s0960-894x(02)00143-9
10980170 11576 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 4 2 5 2.7 COc1cc(C(=O)N/N=C/c2ccnc3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104137 11576 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 4 2 5 2.7 COc1cc(C(=O)N/N=C/c2ccnc3ccccc23)ccc1O 10.1021/jm000547o
44319276 212888 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85741 212888 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL437471 220503 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
58352836 117005 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237885 117005 0 None - 0 Mouse 5.0 pIC50 = 5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(C(F)(F)F)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
11632336 120758 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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
ChEMBL 381 4 3 6 2.9 Cc1cccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326180 120758 0 None - 0 Rat 4.0 pIC50 = 4 Binding
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
ChEMBL 381 4 3 6 2.9 Cc1cccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)c1 10.1016/j.bmcl.2014.07.025
CHEMBL441011 220657 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](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 10.1021/jm010091q
16100297 143717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 504 8 3 4 5.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2)CC1 10.1021/jm058026u
CHEMBL374293 143717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 504 8 3 4 5.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2)CC1 10.1021/jm058026u
164626834 193254 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876838 193254 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3015 98 46 43 -12.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11952211 94726 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL234087 94726 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
16100327 143987 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 479 8 3 3 5.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccccc2)CC1 10.1021/jm058026u
CHEMBL374994 143987 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 479 8 3 3 5.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccccc2)CC1 10.1021/jm058026u
11599295 190580 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL480501 190580 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 554 6 2 7 6.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2008.05.072
11365464 75684 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922707 75684 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 5.5 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
10951864 51564 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 560 6 2 5 5.6 O=C(N/N=C/c1ccc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152184 51564 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 560 6 2 5 5.6 O=C(N/N=C/c1ccc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10974243 53946 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 635 7 3 6 5.6 O=C(N/N=C/c1ccc(OCC(=O)N2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154316 53946 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 635 7 3 6 5.6 O=C(N/N=C/c1ccc(OCC(=O)N2CCC(O)(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10434112 58306 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 454 5 2 5 4.1 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL158295 58306 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 454 5 2 5 4.1 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
129010862 155213 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 3 8.8 CCC[C@H](c1ccc(C(=O)NCC(F)(F)C(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL3937819 155213 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 3 8.8 CCC[C@H](c1ccc(C(=O)NCC(F)(F)C(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
44319474 113830 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315613 113830 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10363819 113854 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
CHEMBL315828 113854 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
9906120 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
CHEMBL25637 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
44372478 58629 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 58629 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL5277926 200737 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysisDisplacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysis
ChEMBL 342 6 1 1 6.7 CCCc1c(C(C)C)cc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/j.ejmech.2018.04.061
45381381 117054 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 117054 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
71243036 117055 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 117055 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
16225177 75759 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922923 75759 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2011.09.105
145969298 171880 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227229 171880 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ccccc2c1 10.1016/j.bmc.2018.02.036
11387112 75688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922711 75688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 538 6 2 7 4.7 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189697 130142 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616676 130142 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccncc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
44373547 59207 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 466 9 2 6 5.0 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL159071 59207 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 466 9 2 6 5.0 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
9906120 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL25637 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
9906120 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL25637 102061 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
44318988 212786 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL84917 212786 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
19072340 55337 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155687 55337 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
135819149 17223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 17223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
44319258 212768 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84759 212768 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1016/s0960-894x(01)00498-x
71203427 117041 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237919 117041 0 None - 0 Mouse 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353778 117024 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237903 117024 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10416258 63706 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644190 63706 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
53321835 63717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644201 63717 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
53319214 63719 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644203 63719 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 11 2 6 6.7 O=C(O)CCCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
56602866 133843 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 597 10 2 6 6.4 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
CHEMBL3656282 133843 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 597 10 2 6 6.4 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
22005341 106750 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(F)c1 10.1016/s0960-894x(02)00143-9
CHEMBL286555 106750 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(F)c1 10.1016/s0960-894x(02)00143-9
20647512 100856 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1F 10.1016/s0960-894x(02)00143-9
CHEMBL24905 100856 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 375 8 1 2 6.5 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1F 10.1016/s0960-894x(02)00143-9
127047121 146742 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
CHEMBL3799820 146742 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 519 7 2 4 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1 10.1016/j.bmc.2016.04.053
CHEMBL412352 219764 0 None - 1 Rat 7.0 pIC50 = 7.0 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
164620673 192797 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870505 192797 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 97 45 41 -11.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(C)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372720 55349 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL155694 55349 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
44418929 89371 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 582 10 2 4 7.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)c2csc3ccc(Cl)cc23)C(c2ccccc2)c2ccccc2)cc1 10.1021/jm058026u
CHEMBL217901 89371 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 582 10 2 4 7.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)c2csc3ccc(Cl)cc23)C(c2ccccc2)c2ccccc2)cc1 10.1021/jm058026u
9841863 66832 26 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL17370 66832 26 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
22496412 179483 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 593 10 2 5 8.6 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C4=CCCCC4)cc3)n2)cc1 10.1021/jm8016249
CHEMBL450411 179483 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 593 10 2 5 8.6 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C4=CCCCC4)cc3)n2)cc1 10.1021/jm8016249
44389598 71646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 71646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
42617999 195154 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 624 10 3 6 6.3 O=C(NC[C@@H](O)C(=O)O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501392 195154 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 624 10 3 6 6.3 O=C(NC[C@@H](O)C(=O)O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22496557 200040 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL523847 200040 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
135819133 121191 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 121191 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10257357 148616 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL386446 148616 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
16225179 75762 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922926 75762 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 618 11 2 4 8.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57401359 75777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922940 75777 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 592 13 2 4 7.8 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11284556 75690 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922713 75690 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 572 7 2 9 4.6 COc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189578 130126 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616589 130126 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 699 12 2 6 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC(F)(F)F)cc3)nc21 10.1016/j.bmcl.2015.08.015
11082135 126389 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccc(F)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346464 126389 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccc(F)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164617806 191461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4849980 191461 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2984 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164625627 192564 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3389 111 53 50 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4866685 192564 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3389 111 53 50 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
71456151 85214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1cccc2c(OCc3ccc(OC(F)(F)F)cc3)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111565 85214 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1cccc2c(OCc3ccc(OC(F)(F)F)cc3)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44319713 113945 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL316361 113945 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
16224190 75760 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 544 11 2 4 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(C)cc(C)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922924 75760 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 544 11 2 4 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cc(C)cc(C)c1 10.1016/j.bmcl.2011.09.105
58353839 117078 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
CHEMBL3238238 117078 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
10324097 63636 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643955 63636 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
10461010 63702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644186 63702 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 8 2 7 5.9 O=C(NCc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11786041 196419 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 540 7 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2C2CCCC2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL515045 196419 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 540 7 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2C2CCCC2)CC1 10.1016/j.bmcl.2008.05.072
11145271 171543 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 479 8 2 6 4.3 COc1cc(OCCN2CCc3ccccc3C2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL421795 171543 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 479 8 2 6 4.3 COc1cc(OCCN2CCc3ccccc3C2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL328942 218095 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL 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 10.1021/jm960130b
44361298 128269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL358250 128269 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
11024350 213195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 343 5 1 2 5.1 Fc1ccc(-c2[nH]c(CCc3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87858 213195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 343 5 1 2 5.1 Fc1ccc(-c2[nH]c(CCc3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
135542439 12244 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 306 3 3 4 3.0 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
CHEMBL107526 12244 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 306 3 3 4 3.0 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
44372948 58780 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 58780 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353013 117016 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237895 117016 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11756248 63689 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644173 63689 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
10415955 63710 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644194 63710 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
22999282 60584 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 6 3 5 2.8 NC(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL160419 60584 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 6 3 5 2.8 NC(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL268534 217535 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H]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 10.1021/jm990559d
11760806 11868 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 5 2 5 4.4 COc1cc(C(=O)N/N=C/c2ccc(-c3ccc(C)c(Cl)c3)o2)ccc1O 10.1021/jm000547o
CHEMBL105565 11868 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 5 2 5 4.4 COc1cc(C(=O)N/N=C/c2ccc(-c3ccc(C)c(Cl)c3)o2)ccc1O 10.1021/jm000547o
16100312 143988 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 6 4.5 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC3(CC2)OCCO3)cc1 10.1021/jm058026u
CHEMBL375000 143988 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 6 4.5 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC3(CC2)OCCO3)cc1 10.1021/jm058026u
11650288 88160 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
CHEMBL2159333 88160 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cccc(OC(F)(F)F)c3c2)cc1 10.1021/jm300579z
16100311 143197 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.2 CCCC1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL373542 143197 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.2 CCCC1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
10257357 148616 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat glucagon receptorInhibition of rat glucagon receptor
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm058026u
CHEMBL386446 148616 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat glucagon receptorInhibition of rat glucagon receptor
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm058026u
73355439 99359 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 0 3 5.7 CSc1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
CHEMBL2435137 99359 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 0 3 5.7 CSc1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
CHEMBL437095 220485 0 None - 1 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
127047256 146549 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798581 146549 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 595 8 2 4 7.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(-c2ccccc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL429198 220291 0 None - 1 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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 10.1021/jm960800d
10413333 69793 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
CHEMBL178768 69793 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 491 8 1 4 7.1 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(Cc1ccc(Cl)cc1Cl)C(C)C)C2 10.1016/j.bmcl.2005.01.003
10282162 179200 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 599 9 4 4 6.2 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(F)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL447684 179200 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 599 9 4 4 6.2 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(F)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
44319713 113945 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL316361 113945 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1016/s0960-894x(01)00498-x
44319495 212892 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85807 212892 3 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353323 117061 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238221 117061 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353338 117062 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 117062 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 117063 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 117063 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11456034 176238 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 8 3 7 7.1 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)c3ccc(Oc4ccc(Cl)cc4)c(Cl)c3)nc2c1 10.1016/j.bmcl.2008.05.072
CHEMBL442855 176238 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 8 3 7 7.1 Cc1ccc2[nH]c(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)c3ccc(Oc4ccc(Cl)cc4)c(Cl)c3)nc2c1 10.1016/j.bmcl.2008.05.072
57391519 75679 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922702 75679 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 4.9 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
164620899 192472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3403 112 53 50 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865371 192472 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3403 112 53 50 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL442135 220687 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]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 10.1021/jm010091q
CHEMBL409654 219555 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None None 10.1021/jm010091q
10864173 56605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC(=O)N2CCc3ccccc3C2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156772 56605 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC(=O)N2CCc3ccccc3C2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164624163 192594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4867132 192594 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2970 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372870 60417 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 60417 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44318950 113783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315311 113783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
9843239 113850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315800 113850 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58353046 117058 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 117058 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469443 117084 1 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238246 117084 1 None - 1 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353156 117027 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 117027 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
51031037 117039 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 117039 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10077369 63704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644188 63704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 603 8 2 8 6.4 CC(c1ccc(C(=O)Nc2nn[nH]n2)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
9871912 199403 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 537 10 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccccc3)cs2)cc1 10.1021/jm8016249
CHEMBL521650 199403 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 537 10 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccccc3)cs2)cc1 10.1021/jm8016249
44431016 151022 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL390469 151022 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 574 8 2 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11102467 53887 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL154269 53887 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL429724 220323 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H]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 10.1021/jm990559d
9836535 168918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 315 3 1 2 4.9 Fc1ccc(-c2[nH]c(-c3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL416169 168918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 315 3 1 2 4.9 Fc1ccc(-c2[nH]c(-c3ccccc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372671 126895 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL351104 126895 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10246001 170285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL420232 170285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353544 117020 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 117020 0 None - 0 Mouse 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
56602934 133858 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 503 8 2 4 5.0 CC(C)[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656297 133858 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 503 8 2 4 5.0 CC(C)[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
44373635 60272 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 452 8 2 5 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160138 60272 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 452 8 2 5 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10215420 105276 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL276063 105276 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 345 4 1 3 5.0 COc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
22496546 195231 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 649 10 2 5 8.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL502694 195231 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 649 10 2 5 8.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)cs2)ccc1C(C)C 10.1021/jm8016249
44278220 175850 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
91931634 175850 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
CHEMBL439690 175850 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
10962393 57126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 521 10 3 6 5.0 COc1cc(OCCNCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL157226 57126 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 521 10 3 6 5.0 COc1cc(OCCNCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
164626335 193144 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875380 193144 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3141 102 49 45 -14.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CN)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
44372846 60363 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160238 60363 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
16100313 90028 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 591 13 3 4 7.4 CCCC1(CCC)CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL218740 90028 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 591 13 3 4 7.4 CCCC1(CCC)CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44389598 71646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
CHEMBL182148 71646 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 435 6 1 4 5.9 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)C1CCCc3ccccc31)C2 10.1016/j.bmcl.2005.01.003
10231964 192535 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NCC(O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL486634 192535 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NCC(O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10145603 195849 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 611 10 4 5 6.1 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL509710 195849 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 611 10 4 5 6.1 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
10280734 199261 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 547 9 4 4 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL520893 199261 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 547 9 4 4 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
58353046 117058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238218 117058 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 617 8 2 6 6.9 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44561584 193505 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 8 3 6 4.4 Cn1c(N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL488682 193505 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 8 3 6 4.4 Cn1c(N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57401963 75675 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922698 75675 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 8 2 8 6.1 CCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
57393252 75746 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922843 75746 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 632 8 2 8 6.2 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL413890 219876 23 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
10907780 126412 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 553 9 3 7 5.4 COc1cc(NC(=O)CSc2ccc(OC(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346694 126412 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 553 9 3 7 5.4 COc1cc(NC(=O)CSc2ccc(OC(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10951675 53507 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 541 9 3 5 6.4 O=C(N/N=C/c1ccc(OCCNCc2ccc(Cl)c(Cl)c2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL153950 53507 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 541 9 3 5 6.4 O=C(N/N=C/c1ccc(OCCNCc2ccc(Cl)c(Cl)c2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
60171060 88178 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159350 88178 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 583 10 2 6 6.9 COc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
44373083 59144 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 59144 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372701 59311 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159198 59311 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372397 60521 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160372 60521 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372688 56202 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 56202 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44318935 212810 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85102 212810 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353067 117057 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 117057 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71243097 117063 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238223 117063 0 None - 0 Mouse 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44373783 126963 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 438 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC2CCCCO2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
CHEMBL351724 126963 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 438 6 2 5 4.9 O=C(N/N=C/c1ccc(OCC2CCCCO2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
16100302 143195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2)CC1 10.1021/jm058026u
CHEMBL373541 143195 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 11 3 4 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2)CC1 10.1021/jm058026u
44318950 113783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL315311 113783 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
19072347 59285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159163 59285 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10030697 185853 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10318451 212855 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85534 212855 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
68864367 120750 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 416 4 3 4 4.5 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(F)c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326171 120750 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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
ChEMBL 416 4 3 4 4.5 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(F)c1 10.1016/j.bmcl.2014.07.025
22005335 101206 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL25115 101206 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
22005335 101206 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(02)00143-9
CHEMBL25115 101206 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 339 8 1 2 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(02)00143-9
12967031 118349 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL328126 118349 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
44418928 90131 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 523 13 3 4 5.8 CCCCC(CC)N(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm058026u
CHEMBL219308 90131 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 523 13 3 4 5.8 CCCCC(CC)N(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(OC(F)(F)F)cc1 10.1021/jm058026u
44372676 126414 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL346698 126414 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
3505 8993 45 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
5311276 8993 45 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
CHEMBL351772 8993 45 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1007/s00044-013-0801-3
127047122 146692 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
CHEMBL3799499 146692 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 533 7 2 4 6.6 Cc1ccccc1-c1cc(-c2cc(Cl)cc(Cl)c2)nn1C1CCc2cc(C(=O)NCCC(=O)O)ccc21 10.1016/j.bmc.2016.04.053
127047255 146800 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
CHEMBL3800146 146800 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 525 7 2 5 6.3 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccs1 10.1016/j.bmc.2016.04.053
164618212 192168 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4860642 192168 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3029 99 46 43 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CSCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11950794 168010 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411831 168010 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 599 6 3 6 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
71202713 117077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238237 117077 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL267876 217514 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
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)
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN=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 10.1021/jm000453e
45381380 117049 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237927 117049 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71202743 117064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3238224 117064 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)c1 10.1021/jm401858f
44561327 197233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL517861 197233 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 6 2 7 5.3 Cc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
122189705 130150 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616684 130150 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 598 9 2 6 7.0 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(C#N)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170968 88173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159345 88173 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 511 8 2 5 5.5 COc1ccc2cc(-c3cc(C(F)(F)F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
164616848 191728 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4853767 191728 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170768 88156 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159329 88156 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 573 9 2 5 6.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11733947 168544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 510 8 3 6 4.6 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL413964 168544 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 510 8 3 6 4.6 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
44318934 212775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84840 212775 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
44319495 212892 3 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85807 212892 3 None - 0 Human 6.8 pIC50 = 6.8 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
12967034 126802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 126802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373192 126514 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 126514 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353369 117028 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 117028 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
44373781 61715 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 476 8 2 6 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(F)c(F)c1 10.1016/s0960-894x(01)00819-8
CHEMBL161431 61715 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 476 8 2 6 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(F)c(F)c1 10.1016/s0960-894x(01)00819-8
44361158 127716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL356089 127716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c([C@@H](C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
10093802 113691 4 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL314701 113691 4 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
10318451 212855 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL85534 212855 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3cccc(Br)c3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
9998923 113683 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314652 113683 2 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352935 117018 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 117018 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353679 117035 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 117035 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
70900317 117042 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237920 117042 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44373553 60862 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 422 7 2 4 5.5 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cc2)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160652 60862 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 422 7 2 4 5.5 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cc2)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL2372773 217065 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H]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 10.1021/jm990559d
22496358 194098 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL493019 194098 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100304 90120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 641 9 3 4 7.2 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2Br)CC1 10.1021/jm058026u
CHEMBL219252 90120 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 641 9 3 4 7.2 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2Br)CC1 10.1021/jm058026u
10435275 130642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL362657 130642 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 479 8 1 4 6.7 CCC(CC)C(=O)Nc1sc(C(=O)N(Cc2ccc(Cl)cc2Cl)C(C)C)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
135819157 16742 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 16742 3 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
16100300 144017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL375167 144017 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
16225178 75751 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 586 12 2 4 7.7 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1Cc1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922915 75751 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 586 12 2 4 7.7 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1Cc1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
57397957 75769 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 598 12 2 4 7.7 CCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922932 75769 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 598 12 2 4 7.7 CCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57392671 75776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922939 75776 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 646 13 2 4 8.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(C(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
53469628 117074 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 117074 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11260553 182999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 5.4 CCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459458 182999 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 5.4 CCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11261540 195613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 562 8 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL506520 195613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 562 8 2 7 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2Cc2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
60170855 88162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159335 88162 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 599 11 2 5 7.8 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
11048232 57180 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 428 7 2 5 3.6 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL157280 57180 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 428 7 2 5 3.6 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
11585452 88165 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159338 88165 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 641 9 2 5 8.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
58353126 117056 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238216 117056 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 635 8 2 6 7.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
70900317 117042 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237920 117042 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
68862614 120753 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 466 4 3 4 5.4 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(C(F)(F)F)c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326174 120753 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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
ChEMBL 466 4 3 4 5.4 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(C(F)(F)F)c1 10.1016/j.bmcl.2014.07.025
44561557 185678 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 4.6 Cn1c(N(Cc2ccc(C(=O)NCc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL469904 185678 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 500 7 2 7 4.6 Cn1c(N(Cc2ccc(C(=O)NCc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11433550 75677 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922700 75677 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 9 2 9 5.3 COCCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
44373923 61725 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 478 6 2 7 5.2 CC(C)(C)c1nc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)no1 10.1016/s0960-894x(01)00819-8
CHEMBL161505 61725 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 478 6 2 7 5.2 CC(C)(C)c1nc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)no1 10.1016/s0960-894x(01)00819-8
9952509 213157 15 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87588 213157 15 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372577 60446 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 238 2 1 1 3.9 Fc1ccc(-c2cc[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160314 60446 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 238 2 1 1 3.9 Fc1ccc(-c2cc[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
9929037 60658 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160490 60658 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
10257629 194054 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
44372720 55349 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 55349 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
10255803 63692 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644176 63692 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
164629129 193256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876913 193256 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2997 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
71452715 85656 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 6 2 6 3.5 CC(C)S(=O)(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
CHEMBL2112904 85656 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 6 2 6 3.5 CC(C)S(=O)(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)c2ccccc12 10.1021/jm0208572
9914410 193236 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 513 9 4 4 5.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccccc2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487662 193236 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 513 9 4 4 5.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccccc2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
16100314 90231 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 544 10 3 5 6.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cccc([N+](=O)[O-])c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
CHEMBL219968 90231 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 544 10 3 5 6.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cccc([N+](=O)[O-])c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
44372847 60419 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160289 60419 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
12967035 58611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 58611 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
57397956 75757 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922921 75757 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
57396140 75771 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 12 2 4 8.0 CC(C)CC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922934 75771 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 612 12 2 4 8.0 CC(C)CC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
71243036 117055 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
CHEMBL3238215 117055 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 649 9 2 6 7.3 CC1(CC[C@H](c2ccc(C(=O)NCc3nn[nH]n3)cc2)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)CC1 10.1021/jm401858f
3505 8993 45 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 8993 45 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 8993 45 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
44372471 55335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 55335 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353338 117062 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238222 117062 0 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)c(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58352935 117018 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237897 117018 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 8 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2CCc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353695 117036 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 117036 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11785044 196445 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL515202 196445 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL328942 218095 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL 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 10.1021/jm960130b
10053886 198543 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
12967034 126802 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 126802 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58352925 117023 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237902 117023 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353369 117028 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
