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Compile Data Set for Download or QSAR

Found 1367 hits of