CHEMBL3237907 117028 0 None - 0 Mouse 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 517 7 2 4 5.5 Cc1cccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)C2=O)c1 10.1021/jm401858f
10436554 63639 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643958 63639 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
122189571 130119 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616582 130119 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(OC)cc3)c21 10.1016/j.bmcl.2015.08.015
56602932 133850 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 543 9 2 4 5.4 CC1(C2CCCCC2)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656289 133850 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 543 9 2 4 5.4 CC1(C2CCCCC2)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
56602931 133851 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 475 8 2 4 3.8 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656290 133851 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 475 8 2 4 3.8 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
56602995 133856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 501 8 2 4 4.7 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)C1CC1 nan
CHEMBL3656295 133856 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 501 8 2 4 4.7 CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)C1CC1 nan
16100319 90114 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 8 3 4 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL219191 90114 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 8 3 4 6.0 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
11559533 146952 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 359 7 0 3 4.9 O=C(c1ccc(OCCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
CHEMBL380387 146952 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 359 7 0 3 4.9 O=C(c1ccc(OCCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
16100336 90166 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 513 11 3 3 5.4 CCCCc1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
CHEMBL219446 90166 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 513 11 3 3 5.4 CCCCc1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
135819146 117103 9 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 117103 9 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10144633 179206 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 571 9 4 4 6.4 CC(C)(C)c1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
CHEMBL447742 179206 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 571 9 4 4 6.4 CC(C)(C)c1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
11157621 75674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922697 75674 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 7 2 8 5.7 CCn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11238073 75680 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922703 75680 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL439289 220613 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL None None None CN[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2005.01.003
44372948 58780 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 58780 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
145969968 171858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226972 171858 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 615 10 2 5 8.2 CCOc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
44373676 59230 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 524 9 2 7 5.3 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL159093 59230 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 524 9 2 7 5.3 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(OC(F)(F)F)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL328942 218095 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL 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 10.1021/jm960130b
44372406 126594 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL348401 126594 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
6862006 179099 12 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 290 3 2 3 3.3 O=C(N/N=C/c1cccc2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
CHEMBL447535 179099 12 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 290 3 2 3 3.3 O=C(N/N=C/c1cccc2ccccc12)c1ccc(O)cc1 10.1021/jm000547o
22496449 181216 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
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
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
22005118 38576 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 399 11 1 2 7.5 CCCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140636 38576 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 399 11 1 2 7.5 CCCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22005111 126211 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 297 5 1 2 5.1 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL344911 126211 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 297 5 1 2 5.1 CCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
44369318 51856 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 444 6 2 5 4.4 CC(C)CS(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL152461 51856 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 444 6 2 5 4.4 CC(C)CS(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
1148 8705 34 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
619101 8705 34 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
CHEMBL179281 8705 34 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 346 6 1 3 5.5 CCC(C(=O)Nc1sc2c(c1C#N)CCC(C2)C(CC)(C)C)CC 10.1016/j.bmcl.2005.01.003
127046644 146356 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3797325 146356 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 563 8 2 5 6.7 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(c2)CCO3)cc1 10.1016/j.bmc.2016.04.053
16100305 90103 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 617 11 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2C(F)(F)F)CC1 10.1021/jm058026u
CHEMBL219138 90103 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 617 11 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OCC3CC3)cc2C(F)(F)F)CC1 10.1021/jm058026u
164613898 191501 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4850520 191501 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2969 96 46 42 -13.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL442499 220693 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
57403704 75748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922845 75748 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 7 2 8 5.9 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11812426 85658 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 451 5 2 7 3.7 CN(C)c1ccc(C(=O)n2cc(/C=N/NC(=O)c3ccc(O)c(C#N)c3)c3ccccc32)cc1 10.1021/jm0208572
CHEMBL2112907 85658 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 451 5 2 7 3.7 CN(C)c1ccc(C(=O)n2cc(/C=N/NC(=O)c3ccc(O)c(C#N)c3)c3ccccc32)cc1 10.1021/jm0208572
10995358 51808 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 565 10 3 5 5.9 O=C(N/N=C/c1ccc(OCCNCCc2ccc(Br)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152409 51808 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 565 10 3 5 5.9 O=C(N/N=C/c1ccc(OCCNCCc2ccc(Br)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
135819137 99626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL24388 99626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
9929037 60658 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 60658 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
135819149 17223 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 17223 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
10338890 212801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85009 212801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58353838 117060 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238220 117060 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353544 117020 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237899 117020 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.4 CC(Cc1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
71203427 117041 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237919 117041 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 7 3 5 5.5 C[C@H](c1ccc(C(=O)NC[C@@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL266411 217461 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]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 10.1021/jm990559d
135819137 99626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
CHEMBL24388 99626 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 2 3 6.1 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00143-9
19072347 59285 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL159163 59285 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 329 3 2 2 5.1 Nc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44319442 213104 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 383 3 1 3 5.3 Fc1ccc(-c2[nH]c(-c3ccc(Br)o3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87248 213104 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 383 3 1 3 5.3 Fc1ccc(-c2[nH]c(-c3ccc(Br)o3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44373707 61724 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 483 10 2 5 5.7 COc1cc(CCNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL161494 61724 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 483 10 2 5 5.7 COc1cc(CCNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
22004948 100096 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 387 9 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(CO)c1 10.1016/s0960-894x(02)00143-9
CHEMBL24527 100096 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 387 9 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)c(CO)c1 10.1016/s0960-894x(02)00143-9
145968206 171971 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228703 171971 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 533 9 2 5 6.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
53469258 117072 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
CHEMBL3238232 117072 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 8 2 6 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC12CCCCC2 10.1021/jm401858f
16100310 85880 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 576 10 3 5 4.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCN(C(=O)C3CC3)CC2)cc1 10.1021/jm058026u
CHEMBL2113259 85880 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 576 10 3 5 4.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCN(C(=O)C3CC3)CC2)cc1 10.1021/jm058026u
44561440 179368 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL448921 179368 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 584 9 2 8 6.5 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(OCC3CCCC3)ccc21 10.1016/j.bmcl.2008.05.072
44561391 182441 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 502 6 3 8 4.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(O)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL458145 182441 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 502 6 3 8 4.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(O)ccc21 10.1016/j.bmcl.2008.05.072
11249762 190620 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL480692 190620 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 544 9 2 8 5.7 CCCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
44561439 197980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL518939 197980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 530 8 2 8 5.3 CCOc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
122189573 130121 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616584 130121 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189696 130141 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616675 130141 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 650 10 3 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
129010852 149563 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2ccccc12 nan
CHEMBL3892787 149563 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 519 10 2 3 7.8 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2ccccc12 nan
11444850 75742 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922839 75742 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 606 8 2 8 6.1 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
9955419 52062 5 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against human glucagon receptorAntagonist activity against human glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1016/j.bmcl.2014.07.025
CHEMBL152640 52062 5 None - 1 Human 8.6 pIC50 = 8.6 Binding
Antagonist activity against human glucagon receptorAntagonist activity against human glucagon receptor
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1016/j.bmcl.2014.07.025
46853083 167101 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 593 8 2 5 8.1 CCC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL4110618 167101 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 593 8 2 5 8.1 CCC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
9955419 52062 5 None - 1 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL152640 52062 5 None - 1 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 450 5 2 5 5.3 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(C#N)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL413666 219859 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](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 10.1021/jm960130b
11952035 158249 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL396215 158249 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
46853084 166635 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 607 9 2 5 7.8 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL4106672 166635 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 607 9 2 5 7.8 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
57518490 88164 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
CHEMBL2159337 88164 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 641 9 2 5 8.4 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(OC(F)(F)F)ccc2c1 10.1021/jm300579z
122189709 130154 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616688 130154 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 643 12 2 5 8.7 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189722 130168 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616701 130168 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 601 9 2 5 7.5 COc1ccc(C(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
11273570 75691 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922714 75691 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 620 8 2 9 5.3 CCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11038653 51874 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 522 6 2 6 5.4 N#Cc1cc(C(=O)N/N=C/c2ccc(N(C(=O)C3CCCC3)C(=O)C3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL152477 51874 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 522 6 2 6 5.4 N#Cc1cc(C(=O)N/N=C/c2ccc(N(C(=O)C3CCCC3)C(=O)C3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
44373213 126615 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 126615 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819157 16742 3 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 16742 3 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
11570626 9328 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
9135 9328 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
CHEMBL1933349 9328 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
DB12044 9328 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmc.2018.02.036
10073574 52201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1021/jm0208572
CHEMBL152765 52201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1021/jm0208572
10073574 52201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL152765 52201 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 473 9 2 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44319258 212768 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1007/s00044-013-0869-9
CHEMBL84759 212768 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cnccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccc(F)cc1 10.1007/s00044-013-0869-9
CHEMBL439271 220608 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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 10.1021/jm960800d
44373192 126514 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 126514 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
12967031 118349 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL328126 118349 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
135503676 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
CHEMBL107070 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagonBinding affinity towards human Glucagon Receptor by the displacement of [125I]-glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
58352937 117069 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 117069 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
141465320 171944 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4228215 171944 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 521 8 2 4 6.6 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1 10.1016/j.bmc.2018.02.036
11068219 56453 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1cccc2c(CO)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156654 56453 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1cccc2c(CO)cccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
135503676 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
CHEMBL107070 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
135538098 170157 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 3 4 5 2.6 Nc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL419364 170157 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 321 3 4 5 2.6 Nc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
135819157 16742 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 16742 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10393937 195167 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL427744 220149 0 None - 1 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
CHEMBL438218 220534 0 None - 1 Rat 5.7 pIC50 = 5.7 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
9902041 68615 18 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17736 68615 18 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10592750 113930 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL316264 113930 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 333 3 1 2 5.1 Fc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
53323247 63633 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 444 6 1 4 6.2 O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643952 63633 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 444 6 1 4 6.2 O=C(O)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
56602933 133859 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 5.5 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656298 133859 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 5.5 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
11383934 58559 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 8 2 7 3.3 COc1cc(CO/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1C(C)C 10.1016/s0960-894x(01)00819-8
CHEMBL158497 58559 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 397 8 2 7 3.3 COc1cc(CO/C=N/NC(=O)c2ccc(O)c(C#N)c2)cc(OC)c1C(C)C 10.1016/s0960-894x(01)00819-8
22005295 40925 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 311 8 1 2 5.1 CCCCCc1c(CC)nc(CC)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
CHEMBL142589 40925 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 311 8 1 2 5.1 CCCCCc1c(CC)nc(CC)c(CO)c1-c1ccccc1 10.1016/s0960-894x(01)00766-1
127046645 146423 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3797757 146423 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.9 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NC(C)CC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
135503676 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL107070 12157 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
58352803 117059 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238219 117059 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
16100296 209618 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL62444 209618 46 None - 1 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
44278221 168457 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
91931633 168457 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
CHEMBL413208 168457 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 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 10.1021/jm000453e
11114038 51471 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152103 51471 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111214 51471 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372888 60737 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160550 60737 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
15407872 66908 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL17396 66908 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0869-9
16100303 90055 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2OC(F)(F)F)CC1 10.1021/jm058026u
CHEMBL218871 90055 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(C#N)cc2OC(F)(F)F)CC1 10.1021/jm058026u
11952035 93592 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232239 93592 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
22496449 181216 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
11950971 157683 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL395759 157683 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
45381379 117050 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237928 117050 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
90655064 117068 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238228 117068 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11951857 103762 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL266489 103762 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 7 3 6 7.1 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
11826682 126307 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 5 2 5 5.1 N#Cc1cc(C(=O)N/N=C/c2cccc3c2ccn3Cc2ccc(C(F)(F)F)cc2)ccc1O 10.1021/jm0208572
CHEMBL345713 126307 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 5 2 5 5.1 N#Cc1cc(C(=O)N/N=C/c2cccc3c2ccn3Cc2ccc(C(F)(F)F)cc2)ccc1O 10.1021/jm0208572
10982999 171732 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 437 7 2 4 4.4 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL422506 171732 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 437 7 2 4 4.4 CCN(CC)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
9957123 126716 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(OC(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL349552 126716 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(OC(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
9929037 60658 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 60658 0 None - 0 Mouse 6.7 pIC50 = 6.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10076995 63711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644195 63711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
11186974 40734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142414 40734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 6 1 2 6.1 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44319495 212892 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85807 212892 3 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3cccc(Oc4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
10338890 212801 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85009 212801 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
135819133 121191 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 121191 3 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity of second diastereomer (D2) against human glucagon receptor was determinedBinding affinity of second diastereomer (D2) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
44372847 60419 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160289 60419 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44318988 212786 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84917 212786 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3ccc(Br)s3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352940 117022 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237901 117022 0 None - 0 Mouse 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
1714260 212791 21 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 374 3 1 1 6.2 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL84952 212791 21 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 374 3 1 1 6.2 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccccc3)[nH]2)cc1 10.1007/s00044-013-0869-9
59092268 85660 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 470 6 2 5 4.8 O=C(N/N=C/c1ccc(CS(=O)(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2112909 85660 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 470 6 2 5 4.8 O=C(N/N=C/c1ccc(CS(=O)(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
20775791 195478 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 597 10 3 7 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL504260 195478 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 597 10 3 7 5.7 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100298 90130 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm058026u
CHEMBL219307 90130 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(Cl)c(Cl)c2)CC1 10.1021/jm058026u
16100296 79187 46 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
CHEMBL198736 79187 46 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
16223791 75761 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922925 75761 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 614 12 2 5 7.4 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC)c(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
45381051 117046 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237924 117046 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353067 117057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238217 117057 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 619 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(F)cc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9824797 52500 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1021/jm0208572
CHEMBL153038 52500 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1021/jm0208572
44373782 126639 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 9 2 6 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL348785 126639 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 9 2 6 5.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10338890 212801 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85009 212801 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
16100296 79187 46 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
CHEMBL198736 79187 46 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm7015599
12967034 126802 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of MgBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of Mg
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350255 126802 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of MgBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in absence of Mg
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373083 59144 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 59144 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
145969316 171910 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227667 171910 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4ccccc4C(F)(F)F)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
11352330 193352 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 490 8 2 5 5.4 Cn1c(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL487828 193352 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 490 8 2 5 5.4 Cn1c(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44372701 59311 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL159198 59311 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372700 175389 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL436022 175389 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58353662 117026 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 117026 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL412679 219793 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
44275043 105476 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 354 8 2 3 5.8 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1N 10.1016/s0960-894x(02)00143-9
CHEMBL277627 105476 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 354 8 2 3 5.8 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1N 10.1016/s0960-894x(02)00143-9
135504174 12192 4 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 309 4 3 4 2.6 COc1cc(C(=O)N/N=C/c2c[nH]c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL107258 12192 4 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 309 4 3 4 2.6 COc1cc(C(=O)N/N=C/c2c[nH]c3ccccc23)ccc1O 10.1021/jm000547o
60170766 88153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
CHEMBL2159326 88153 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2cccc(OC(F)(F)F)c2)cc1 10.1021/jm300579z
164617749 191348 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 52 49 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CN(CCCC(=O)O)C(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4848485 191348 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 52 49 -17.3 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CN(CCCC(=O)O)C(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
16224591 75756 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922920 75756 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(OC(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
71243005 117047 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237925 117047 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469443 117084 1 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238246 117084 1 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.6 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11283703 181874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 8 2 7 5.8 CCCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL456877 181874 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 8 2 7 5.8 CCCn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
11410772 75462 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
CHEMBL1921810 75462 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 592 7 2 9 4.8 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(OC(F)(F)F)ccc21 10.1016/j.bmcl.2011.09.085
44372720 55349 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL155694 55349 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
22004988 171950 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL422833 171950 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 9 1 2 7.3 CCCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
10076778 63712 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 10 2 5 6.5 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)NCCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.11.074
CHEMBL1644196 63712 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 10 2 5 6.5 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)NCCC(=O)O)cc2)n1 10.1016/j.bmcl.2010.11.074
11704225 120763 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 409 5 3 6 3.8 CC(C)c1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326186 120763 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 409 5 3 6 3.8 CC(C)c1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
44319713 113945 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1007/s00044-013-0869-9
CHEMBL316361 113945 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 447 9 1 4 7.0 CCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCC)c1 10.1007/s00044-013-0869-9
16100301 176035 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 578 11 3 4 6.0 CCN(CC)C(=O)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
CHEMBL441160 176035 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 578 11 3 4 6.0 CCN(CC)C(=O)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
44278463 103256 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 2637 85 37 35 -9.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](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)Cc1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
91931631 103256 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 2637 85 37 35 -9.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](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)Cc1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
CHEMBL262418 103256 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL 2637 85 37 35 -9.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](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)Cc1ccccc1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
135819149 17223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 17223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of second enantiomer (E2) against human glucagon receptor was determinedBinding affinity of second enantiomer (E2) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
22496358 194098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL493019 194098 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44372847 60419 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160289 60419 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 328 3 1 1 5.9 Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
3505 8993 45 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 8993 45 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 8993 45 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
10461326 63703 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 2 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644187 63703 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 2 6 6.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(OC(F)(F)F)cc2)cc1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL413030 219826 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H]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]2CCCCNC(=O)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)Cc3c[nH]cn3)[C@H](C)O)[C@H](C)O)C(=O)N[C@@H](Cc3ccc(O)cc3)C(=O)N[C@H](CO)C(=O)N2)C(=O)N[C@@H](CCCCN)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 10.1021/jm990559d
22005250 41352 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.5 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142944 41352 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 7 1 2 6.5 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44319474 113830 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL315613 113830 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
58352863 117025 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237904 117025 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10873618 57866 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 426 7 2 5 3.6 CCN(CC)C(=O)Cn1ccc2c(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cccc21 10.1021/jm0208572
CHEMBL157913 57866 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 426 7 2 5 3.6 CCN(CC)C(=O)Cn1ccc2c(/C=N/NC(=O)c3ccc(O)c(Cl)c3)cccc21 10.1021/jm0208572
44372700 175389 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL436022 175389 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccccc3Br)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
57394374 75774 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922937 75774 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 608 14 2 5 7.5 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
68243839 117065 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
CHEMBL3238225 117065 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 613 9 2 7 6.3 COc1ccc(C2=N[C@]3(CC[C@@H](C(C)(C)C)CC3)N([C@H](CCC(C)(C)C)c3ccc(C(=O)NCc4nn[nH]n4)cc3)C2=O)cc1 10.1021/jm401858f
122189699 130144 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
CHEMBL3616678 130144 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)cn1 10.1016/j.bmcl.2015.08.015
12967035 58611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 58611 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44373103 60917 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160690 60917 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
11142525 12469 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 346 5 2 4 3.8 COc1cc(C(=O)N/N=C/c2ccc(-c3ccccc3)cc2)ccc1O 10.1021/jm000547o
CHEMBL107802 12469 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 346 5 2 4 3.8 COc1cc(C(=O)N/N=C/c2ccc(-c3ccccc3)cc2)ccc1O 10.1021/jm000547o
20775792 195560 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 9 3 6 5.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL505685 195560 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 9 3 6 5.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100315 90077 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 5.7 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
CHEMBL219010 90077 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 5.7 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)C2Cc3ccccc3C2)cc1 10.1021/jm058026u
44372677 60532 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL160380 60532 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
11048896 55130 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 464 5 2 5 3.3 CN1CCN(C(=O)Cc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)CC1 10.1021/jm0208572
CHEMBL155449 55130 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 464 5 2 5 3.3 CN1CCN(C(=O)Cc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)CC1 10.1021/jm0208572
10369510 179897 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 523 8 4 4 5.1 Cc1cc(C)cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)c1 10.1021/jm7015599
CHEMBL452067 179897 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 523 8 4 4 5.1 Cc1cc(C)cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)c1 10.1021/jm7015599
44319474 113830 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315613 113830 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccc(Oc4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
135503676 12157 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards rat Glucagon ReceptorBinding affinity towards rat Glucagon Receptor
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
CHEMBL107070 12157 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards rat Glucagon ReceptorBinding affinity towards rat Glucagon Receptor
ChEMBL 340 3 3 4 3.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm000547o
10257357 148616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm058026u
CHEMBL386446 148616 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm058026u
9869430 128745 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 6.1 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(Cl)c(Cl)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL359126 128745 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 6.1 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(Cl)c(Cl)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
11049977 126425 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL346801 126425 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44373213 126615 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 126615 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
12967035 58611 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158535 58611 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
9952509 213157 15 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL87588 213157 15 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
53469821 117079 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238240 117079 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 655 10 2 4 8.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
68864642 120752 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 476 4 3 4 5.2 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(Br)c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326173 120752 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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
ChEMBL 476 4 3 4 5.2 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(Br)c1 10.1016/j.bmcl.2014.07.025
9985258 185762 10 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
44372405 58774 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158671 58774 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
10077065 63708 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)NCCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644192 63708 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 587 10 2 7 4.8 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)NCCC(=O)O)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
44373585 58643 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 464 9 3 7 4.6 COc1cc(/C=N/NC(=O)c2ccc(O)c(O)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158556 58643 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 464 9 3 7 4.6 COc1cc(/C=N/NC(=O)c2ccc(O)c(O)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
11625113 120759 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 381 4 3 6 2.9 Cc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326181 120759 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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
ChEMBL 381 4 3 6 2.9 Cc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
145967583 171731 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4225050 171731 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 547 9 2 5 6.8 COc1ccc2cc(-c3c(C)c(-c4cccc(C)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
145970933 171930 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4227967 171930 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 557 8 2 4 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
129010851 157763 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 553 10 2 3 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C)cc(Cl)cc12 nan
CHEMBL3958315 157763 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 553 10 2 3 8.4 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C)cc(Cl)cc12 nan
135819143 16750 7 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114799 16750 7 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 373 7 2 3 6.2 CCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
16223987 75754 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922918 75754 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 600 12 2 5 7.2 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
16224781 75764 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
CHEMBL1922928 75764 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 11 2 6 6.1 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2c(c1)OCCO2 10.1016/j.bmcl.2011.09.105
53325824 63701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 9 3 6 5.6 O=C(NC[C@@H](O)C(=O)O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644185 63701 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 9 3 6 5.6 O=C(NC[C@@H](O)C(=O)O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11949739 168012 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411833 168012 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 641 7 3 3 8.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11037917 56869 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 7 3 6 3.9 COc1cc(NC(=O)Cc2ccc(Cl)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL157000 56869 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 462 7 3 6 3.9 COc1cc(NC(=O)Cc2ccc(Cl)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
45381379 117050 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237928 117050 0 None - 0 Mouse 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145967899 171869 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
CHEMBL4227099 171869 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 574 8 2 5 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2c(ccn2C)c1 10.1016/j.bmc.2018.02.036
10066912 212941 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL86250 212941 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319712 112709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3cc(Br)cs3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL312825 112709 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 399 3 1 3 5.8 Fc1ccc(-c2[nH]c(-c3cc(Br)cs3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58353695 117036 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237914 117036 0 None - 0 Mouse 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
135501650 12458 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1O 10.1021/jm000547o
CHEMBL107795 12458 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)cc1O 10.1021/jm000547o
44372650 60568 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160401 60568 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44372688 56202 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL156458 56202 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
11113699 54109 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1ccc2c(ccn2Cc2ccc(OC(F)(F)F)cc2)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154437 54109 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 487 6 2 5 5.7 O=C(N/N=C/c1ccc2c(ccn2Cc2ccc(OC(F)(F)F)cc2)c1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
11024220 53457 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 338 4 3 4 2.9 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm0208572
CHEMBL153905 53457 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 338 4 3 4 2.9 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm0208572
11782911 126293 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 345 4 3 5 2.7 N#Cc1cc(C(=O)N/N=C/c2ccc(CO)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL345589 126293 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 345 4 3 5 2.7 N#Cc1cc(C(=O)N/N=C/c2ccc(CO)c3ccccc23)ccc1O 10.1021/jm0208572
10093802 113691 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314701 113691 4 None - 0 Human 6.5 pIC50 = 6.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
44372556 55924 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL156207 55924 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44373191 126492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347462 126492 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
9952509 213157 15 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL87588 213157 15 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccc(Br)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
10882636 11634 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 350 5 2 5 3.3 COc1cc(C(=O)N/N=C/c2ccc(OC)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104338 11634 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 350 5 2 5 3.3 COc1cc(C(=O)N/N=C/c2ccc(OC)c3ccccc23)ccc1O 10.1021/jm000547o
11640146 120598 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 409 6 3 6 3.6 CCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3325456 120598 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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
ChEMBL 409 6 3 6 3.6 CCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
10481623 63637 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643956 63637 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
9983854 63688 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644172 63688 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)n(C3CCCCC3)n2)cc1 10.1016/j.bmcl.2010.11.074
53325825 63718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644202 63718 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
11034750 176190 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 326 4 2 4 3.5 COc1cc(C(=O)N/N=C/c2ccc(C(C)(C)C)cc2)ccc1O 10.1021/jm000547o
CHEMBL442389 176190 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 326 4 2 4 3.5 COc1cc(C(=O)N/N=C/c2ccc(C(C)(C)C)cc2)ccc1O 10.1021/jm000547o
16100321 144671 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 564 8 4 5 5.5 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)NO)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL376322 144671 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 564 8 4 5 5.5 CC(C)(C)C1CCC(N(Cc2ccc(C(=O)NCC(=O)NO)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44373192 126514 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347663 126514 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
122189580 130128 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616591 130128 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 637 10 2 6 7.7 COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189702 130147 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616681 130147 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 675 9 2 5 8.8 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(C(F)(F)F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189711 130156 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616690 130156 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 12 2 5 8.4 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccccc3)cc21 10.1016/j.bmcl.2015.08.015
11308245 75739 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922836 75739 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 648 10 2 9 6.1 CCCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
23550062 63632 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1643951 63632 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 559 7 3 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2010.11.074
129010863 158850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
CHEMBL3967446 158850 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 633 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCS(=O)(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(Br)cc(C)cc12 nan
122189716 130161 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616695 130161 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 660 13 2 7 7.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)nc3)cc21 10.1016/j.bmcl.2015.08.015
11950795 93593 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232241 93593 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11145871 56552 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 531 6 2 5 6.2 O=C(N/N=C/c1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156724 56552 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 531 6 2 5 6.2 O=C(N/N=C/c1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
122189719 130164 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616698 130164 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 683 12 2 5 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)c(F)c(F)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL267189 217492 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None None 10.1021/jm010091q
CHEMBL413890 219876 23 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Compound was evaluated for its ability to displace radiolabeled glucagonCompound was evaluated for its ability to displace radiolabeled glucagon
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
11952211 160520 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL398180 160520 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10032265 193101 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487476 193101 1 None - 1 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
44372904 60747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160561 60747 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819133 121191 3 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 121191 3 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
44372688 56202 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 56202 0 None - 0 Mouse 7.5 pIC50 = 7.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
11490222 75683 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922706 75683 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 590 6 2 8 5.3 Cc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
145969571 171947 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228281 171947 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 561 8 2 5 7.4 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2occc2c1 10.1016/j.bmc.2018.02.036
22004872 41278 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL142886 41278 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44372701 59311 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL159198 59311 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3ccc(Br)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
10133915 68543 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL17722 68543 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319276 212888 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL85741 212888 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 391 4 1 2 6.6 Fc1ccc(-c2[nH]c(-c3ccc(-c4ccccc4)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
44372478 58629 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 58629 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10076914 63705 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644189 63705 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 579 9 2 6 5.9 O=C(O)CNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
22005388 101248 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(F)c1 10.1016/s0960-894x(02)00143-9
CHEMBL25137 101248 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(F)c1 10.1016/s0960-894x(02)00143-9
44373464 126480 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 496 9 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C(=O)O)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL347370 126480 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 496 9 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C(=O)O)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44372478 58629 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 58629 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44369291 51927 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 469 7 2 5 5.4 O=C(N/N=C/c1cn(Cc2ccc(OC(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152537 51927 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 469 7 2 5 5.4 O=C(N/N=C/c1cn(Cc2ccc(OC(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
57399593 75755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922919 75755 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 584 11 2 4 7.3 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(F)(F)F)cc1 10.1016/j.bmcl.2011.09.105
58352937 117069 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238229 117069 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 9 2 6 7.2 CC(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
44561390 182815 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459032 182815 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 480 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C(C)(C)C)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
57403703 75745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922842 75745 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL437860 220515 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
44373486 58870 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 516 9 2 6 6.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2Cl)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158753 58870 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 516 9 2 6 6.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2Cl)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
71243005 117047 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237925 117047 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 637 10 2 6 7.3 CCCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145967924 171907 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
CHEMBL4227634 171907 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccccc1-c1ccccc1 10.1016/j.bmc.2018.02.036
22496395 194127 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 569 9 2 5 7.9 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)n2)cc1 10.1021/jm8016249
CHEMBL493233 194127 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 569 9 2 5 7.9 CC(C)(C)c1ccc(-c2csc(N(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)n2)cc1 10.1021/jm8016249
127047120 146504 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
CHEMBL3798231 146504 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 7 2 6 6.0 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2c(c1)OCCO2 10.1016/j.bmc.2016.04.053
16225394 75753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922917 75753 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 550 11 2 4 7.0 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2011.09.105
10054055 195205 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)[C@H]1CC[C@@]2(CCN(c3ccc(OC(F)(F)F)cc3)C(=O)N2Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL502203 195205 12 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 585 6 2 6 6.2 CC(C)(C)[C@H]1CC[C@@]2(CCN(c3ccc(OC(F)(F)F)cc3)C(=O)N2Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)CC1 10.1016/j.bmcl.2008.05.072
44372396 60829 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 252 2 1 1 4.2 Cc1cc(-c2ccc(F)cc2)c(-c2ccncc2)[nH]1 10.1007/s00044-013-0801-3
CHEMBL160627 60829 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 252 2 1 1 4.2 Cc1cc(-c2ccc(F)cc2)c(-c2ccncc2)[nH]1 10.1007/s00044-013-0801-3
44319591 113357 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314238 113357 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
58352952 117029 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237908 117029 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10044081 69377 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nnc(CC(C)C)o2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL178302 69377 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nnc(CC(C)C)o2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
145968140 171870 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227111 171870 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.2 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3Cc3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
10928006 126986 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 4 3 4 4.9 CC(C)(C)C(=O)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL352005 126986 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 4 3 4 4.9 CC(C)(C)C(=O)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
11114038 51471 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152103 51471 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2111214 51471 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 519 8 3 5 5.4 COc1cc(NC(=O)CCc2ccc(C(F)(F)F)cc2)ccc1/C=N/NC(=O)c1ccc(O)c(Cl)c1 10.1021/jm0208572
9956429 56468 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 5.8 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(C(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156666 56468 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 471 5 2 4 5.8 O=C(N/N=C/c1cccc2c1ccn2Cc1ccc(C(F)(F)F)cc1)c1ccc(O)c(Cl)c1 10.1021/jm0208572
58353679 117035 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237913 117035 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(OC(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53316573 63716 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
CHEMBL1644200 63716 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1cccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)c1 10.1016/j.bmcl.2010.11.074
44373586 60950 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160715 60950 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(C)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
58352868 117019 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237898 117019 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58353156 117027 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237906 117027 0 None - 0 Mouse 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44318935 212810 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL85102 212810 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
71454981 88172 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
CHEMBL2159344 88172 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 589 9 2 4 8.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccccc1C1CCCCC1 10.1021/jm300579z
11952211 160520 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL398180 160520 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
22496457 179337 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448561 179337 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
57396139 75763 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922927 75763 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 12 2 5 7.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc2cc(OC)ccc2c1 10.1016/j.bmcl.2011.09.105
22496451 184797 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 625 10 2 6 8.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(SC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL464663 184797 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 625 10 2 6 8.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(SC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL2114176 216029 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1ccccc1)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 10.1021/jm960130b
12967033 60843 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160638 60843 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372923 126320 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 126320 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 126414 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 126414 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353025 117034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 117034 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11950795 93593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232241 93593 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 603 8 3 4 7.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
44372638 57420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL157529 57420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
9998923 113683 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL314652 113683 2 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 365 3 1 2 6.1 Fc1ccc(-c2[nH]c(-c3cccc4ccccc34)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
9843239 113850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315800 113850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 387 3 1 2 6.8 CC(C)(C)c1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
135442286 12214 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(O)c1 10.1021/jm000547o
CHEMBL107388 12214 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 322 3 4 5 2.7 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(O)c1 10.1021/jm000547o
56602867 133845 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 547 10 2 6 5.2 CC(C)CC1(C)N=C(c2cccc(F)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
CHEMBL3656284 133845 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 547 10 2 6 5.2 CC(C)CC1(C)N=C(c2cccc(F)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nnn[nH]2)cc1 nan
135542465 12230 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 374 3 3 4 4.3 O=C(N/N=C/c1ccc(O)c2ccccc12)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm000547o
CHEMBL107473 12230 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 374 3 3 4 4.3 O=C(N/N=C/c1ccc(O)c2ccccc12)c1cc(Cl)c(O)c(Cl)c1 10.1021/jm000547o
122189707 130152 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
CHEMBL3616686 130152 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 605 10 2 8 5.9 COc1nccc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)n1 10.1016/j.bmcl.2015.08.015
16100299 90081 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 521 9 3 3 6.7 CC(C)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
CHEMBL219030 90081 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 521 9 3 3 6.7 CC(C)c1ccc(NC(=O)N(Cc2ccc(C(=O)NCCC(=O)O)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)cc1 10.1021/jm058026u
11048133 54134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 6 2 4 4.4 CCN(CC)C(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154460 54134 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 423 6 2 4 4.4 CCN(CC)C(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44372638 57420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 57420 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
22005015 42080 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 9 1 2 6.8 CCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL143664 42080 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 371 9 1 2 6.8 CCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
89568983 133854 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 3 4 4.9 CC1(C2CCCCC2)NC(c2cccc(C(F)(F)F)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656293 133854 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 3 4 4.9 CC1(C2CCCCC2)NC(c2cccc(C(F)(F)F)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
44411371 146319 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 411 9 1 4 6.0 COc1ccc(NCCCOc2ccc(C(=O)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2006.02.013
CHEMBL379600 146319 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 411 9 1 4 6.0 COc1ccc(NCCCOc2ccc(C(=O)c3cccc4ccccc34)cc2)cc1 10.1016/j.bmcl.2006.02.013
44369018 54788 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 430 5 2 5 4.1 CC(C)S(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL155021 54788 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 430 5 2 5 4.1 CC(C)S(=O)(=O)c1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
11952035 158249 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL396215 158249 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 585 6 3 6 6.5 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10257357 148616 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL386446 148616 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 565 9 3 3 7.4 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
16100334 90149 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
CHEMBL219384 90149 2 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
53469058 117071 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C)CC2 10.1021/jm401858f
CHEMBL3238231 117071 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C)CC2 10.1021/jm401858f
10053841 63698 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644182 63698 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
22496365 195632 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 621 11 2 6 8.2 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL506800 195632 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 621 11 2 6 8.2 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
164616563 192185 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4861024 192185 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2983 97 46 42 -12.8 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164612071 191335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3198 104 49 45 -13.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4848344 191335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3198 104 49 45 -13.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H](N)CC(C)C)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164622383 192720 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4869368 192720 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3019 97 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc(F)c(F)c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
9946911 60695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160525 60695 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58352834 117032 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237910 117032 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046098 146861 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3800525 146861 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2ccccc2c1 10.1016/j.bmc.2016.04.053
10383925 85725 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112991 85725 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 360 7 1 6 4.6 CCC(CC)C(=O)Nc1sc(-c2nc(CC(C)C)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
3505 8993 45 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 8993 45 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 8993 45 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
57390854 75772 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922935 75772 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 596 11 2 4 7.3 O=C(O)CCNC(=O)c1ccc(C[C@H](CC2CC2)C(=O)c2cc3cc(Cl)ccc3n2-c2cccc(C(F)(F)F)c2)cc1 10.1016/j.bmcl.2011.09.105
176155 10937 0 None - 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL10 10937 0 None - 4 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 377 4 1 3 4.7 C[S+]([O-])c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
164628244 193226 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876499 193226 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3025 98 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164609866 192006 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)C[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4857992 192006 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)C[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
164624086 192482 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4865509 192482 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3084 100 48 44 -13.9 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
60170767 88154 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
CHEMBL2159327 88154 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 7.2 CCCOc1ccc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1021/jm300579z
44372846 60363 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160238 60363 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 342 4 1 1 6.1 CCc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58353206 117044 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237922 117044 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145971078 171787 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
CHEMBL4225922 171787 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 597 9 2 4 8.3 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc(-c2ccccc2)c1 10.1016/j.bmc.2018.02.036
56602804 117073 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3238233 117073 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 555 8 2 6 5.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
10030697 185853 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44373192 126514 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL347663 126514 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 402 6 1 2 7.1 CC(C)COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
22496384 193926 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL491920 193926 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
45381049 117066 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238226 117066 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
57400189 75682 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922705 75682 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 542 6 2 8 4.6 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2011.09.085
11102152 56686 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 5 3 4 5.1 O=C(N/N=C/c1ccc(NC(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156837 56686 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 435 5 3 4 5.1 O=C(N/N=C/c1ccc(NC(=O)C2CCCC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372888 60737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160550 60737 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44318935 212810 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL85102 212810 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3ccc(-c4ccccc4)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
10436553 63634 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643953 63634 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
44389584 71367 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 395 7 1 4 5.0 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccccc1)C2 10.1016/j.bmcl.2005.01.003
CHEMBL181669 71367 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 395 7 1 4 5.0 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccccc1)C2 10.1016/j.bmcl.2005.01.003
10415723 63700 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644184 63700 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 573 7 2 7 6.2 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
122189723 130169 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616702 130169 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 587 9 2 5 7.0 COc1ccc(C(F)(F)F)cc1-c1nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
44372405 58774 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158671 58774 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
135533241 12156 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 324 3 3 4 3.2 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm000547o
CHEMBL107069 12156 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 324 3 3 4 3.2 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(F)c1 10.1021/jm000547o
141465346 171959 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4228470 171959 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 535 8 2 4 7.0 Cc1ccc(-c2c(C)c(-c3cc(Cl)cc(Cl)c3)nn2C(C)c2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmc.2018.02.036
44373462 171573 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2cc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL421833 171573 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2cc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc32)cc1 10.1016/s0960-894x(01)00819-8
127047253 146850 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3800473 146850 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 553 7 2 4 6.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(Cl)cc1 10.1016/j.bmc.2016.04.053
145989480 171988 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228938 171988 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 560 8 3 4 7.1 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2[nH]ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL2114177 216030 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](C)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 10.1021/jm960130b
44372870 60417 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 60417 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10232009 193240 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 583 9 4 4 6.5 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487668 193240 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 583 9 4 4 6.5 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
45381381 117054 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238214 117054 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 663 8 2 6 7.1 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(F)(F)F)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
11785044 182998 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459457 182998 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 486 6 2 7 5.0 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44561479 185906 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
CHEMBL471979 185906 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2c1 10.1016/j.bmcl.2008.05.072
44561438 196182 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
CHEMBL513067 196182 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 516 7 2 8 5.0 COc1ccc2c(c1)nc(N(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)[C@H]1CC[C@H](C(C)(C)C)CC1)n2C 10.1016/j.bmcl.2008.05.072
11421826 75673 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922696 75673 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 8 5.2 Cn1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
122189570 130118 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616581 130118 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 645 12 2 6 8.0 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189576 130124 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616587 130124 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 628 11 2 4 8.9 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189581 130129 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616592 130129 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 639 10 2 6 7.4 COc1cc(F)c(F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189703 130148 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616682 130148 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 625 9 2 5 7.9 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(Cl)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189712 130157 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616691 130157 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 693 13 2 6 9.0 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3Cl)cc21 10.1016/j.bmcl.2015.08.015
122189718 130163 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616697 130163 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 649 12 2 6 8.8 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)s3)cc21 10.1016/j.bmcl.2015.08.015
122189720 130165 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616699 130165 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 10 2 5 8.2 COc1ccc(C(F)(F)F)cc1-c1nn(C(c2ccc(C(=O)NCCC(=O)O)cc2)C(C)C)c2cc(-c3ccc(C)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189721 130167 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 615 10 2 5 7.9 CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616700 130167 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 615 10 2 5 7.9 CCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(C)cc3)cc21 10.1016/j.bmcl.2015.08.015
11621378 88181 3 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159353 88181 3 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 605 9 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4F)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11952211 94726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL234087 94726 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 589 8 3 4 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL2115191 216040 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)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 10.1021/jm960130b
60170857 88170 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159342 88170 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 599 9 2 4 8.6 CC(C)c1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
44368911 126634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1021/jm0208572
CHEMBL348702 126634 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1021/jm0208572
11421820 75687 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922710 75687 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 576 6 2 7 5.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(C)(C)C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
60170856 88169 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159341 88169 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 571 8 2 4 7.8 Cc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
10053876 53771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 574 7 2 5 5.5 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154159 53771 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 574 7 2 5 5.5 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
46853082 167537 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 617 12 2 5 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(-c3ccnn3C)cc(F)cc12 nan
CHEMBL4114029 167537 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 617 12 2 5 8.4 CCCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(-c3ccnn3C)cc(F)cc12 nan
11952214 93594 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232242 93594 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 584 7 2 6 6.0 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Cc2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11950971 157683 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL395759 157683 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 605 8 3 5 6.8 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)NCCC(=O)O)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11952394 93787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232448 93787 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 569 5 3 5 6.9 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(Cl)cc(Cl)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
10864579 53754 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 551 6 2 6 4.8 N#Cc1cc(C(=O)N/N=C/c2ccc(C(=O)N3CCN(Cc4ccc(Cl)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL154149 53754 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 551 6 2 6 4.8 N#Cc1cc(C(=O)N/N=C/c2ccc(C(=O)N3CCN(Cc4ccc(Cl)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
12967032 60411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160281 60411 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
12967033 60843 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160638 60843 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372923 126320 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 126320 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 126414 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 126414 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44373191 126492 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347462 126492 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
135819149 17223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL116413 17223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity of first diastereomer (D1) against human glucagon receptor was determinedBinding affinity of first diastereomer (D1) against human glucagon receptor was determined
ChEMBL 341 6 2 3 5.7 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccccc1O 10.1016/s0960-894x(02)00736-9
CHEMBL267885 217515 0 None - 1 Rat 7.4 pIC50 = 7.4 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
122189706 130151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616685 130151 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 11 2 7 6.7 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(C(=O)c2ccc(N(C)C)cc2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
10474631 112729 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL312928 112729 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
11678967 88157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
CHEMBL2159330 88157 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3c(OC(F)(F)F)cccc3c2)cc1 10.1021/jm300579z
44372454 126324 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345863 126324 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372677 60532 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160380 60532 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44319591 113357 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314238 113357 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
51031037 117039 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237917 117039 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 581 6 2 6 5.8 C[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22005204 38442 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 329 6 1 2 5.6 CCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140514 38442 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 329 6 1 2 5.6 CCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
9844728 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysisDisplacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysis
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/j.ejmech.2018.04.061
CHEMBL1196711 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysisDisplacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysis
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/j.ejmech.2018.04.061
CHEMBL557974 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysisDisplacement of [125I]-glucagon from GCGR in Sprague-Dawley rat liver assessed as decrease in glucagon-stimulated CAMP production incubated for 45 mins by scintillation counter analysis
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/j.ejmech.2018.04.061
58353350 117033 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237911 117033 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9844728 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Tested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liverTested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liver
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/S0960-894X(00)80587-9
CHEMBL1196711 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Tested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liverTested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liver
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/S0960-894X(00)80587-9
CHEMBL557974 20734 5 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Tested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liverTested against glucagon receptor for its ability to displace radiolabeled ([125I]-glucagon) in male Dawley rat liver
ChEMBL 414 7 0 4 5.5 CN(C)CCCN(C)c1nc2cc(Cl)c(Cl)cc2nc1/C=C/c1ccccc1 10.1016/S0960-894X(00)80587-9
10970292 52955 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL153438 52955 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 354 4 3 4 3.5 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
127046643 146574 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798761 146574 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 577 8 2 4 8.0 CC(CC(=O)O)NC(=O)c1ccc(C(C)n2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmc.2016.04.053
127047907 146700 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799556 146700 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 627 7 1 5 8.2 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)N4CCC(C(=O)O)CC4)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
10053886 198543 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
57393262 75678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922701 75678 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1cccc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
45381051 117046 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237924 117046 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CCCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
45381380 117049 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237927 117049 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 623 8 2 6 6.8 CC(C)C[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22496441 185996 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 587 11 2 7 7.0 COc1ccccc1-c1csc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(SC(F)(F)F)cc2)n1 10.1021/jm8016249
CHEMBL472586 185996 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 587 11 2 7 7.0 COc1ccccc1-c1csc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(SC(F)(F)F)cc2)n1 10.1021/jm8016249
44372946 58530 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1007/s00044-013-0801-3
CHEMBL158477 58530 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1007/s00044-013-0801-3
12967032 60411 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160281 60411 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
12967033 60843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL160638 60843 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
10324098 63638 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643957 63638 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cc2cc(-c3ccc(OC(F)(F)F)cc3)nn2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
56602930 133852 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 4.8 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656291 133852 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 517 10 2 4 4.8 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
9929037 60658 0 None - 0 Mouse 4.4 pIC50 = 4.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 60658 0 None - 0 Mouse 4.4 pIC50 = 4.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
10032265 193101 1 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL487476 193101 1 None - 1 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to GlucR in rat liver membraneBinding affinity to GlucR in rat liver membrane
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10326056 63696 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644180 63696 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 589 8 2 8 5.8 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
44372638 57420 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 57420 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
68863912 120751 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 432 4 3 4 5.0 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(Cl)c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326172 120751 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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
ChEMBL 432 4 3 4 5.0 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c(Cl)c1 10.1016/j.bmcl.2014.07.025
53323150 63713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 8 2 7 6.1 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)n1 10.1016/j.bmcl.2010.11.074
CHEMBL1644197 63713 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 8 2 7 6.1 CC(c1ccc(Cl)cc1)c1cc(-c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)n1 10.1016/j.bmcl.2010.11.074
11045195 12013 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 312 5 2 4 3.3 COc1cc(C(=O)N/N=C/c2ccc(C(C)C)cc2)ccc1O 10.1021/jm000547o
CHEMBL106320 12013 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 312 5 2 4 3.3 COc1cc(C(=O)N/N=C/c2ccc(C(C)C)cc2)ccc1O 10.1021/jm000547o
11078726 12100 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 354 5 2 5 3.1 COc1cc(C(=O)N/N=C/c2ccc(OC(F)(F)F)cc2)ccc1O 10.1021/jm000547o
CHEMBL106795 12100 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 354 5 2 5 3.1 COc1cc(C(=O)N/N=C/c2ccc(OC(F)(F)F)cc2)ccc1O 10.1021/jm000547o
58353662 117026 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237905 117026 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53469056 117070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
CHEMBL3238230 117070 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 623 9 2 6 6.9 CC[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@H](CCC(C)(C)C)c1ccc(C(=O)NCc2nn[nH]n2)cc1 10.1021/jm401858f
44324149 213822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL91652 213822 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 360 4 1 2 6.3 CSc1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44373213 126615 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL348555 126615 0 None - 0 Mouse 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 387 6 2 2 6.9 CCCNc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
22496445 178585 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
58352858 117030 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 117030 0 None - 0 Mouse 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11646890 120762 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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
ChEMBL 395 5 3 6 3.2 CCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326185 120762 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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
ChEMBL 395 5 3 6 3.2 CCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
11113396 54183 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 466 8 2 5 3.5 CN(C)CCN(C)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154498 54183 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 466 8 2 5 3.5 CN(C)CCN(C)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44372946 58530 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
CHEMBL158477 58530 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
57390853 75768 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
CHEMBL1922931 75768 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
10257629 194054 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
12967032 60411 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160281 60411 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
58353025 117034 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237912 117034 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)ccc2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
16225393 75758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922922 75758 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 534 11 2 4 6.5 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(F)c1 10.1016/j.bmcl.2011.09.105
16100296 90119 46 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL219244 90119 46 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
11081564 54169 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 496 7 3 6 4.2 COc1cc(NC(=O)Cc2cccc(C(F)(F)F)c2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
CHEMBL154485 54169 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 496 7 3 6 4.2 COc1cc(NC(=O)Cc2cccc(C(F)(F)F)c2)ccc1/C=N/NC(=O)c1ccc(O)c(C#N)c1 10.1021/jm0208572
58352954 117040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237918 117040 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 567 5 2 6 6.1 C[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
127046099 146688 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799468 146688 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 599 8 2 5 7.4 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C3CCc4cc(C(=O)NCCC(=O)O)ccc43)ccc2c1 10.1016/j.bmc.2016.04.053
12967035 58611 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
CHEMBL158535 58611 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 386 6 1 2 6.6 C=CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1007/s00044-013-0801-3
22496477 179556 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL451288 179556 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL2369985 216544 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL None None None CCCC[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(=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 10.1021/jm960800d
CHEMBL268636 217541 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
CHEMBL438045 220527 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Compound was evaluated for its ability to displace radiolabeled glucagonCompound was evaluated for its ability to displace radiolabeled glucagon
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
CHEMBL441209 220666 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](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(N)=O)[C@@H](C)O 10.1016/0960-894X(95)00307-F
22496371 176705 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 605 10 2 5 8.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL444126 176705 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 605 10 2 5 8.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44373730 61723 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 9 2 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2F)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL161483 61723 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 9 2 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(F)c2F)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10030948 63693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 9 2 5 7.0 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1644177 63693 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 571 9 2 5 7.0 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)CC1 10.1016/j.bmcl.2010.11.074
9555433 11721 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1cc(C(=O)N/N=C/c2cccc3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104761 11721 1 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1cc(C(=O)N/N=C/c2cccc3ccccc23)ccc1O 10.1021/jm000547o
22005048 106482 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 369 9 1 3 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(OC)c1 10.1016/s0960-894x(02)00143-9
CHEMBL284699 106482 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 369 9 1 3 6.2 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(OC)c1 10.1016/s0960-894x(02)00143-9
44561285 179884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 434 4 2 3 6.4 O=C(NC(=O)c1ccccc1Cl)Nc1ccc(Oc2ccc(Cl)cc2)c(Cl)c1 10.1016/j.bmcl.2008.05.072
CHEMBL452040 179884 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 434 4 2 3 6.4 O=C(NC(=O)c1ccccc1Cl)Nc1ccc(Oc2ccc(Cl)cc2)c(Cl)c1 10.1016/j.bmcl.2008.05.072
11813262 56608 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 8 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(Cl)c1OCCN1CCc2ccccc2C1 10.1021/jm0208572
CHEMBL156777 56608 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 513 8 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc(Cl)c1OCCN1CCc2ccccc2C1 10.1021/jm0208572
44372870 60417 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 60417 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
11952213 93533 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL232037 93533 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 570 6 2 6 6.1 CC(C)(C)[C@H]1CC[C@H](N(C(=O)c2ccc(OC(F)(F)F)cc2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
11102467 53887 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154269 53887 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 453 8 2 5 4.2 CCN(CC)C(=O)COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
9841863 66832 26 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL17370 66832 26 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372406 126594 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL348401 126594 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
9841863 66832 26 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17370 66832 26 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 361 4 1 3 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58352858 117030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237909 117030 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10483611 63695 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644179 63695 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 593 10 2 6 6.3 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
6875509 11979 9 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1ccc(/C=N/NC(=O)c2ccc(O)cc2)c2ccccc12 10.1021/jm000547o
CHEMBL106134 11979 9 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 320 4 2 4 3.3 COc1ccc(/C=N/NC(=O)c2ccc(O)cc2)c2ccccc12 10.1021/jm000547o
10960967 170319 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 430 6 2 5 5.0 COc1cc(C(=O)N/N=C/c2cccc(Oc3cccc(C(F)(F)F)c3)c2)ccc1O 10.1021/jm000547o
CHEMBL420290 170319 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 430 6 2 5 5.0 COc1cc(C(=O)N/N=C/c2cccc(Oc3cccc(C(F)(F)F)c3)c2)ccc1O 10.1021/jm000547o
44373083 59144 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL158989 59144 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
56602803 133847 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 495 9 2 4 5.0 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
CHEMBL3656286 133847 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 495 9 2 4 5.0 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
141465337 171867 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
CHEMBL4227068 171867 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 541 8 2 4 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(Cc2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc(Cl)cc1 10.1016/j.bmc.2018.02.036
10211943 180021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 675 11 4 7 5.4 CS(=O)(=O)c1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)ccc1OC(F)(F)F 10.1021/jm7015599
CHEMBL452451 180021 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 675 11 4 7 5.4 CS(=O)(=O)c1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3=CCCCC3)cc2)ccc1OC(F)(F)F 10.1021/jm7015599
122189693 130138 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616672 130138 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 659 9 2 5 8.2 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
60170971 88176 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159348 88176 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4ccc(Cl)c(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
9825482 52643 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 459 5 2 4 6.0 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c1C 10.1021/jm0208572
CHEMBL153157 52643 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 459 5 2 4 6.0 Cc1cc(C)c(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c1C 10.1021/jm0208572
9885993 213300 10 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL88486 213300 10 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 1 2 5.3 C[S+]([O-])c1ccc(-c2cc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL263603 217361 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None None 10.1021/jm010091q
57396141 75775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922938 75775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 662 14 2 5 8.4 CCCCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(OC(F)(F)F)ccc2n1-c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2011.09.105
11102344 51683 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 5 2 4 5.7 Cc1cc(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c(C)c1 10.1021/jm0208572
CHEMBL152293 51683 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 445 5 2 4 5.7 Cc1cc(C)c(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)c(C)c1 10.1021/jm0208572
10907299 51859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 505 7 3 4 5.6 O=C(N/N=C/c1ccc(C(=O)NCCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152464 51859 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 505 7 3 4 5.6 O=C(N/N=C/c1ccc(C(=O)NCCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44373083 59144 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL158989 59144 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 339 3 1 2 5.4 N#Cc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
9946911 60695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL160525 60695 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 359 4 1 3 5.5 O=[N+]([O-])c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
44372471 55335 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 55335 0 None - 0 Mouse 7.3 pIC50 = 7.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
57882748 146741 13 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL3799802 146741 13 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
122189698 130143 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
CHEMBL3616677 130143 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1cncc(-c2nn(C(C)c3ccc(C(=O)NCCC(=O)O)cc3)c3cc(-c4ccc(OC(F)(F)F)cc4)ccc23)c1 10.1016/j.bmcl.2015.08.015
22496449 181216 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44373527 58354 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 493 10 2 8 4.8 COc1cc(/C=N/NC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158330 58354 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 493 10 2 8 4.8 COc1cc(/C=N/NC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
44319257 113857 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccc(F)cc2)ccn1 10.1007/s00044-013-0869-9
CHEMBL315836 113857 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 363 3 1 2 5.9 Cc1cc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccc(F)cc2)ccn1 10.1007/s00044-013-0869-9
CHEMBL409611 219550 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL None None None CC(C)C[C@@H](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](CO)NC(=O)[C@H](N)Cc1c[nH]cn1)[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](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](CCS)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C=O)[C@H](C)O)C(C)C 10.1021/jm960800d
44372677 60532 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160380 60532 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372923 126320 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345834 126320 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 430 9 1 2 8.0 CCCCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372676 126414 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL346698 126414 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 374 5 1 2 6.5 CCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372454 126324 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345863 126324 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
58353104 117045 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237923 117045 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145971123 171855 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4226911 171855 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 572 8 2 5 7.2 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1ccc2ncccc2c1 10.1016/j.bmc.2018.02.036
135819135 101114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1O 10.1016/s0960-894x(02)00143-9
CHEMBL25066 101114 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1O 10.1016/s0960-894x(02)00143-9
135819157 16742 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL114762 16742 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 345 5 2 3 5.5 CCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
10144925 198625 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL519903 198625 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 581 9 4 4 6.4 O=C(NC[C@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
10393937 195167 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
57401358 75750 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 7 2 7 5.6 O=C(Nc1nnn[nH]1)c1ccc(Cn2c(C(=O)c3ccc(OC(F)(F)F)cc3)cc3ccc(C(F)(F)F)cc32)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922914 75750 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 574 7 2 7 5.6 O=C(Nc1nnn[nH]1)c1ccc(Cn2c(C(=O)c3ccc(OC(F)(F)F)cc3)cc3ccc(C(F)(F)F)cc32)cc1 10.1016/j.bmcl.2011.09.105
10962252 52182 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 507 7 3 5 5.6 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)Nc1ccc(Cl)cc1 10.1021/jm0208572
CHEMBL152747 52182 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 507 7 3 5 5.6 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)Nc1ccc(Cl)cc1 10.1021/jm0208572
44319617 113335 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314181 113335 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 441 3 1 2 5.5 Fc1ccc(-c2[nH]c(-c3ccc(I)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL2115192 216041 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)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 10.1021/jm960130b
56602869 133844 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 583 9 2 6 6.7 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)Nc2nnn[nH]2)cc1 nan
CHEMBL3656283 133844 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 583 9 2 6 6.7 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)Nc2nnn[nH]2)cc1 nan
56602870 133853 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 559 10 2 5 5.0 CC1(C2CCCCC2)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656292 133853 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 559 10 2 5 5.0 CC1(C2CCCCC2)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL438574 220557 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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](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 10.1021/jm960800d
CHEMBL411289 219656 0 None - 1 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
57396138 75752 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
CHEMBL1922916 75752 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 572 11 2 4 7.6 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1ccc(C(C)(C)C)cc1 10.1016/j.bmcl.2011.09.105
53469628 117074 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238234 117074 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 641 9 2 4 8.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353132 117004 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237884 117004 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 6.0 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
58352762 117038 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237916 117038 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53320525 63715 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 643 9 2 7 7.7 CC(c1ccc(Cl)cc1)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644199 63715 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 643 9 2 7 7.7 CC(c1ccc(Cl)cc1)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)cc1 10.1016/j.bmcl.2010.11.074
136055807 60270 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 10 2 5 5.7 COc1cc(CC/N=C(\N)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160135 60270 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 482 10 2 5 5.7 COc1cc(CC/N=C(\N)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
20674619 213224 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 4 0 4 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)n2C)cc1 10.1007/s00044-013-0869-9
CHEMBL88045 213224 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 4 0 4 5.7 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)n2C)cc1 10.1007/s00044-013-0869-9
60170765 88152 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccccc2OC(F)(F)F)cc1 10.1021/jm300579z
CHEMBL2159325 88152 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccccc2OC(F)(F)F)cc1 10.1021/jm300579z
16100333 90048 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 599 11 3 5 6.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC(Oc3ccccc3)CC2)cc1 10.1021/jm058026u
CHEMBL218833 90048 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 599 11 3 5 6.2 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC(Oc3ccccc3)CC2)cc1 10.1021/jm058026u
9891138 212925 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 475 11 1 4 7.8 CCCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL86086 212925 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 475 11 1 4 7.8 CCCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCCC)c1 10.1016/s0960-894x(01)00498-x
10030697 185853 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
10053886 198543 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44368911 126634 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL348702 126634 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 472 7 2 4 6.7 CC(C)c1ccc(COc2ccc(/C=N/NC(=O)c3ccc(O)c(Cl)c3)c3ccccc23)cc1 10.1016/s0960-894x(01)00819-8
10992755 54208 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 388 4 3 4 4.1 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1Cl 10.1021/jm0208572
CHEMBL154514 54208 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 388 4 3 4 4.1 O=C(N/N=C/c1ccc(CO)c2ccccc12)c1ccc(O)c(Cl)c1Cl 10.1021/jm0208572
58352834 117032 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237910 117032 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 503 7 2 4 5.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
53325823 63690 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644174 63690 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.2 O=C(Nc1nn[nH]n1)c1ccc(Cc2cn(-c3ccc(OC(F)(F)F)cc3)nc2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
22496373 194281 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.4 O=C(O)CCNC(=O)c1ccc(CN(c2nc(-c3ccc(Cl)c(Cl)c3)cs2)C2CCCc3ccccc32)cc1 10.1021/jm8016249
CHEMBL494248 194281 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.4 O=C(O)CCNC(=O)c1ccc(CN(c2nc(-c3ccc(Cl)c(Cl)c3)cs2)C2CCCc3ccccc32)cc1 10.1021/jm8016249
10257629 194054 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL427644 220139 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
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
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H]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 10.1021/jm990559d
10864629 54189 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccccc2OC(F)(F)F)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL154505 54189 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 557 10 3 6 6.0 O=C(N/N=C/c1ccc(OCCNCc2ccccc2OC(F)(F)F)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
22496459 194021 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
58352762 117038 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237916 117038 0 None - 0 Mouse 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 537 7 2 4 5.9 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccccc2Cl)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10210150 192551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 573 9 4 5 5.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
CHEMBL486650 192551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 573 9 4 5 5.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm7015599
58353104 117045 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237923 117045 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 609 8 2 6 6.5 CCC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11250000 75681 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
CHEMBL1922704 75681 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 566 9 2 9 4.7 CCCOc1ccc2c(c1)n(Cc1ccc(C(=O)Nc3nnn[nH]3)cc1)/c(=N\c1ccc(OC(F)(F)F)cc1)n2C 10.1016/j.bmcl.2011.09.085
16100296 209618 46 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL62444 209618 46 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
141465319 171922 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
CHEMBL4227906 171922 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 527 8 2 5 6.7 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccs1 10.1016/j.bmc.2018.02.036
11633206 120764 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 423 7 3 6 4.0 CCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326187 120764 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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
ChEMBL 423 7 3 6 4.0 CCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
44411059 84045 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 345 6 0 3 4.5 O=C(c1ccc(OCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
CHEMBL208053 84045 0 None - 0 Human 4.3 pIC50 = 4.3 Binding
Inhibition of [125I]glucagon binding to glucagon receptorInhibition of [125I]glucagon binding to glucagon receptor
ChEMBL 345 6 0 3 4.5 O=C(c1ccc(OCCN2CCCC2)cc1)c1cccc2ccccc12 10.1016/j.bmcl.2006.02.013
10393937 195167 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Mouse 6.3 pIC50 = 6.3 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL437465 220502 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[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)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 10.1021/jm010091q
58352925 117023 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237902 117023 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 543 8 2 4 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C3CC3)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44418927 143335 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2C#N)CC1 10.1021/jm058026u
CHEMBL373824 143335 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 588 9 3 5 6.3 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2C#N)CC1 10.1021/jm058026u
16100300 144017 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm058026u
CHEMBL375167 144017 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 615 8 3 3 7.6 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm058026u
16100296 209618 46 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat glucagon receptorInhibition of rat glucagon receptor
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL62444 209618 46 None - 1 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat glucagon receptorInhibition of rat glucagon receptor
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL410553 219604 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CSSC[C@H](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](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)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/jm010091q
145969278 171850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
CHEMBL4226770 171850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 571 8 2 4 7.8 Cc1c(-c2cc(Cl)cc(Cl)c2)nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c1-c1cccc2ccccc12 10.1016/j.bmc.2018.02.036
10438267 63709 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644193 63709 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 583 8 2 9 4.3 CS(=O)(=O)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)n(Cc3ccc(C(=O)Nc4nn[nH]n4)cc3)n2)cc1 10.1016/j.bmcl.2010.11.074
127046968 146681 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
CHEMBL3799439 146681 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 579 9 2 6 6.3 COc1cc(OC)cc(-c2cc(-c3cc(Cl)cc(Cl)c3)nn2C2CCc3cc(C(=O)NCCC(=O)O)ccc32)c1 10.1016/j.bmc.2016.04.053
16100335 90261 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 545 9 3 4 5.9 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC(=C3CC3)CC2)cc1 10.1021/jm058026u
CHEMBL220184 90261 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 545 9 3 4 5.9 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCC(=C3CC3)CC2)cc1 10.1021/jm058026u
164621209 193031 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4873721 193031 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2982 98 46 42 -12.5 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
16224191 75765 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
CHEMBL1922929 75765 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 567 11 2 5 6.9 CCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cnc2ccccc2c1 10.1016/j.bmcl.2011.09.105
44369073 126365 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1ccc(OCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
CHEMBL346226 126365 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 514 7 2 5 6.4 O=C(N/N=C/c1ccc(OCc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1016/s0960-894x(01)00819-8
22496449 181216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL455323 181216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100332 90051 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 10 3 4 6.0 CC(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL218838 90051 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 549 10 3 4 6.0 CC(C)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44372650 60568 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160401 60568 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 344 4 1 2 5.6 COc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44319496 213160 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3cccc(-c4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL87611 213160 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3cccc(-c4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
127047385 146426 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
CHEMBL3797782 146426 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 569 7 2 4 7.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1cccc2ccccc12 10.1016/j.bmc.2016.04.053
56602802 133848 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 491 7 2 6 4.5 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
CHEMBL3656287 133848 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 491 7 2 6 4.5 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
44372471 55335 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL155686 55335 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 422 6 1 2 7.5 CCCOc1ccc(Cl)cc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10167904 180437 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 615 10 4 5 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL453457 180437 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 615 10 4 5 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc(SC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
10168348 181167 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 643 9 4 6 6.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc3c(c2)C(F)(F)OC(F)(F)O3)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL455214 181167 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 643 9 4 6 6.1 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2ccc3c(c2)C(F)(F)OC(F)(F)O3)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
58353063 117021 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237900 117021 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
11352811 185779 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
CHEMBL470955 185779 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 514 6 2 7 5.6 Cc1cc2nc(N(Cc3ccc(C(=O)Nc4nnn[nH]4)cc3)[C@H]3CC[C@H](C(C)(C)C)CC3)n(C)c2cc1C 10.1016/j.bmcl.2008.05.072
44561480 185941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472154 185941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 504 6 2 7 5.1 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(F)ccc21 10.1016/j.bmcl.2008.05.072
54765284 75743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922840 75743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 618 8 2 8 5.9 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189704 130149 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616683 130149 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)c(F)c(F)c2)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL437648 220507 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]1CCC(=O)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2c[nH]cn2)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 10.1021/jm010091q
11039347 52125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 608 7 2 6 5.6 N#Cc1cc(C(=O)N/N=C/c2ccc(OCC(=O)N3CC=C(c4ccc(Br)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL152691 52125 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 608 7 2 6 5.6 N#Cc1cc(C(=O)N/N=C/c2ccc(OCC(=O)N3CC=C(c4ccc(Br)cc4)CC3)c3ccccc23)ccc1O 10.1021/jm0208572
46853081 167543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 564 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
CHEMBL4114081 167543 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 564 10 2 4 8.0 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1csc2c(C#N)cc(Cl)cc12 nan
11103530 171556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 542 10 2 5 5.1 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL421809 171556 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 542 10 2 5 5.1 CN(C)CCN(Cc1ccccc1)C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL414077 219887 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None None 10.1021/jm010091q
10971714 85659 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 414 5 2 6 4.2 N#Cc1cc(C(=O)N/N=C/c2cn(C(=O)CC3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
CHEMBL2112908 85659 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 414 5 2 6 4.2 N#Cc1cc(C(=O)N/N=C/c2cn(C(=O)CC3CCCC3)c3ccccc23)ccc1O 10.1021/jm0208572
10093802 113691 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL314701 113691 4 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 423 5 1 3 7.3 Clc1ccc(-c2nc(-c3ccccc3Oc3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
9891138 212925 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 475 11 1 4 7.8 CCCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCCC)c1 10.1016/s0960-894x(01)00498-x
CHEMBL86086 212925 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 475 11 1 4 7.8 CCCCOc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)c(OCCCC)c1 10.1016/s0960-894x(01)00498-x
11570626 9328 46 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
9135 9328 46 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
CHEMBL1933349 9328 46 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
DB12044 9328 46 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1021/jm300579z
11814151 51590 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 617 7 2 5 6.4 O=C(N/N=C/c1ccc(OCC(=O)N2CC=C(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152207 51590 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 617 7 2 5 6.4 O=C(N/N=C/c1ccc(OCC(=O)N2CC=C(c3ccc(Br)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
60171061 88179 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
CHEMBL2159351 88179 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 611 12 2 6 7.6 CCCOc1cc(Cl)cc(-c2cc(-c3ccc4cc(OC)ccc4c3)n([C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)n2)c1 10.1021/jm300579z
59091612 85657 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 576 8 2 6 6.0 O=C(N/N=C/c1ccc(CS(=O)(=O)Cc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL2112906 85657 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 576 8 2 6 6.0 O=C(N/N=C/c1ccc(CS(=O)(=O)Cc2ccc(OC(F)(F)F)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372946 58530 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
CHEMBL158477 58530 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1cccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)c1 10.1016/s0960-894x(99)00081-5
44372888 60737 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160550 60737 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 330 3 1 1 6.1 Clc1ccc(-c2cc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372671 126895 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL351104 126895 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372478 58629 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158548 58629 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 296 3 1 1 5.5 CC(C)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372477 60977 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160735 60977 0 None - 0 Mouse 7.2 pIC50 = 7.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 336 3 1 1 6.4 Clc1ccc(-c2cc(C3CCCCC3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
145989050 172001 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4229115 172001 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL437048 220480 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
11699553 88155 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
CHEMBL2159328 88155 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 543 8 2 4 6.9 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccccc3c2)cc1 10.1021/jm300579z
71202679 117075 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238235 117075 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 637 7 2 6 7.9 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
57882748 146741 13 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799802 146741 13 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
56602868 133846 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 587 11 2 4 7.2 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656285 133846 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 587 11 2 4 7.2 CC(C)CC1(C)N=C(c2cc(Cl)cc(Cl)c2)C(=O)N1[C@H](CCC(C)(C)C)c1ccc(C(=O)NCCC(=O)O)cc1 nan
22004897 38127 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 313 5 1 2 5.3 C=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140209 38127 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 313 5 1 2 5.3 C=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22005133 101686 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(O)c1 10.1016/s0960-894x(02)00143-9
CHEMBL25421 101686 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 355 8 2 3 5.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1cccc(O)c1 10.1016/s0960-894x(02)00143-9
135437141 11961 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 370 4 3 5 3.7 COc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)cc(Cl)c1O 10.1021/jm000547o
CHEMBL106058 11961 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 370 4 3 5 3.7 COc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)cc(Cl)c1O 10.1021/jm000547o
44319496 213160 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3cccc(-c4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL87611 213160 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 407 4 1 2 7.1 Clc1ccc(-c2nc(-c3cccc(-c4ccccc4)c3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
16100316 148458 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 583 10 3 4 7.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
CHEMBL385528 148458 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 583 10 3 4 7.1 O=C(O)CCNC(=O)c1ccc(CN(C(=O)Nc2ccc(OC(F)(F)F)cc2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm058026u
71450867 85397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 500 9 4 5 4.1 NC(=O)[C@H](Cc1ccccc1)NCc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL2112329 85397 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 500 9 4 5 4.1 NC(=O)[C@H](Cc1ccccc1)NCc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
58353839 117078 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
CHEMBL3238238 117078 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 655 9 2 4 8.7 C[C@H](CC(=O)O)NC(=O)c1ccc([C@@H](CCC(C)(C)C)N2C(=O)C(c3cc(Cl)cc(Cl)c3)=N[C@]23CC[C@@H](C(C)(C)C)CC3)cc1 10.1021/jm401858f
44369346 126541 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 403 5 2 4 4.8 O=C(N/N=C/c1cn(Cc2ccccc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL347922 126541 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 403 5 2 4 4.8 O=C(N/N=C/c1cn(Cc2ccccc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44431012 157685 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL395760 157685 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 607 7 3 7 6.0 O=C(Nc1nn[nH]n1)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
58353350 117033 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237911 117033 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(Cl)c2F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
56602805 133842 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 541 7 2 6 5.7 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656281 133842 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 541 7 2 6 5.7 CC(C)(C)CC[C@H](c1ccc(C(=O)Nc2nnn[nH]2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
11757679 63694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
CHEMBL1644178 63694 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 567 7 2 7 6.6 CC(C)(C)[C@H]1CC[C@H](c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)Nc3nn[nH]n3)cc2)CC1 10.1016/j.bmcl.2010.11.074
44369100 51744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 493 7 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1NC(=O)Cc1csc2ccccc12 10.1021/jm0208572
CHEMBL152348 51744 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 493 7 3 6 5.2 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1NC(=O)Cc1csc2ccccc12 10.1021/jm0208572
145967741 171970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4228690 171970 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
11003592 12064 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 387 5 2 5 4.3 CCn1c2ccccc2c2cc(/C=N/NC(=O)c3ccc(O)c(OC)c3)ccc21 10.1021/jm000547o
CHEMBL106577 12064 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 387 5 2 5 4.3 CCn1c2ccccc2c2cc(/C=N/NC(=O)c3ccc(O)c(OC)c3)ccc21 10.1021/jm000547o
22496459 194021 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
11238814 75676 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
CHEMBL1922699 75676 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 604 7 2 8 6.3 CC(C)n1/c(=N/c2ccc(OC(F)(F)F)cc2)n(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2011.09.085
11678966 88159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
CHEMBL2159332 88159 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3ccc(OC(F)(F)F)cc3c2)cc1 10.1021/jm300579z
44373649 126924 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 481 9 2 5 6.4 COc1cc(/C=C/C(=O)Nc2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL351333 126924 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 481 9 2 5 6.4 COc1cc(/C=C/C(=O)Nc2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
9985258 185762 10 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
90655065 117082 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238243 117082 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 667 9 4 7 7.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC2=NNNN2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL269490 217571 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCC(=O)NCCCC[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)N[C@@H](CCCCN)C(=O)N1)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)O)[C@@H](C)O 10.1021/jm010091q
58352821 117037 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237915 117037 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44373191 126492 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL347462 126492 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 446 9 1 3 7.6 CCCOc1cccc(OCCC)c1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
73355438 99358 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 0 3 4.7 C[S+]([O-])c1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
CHEMBL2435136 99358 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 376 4 0 3 4.7 C[S+]([O-])c1ccc(C2=NC(c3ccncc3)=C(c3ccc(F)cc3)C2)cc1 10.1007/s00044-013-0801-3
11951681 103631 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL265337 103631 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 609 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(C2CCCCC2)cc1 10.1016/j.bmcl.2006.11.014
22496445 178585 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44373924 61707 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 498 9 2 8 4.1 COC(=O)C(Oc1c(OC)cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc1OC)c1ccccc1 10.1016/s0960-894x(01)00819-8
CHEMBL161401 61707 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 498 9 2 8 4.1 COC(=O)C(Oc1c(OC)cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)cc1OC)c1ccccc1 10.1016/s0960-894x(01)00819-8
44373502 176871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 448 9 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)cc2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL444343 176871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 448 9 2 6 4.9 COc1cc(/C=N/NC(=O)c2ccc(O)cc2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
118711433 120761 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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
ChEMBL 385 4 3 6 2.8 O=C(NNC(=O)c1occc1-c1ccc(F)cc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326183 120761 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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
ChEMBL 385 4 3 6 2.8 O=C(NNC(=O)c1occc1-c1ccc(F)cc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
10145290 180002 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 595 10 3 4 7.0 CO[C@H](CNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1)C(=O)O 10.1021/jm7015599
CHEMBL452310 180002 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 595 10 3 4 7.0 CO[C@H](CNC(=O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1)C(=O)O 10.1021/jm7015599
3505 8993 45 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
5311276 8993 45 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
CHEMBL351772 8993 45 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1ccc(cc1c1cc([nH]c1c1ccncc1)c1ccc(cc1)Cl)Br 10.1016/s0960-894x(99)00081-5
10211765 177713 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 659 9 4 4 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Br)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL445532 177713 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 659 9 4 4 6.8 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Br)cc(C(F)(F)F)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1021/jm7015599
58353838 117060 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238220 117060 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 651 8 2 6 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(C(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44561519 185966 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
CHEMBL472325 185966 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 564 6 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Br)ccc21 10.1016/j.bmcl.2008.05.072
11478813 75692 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922715 75692 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 586 8 2 9 5.0 CCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11284982 75740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922837 75740 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 614 10 2 9 5.8 CCCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
57391489 75744 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922841 75744 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 634 9 2 9 5.7 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1cccc(OC(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
122189572 130120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616583 130120 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cc(-c3ccc(C)cc3)ccc21 10.1016/j.bmcl.2015.08.015
122189579 130127 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616590 130127 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 687 11 2 7 8.0 COc1ccc(OC(F)(F)F)cc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
122189695 130140 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616674 130140 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 627 9 2 5 7.5 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(F)cc(F)c2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189717 130162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616696 130162 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 681 12 2 5 9.2 CCCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3cc(F)cc(Cl)c3)cc21 10.1016/j.bmcl.2015.08.015
11826907 54050 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 477 6 2 4 5.3 CCC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL154400 54050 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 477 6 2 4 5.3 CCC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
70695695 85190 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 486 8 4 5 4.5 NC(=O)[C@@H](Cc1ccccc1)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL2111262 85190 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 486 8 4 5 4.5 NC(=O)[C@@H](Cc1ccccc1)Nc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
11527207 88168 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
CHEMBL2159340 88168 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 591 8 2 4 8.1 C[C@@H](c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc2cc(Cl)ccc2c1 10.1021/jm300579z
60170970 88175 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159347 88175 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)ccc4Cl)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11949740 163504 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL407028 163504 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 637 5 3 5 7.6 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)C2CCc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
57393253 75747 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922844 75747 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 636 8 2 8 6.0 CCCOc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(F)c(C(F)(F)F)c1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
121370791 152626 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.3 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2c(C#N)cc(Cl)cc12 nan
CHEMBL3917291 152626 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).Binding Assay: A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 272, 7765-9 (1997); Cascieri, et. al. J Biol Chem 274, 8694-7 (1999)). To determine antagonistic binding affinity of compounds, 0.001-0.003 mg of cell membranes from these cells were pre-incubated with 0.100 mg WGA-coated PVT SPA beads (Amersham) for 20 minutes at room temperature in 25 μL of a buffer containing 50 mM Tris-HCl (pH 7.5), 5 mM MgCl2, 2 mM EDTA, 0.1% BSA and 3% glycerol in Costar 384 well plates with clear bottoms (#3706). Next, 25 μL of 125I-Glucagon (New England Nuclear, MA) (1×10−14 mol per well) and either 1 μL solutions of test compounds or 0.001 mM unlabeled glucagon or DMSO were added and mixed. After 4-12 hours incubation at room temperature, the radioactivity bound to the cell membranes was determined in a radioactive emission detection counter (Wallac-Microbeta).
ChEMBL 578 10 2 4 8.3 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)C(c1ccc(Cl)cc1)c1c(C)sc2c(C#N)cc(Cl)cc12 nan
10918616 53144 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccccc3F)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL153641 53144 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 544 6 2 5 5.0 O=C(N/N=C/c1ccc(CC(=O)N2CCN(c3ccccc3F)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
44372677 60532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160380 60532 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 360 4 1 2 6.1 COc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
145968045 171725 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4224961 171725 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3c(C)c(-c4cccc(C(F)(F)F)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
9902041 68615 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL17736 68615 18 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 330 3 2 3 4.5 Nc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44372688 56202 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 56202 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372397 60521 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160372 60521 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 254 2 1 1 4.4 Clc1ccc(-c2ccc(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372904 60747 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160561 60747 0 None - 0 Mouse 6.2 pIC50 = 6.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10066912 212941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL86250 212941 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 357 4 1 2 6.1 CC(C)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
22005069 38199 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 10 1 2 7.1 CCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140268 38199 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 385 10 1 2 7.1 CCCCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004955 100258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL24616 100258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22004955 100258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR)Tested for its inhibitory activity against human glucagon receptor (hGR)
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL24616 100258 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR)Tested for its inhibitory activity against human glucagon receptor (hGR)
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
44342725 16741 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
CHEMBL114761 16741 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity against human glucagon receptor was determinedBinding affinity against human glucagon receptor was determined
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00736-9
44372638 57420 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 57420 0 None - 0 Mouse 5.2 pIC50 = 5.2 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uMBinding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2 at 1 uM
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44418950 90223 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 555 12 2 4 5.8 O=C(O)CCNC(=O)c1ccc(CN(CCC(c2ccccc2)c2ccccc2)C(=O)c2ccc(Cl)nc2)cc1 10.1021/jm058026u
CHEMBL219882 90223 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 555 12 2 4 5.8 O=C(O)CCNC(=O)c1ccc(CN(CCC(c2ccccc2)c2ccccc2)C(=O)c2ccc(Cl)nc2)cc1 10.1021/jm058026u
44342725 16741 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL114761 16741 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 341 5 1 2 6.1 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
44275085 105871 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 327 4 1 2 6.3 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL280724 105871 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 327 4 1 2 6.3 CC(C)=Cc1c(C(C)C)nc(C(C)C)c(O)c1-c1ccc(F)cc1 10.1016/s0960-894x(02)00143-9
127047254 146716 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
CHEMBL3799656 146716 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 509 7 2 5 5.9 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccco1 10.1016/j.bmc.2016.04.053
45381153 117043 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
CHEMBL3237921 117043 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
122189700 130145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
CHEMBL3616679 130145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 604 10 2 7 6.5 COc1ncccc1-c1nn(C(C)c2ccc(C(=O)NCCC(=O)O)cc2)c2cc(-c3ccc(OC(F)(F)F)cc3)ccc12 10.1016/j.bmcl.2015.08.015
135470389 11715 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 336 4 3 5 3.0 COc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL104735 11715 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 336 4 3 5 3.0 COc1cc(C(=O)N/N=C/c2ccc(O)c3ccccc23)ccc1O 10.1021/jm000547o
58352940 117022 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237901 117022 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.2 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cccc(C(F)(F)F)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10369244 63691 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644175 63691 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 515 9 2 5 5.6 O=C(O)CCNC(=O)c1ccc(Cc2cnn(-c3ccc(OC(F)(F)F)cc3)c2C2CCCCC2)cc1 10.1016/j.bmcl.2010.11.074
10054432 63707 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 1 6 6.6 CN(CCC(=O)O)C(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644191 63707 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 607 10 1 6 6.6 CN(CCC(=O)O)C(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11527170 88163 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159336 88163 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 587 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
10973527 56678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 537 9 3 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1NC(=O)COc1ccc(OC(F)(F)F)cc1 10.1021/jm0208572
CHEMBL156828 56678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 537 9 3 7 4.7 COc1cc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc1NC(=O)COc1ccc(OC(F)(F)F)cc1 10.1021/jm0208572
53324505 63714 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 647 11 2 5 8.2 CC(c1ccc(Cl)cc1)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644198 63714 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 647 11 2 5 8.2 CC(c1ccc(Cl)cc1)c1ccc(-c2cc(-c3ccc(OC(F)(F)F)cc3)nn2Cc2ccc(C(=O)NCCC(=O)O)cc2)cc1 10.1016/j.bmcl.2010.11.074
44318934 212775 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL84840 212775 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 387 6 1 2 6.8 CCCCc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL2369127 216370 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]glucagon binding towards Glucagon receptorInhibition of [125I]glucagon binding towards Glucagon receptor
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](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 10.1021/jm960130b
44373463 175305 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1c(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc(OCc2ccc(C(C)C)cc2)c1C 10.1016/s0960-894x(01)00819-8
CHEMBL435445 175305 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 450 7 2 4 6.1 Cc1c(/C=N/NC(=O)c2ccc(O)c(Cl)c2)ccc(OCc2ccc(C(C)C)cc2)c1C 10.1016/s0960-894x(01)00819-8
11057703 85306 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 368 5 2 4 4.1 COCc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL2112041 85306 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 368 5 2 4 4.1 COCc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44318950 113783 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL315311 113783 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Affinity for human glucagon receptor in presence of Mg2+Affinity for human glucagon receptor in presence of Mg2+
ChEMBL 457 3 1 2 6.1 Clc1ccc(-c2nc(-c3ccc(I)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
45381153 117043 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
CHEMBL3237921 117043 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 607 7 2 6 6.2 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cc(Cl)cc(Cl)c1)C(=O)N2[C@@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)C1CC1 10.1021/jm401858f
22005107 42103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 7 1 2 6.0 CCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL143698 42103 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 343 7 1 2 6.0 CCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22005273 38196 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 301 4 1 2 4.9 Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140267 38196 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 301 4 1 2 4.9 Cc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
10030697 185853 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL471580 185853 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
11950972 168011 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
CHEMBL411832 168011 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 601 6 3 7 6.3 CC(C)(C)[C@H]1CC[C@H](N(C(=O)Nc2ccc(OC(F)(F)F)cc2)C2CCOc3cc(C(=O)Nc4nn[nH]n4)ccc32)CC1 10.1016/j.bmcl.2006.11.014
22496477 179556 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL451288 179556 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
58352961 117007 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237887 117007 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1cccc(Cl)c1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
20776097 176220 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 613 9 2 5 7.9 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL442651 176220 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 613 9 2 5 7.9 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
122189574 130122 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
CHEMBL3616585 130122 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 629 11 2 5 8.3 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2cc(C(F)(F)F)ccc2OC)c2cccc(-c3ccc(C)cc3)c21 10.1016/j.bmcl.2015.08.015
44278169 166018 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
IC50 value was expressed for inhibition of [125]glucagon specific binding.IC50 value was expressed for inhibition of [125]glucagon specific binding.
ChEMBL 2699 87 36 34 -7.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](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](Cc1ccc2ccccc2c1)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 10.1021/jm000453e
91931637 166018 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
IC50 value was expressed for inhibition of [125]glucagon specific binding.IC50 value was expressed for inhibition of [125]glucagon specific binding.
ChEMBL 2699 87 36 34 -7.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](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](Cc1ccc2ccccc2c1)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 10.1021/jm000453e
CHEMBL409896 166018 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
IC50 value was expressed for inhibition of [125]glucagon specific binding.IC50 value was expressed for inhibition of [125]glucagon specific binding.
ChEMBL 2699 87 36 34 -7.0 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](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](Cc1ccc2ccccc2c1)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 10.1021/jm000453e
10474631 112729 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL312928 112729 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 375 3 1 2 5.6 Brc1ccc(-c2nc(-c3ccccc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
16100331 103794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 606 12 3 5 5.3 CCN(CC)C(=O)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
CHEMBL266715 103794 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 606 12 3 5 5.3 CCN(CC)C(=O)C1CCC(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1021/jm058026u
44373564 59025 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 518 10 2 7 5.1 COc1cc(/C=N/NS(=O)(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL158886 59025 0 None - 0 Human 4.1 pIC50 = 4.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 518 10 2 7 5.1 COc1cc(/C=N/NS(=O)(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
10257629 194054 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL492813 194054 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.5 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
44372688 56202 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL156458 56202 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 388 6 1 2 6.9 CCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
10282059 180003 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 593 9 4 4 5.9 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Br)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
CHEMBL452311 180003 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 593 9 4 4 5.9 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cccc(Br)c2)c2ccc(C3CCCCC3)cc2)cc1 10.1021/jm7015599
11764615 194991 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL499160 194991 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
122189575 130123 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616586 130123 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 644 12 2 5 8.6 CCCC(c1ccc(C(=O)NCCC(=O)O)cc1)n1cc(-c2cc(C(F)(F)F)ccc2OC)c2ccc(-c3ccc(OC)cc3)cc21 10.1016/j.bmcl.2015.08.015
122189701 130146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
CHEMBL3616680 130146 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranesDisplacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes
ChEMBL 609 9 2 5 7.4 CC(c1ccc(C(=O)NCCC(=O)O)cc1)n1nc(-c2ccc(F)cc2F)c2ccc(-c3ccc(OC(F)(F)F)cc3)cc21 10.1016/j.bmcl.2015.08.015
164612237 191658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4852725 191658 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3371 111 53 49 -17.2 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11657413 88158 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
CHEMBL2159331 88158 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 627 9 2 5 7.8 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc3cc(OC(F)(F)F)ccc3c2)cc1 10.1021/jm300579z
11592461 88171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159343 88171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 601 10 2 5 7.9 CCOc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11490393 75689 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922712 75689 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 606 7 2 9 5.0 COc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11456187 75738 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922835 75738 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 600 9 2 9 5.4 CCCOc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
11091831 54838 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 463 5 2 4 4.9 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
CHEMBL155065 54838 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 463 5 2 4 4.9 CC1CCCCN1C(=O)Cc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1021/jm0208572
44369092 57290 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 463 6 3 4 6.2 O=C(N/N=C/c1ccc(NCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL157380 57290 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 463 6 3 4 6.2 O=C(N/N=C/c1ccc(NCc2ccc(Cl)cc2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
10363819 113854 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
CHEMBL315828 113854 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 403 7 1 3 6.6 CCCCOc1ccccc1-c1[nH]c(-c2ccc(Cl)cc2)nc1-c1ccncc1 10.1016/s0960-894x(01)00498-x
12967031 118349 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL328126 118349 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372948 58780 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL158676 58780 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 402 7 1 2 7.2 CCCCOc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
145970930 171929 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227964 171929 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4ccc(Cl)c(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
11180162 75686 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922709 75686 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 534 6 2 7 4.9 CCc1cc(C(F)(F)F)cc2c1n(C)/c(=N/c1ccc(C)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
16100306 143449 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1021/jm058026u
CHEMBL374022 143449 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 547 8 3 3 6.8 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cc(Cl)cc(Cl)c2)CC1 10.1021/jm058026u
12967034 126802 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL350255 126802 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 408 3 1 1 6.8 Clc1ccc(-c2cc(-c3cccc(Br)c3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
5169 105523 109 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 331 3 2 3 4.7 Oc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL278041 105523 109 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 331 3 2 3 4.7 Oc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
44319591 113357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL314238 113357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 349 3 1 2 5.6 Fc1ccc(-c2[nH]c(-c3ccc(Cl)cc3)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
164624673 192770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4870133 192770 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3012 98 46 42 -12.4 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)C(Cc1ccccc1)C(=O)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
12967031 118349 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL328126 118349 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3ccc(Cl)cc3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
44372671 126895 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL351104 126895 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the murine glucagon receptor (GGR) expressed on CHO cells in absence of Mg+2
ChEMBL 388 5 1 3 5.8 O=C(OCc1ccccc1)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
56602806 133841 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 2 4 6.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL3656280 133841 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 545 9 2 4 6.1 CC(C)(C)CC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=NC1(C)C nan
CHEMBL411785 219734 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
IC50 value was expressed as inhibition of [125]glucagon specific binding.IC50 value was expressed as inhibition of [125]glucagon specific binding.
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(C)=O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/jm000453e
22005361 106684 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(Cl)cc1 10.1016/s0960-894x(02)00143-9
CHEMBL286098 106684 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 373 8 1 2 6.9 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(Cl)cc1 10.1016/s0960-894x(02)00143-9
135819146 117103 9 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL323913 117103 9 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 359 6 2 3 5.8 CCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
135819133 121191 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
CHEMBL333147 121191 3 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity of first enantiomer (E1) against human glucagon receptor was determinedBinding affinity of first enantiomer (E1) against human glucagon receptor was determined
ChEMBL 387 8 2 3 6.6 CCCCCc1c(C(C)C)nc(C(C)C)c(C(C)O)c1-c1ccc(F)cc1O 10.1016/s0960-894x(02)00736-9
15407872 66908 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17396 66908 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 340 3 1 3 4.8 N#Cc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
58352821 117037 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237915 117037 0 None - 0 Mouse 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 587 8 2 5 6.1 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(OC(F)(F)F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44372405 58774 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
CHEMBL158671 58774 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 314 3 1 1 5.6 Fc1ccc(-c2cc(-c3ccccc3)[nH]c2-c2ccncc2)cc1 10.1007/s00044-013-0801-3
20776096 179340 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448584 179340 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 629 10 2 6 7.8 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
60170969 88174 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159346 88174 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 499 8 2 5 5.8 COc1ccc2cc(-c3cc(C(C)(C)C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
9929037 60658 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160490 60658 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 364 3 1 1 6.7 Clc1ccc(-c2cc(-c3ccc(Cl)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
58353063 117021 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237900 117021 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 555 7 2 4 6.0 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(F)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10097880 63635 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1643954 63635 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 511 7 2 7 5.3 O=C(Nc1nn[nH]n1)c1ccc(Cn2nc(C3CCCCC3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
11068479 12009 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 363 5 2 5 3.4 COc1cc(C(=O)N/N=C/c2ccc(N(C)C)c3ccccc23)ccc1O 10.1021/jm000547o
CHEMBL106294 12009 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 363 5 2 5 3.4 COc1cc(C(=O)N/N=C/c2ccc(N(C)C)c3ccccc23)ccc1O 10.1021/jm000547o
11764614 195470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
CHEMBL504156 195470 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 631 8 4 4 6.5 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NC[C@H](O)C(=O)O)cc2)C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)CC1 10.1021/jm7015599
58353206 117044 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237922 117044 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 595 7 2 6 6.2 CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10053886 198543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL519776 198543 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 575 10 2 6 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(Cl)cc2)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44431011 103630 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 611 9 3 5 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
CHEMBL265336 103630 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cellsDisplacement of [125]glucagon from human glucagon receptor expressed in CHO cells
ChEMBL 611 9 3 5 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2N(C(=O)Nc1ccc(OC(F)(F)F)cc1)c1ccc(OC(F)(F)F)cc1 10.1016/j.bmcl.2006.11.014
135544439 115629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 3 3 4 3.8 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Br)c1 10.1021/jm000547o
CHEMBL321010 115629 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity for human Glucagon ReceptorBinding affinity for human Glucagon Receptor
ChEMBL 384 3 3 4 3.8 O=C(N/N=C/c1ccc(O)c2ccccc12)c1ccc(O)c(Br)c1 10.1021/jm000547o
22496459 194021 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity to glucagon receptor in mouse liver membrane by membrane filter assayBinding affinity to glucagon receptor in mouse liver membrane by membrane filter assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44372870 60417 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160287 60417 0 None - 0 Mouse 6.1 pIC50 = 6.1 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of 125 I-glucagon to the murine glucagon receptor (mGLUR) expressed on CHO cells in presence of Mg+2
ChEMBL 466 6 1 2 7.6 CCCOc1cc(Br)ccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
56602997 133855 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 491 9 2 5 3.4 CC1(C)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
CHEMBL3656294 133855 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 491 9 2 5 3.4 CC1(C)N=C(c2ccc(OC(F)(F)F)cc2)C(=O)N1CCc1ccc(C(=O)NCCC(=O)O)cc1 nan
45381049 117066 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238226 117066 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 618 8 2 7 6.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cncc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
9985625 63699 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644183 63699 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2010.11.074
9824797 52500 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL153038 52500 0 None - 1 Human 7.1 pIC50 = 7.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 445 6 2 4 5.9 CC(C)c1ccc(Cn2ccc3c(/C=N/NC(=O)c4ccc(O)c(Cl)c4)cccc32)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL414490 219913 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Glucagon receptor binding measured as 50% inhibitory concentrationGlucagon receptor binding measured as 50% inhibitory concentration
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2c[nH]cn2)C(=O)N[C@@H]([C@@H](C)O)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 10.1021/jm010091q
127047904 146607 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
CHEMBL3799017 146607 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 601 9 2 5 7.7 COc1ccc2cc(-c3cc(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCC(C)C(=O)O)cc3)ccc2c1 10.1016/j.bmc.2016.04.053
56602747 133849 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 505 8 2 6 4.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
CHEMBL3656288 133849 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.Glucagon Receptor Binding Assay: Recombinant human glucagon receptor (huGlucR) membranes and mouse glucagon receptor (mGlucR) membranes were prepared in-house from huGlucR/clone 103c/CHO and mouse liver tissue, respectively. 0.03 ug/li huGluR membranes (or 0.5 ug/ml mGlucR) was incubated in assay buffer containing 0.05 nM 125I-Glucagon (Perkin Elmer, NEX 207) and varying concentrations of antagonist at room temperature for 60 to 90 (assay buffer: 50 mM HEPES, 1 mM MgCl2, 1 mM CaCl2, 1 mg/ml BSA, COMPLETE protease inhibitor cocktail, pH 7.4). The total volume of the assay was 200 ul. The assay was performed at room temperature using 96-deep well plate.
ChEMBL 505 8 2 6 4.2 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nnn[nH]2)cc1)N1C(=O)C(c2cccc(F)c2)=NC1(C)C nan
58352863 117025 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237904 117025 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 521 7 2 4 5.4 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
44561287 195459 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 613 9 2 8 8.0 O=C(Nc1nnn[nH]1)c1ccc(CN(c2ccc(Oc3ccc(Cl)cc3)c(Cl)c2)c2nc(-c3ccccc3)cs2)cc1 10.1016/j.bmcl.2008.05.072
CHEMBL503919 195459 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 613 9 2 8 8.0 O=C(Nc1nnn[nH]1)c1ccc(CN(c2ccc(Oc3ccc(Cl)cc3)c(Cl)c2)c2nc(-c3ccccc3)cs2)cc1 10.1016/j.bmcl.2008.05.072
22496445 178585 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44373103 60917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160690 60917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 386 5 1 3 5.7 CCOC(=O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372856 126800 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 370 3 1 1 6.8 CC(C)(C)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL350237 126800 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 370 3 1 1 6.8 CC(C)(C)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
71202712 117076 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238236 117076 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 657 9 3 5 7.3 CC(C)(C)CC[C@H](c1ccc(C(=O)NC[C@H](O)C(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22496431 176605 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 647 11 2 5 9.6 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(Cl)cc3)c(-c3ccccc3)s2)cc1 10.1021/jm8016249
CHEMBL443971 176605 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 647 11 2 5 9.6 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C3=CCCCC3)cc2)c2nc(-c3ccc(Cl)cc3)c(-c3ccccc3)s2)cc1 10.1021/jm8016249
22496459 194021 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL492605 194021 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
9985625 63699 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
CHEMBL1644183 63699 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3cc(Cl)cc(Cl)c3)cc2-c2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm300579z
44319681 212883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 4 0 4 5.7 CSc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)n2C)cc1 10.1007/s00044-013-0869-9
CHEMBL85713 212883 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 375 4 0 4 5.7 CSc1ccc(-c2nc(-c3ccncc3)c(-c3ccc(F)cc3)n2C)cc1 10.1007/s00044-013-0869-9
11532336 120754 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 443 5 3 6 4.3 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326175 120754 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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
ChEMBL 443 5 3 6 4.3 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
10450820 56948 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 354 4 2 4 4.0 COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
CHEMBL157064 56948 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 354 4 2 4 4.0 COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12 10.1016/s0960-894x(01)00819-8
3652254 130466 7 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 364 7 2 3 4.8 CCC(CC)C(=O)Nc1sc2c(c1C(N)=O)CCC(C(C)(C)CC)C2 10.1016/j.bmcl.2005.01.003
CHEMBL362169 130466 7 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 364 7 2 3 4.8 CCC(CC)C(=O)Nc1sc2c(c1C(N)=O)CCC(C(C)(C)CC)C2 10.1016/j.bmcl.2005.01.003
10133915 68543 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
CHEMBL17722 68543 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50Binding affinity towards human glucagon receptor in absence of Mg2+ expressed as IC50
ChEMBL 373 4 1 4 4.7 COC(=O)c1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(01)00498-x
44373708 62056 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 10 3 6 5.2 COc1cc(CNNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL161827 62056 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 484 10 3 6 5.2 COc1cc(CNNC(=O)c2ccc(O)c(Cl)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
11754125 85726 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
CHEMBL2112992 85726 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 462 7 1 6 6.3 CCC(CC)C(=O)Nc1sc(-c2nc(Cc3ccc(Cl)cc3Cl)no2)c(C)c1C#N 10.1016/j.bmcl.2005.01.003
11827809 53383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 556 9 3 6 4.7 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)NC1CCN(Cc2ccccc2)C1 10.1021/jm0208572
CHEMBL153838 53383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 556 9 3 6 4.7 O=C(COc1ccc(/C=N/NC(=O)c2ccc(O)c(Cl)c2)c2ccccc12)NC1CCN(Cc2ccccc2)C1 10.1021/jm0208572
58352868 117019 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237898 117019 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 585 8 2 4 6.6 CC(CN1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2)c1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
127045652 146482 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
CHEMBL3798135 146482 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting methodDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHO-K1 cells after 3 hrs by scintillation counting method
ChEMBL 537 7 2 4 6.4 O=C(O)CCNC(=O)c1ccc2c(c1)CCC2n1nc(-c2cc(Cl)cc(Cl)c2)cc1-c1ccc(F)cc1 10.1016/j.bmc.2016.04.053
11617576 120756 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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
ChEMBL 367 4 3 6 2.6 O=C(NNC(=O)c1occc1-c1ccccc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
CHEMBL3326178 120756 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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
ChEMBL 367 4 3 6 2.6 O=C(NNC(=O)c1occc1-c1ccccc1)c1ccc(O)c([N+](=O)[O-])c1 10.1016/j.bmcl.2014.07.025
9916972 181808 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 613 10 4 5 6.2 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
CHEMBL456738 181808 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 613 10 4 5 6.2 COc1cc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc(C(F)(F)F)c1 10.1021/jm7015599
10282370 195476 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 608 9 4 5 6.0 N#Cc1ccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc1C(F)(F)F 10.1021/jm7015599
CHEMBL504245 195476 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 608 9 4 5 6.0 N#Cc1ccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)cc1C(F)(F)F 10.1021/jm7015599
10144347 201171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 561 10 4 5 5.9 CSc1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
CHEMBL528775 201171 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Binding affinity to human cloned GluR expressed in BHK cellsBinding affinity to human cloned GluR expressed in BHK cells
ChEMBL 561 10 4 5 5.9 CSc1cccc(NC(=O)N(Cc2ccc(C(=O)NC[C@@H](O)C(=O)O)cc2)c2ccc(C3CCCCC3)cc2)c1 10.1021/jm7015599
164628536 193244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4876736 193244 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 2971 96 46 42 -12.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](O)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
11432140 182908 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL459208 182908 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 506 7 2 7 5.7 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(C3CCCCC3)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44561556 196058 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
CHEMBL511964 196058 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 554 6 2 7 6.3 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)[C@H]2CC[C@H](C(C)(C)C)CC2)nc2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2008.05.072
57399594 75767 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
CHEMBL1922930 75767 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by scintillation proximity assay
ChEMBL 585 11 2 5 6.7 CCC[C@@H](Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)c1cc2cc(Cl)ccc2n1-c1cccc(C(F)(F)F)n1 10.1016/j.bmcl.2011.09.105
10929597 56765 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 540 7 2 5 4.9 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccccc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL156904 56765 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 540 7 2 5 4.9 O=C(N/N=C/c1ccc(CC(=O)N2CCN(Cc3ccccc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
60171062 88180 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
CHEMBL2159352 88180 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assayDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay
ChEMBL 601 9 2 5 7.5 COc1ccc2cc(-c3cc(-c4cc(C(F)(F)F)ccc4C)nn3[C@@H](C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1021/jm300579z
11353908 75741 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
CHEMBL1922838 75741 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation countingDisplacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting
ChEMBL 600 8 2 9 5.4 CC(C)Oc1cc(Cl)cc2c1n(C)/c(=N/c1ccc(OC(F)(F)F)cc1)n2Cc1ccc(C(=O)Nc2nnn[nH]2)cc1 10.1016/j.bmcl.2011.09.085
44372638 57420 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL157529 57420 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 332 3 1 1 5.7 Fc1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1016/s0960-894x(99)00081-5
44372454 126324 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL345863 126324 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 326 4 1 3 4.6 CCOC(=O)c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
44372406 126594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL348401 126594 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2
ChEMBL 320 3 1 1 5.9 Fc1ccc(-c2cc(C3CCCCC3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
58353323 117061 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238221 117061 0 None - 0 Mouse 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 601 8 2 6 6.4 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2ccc(F)cc2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
145967685 171889 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
CHEMBL4227364 171889 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysisDisplacement of [125I]-glucagon from wild type human glucagon receptor expressed in CHOK1 cells after 3 hrs by micro beta scintillation counting analysis
ChEMBL 601 9 2 5 7.8 COc1ccc2cc(-c3c(C)c(-c4cc(Cl)cc(Cl)c4)nn3C(C)c3ccc(C(=O)NCCC(=O)O)cc3)ccc2c1 10.1016/j.bmc.2018.02.036
11352703 185677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 508 7 2 8 4.6 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
CHEMBL469903 185677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 508 7 2 8 4.6 Cn1c(N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2ccc(OC(F)(F)F)cc2)nc2ccccc21 10.1016/j.bmcl.2008.05.072
44372376 172163 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 358 4 2 2 5.2 O=C(O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
CHEMBL423781 172163 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human glucagon receptorAntagonist activity at human glucagon receptor
ChEMBL 358 4 2 2 5.2 O=C(O)c1ccc(-c2cc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0801-3
10246001 170285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
CHEMBL420232 170285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 329 3 1 2 5.3 Cc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)[nH]2)cc1 10.1007/s00044-013-0869-9
9886904 213127 19 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccccc3Br)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
CHEMBL87365 213127 19 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 393 3 1 2 5.7 Fc1ccc(-c2[nH]c(-c3ccccc3Br)nc2-c2ccncc2)cc1 10.1007/s00044-013-0869-9
11049295 53721 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 493 7 3 7 4.8 COc1ccc2oc(C(=O)Nc3ccc(/C=N/NC(=O)c4ccc(O)c(Cl)c4)c(OC)c3)cc2c1 10.1021/jm0208572
CHEMBL154125 53721 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 493 7 3 7 4.8 COc1ccc2oc(C(=O)Nc3ccc(/C=N/NC(=O)c4ccc(O)c(Cl)c4)c(OC)c3)cc2c1 10.1021/jm0208572
18926938 175386 25 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 331 6 1 3 4.8 COCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL436011 175386 25 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 331 6 1 3 4.8 COCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22005050 101441 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1F 10.1016/s0960-894x(02)00143-9
CHEMBL25255 101441 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Tested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cellsTested for its inhibitory activity against human glucagon receptor (hGR) expressed in CHO cells
ChEMBL 357 8 1 2 6.4 CCCCCc1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccccc1F 10.1016/s0960-894x(02)00143-9
44372904 60747 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
CHEMBL160561 60747 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 388 5 1 2 6.9 CC(C)Oc1ccccc1-c1cc(-c2ccc(Cl)cc2)[nH]c1-c1ccncc1 10.1016/s0960-894x(99)00081-5
9985258 185762 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
10393937 195167 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL501628 195167 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 609 10 2 6 7.3 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
44389632 70044 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
CHEMBL179181 70044 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cellsInhibitory concentration towards binding of [125I]glucagon to the human glucagon receptor expressed in CHO cells
ChEMBL 463 7 1 4 6.3 CCC(CC)C(=O)Nc1sc2c(c1C#N)CCC(N(C)Cc1ccc(Cl)cc1Cl)C2 10.1016/j.bmcl.2005.01.003
9985258 185762 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL470729 185762 10 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 559 9 2 5 7.0 O=C(O)CCNC(=O)c1ccc(CN(c2ccc(C(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
22496557 200040 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
CHEMBL523847 200040 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 5 7.8 Cc1cc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)ccc1C(C)C 10.1021/jm8016249
22496457 179337 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL448561 179337 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 579 9 2 5 7.6 O=C(O)CCNC(=O)c1ccc(N(Cc2ccc3c(c2)Cc2ccccc2-3)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
118711432 120760 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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
ChEMBL 397 5 3 7 2.6 COc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326182 120760 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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
ChEMBL 397 5 3 7 2.6 COc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
21704177 213223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 362 4 0 4 5.9 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)o2)cc1 10.1007/s00044-013-0869-9
CHEMBL88044 213223 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assayInhibition of human glucagon receptor expressed in CHO cell membranes by radioligand displacement assay
ChEMBL 362 4 0 4 5.9 CSc1ccc(-c2nc(-c3ccc(F)cc3)c(-c3ccncc3)o2)cc1 10.1007/s00044-013-0869-9
58353232 117009 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237889 117009 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 523 7 2 4 5.3 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(Cl)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
44373554 60423 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 463 9 3 7 4.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
CHEMBL160291 60423 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
In vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagonIn vitro inhibitory activity against human glucagon receptor using [127I]-labeled glucagon
ChEMBL 463 9 3 7 4.5 COc1cc(/C=N/NC(=O)c2ccc(O)c(N)c2)cc(OC)c1OCc1ccc(C(C)C)cc1 10.1016/s0960-894x(01)00819-8
58352952 117029 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237908 117029 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2ccc(Cl)c(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
10008376 63697 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
CHEMBL1644181 63697 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 577 9 2 5 6.7 O=C(O)CCNC(=O)c1ccc(Cn2nc(-c3ccc(OC(F)(F)F)cc3)cc2-c2cc(Cl)cc(Cl)c2)cc1 10.1016/j.bmcl.2010.11.074
164627630 193119 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4875003 193119 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3033 97 46 42 -11.7 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
12967033 60843 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160638 60843 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 382 3 1 1 6.9 Fc1ccc(-c2cc(-c3ccc(Cl)cc3Cl)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
11238149 195698 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 548 7 2 7 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2-c2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
CHEMBL507829 195698 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]glucagon from human GCGR expressed in CHO cellsDisplacement of [125I]glucagon from human GCGR expressed in CHO cells
ChEMBL 548 7 2 7 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)Nc3nnn[nH]3)cc2)c2nc3ccccc3n2-c2ccccc2)CC1 10.1016/j.bmcl.2008.05.072
68862222 120748 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 398 4 3 4 4.4 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326165 120748 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 398 4 3 4 4.4 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)cc1 10.1016/j.bmcl.2014.07.025
68862226 120755 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 428 5 3 5 4.4 COc1cc(C(=O)NNC(=O)c2occ(-c3ccccc3)c2-c2ccccc2)ccc1O 10.1016/j.bmcl.2014.07.025
CHEMBL3326176 120755 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 428 5 3 5 4.4 COc1cc(C(=O)NNC(=O)c2occ(-c3ccccc3)c2-c2ccccc2)ccc1O 10.1016/j.bmcl.2014.07.025
22004908 38247 25 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 345 5 1 4 4.4 COC(=O)c1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
CHEMBL140317 38247 25 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibitory concentration against binding to the human glucagon receptor (hGR)Inhibitory concentration against binding to the human glucagon receptor (hGR)
ChEMBL 345 5 1 4 4.4 COC(=O)c1c(C(C)C)nc(C(C)C)c(CO)c1-c1ccc(F)cc1 10.1016/s0960-894x(01)00766-1
22496445 178585 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL446821 178585 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assayBinding affinity to human recombinant glucagon receptor expressed in BHK cells by membrane filter assay
ChEMBL 581 10 2 6 6.7 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
90655064 117068 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3238228 117068 0 None - 0 Mouse 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 652 8 2 7 6.7 CC(C)(C)CC[C@H](c1ccc(C(=O)NCc2nn[nH]n2)cc1)N1C(=O)C(c2cnccc2C(F)(F)F)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
58353013 117016 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
CHEMBL3237895 117016 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from recombinant human GCGR expressed in CHO cells after 60 mins by scintillation counting analysis
ChEMBL 571 7 2 4 6.5 C[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)N1C(=O)C(c2cc(Cl)cc(Cl)c2)=N[C@]12CC[C@@H](C(C)(C)C)CC2 10.1021/jm401858f
22496384 193926 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL491920 193926 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 558 9 2 4 7.1 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(Cl)cc2)c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm8016249
16100334 90149 2 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm058026u
CHEMBL219384 90149 2 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human cloned glucagon receptor expressed in BHK cellsInhibition of human cloned glucagon receptor expressed in BHK cells
ChEMBL 557 9 3 4 6.3 CC(C)(C)c1ccc(N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1021/jm058026u
11731304 51983 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 546 7 2 5 5.9 O=C(N/N=C/c1ccc(CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
CHEMBL152579 51983 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cellsIn vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells
ChEMBL 546 7 2 5 5.9 O=C(N/N=C/c1ccc(CN2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12)c1ccc(O)c(Cl)c1 10.1021/jm0208572
58353489 117008 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
CHEMBL3237888 117008 0 None - 0 Mouse 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysisDisplacement of [125I]-glucagon from GCGR in mouse liver membranes after 60 mins by scintillation counting analysis
ChEMBL 557 7 2 4 5.7 CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(c1ccc(C(F)(F)F)cc1)C(=O)N2Cc1ccc(C(=O)NCCC(=O)O)cc1 10.1021/jm401858f
68860750 120765 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326188 120765 1 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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
ChEMBL 437 8 3 6 4.4 CCCCCc1ccc(-c2ccoc2C(=O)NNC(=O)c2ccc(O)c([N+](=O)[O-])c2)cc1 10.1016/j.bmcl.2014.07.025
118711430 120749 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 399 4 3 5 3.8 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)nc1 10.1016/j.bmcl.2014.07.025
CHEMBL3326170 120749 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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
ChEMBL 399 4 3 5 3.8 O=C(NNC(=O)c1occ(-c2ccccc2)c1-c1ccccc1)c1ccc(O)nc1 10.1016/j.bmcl.2014.07.025
22496448 194100 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
CHEMBL493020 194100 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 574 10 2 5 6.9 O=C(O)CCNC(=O)c1ccc(CC(c2ccc(OC(F)(F)F)cc2)c2nc(-c3ccc(Cl)cc3)cs2)cc1 10.1021/jm8016249
164609271 191207 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3357 110 52 49 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CN(CCC(=O)O)C(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
CHEMBL4846293 191207 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting methodDisplacement of 125I-glucagon from human GCGR expressed in HEK293 cells membranes incubated for 6 hrs by liquid scintillation counting method
ChEMBL 3357 110 52 49 -17.6 CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CN(CCC(=O)O)C(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02069
20775916 193868 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 7.1 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
CHEMBL491352 193868 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assayDisplacement of [125I]porcine glucagon from human recombinant glucagon receptor expressed in BHK cells by scintillation proximity assay
ChEMBL 565 9 2 5 7.1 O=C(O)CCNC(=O)c1ccc(CN(c2ccc3c(c2)CCC3)c2nc(-c3ccc(Cl)c(Cl)c3)cs2)cc1 10.1021/jm8016249
12967032 60411 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL160281 60411 0 None - 0 Human 6.0 pIC50 = 6 Binding
Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2Binding affinity towards glucagon receptor determined by reduction in binding of [125I]glucagon to the human glucagon receptor (GGR) expressed on CHO cells in presence of Mg+2
ChEMBL 348 3 1 1 6.2 Fc1ccc(-c2cc(-c3cccc(Cl)c3)[nH]c2-c2ccncc2)cc1 10.1016/s0960-894x(99)00081-5
CHEMBL437095 220485 0 None - 1 Rat 6.4 pKd = 6.4 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
CHEMBL2369990 216545 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
CHEMBL438218 220534 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
CHEMBL438574 220557 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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](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 10.1021/jm960800d
CHEMBL409611 219550 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CC(C)C[C@@H](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](CO)NC(=O)[C@H](N)Cc1c[nH]cn1)[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](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](CCS)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C=O)[C@H](C)O)C(C)C 10.1021/jm960800d
CHEMBL429198 220291 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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 10.1021/jm960800d
CHEMBL442499 220693 0 None - 1 Rat 6.3 pKd = 6.3 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](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 10.1021/jm960800d
CHEMBL268636 217541 0 None - 1 Rat 8.2 pKd = 8.2 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
CHEMBL441209 220666 0 None - 1 Rat 8.2 pKd = 8.2 Binding
pA2 value towards glucagon receptor relative to glucagon was calculatedpA2 value towards glucagon receptor relative to glucagon was calculated
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](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(N)=O)[C@@H](C)O 10.1016/0960-894X(95)00307-F
CHEMBL267885 217515 0 None - 1 Rat 6.2 pKd = 6.2 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@H](NC(=O)CNC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
CHEMBL412352 219764 0 None - 1 Rat 6.2 pKd = 6.2 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
CHEMBL427744 220149 0 None - 1 Rat 6.2 pKd = 6.2 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
CHEMBL439271 220608 0 None - 1 Rat 6.2 pKd = 6.2 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](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 10.1021/jm960800d
CHEMBL427744 220149 0 None - 1 Rat 6.1 pKd = 6.1 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@H](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 10.1021/jm960800d
CHEMBL411289 219656 0 None - 1 Rat 6.1 pKd = 6.1 Binding
pA2 value against Glucagon ReceptorpA2 value against Glucagon Receptor
ChEMBL None None None CSCC[C@@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](CO)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CO)NC(=O)[C@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](N)CO)[C@H](C)O)[C@H](C)O)C(C)C)C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](C(N)=O)[C@H](C)O 10.1021/jm960800d
60152349 96909 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 476 10 3 7 3.8 CCCC(Nc1cnc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381823 96909 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 476 10 3 7 3.8 CCCC(Nc1cnc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71059951 136687 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)c(F)c2)cn1 nan
CHEMBL3675841 136687 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)c(F)c2)cn1 nan
71059820 136746 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3F)cc2)cn1 nan
CHEMBL3675899 136746 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3F)cc2)cn1 nan
57391684 76208 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 441 10 2 5 4.7 CCCC(Oc1cnn(-c2cccc(Cl)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933356 76208 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 441 10 2 5 4.7 CCCC(Oc1cnn(-c2cccc(Cl)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
44304965 170017 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 523 9 3 4 5.7 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cnc3ccccc3c2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL418468 170017 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 523 9 3 4 5.7 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2cnc3ccccc3c2)cc1 10.1016/j.bmcl.2004.02.056
44304524 209718 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 548 10 3 3 6.8 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62892 209718 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 548 10 3 3 6.8 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
68186290 96916 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 477 10 2 7 3.8 CCCC(Oc1cnc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381830 96916 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 477 10 2 7 3.8 CCCC(Oc1cnc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
60152737 96924 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 441 10 2 5 4.7 CCCC(Oc1ccc(-n2cc(Cl)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381838 96924 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 441 10 2 5 4.7 CCCC(Oc1ccc(-n2cc(Cl)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
60151793 96931 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CCCC(Oc1ccc(-n2cc(C(F)(F)F)c(C)n2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381845 96931 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CCCC(Oc1ccc(-n2cc(C(F)(F)F)c(C)n2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
57402151 76204 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2cccc(C)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933352 76204 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2cccc(C)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
44304982 209616 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 566 10 4 5 5.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62432 209616 0 None - 1 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 566 10 4 5 5.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCC(O)C(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
57400348 76213 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 476 10 2 6 4.4 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cn2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933361 76213 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 476 10 2 6 4.4 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cn2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
60152601 96913 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 502 10 3 5 5.7 CCCC(Nc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381827 96913 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 502 10 3 5 5.7 CCCC(Nc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
57391686 76216 0 None 44 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933364 76216 0 None 44 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
86766115 137309 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3680822 137309 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
10829406 49497 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 318 4 2 4 3.9 O=C(CSc1nc2ccccc2[nH]1)c1ccc(O)c(Cl)c1 10.1021/jm9810304
CHEMBL150172 49497 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 318 4 2 4 3.9 O=C(CSc1nc2ccccc2[nH]1)c1ccc(O)c(Cl)c1 10.1021/jm9810304
71060079 136745 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 10 3 5 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3OC(F)(F)F)cc2)cn1 nan
CHEMBL3675898 136745 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 10 3 5 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3OC(F)(F)F)cc2)cn1 nan
57396928 76212 0 None 11 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933360 76212 0 None 11 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
60151935 96922 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 473 9 2 5 4.6 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CC2)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381836 96922 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 473 9 2 5 4.6 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CC2)cc1 10.1016/j.bmcl.2013.03.014
71060058 136698 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1cccc(-c2ccc(C(=O)NCCC(=O)O)nc2)c1CNc1ccc(-c2ccc(Cl)cc2)cc1 nan
CHEMBL3675852 136698 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1cccc(-c2ccc(C(=O)NCCC(=O)O)nc2)c1CNc1ccc(-c2ccc(Cl)cc2)cc1 nan
71059850 136722 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 8 3 4 5.3 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
CHEMBL3675875 136722 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 8 3 4 5.3 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
71239397 130268 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 463 8 3 4 5.5 Cc1cc2cc(F)ccc2nc1NC(c1ccc(C(=O)NCCC(=O)O)cc1)C1CC(C)(C)C1 10.1016/j.bmcl.2015.07.092
CHEMBL3617569 130268 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 463 8 3 4 5.5 Cc1cc2cc(F)ccc2nc1NC(c1ccc(C(=O)NCCC(=O)O)cc1)C1CC(C)(C)C1 10.1016/j.bmcl.2015.07.092
60151939 96934 38 None 223 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCC[C@H](Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381848 96934 38 None 223 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCC[C@H](Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
86766099 136675 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)c(Cl)c2)cn1 nan
CHEMBL3675830 136675 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)c(Cl)c2)cn1 nan
86674271 136708 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
CHEMBL3675861 136708 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
60151937 96923 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 461 9 2 5 4.6 CCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381837 96923 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 461 9 2 5 4.6 CCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
57391685 76214 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 476 10 2 6 4.4 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)nc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933362 76214 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 476 10 2 6 4.4 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)nc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
57396925 76203 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2ccccc2C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933351 76203 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2ccccc2C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71060099 136657 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 2 4 6.6 CN(Cc1ccc(Cl)cc1-c1ccc(C(=O)NCCC(=O)O)nc1)c1ccc(-c2ccc(Cl)cc2)cc1 nan
CHEMBL3675813 136657 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 2 4 6.6 CN(Cc1ccc(Cl)cc1-c1ccc(C(=O)NCCC(=O)O)nc1)c1ccc(-c2ccc(Cl)cc2)cc1 nan
57388936 130270 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 501 10 3 6 5.0 CC(C)C[C@H](Nc1ccc(C(=O)NCCC(=O)O)cn1)c1cnc(-c2ccc(C(F)(F)F)cc2)nc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617571 130270 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 501 10 3 6 5.0 CC(C)C[C@H](Nc1ccc(C(=O)NCCC(=O)O)cn1)c1cnc(-c2ccc(C(F)(F)F)cc2)nc1 10.1016/j.bmcl.2015.07.092
71060112 137312 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)cc2)cn1 nan
CHEMBL3680825 137312 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)cc2)cn1 nan
86766105 136689 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)c(C(F)(F)F)c2)cn1 nan
CHEMBL3675843 136689 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)c(C(F)(F)F)c2)cn1 nan
86766104 136682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)c(Cl)c2)cn1 nan
CHEMBL3675837 136682 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)c(Cl)c2)cn1 nan
71060104 137316 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.3 Cc1cc(F)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3680829 137316 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.3 Cc1cc(F)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71059986 136684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
CHEMBL3675839 136684 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
60152600 96907 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 474 10 3 5 5.0 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381821 96907 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 474 10 3 5 5.0 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
60152081 96935 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCC[C@@H](Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381849 96935 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCC[C@@H](Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
10552082 103649 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 464 8 3 8 4.3 COC(=O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(O)c4)nc3c2)c1 10.1021/jm9810304
CHEMBL265552 103649 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 464 8 3 8 4.3 COC(=O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(O)c4)nc3c2)c1 10.1021/jm9810304
71472272 130271 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
CHEMBL3617572 130271 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl 10.1016/j.bmcl.2015.07.092
57393426 76217 0 None 30 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933365 76217 0 None 30 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
71472272 130271 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl nan
CHEMBL3617572 130271 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 635 9 3 4 8.2 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl nan
60152477 96908 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 3 6 4.4 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381822 96908 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 3 6 4.4 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71614522 96920 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 8 2 5 5.3 CC(C)(C)C(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381834 96920 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 8 2 5 5.3 CC(C)(C)C(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
60152880 96926 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 425 10 2 5 4.1 CCCC(Oc1ccc(-n2cc(F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381840 96926 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 425 10 2 5 4.1 CCCC(Oc1ccc(-n2cc(F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71060139 137330 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(C3=CCCCC3)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
CHEMBL3680843 137330 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(C3=CCCCC3)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
71060120 136683 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675838 136683 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
71060059 137313 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 3 4 6.8 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3680826 137313 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 3 4 6.8 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71059985 136700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675854 136700 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
10716305 172316 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 406 7 3 6 4.5 O=C(CSc1nc2cc(OCc3ccccc3)ccc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
CHEMBL424134 172316 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 406 7 3 6 4.5 O=C(CSc1nc2cc(OCc3ccccc3)ccc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
86766113 136739 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 598 9 3 5 6.5 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1cc(F)cc(C(F)(F)F)c1 nan
CHEMBL3675892 136739 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 598 9 3 5 6.5 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1cc(F)cc(C(F)(F)F)c1 nan
71059622 136643 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 485 9 3 4 5.9 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675798 136643 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 485 9 3 4 5.9 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
57393425 76215 0 None 54 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933363 76215 0 None 54 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
86766096 136669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.6 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3675825 136669 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.6 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71060023 136660 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675816 136660 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71060056 136719 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(F)c2)cn1 nan
CHEMBL3675872 136719 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(F)c2)cn1 nan
71059831 136707 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2c(Cl)cc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3675860 136707 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2c(Cl)cc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71059925 136686 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)c(Cl)c2)cn1 nan
CHEMBL3675840 136686 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)c(Cl)c2)cn1 nan
60152878 96925 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 421 10 2 5 4.3 CCCC(Oc1ccc(-n2cc(C)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381839 96925 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 421 10 2 5 4.3 CCCC(Oc1ccc(-n2cc(C)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71060029 136693 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 5 6.5 COc1ccc(-c2ccc(C(=O)NCCC(=O)O)nc2)c(CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)c1 nan
CHEMBL3675847 136693 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 5 6.5 COc1ccc(-c2ccc(C(=O)NCCC(=O)O)nc2)c(CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)c1 nan
57396927 76211 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 437 11 2 6 4.0 CCCC(Oc1cnn(-c2ccc(OC)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933359 76211 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 437 11 2 6 4.0 CCCC(Oc1cnn(-c2ccc(OC)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71059930 137323 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 511 10 3 4 6.5 CC(C)c1ccc(CNc2ccc(-c3ccc(F)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
CHEMBL3680836 137323 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 511 10 3 4 6.5 CC(C)c1ccc(CNc2ccc(-c3ccc(F)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
122190363 130274 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617575 130274 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 10.1016/j.bmcl.2015.07.092
86674265 136705 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675859 136705 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(Cl)c2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
86766103 136681 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)cc2)cn1 nan
CHEMBL3675836 136681 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)cc2)cn1 nan
71060089 137326 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3680839 137326 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3)c(Cl)c2)cn1 nan
60152219 96936 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381850 96936 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
11793430 45788 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 368 4 3 5 4.3 O=C(CSc1nc2cc(Cl)c(Cl)cc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
CHEMBL146839 45788 0 None - 1 Human 4.7 pKi = 4.7 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 368 4 3 5 4.3 O=C(CSc1nc2cc(Cl)c(Cl)cc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
3515 9621 12 None - 1 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cellsCompound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cells
ChEMBL 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 10.1021/jm9810304
4206177 9621 12 None - 1 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cellsCompound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cells
ChEMBL 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 10.1021/jm9810304
CHEMBL346451 9621 12 None - 1 Human 4.7 pKi = 4.7 Binding
Compound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cellsCompound was evaluated for its binding affinity towards cloned human Glucagon receptor in BHK cells
ChEMBL 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 10.1021/jm9810304
86766098 136672 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)cc3Cl)c(Cl)c2)cn1 nan
CHEMBL3675828 136672 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)cc3Cl)c(Cl)c2)cn1 nan
86674274 136725 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 607 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3675878 136725 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 607 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
86766094 136666 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
CHEMBL3675822 136666 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
71060095 136752 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 603 10 3 5 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(OC(F)(F)F)cc3)c(Cl)c2)cn1 nan
CHEMBL3675905 136752 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 603 10 3 5 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(OC(F)(F)F)cc3)c(Cl)c2)cn1 nan
57391683 76207 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 435 11 2 5 4.6 CCCC(Oc1cnn(-c2ccc(CC)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933355 76207 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 435 11 2 5 4.6 CCCC(Oc1cnn(-c2ccc(CC)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
57403898 76210 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 437 11 2 6 4.0 CCCC(Oc1cnn(-c2cccc(OC)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933358 76210 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 437 11 2 6 4.0 CCCC(Oc1cnn(-c2cccc(OC)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
57388856 130269 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 500 10 3 5 5.6 CC(C)C[C@@H](Nc1cnc(C(=O)NCCC(=O)O)nc1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617570 130269 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 500 10 3 5 5.6 CC(C)C[C@@H](Nc1cnc(C(=O)NCCC(=O)O)nc1)c1ccc(-c2ccc(C(F)(F)F)cc2)cc1 10.1016/j.bmcl.2015.07.092
86674251 136670 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 639 9 3 4 8.1 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3675826 136670 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 639 9 3 4 8.1 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
71059981 136647 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675803 136647 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
86766101 136678 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)c(Cl)c2)cn1 nan
CHEMBL3675833 136678 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)c(Cl)c2)cn1 nan
71060088 136696 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3F)c(Cl)c2)cn1 nan
CHEMBL3675850 136696 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3F)c(Cl)c2)cn1 nan
71059950 136726 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
CHEMBL3675879 136726 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
60152733 96914 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 2 5 5.0 CCCC(Oc1ccc(-n2cnc(C(F)(F)F)c2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381828 96914 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 2 5 5.0 CCCC(Oc1ccc(-n2cnc(C(F)(F)F)c2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
86766100 136677 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3F)c(Cl)c2)cn1 nan
CHEMBL3675832 136677 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3F)c(Cl)c2)cn1 nan
86766110 136730 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 623 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)c(Cl)c2)cn1 nan
CHEMBL3675883 136730 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 623 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3cccc(C(F)(F)F)c3Cl)c(Cl)c2)cn1 nan
71059855 136673 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl nan
CHEMBL3675829 136673 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1Cl nan
71060044 136731 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 589 9 3 4 7.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
CHEMBL3675884 136731 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 589 9 3 4 7.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(Cl)c2)cn1 nan
68178613 96915 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 476 10 2 6 4.4 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381829 96915 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 476 10 2 6 4.4 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)nc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71059810 137320 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.6 CC(Nc1ccc(-c2ccc(F)cc2)cc1)c1ccc(Cl)cc1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
CHEMBL3680833 137320 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.6 CC(Nc1ccc(-c2ccc(F)cc2)cc1)c1ccc(Cl)cc1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
86674270 136711 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
CHEMBL3675864 136711 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
71060025 136712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(NCc2cc(Cl)c(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
CHEMBL3675865 136712 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(NCc2cc(Cl)c(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
71060108 136710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)c(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3675863 136710 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(Cl)ccc1-c1ccc(NCc2cc(Cl)c(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71059696 137331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 551 10 3 4 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C3CCCCC3)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
CHEMBL3680844 137331 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 551 10 3 4 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C3CCCCC3)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
86766097 136671 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3675827 136671 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 655 9 3 4 8.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
71059685 136661 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 567 9 3 4 7.2 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3675817 136661 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 567 9 3 4 7.2 Cc1cc(Cl)ccc1-c1ccc(NCc2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71059940 136727 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 573 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3F)c(Cl)c2)cn1 nan
CHEMBL3675880 136727 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 573 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3F)c(Cl)c2)cn1 nan
122190361 130265 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 482 11 3 5 5.7 CCC[C@H](Nc1ccc(-n2cc(-c3ccccc3)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617566 130265 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 482 11 3 5 5.7 CCC[C@H](Nc1ccc(-n2cc(-c3ccccc3)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2015.07.092
44304787 168180 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 568 10 3 4 6.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCC(F)C(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL412661 168180 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 568 10 3 4 6.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCC(F)C(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
44304570 209678 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 500 10 3 3 5.7 CCc1ccc(NC(=O)C(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62738 209678 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 500 10 3 3 5.7 CCc1ccc(NC(=O)C(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(C(C)(C)C)cc2)cc1 10.1016/j.bmcl.2004.02.056
71059819 136662 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)cc3Cl)cc2)cn1 nan
CHEMBL3675818 136662 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)cc3Cl)cc2)cn1 nan
86766109 136729 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 623 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3675882 136729 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 623 9 3 4 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
71060084 136680 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3F)cc2)cn1 nan
CHEMBL3675835 136680 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3F)cc2)cn1 nan
86766102 136679 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 639 9 3 4 8.1 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)c(F)c3)c(Cl)c2)cn1 nan
CHEMBL3675834 136679 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 639 9 3 4 8.1 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)c(F)c3)c(Cl)c2)cn1 nan
71060031 137328 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 3 4 6.8 Cc1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)cc1 nan
CHEMBL3680841 137328 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 9 3 4 6.8 Cc1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)cc1 nan
71059915 137329 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 595 10 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(-c3ccccc3)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3680842 137329 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 595 10 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(-c3ccccc3)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71059856 137315 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)cc2)cn1 nan
CHEMBL3680828 137315 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)cc2)cn1 nan
71059624 136709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(NCc2c(Cl)cc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
CHEMBL3675862 136709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 601 9 3 4 7.9 Cc1cc(NCc2c(Cl)cc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
71059903 136667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
CHEMBL3675823 136667 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
71059924 137311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.3 Cc1cc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)ccc1F nan
CHEMBL3680824 137311 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 9 3 4 6.3 Cc1cc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)ccc1F nan
71060096 137308 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 5 6.5 COc1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)c(Cl)c1 nan
CHEMBL3680821 137308 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 3 5 6.5 COc1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)c(Cl)c1 nan
86766091 136663 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)cc2)cn1 nan
CHEMBL3675819 136663 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3Cl)cc2)cn1 nan
71059914 136713 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675866 136713 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.6 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
71060147 136749 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(F)c3)cc2)cn1 nan
CHEMBL3675902 136749 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(F)c3)cc2)cn1 nan
44304771 210117 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 502 10 4 4 4.6 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(CO)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL64955 210117 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 502 10 4 4 4.6 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(CO)cc2)cc1 10.1016/j.bmcl.2004.02.056
71059934 136751 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 551 9 3 4 7.0 Cc1cc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)ccc1F nan
CHEMBL3675904 136751 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 551 9 3 4 7.0 Cc1cc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)ccc1F nan
86766093 136665 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)cc2)cn1 nan
CHEMBL3675821 136665 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(F)c(C(F)(F)F)c3)cc2)cn1 nan
68157252 96911 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 457 10 2 5 5.2 CCCC(Oc1ccc(-n2cc3ccccc3n2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381825 96911 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 457 10 2 5 5.2 CCCC(Oc1ccc(-n2cc3ccccc3n2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
44304993 169963 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 542 14 3 5 6.7 CCCCCCC(Oc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL418135 169963 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 542 14 3 5 6.7 CCCCCCC(Oc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 10.1016/j.bmcl.2004.02.056
122190362 130272 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 676 10 3 3 10.0 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2cc(C(C)C)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1016/j.bmcl.2015.07.092
CHEMBL3617573 130272 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 676 10 3 3 10.0 Cc1cc(C(F)(F)F)ccc1-c1ccc(NCc2cc(C(C)C)cc(C(F)(F)F)c2-c2ccc(C(=O)NCCC(=O)O)cc2)cc1Cl 10.1016/j.bmcl.2015.07.092
71060110 137319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 581 8 3 4 6.9 Cc1cc(Cl)ccc1-c1ccc(NC(=O)c2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3680832 137319 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 581 8 3 4 6.9 Cc1cc(Cl)ccc1-c1ccc(NC(=O)c2ccc(C(F)(F)F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
86766095 136668 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
CHEMBL3675824 136668 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 587 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
86766111 136732 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 598 9 3 5 6.5 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(F)c(C(F)(F)F)c1 nan
CHEMBL3675885 136732 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 598 9 3 5 6.5 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(F)c(C(F)(F)F)c1 nan
71060131 136753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3c(F)cccc3Cl)cc2)cn1 nan
CHEMBL3675906 136753 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3c(F)cccc3Cl)cc2)cn1 nan
71060020 136650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
CHEMBL3675806 136650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(Cl)c2)cn1 nan
86766107 136704 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675858 136704 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
86766114 136754 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3C(F)(F)F)c(Cl)c2)cn1 nan
CHEMBL3675907 136754 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 605 9 3 4 7.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3C(F)(F)F)c(Cl)c2)cn1 nan
71059970 137317 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3Cl)cc2)cn1 nan
CHEMBL3680830 137317 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3Cl)cc2)cn1 nan
71059932 137318 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 547 8 3 4 6.5 Cc1cc(Cl)ccc1-c1ccc(NC(=O)c2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
CHEMBL3680831 137318 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 547 8 3 4 6.5 Cc1cc(Cl)ccc1-c1ccc(NC(=O)c2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)cc1 nan
71060180 136728 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.6 Cc1ccc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)c(F)c1 nan
CHEMBL3675881 136728 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.6 Cc1ccc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)c(F)c1 nan
71060230 130273 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
CHEMBL3617574 130273 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysisDisplacement of [125I]-glucagon from full length human glucagon receptor expressed in HEK293 cell membranes after 2 hrs by scintillation counting analysis
ChEMBL 552 9 3 3 7.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2015.07.092
71059969 136718 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(F)c2)cn1 nan
CHEMBL3675871 136718 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)c(F)c2)cn1 nan
71060067 136721 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 8 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675874 136721 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 8 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
86674278 137322 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 509 10 3 4 6.4 C=C(C)c1ccc(CNc2ccc(-c3ccc(F)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
CHEMBL3680835 137322 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 509 10 3 4 6.4 C=C(C)c1ccc(CNc2ccc(-c3ccc(F)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
71059965 136717 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)c(F)c2)cn1 nan
CHEMBL3675870 136717 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)c(F)c2)cn1 nan
86766108 136714 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675867 136714 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)c(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71060027 136723 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 8 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
CHEMBL3675876 136723 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 8 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
71060129 136655 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
CHEMBL3675811 136655 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
3491 7367 13 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 342 6 1 1 6.7 CCCc1c(cc(c(c1c1ccc(cc1)F)C(O)C)C(C)C)C(C)C 10.1016/j.bmcl.2011.10.113
5311277 7367 13 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 342 6 1 1 6.7 CCCc1c(cc(c(c1c1ccc(cc1)F)C(O)C)C(C)C)C(C)C 10.1016/j.bmcl.2011.10.113
CHEMBL1933348 7367 13 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 342 6 1 1 6.7 CCCc1c(cc(c(c1c1ccc(cc1)F)C(O)C)C(C)C)C(C)C 10.1016/j.bmcl.2011.10.113
71059818 137327 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)c(Cl)c2)cn1 nan
CHEMBL3680840 137327 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)c(Cl)c3)c(Cl)c2)cn1 nan
71059982 137310 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 513 8 3 4 5.8 Cc1ccc(C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
CHEMBL3680823 137310 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 513 8 3 4 5.8 Cc1ccc(C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
71059891 136695 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(F)c3)cc2)cn1 nan
CHEMBL3675849 136695 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.4 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3cccc(F)c3)cc2)cn1 nan
71059997 137321 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 527 10 3 5 6.1 CC(=O)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)cc1 nan
CHEMBL3680834 137321 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 527 10 3 5 6.1 CC(=O)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)cc1 nan
71059715 137324 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 575 9 3 4 7.8 CC(C)(C)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)cc1 nan
CHEMBL3680837 137324 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 575 9 3 4 7.8 CC(C)(C)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2Cl)cc1 nan
71060081 136747 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(F)c3)cc2)cn1 nan
CHEMBL3675900 136747 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 503 9 3 4 6.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(F)c3)cc2)cn1 nan
86766116 137325 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
CHEMBL3680838 137325 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 8.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(C(F)(F)F)c3)c(Cl)c2)cn1 nan
71060072 136653 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(F)c3)cc2F)cn1 nan
CHEMBL3675809 136653 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(F)c3)cc2F)cn1 nan
71060057 136658 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 567 8 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675814 136658 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 567 8 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
46240797 76202 12 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 520 10 3 2 7.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(Cl)cc1)c1c[nH]c2c(F)cc(C)cc12 10.1016/j.bmcl.2011.10.113
CHEMBL1933350 76202 12 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 520 10 3 2 7.2 CCC[C@H](c1ccc(C(=O)NCCC(=O)O)cc1)[C@H](c1ccc(Cl)cc1)c1c[nH]c2c(F)cc(C)cc12 10.1016/j.bmcl.2011.10.113
9938390 109544 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 588 10 3 4 7.6 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3cc4ccccc4o3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL305151 109544 0 None - 1 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 588 10 3 4 7.6 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3cc4ccccc4o3)cc2)cc1 10.1016/j.bmcl.2004.02.056
71059805 136701 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1ccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
CHEMBL3675855 136701 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1ccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
71060042 137314 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3C(F)(F)F)cc2)cn1 nan
CHEMBL3680827 137314 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.0 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3C(F)(F)F)cc2)cn1 nan
71060077 137332 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 599 10 3 4 8.5 O=C(O)CCNC(=O)c1ccc(-c2cc(C3=CCCCC3)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3680845 137332 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 599 10 3 4 8.5 O=C(O)CCNC(=O)c1ccc(-c2cc(C3=CCCCC3)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71060070 136646 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675802 136646 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
71059983 136737 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 580 9 3 5 6.7 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1Cl nan
CHEMBL3675890 136737 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 580 9 3 5 6.7 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1Cl nan
44304623 209709 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 555 9 2 4 5.2 Cc1ccc(N2CCN(C(=O)C(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)CC2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62863 209709 0 None - 1 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 555 9 2 4 5.2 Cc1ccc(N2CCN(C(=O)C(Cc3ccc(C(=O)NCCC(=O)O)cc3)c3ccc(C(C)(C)C)cc3)CC2)cc1 10.1016/j.bmcl.2004.02.056
71060209 136651 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2F)cn1 nan
CHEMBL3675807 136651 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 571 9 3 4 7.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2F)cn1 nan
60150962 96927 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 407 10 2 5 4.0 CCCC(Oc1ccc(-n2cccn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381841 96927 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 407 10 2 5 4.0 CCCC(Oc1ccc(-n2cccn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
68178611 96928 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 432 10 2 6 3.9 CCCC(Oc1ccc(-n2cc(C#N)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381842 96928 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 432 10 2 6 3.9 CCCC(Oc1ccc(-n2cc(C#N)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
10686727 45612 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 314 5 2 5 3.3 COc1cc(C(=O)CSc2nc3ccccc3[nH]2)ccc1O 10.1021/jm9810304
CHEMBL146683 45612 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 314 5 2 5 3.3 COc1cc(C(=O)CSc2nc3ccccc3[nH]2)ccc1O 10.1021/jm9810304
68156716 96919 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 501 9 2 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CCCC2)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381833 96919 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 501 9 2 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CCCC2)cc1 10.1016/j.bmcl.2013.03.014
2228665 128753 10 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 330 5 3 6 3.0 COc1ccc2[nH]c(SCC(=O)c3ccc(O)c(O)c3)nc2c1 10.1021/jm9810304
CHEMBL359176 128753 10 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 330 5 3 6 3.0 COc1ccc2[nH]c(SCC(=O)c3ccc(O)c(O)c3)nc2c1 10.1021/jm9810304
71060043 136733 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 546 9 3 5 6.0 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
CHEMBL3675886 136733 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 546 9 3 5 6.0 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1 nan
71060068 136740 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675893 136740 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
71059980 136656 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 8 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675812 136656 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 533 8 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
57396928 76212 0 None 11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933360 76212 0 None 11 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71060128 136715 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)c(F)c2)cn1 nan
CHEMBL3675868 136715 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3)c(F)c2)cn1 nan
68178607 96929 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 437 11 2 6 4.0 CCCC(Oc1ccc(-n2cc(OC)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381843 96929 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 437 11 2 6 4.0 CCCC(Oc1ccc(-n2cc(OC)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
86766092 136664 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3C(F)(F)F)cc2)cn1 nan
CHEMBL3675820 136664 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 621 9 3 4 7.9 O=C(O)CCNC(=O)c1ccc(-c2cc(C(F)(F)F)ccc2CNc2ccc(-c3ccc(Cl)cc3C(F)(F)F)cc2)cn1 nan
71059938 136691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
CHEMBL3675845 136691 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
57391686 76216 0 None 44 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933364 76216 0 None 44 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 528 10 3 5 5.6 O=C(O)CCNC(=O)c1ccc(C(CCC(F)(F)F)Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)cc1 10.1016/j.bmcl.2011.10.113
71060094 136688 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 583 10 3 5 6.9 COc1cc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(C(F)(F)F)cc1 nan
CHEMBL3675842 136688 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 583 10 3 5 6.9 COc1cc(NCc2ccc(Cl)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(C(F)(F)F)cc1 nan
68156402 130266 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 516 9 3 7 4.5 CC1(C)CC(C(Nc2cnc(-n3cc(C(F)(F)F)cn3)nc2)c2ccc(C(=O)NCCC(=O)O)cc2)C1 10.1016/j.bmcl.2015.07.092
CHEMBL3617567 130266 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 516 9 3 7 4.5 CC1(C)CC(C(Nc2cnc(-n3cc(C(F)(F)F)cn3)nc2)c2ccc(C(=O)NCCC(=O)O)cc2)C1 10.1016/j.bmcl.2015.07.092
44304913 209634 0 None - 1 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 570 11 3 4 6.2 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(COC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62531 209634 0 None - 1 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 570 11 3 4 6.2 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(COC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.02.056
20742348 209609 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 556 10 3 4 6.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62412 209609 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 556 10 3 4 6.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)cc1 10.1016/j.bmcl.2004.02.056
71060026 136703 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 563 10 3 6 5.3 CS(=O)(=O)c1ccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
CHEMBL3675857 136703 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 563 10 3 6 5.3 CS(=O)(=O)c1ccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c(-c2ccc(C(=O)NCCC(=O)O)nc2)c1 nan
71059992 136652 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2F)cn1 nan
CHEMBL3675808 136652 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 537 9 3 4 6.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)cc3)cc2F)cn1 nan
71239512 130267 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 445 8 3 4 5.3 Cc1cc2ccccc2nc1NC(c1ccc(C(=O)NCCC(=O)O)cc1)C1CC(C)(C)C1 10.1016/j.bmcl.2015.07.092
CHEMBL3617568 130267 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assayDisplacement of [125I]-glucagon from human glucagon receptor expressed in Chem-1 cell membranes after 6 to 10 hrs by scintillation proximity assay
ChEMBL 445 8 3 4 5.3 Cc1cc2ccccc2nc1NC(c1ccc(C(=O)NCCC(=O)O)cc1)C1CC(C)(C)C1 10.1016/j.bmcl.2015.07.092
71060024 136720 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(F)c3)c(F)c2)cn1 nan
CHEMBL3675873 136720 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(Cl)c(F)c3)c(F)c2)cn1 nan
10360917 128482 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 356 4 3 5 4.2 CC(C)(C)c1ccc2[nH]c(SCC(=O)c3ccc(O)c(O)c3)nc2c1 10.1021/jm9810304
CHEMBL358886 128482 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 356 4 3 5 4.2 CC(C)(C)c1ccc2[nH]c(SCC(=O)c3ccc(O)c(O)c3)nc2c1 10.1021/jm9810304
60151938 96918 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CC(C)CC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381832 96918 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 489 10 2 5 5.3 CC(C)CC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
10617488 46331 9 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 345 5 3 7 2.9 O=C(CSc1nc2cc([N+](=O)[O-])ccc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
CHEMBL147331 46331 9 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 345 5 3 7 2.9 O=C(CSc1nc2cc([N+](=O)[O-])ccc2[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
654283 128320 8 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 327 5 3 6 2.9 O=C(CSc1nnc(-c2ccccc2)[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
CHEMBL358546 128320 8 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 327 5 3 6 2.9 O=C(CSc1nnc(-c2ccccc2)[nH]1)c1ccc(O)c(O)c1 10.1021/jm9810304
57402153 76206 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 435 11 2 5 4.6 CCCC(Oc1cnn(-c2cccc(CC)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933354 76206 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 435 11 2 5 4.6 CCCC(Oc1cnn(-c2cccc(CC)c2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71059957 136724 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 535 8 3 4 5.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675877 136724 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 535 8 3 4 5.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2C(=O)Nc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
86766112 136736 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 614 9 3 5 7.1 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)c(C(F)(F)F)c1 nan
CHEMBL3675889 136736 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 614 9 3 5 7.1 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)c(C(F)(F)F)c1 nan
44304835 107694 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 540 14 3 4 7.1 CCCCCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL293907 107694 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 540 14 3 4 7.1 CCCCCCC(Cc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2cc3ccccc3o2)cc1 10.1016/j.bmcl.2004.02.056
44304622 209557 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 616 10 3 3 8.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL62123 209557 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 616 10 3 3 8.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccc(Cl)cc3Cl)cc2)cc1 10.1016/j.bmcl.2004.02.056
44304770 210261 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 570 14 3 4 7.2 CCCCCCC(Oc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL66087 210261 0 None - 1 Human 8.2 pKi = 8.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 570 14 3 4 7.2 CCCCCCC(Oc1ccc(C(=O)NCCC(=O)O)cc1)C(=O)Nc1ccc(-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2004.02.056
91933867 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human GCGR receptorInhibition of human GCGR receptor
ChEMBL 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 10.1016/j.ejmech.2018.04.061
9479 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human GCGR receptorInhibition of human GCGR receptor
ChEMBL 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 10.1016/j.ejmech.2018.04.061
CHEMBL3707351 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human GCGR receptorInhibition of human GCGR receptor
ChEMBL 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 10.1016/j.ejmech.2018.04.061
DB11704 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of human GCGR receptorInhibition of human GCGR receptor
ChEMBL 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 10.1016/j.ejmech.2018.04.061
71060107 136716 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 539 9 3 4 6.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3F)c(F)c2)cn1 nan
CHEMBL3675869 136716 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 539 9 3 4 6.3 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccc(F)cc3F)c(F)c2)cn1 nan
57396926 76209 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 441 10 2 5 4.7 CCCC(Oc1cnn(-c2ccc(Cl)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933357 76209 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 441 10 2 5 4.7 CCCC(Oc1cnn(-c2ccc(Cl)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71060033 136750 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cc(F)cc(F)c3)cc2)cn1 nan
CHEMBL3675903 136750 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 521 9 3 4 6.2 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cc(F)cc(F)c3)cc2)cn1 nan
71059993 136659 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 8 3 4 5.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
CHEMBL3675815 136659 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 517 8 3 4 5.7 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(F)cc3)cc2)cn1 nan
71059829 136743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3)cc2)cn1 nan
CHEMBL3675896 136743 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(C(F)(F)F)c3)cc2)cn1 nan
16100296 209618 46 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.02.056
CHEMBL62444 209618 46 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 563 9 3 4 6.4 CC(C)(C)[C@H]1CC[C@H](N(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(OC(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.02.056
16755686 136600 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.
ChEMBL 565 9 2 5 7.2 Cc1cc(OC(CCC(F)(F)F)c2ccc(C(=O)NCc3nnn[nH]3)cc2)cc(C)c1-c1ccc(C(C)(C)C)cc1 nan
CHEMBL3675643 136600 1 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.
ChEMBL 565 9 2 5 7.2 Cc1cc(OC(CCC(F)(F)F)c2ccc(C(=O)NCc3nnn[nH]3)cc2)cc(C)c1-c1ccc(C(C)(C)C)cc1 nan
71059833 136748 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3Cl)cc2)cn1 nan
CHEMBL3675901 136748 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3Cl)cc2)cn1 nan
68156267 96933 8 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCCC(Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381847 96933 8 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 503 10 2 5 5.6 CCCC(Oc1cc(C)c(-n2cc(C(F)(F)F)cn2)c(C)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71060098 136644 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2ccc(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
CHEMBL3675800 136644 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2ccc(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3)cc2)cn1 nan
71060135 136654 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(Cl)c3)cc2)cn1 nan
CHEMBL3675810 136654 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(Cl)c3)cc2)cn1 nan
71614523 96930 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 478 11 2 6 3.7 CCCC(Oc1ccc(-n2cc(C(=O)N(C)C)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381844 96930 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 478 11 2 6 3.7 CCCC(Oc1ccc(-n2cc(C(=O)N(C)C)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
44304788 210050 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 546 8 3 6 6.2 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL64646 210050 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 546 8 3 6 6.2 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)Nc3nn[nH]n3)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
57393425 76215 0 None 54 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933363 76215 0 None 54 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 474 10 3 5 5.0 CCCC(Nc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
71059641 136645 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2ccc(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675801 136645 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 7.2 O=C(O)CCNC(=O)c1ccc(-c2ccc(Cl)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71059927 136676 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 535 8 3 4 5.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(F)cc3F)cc2)cn1 nan
CHEMBL3675831 136676 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 535 8 3 4 5.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(-c3ccc(F)cc3F)cc2)cn1 nan
71059825 136741 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
CHEMBL3675894 136741 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)c(F)cc2CNc2ccc(-c3ccc(Cl)cc3Cl)cc2)cn1 nan
71614312 96912 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 3 6 4.4 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381826 96912 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 3 6 4.4 CCCC(Nc1ccc(-n2cc(C(F)(F)F)cn2)cn1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71060034 136699 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 510 9 3 5 5.8 N#Cc1cccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
CHEMBL3675853 136699 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 510 9 3 5 5.8 N#Cc1cccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
68156701 96906 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 474 10 3 5 5.0 CCCC(Nc1ccc(-n2cnc(C(F)(F)F)c2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381820 96906 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 474 10 3 5 5.0 CCCC(Nc1ccc(-n2cnc(C(F)(F)F)c2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
71059879 136734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 564 9 3 5 6.2 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1F nan
CHEMBL3675887 136734 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 564 9 3 5 6.2 N#Cc1cc(NCc2cc(F)c(F)cc2-c2ccc(C(=O)NCCC(=O)O)nc2)ccc1-c1ccc(Cl)cc1F nan
68178614 96932 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 461 10 2 5 4.9 CCCC(Oc1ccc(-n2cc3c(n2)CCCC3)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381846 96932 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 461 10 2 5 4.9 CCCC(Oc1ccc(-n2cc3c(n2)CCCC3)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
11570626 9328 46 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2011.10.113
9135 9328 46 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2011.10.113
CHEMBL1933349 9328 46 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2011.10.113
DB12044 9328 46 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 587 9 2 5 7.5 COc1ccc2c(c1)ccc(c2)c1cc(nn1[C@H](c1ccc(cc1)C(=O)NCCC(=O)O)C)c1cc(Cl)cc(c1)Cl 10.1016/j.bmcl.2011.10.113
44304582 210204 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 538 10 3 5 5.3 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-n3cccn3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL65705 210204 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 538 10 3 5 5.3 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-n3cccn3)cc2)cc1 10.1016/j.bmcl.2004.02.056
60151654 96917 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 487 9 2 5 5.0 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CCC2)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381831 96917 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 487 9 2 5 5.0 O=C(O)CCNC(=O)c1ccc(C(Oc2ccc(-n3cc(C(F)(F)F)cn3)cc2)C2CCC2)cc1 10.1016/j.bmcl.2013.03.014
71060134 136744 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3C(F)(F)F)cc2)cn1 nan
CHEMBL3675897 136744 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3ccccc3C(F)(F)F)cc2)cn1 nan
71060115 136692 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 541 9 3 4 7.2 CC(C)(C)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)cc1 nan
CHEMBL3675846 136692 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 541 9 3 4 7.2 CC(C)(C)c1ccc(-c2ccc(NCc3ccc(Cl)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2)cc1 nan
60151936 96921 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 9 2 5 4.9 CC(C)C(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381835 96921 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 9 2 5 4.9 CC(C)C(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
44304581 209872 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 555 10 3 4 6.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(N3CCCCC3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL63923 209872 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 555 10 3 4 6.1 CC(C)(C)c1ccc(C(Cc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(N3CCCCC3)cc2)cc1 10.1016/j.bmcl.2004.02.056
4066568 48023 9 None - 1 Human 4.1 pKi = 4.1 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 317 4 2 6 3.7 O=C(CSc1nc2ccccc2s1)c1ccc(O)c(O)c1 10.1021/jm9810304
CHEMBL148905 48023 9 None - 1 Human 4.1 pKi = 4.1 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 317 4 2 6 3.7 O=C(CSc1nc2ccccc2s1)c1ccc(O)c(O)c1 10.1021/jm9810304
71059943 131219 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(F)c2)cn1 nan
CHEMBL3639747 131219 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(Cl)cc3Cl)c(F)c2)cn1 nan
71060113 136735 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 544 9 3 5 5.8 Cc1ccc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2C#N)c(F)c1 nan
CHEMBL3675888 136735 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 544 9 3 5 5.8 Cc1ccc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2C#N)c(F)c1 nan
44304525 209671 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 500 10 3 3 5.7 CCc1cccc(NC(=O)C(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(C(C)(C)C)cc2)c1 10.1016/j.bmcl.2004.02.056
CHEMBL62704 209671 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 500 10 3 3 5.7 CCc1cccc(NC(=O)C(Cc2ccc(C(=O)NCCC(=O)O)cc2)c2ccc(C(C)(C)C)cc2)c1 10.1016/j.bmcl.2004.02.056
71059999 136742 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 10 3 5 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(OC(F)(F)F)c3)cc2)cn1 nan
CHEMBL3675895 136742 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 569 10 3 5 6.8 O=C(O)CCNC(=O)c1ccc(-c2cc(Cl)ccc2CNc2ccc(-c3cccc(OC(F)(F)F)c3)cc2)cn1 nan
10032265 193101 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL487476 193101 1 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 581 9 4 4 6.4 O=C(NC[C@@H](O)C(=O)O)c1ccc(CN(C(=O)Nc2cc(Cl)cc(Cl)c2)c2ccc(C3=CCCCC3)cc2)cc1 10.1016/j.bmcl.2011.10.113
71059948 136702 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1cccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
CHEMBL3675856 136702 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 499 9 3 4 6.2 Cc1cccc(CNc2ccc(-c3ccc(Cl)cc3)cc2)c1-c1ccc(C(=O)NCCC(=O)O)nc1 nan
60151375 96910 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 2 5 5.0 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
CHEMBL2381824 96910 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albuminDisplacement of [125I]-glucagon-cex from human glucagon receptor by cell based assay in presence of 0.2% bovine serum albumin
ChEMBL 475 10 2 5 5.0 CCCC(Oc1ccc(-n2cc(C(F)(F)F)cn2)cc1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2013.03.014
57393426 76217 0 None 30 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933365 76217 0 None 30 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 500 9 3 5 5.4 O=C(O)CCNC(=O)c1ccc(C(Nc2cnn(-c3ccc(C(F)(F)F)cc3)c2)C2CCCC2)cc1 10.1016/j.bmcl.2011.10.113
44304825 210011 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 550 10 3 4 6.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
CHEMBL64475 210011 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity against human glucagon receptor (h-GlucR) was determinedIn vitro binding affinity against human glucagon receptor (h-GlucR) was determined
ChEMBL 550 10 3 4 6.6 CC(C)(C)c1ccc(C(Oc2ccc(C(=O)NCCC(=O)O)cc2)C(=O)Nc2ccc(-c3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.02.056
57396928 76212 0 None 11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933360 76212 0 None 11 3 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 475 10 2 5 5.0 CCCC(Oc1cnn(-c2ccc(C(F)(F)F)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
10600858 127818 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 482 8 2 7 5.3 COC(=O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(Cl)c4)nc3c2)c1 10.1021/jm9810304
CHEMBL356726 127818 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 482 8 2 7 5.3 COC(=O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(Cl)c4)nc3c2)c1 10.1021/jm9810304
57745249 136601 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.
ChEMBL 551 8 2 5 7.7 Cc1cc(OC(CCC(C)(C)C)c2ccc(C(=O)Nc3nnn[nH]3)cc2)cc(C)c1-c1ccc(C(F)(F)F)cc1 nan
CHEMBL3675644 136601 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.Binding Assay: The binding assays are carried out using a Scintillation Proximity Assay (Amersham) with WGA beads previously blocked with 1% fatty acid free BSA (ICN). The binding buffer contains 25 mM Hepes, pH 7.4, 2.5 mM CaCl2, 1 mM MgCl2, 0.1% fatty acid free BSA, (ICN), 0.003% tween-20, and Roche Complete Inhibitors without EDTA. Glucagon is dissolved in 0.01 N HCl at 1 mg/mL and immediately frozen at −80 degrees C. in 30 μl aliquots. The glucagon aliquot is diluted and used in binding assays within an hour. Test compounds are dissolved in DMSO and serially diluted in DMSO. 10 ul diluted compounds or DMSO is transferred into Corning 3632, opaque clear bottom assay plates containing 90 μl assay binding buffer or cold glucagon (NSB at 1 μM final). 50 μl of 1-125 glucagon (0.15 nM final in reaction), 50 μl of membranes (300 μg/well), and 40 μl of WGA beads (150 mgs/well) are added, covered, and mixed end over end.
ChEMBL 551 8 2 5 7.7 Cc1cc(OC(CCC(C)(C)C)c2ccc(C(=O)Nc3nnn[nH]3)cc2)cc(C)c1-c1ccc(C(F)(F)F)cc1 nan
71059851 136648 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
CHEMBL3675804 136648 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
71080153 136649 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.3 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
CHEMBL3675805 136649 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 519 9 3 4 6.3 O=C(O)CCNC(=O)c1ccc(-c2ccccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)cc2)cn1 nan
71059922 136697 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2c(CNc3ccc(-c4ccc(Cl)cc4)cc3)cccc2C(F)(F)F)cn1 nan
CHEMBL3675851 136697 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 553 9 3 4 6.9 O=C(O)CCNC(=O)c1ccc(-c2c(CNc3ccc(-c4ccc(Cl)cc4)cc3)cccc2C(F)(F)F)cn1 nan
71060102 136738 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 544 9 3 5 5.8 Cc1cc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2C#N)ccc1F nan
CHEMBL3675891 136738 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 544 9 3 5 5.8 Cc1cc(-c2ccc(NCc3cc(F)c(F)cc3-c3ccc(C(=O)NCCC(=O)O)nc3)cc2C#N)ccc1F nan
10694841 48338 0 None - 1 Human 4.0 pKi = 4.0 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 450 8 4 7 4.2 O=C(O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(O)c4)nc3c2)c1 10.1021/jm9810304
CHEMBL149138 48338 0 None - 1 Human 4.0 pKi = 4.0 Binding
Binding affinity towards cloned human glucagon receptor in BHK cells.Binding affinity towards cloned human glucagon receptor in BHK cells.
ChEMBL 450 8 4 7 4.2 O=C(O)c1cccc(COc2ccc3[nH]c(SCC(=O)c4ccc(O)c(O)c4)nc3c2)c1 10.1021/jm9810304
57402152 76205 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2ccc(C)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
CHEMBL1933353 76205 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Glucagon-Cex from human GCGRDisplacement of [125I]Glucagon-Cex from human GCGR
ChEMBL 421 10 2 5 4.3 CCCC(Oc1cnn(-c2ccc(C)cc2)c1)c1ccc(C(=O)NCCC(=O)O)cc1 10.1016/j.bmcl.2011.10.113
86766106 136694 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 4 5 6.0 O=C(O)CCNC(=O)c1ccc(-c2ccc(CO)cc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
CHEMBL3675848 136694 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 549 10 4 5 6.0 O=C(O)CCNC(=O)c1ccc(-c2ccc(CO)cc2CNc2ccc(-c3ccc(Cl)c(Cl)c3)cc2)cn1 nan
71059698 136690 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)c(F)c2)cn1 nan
CHEMBL3675844 136690 0 None - 1 Human 7.0 pKi = 7 Binding
Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.Binding Assay: The binding assay was performed by a filtration method in a 384 well format. Membranes at a final protein concentration of 6 μg/well were incubated with 125I-glucagon at 0.3 nM and in the presence of compound for 2 hours at room temperature in a total reaction volume of 40 μL per well. Assay buffer consisted of 50 mM HEPES, pH 7.4, 5 mM MgCl2, 1 mM CaCl2 and 0.2% BSA. 30 μL of the reaction was then transferred to PEI treated filter plates and followed by filter aspiration. Plates were then washed 5x and allowed to dry at room temperature overnight. The next day the bottom of the plate was covered with seal tape and scintillant was added. Total counts retained by the filters were quantified with a Top Count instrument.
ChEMBL 555 9 3 4 6.5 O=C(O)CCNC(=O)c1ccc(-c2cc(F)ccc2CNc2ccc(-c3ccc(C(F)(F)F)cc3)c(F)c2)cn1 nan
9614 7992 0 None -3 3 Mouse 10.3 pKd = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26020795
9614 7992 0 None 3 3 Rat 10.8 pKd = 10.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26020795
9614 7992 0 None -8 3 Human 9.9 pKd = 9.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26020795
3515 9621 12 None - 1 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 9857085
4206177 9621 12 None - 1 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 9857085
CHEMBL346451 9621 12 None - 1 Human 5.0 pKi = 5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 300 4 3 5 2.9 O=C(c1ccc(c(c1)O)O)CSc1nc2c([nH]1)cccc2 9857085
91933867 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 25656305
91933867 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 26681715
9479 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 25656305
9479 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 26681715
CHEMBL3707351 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 25656305
CHEMBL3707351 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 26681715
DB11704 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 25656305
DB11704 7075 34 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 555 10 2 3 7.9 OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](Oc1cc(C)c(c(c1)C)c1ccc(cc1)C(C)(C)C)CCC(F)(F)F 26681715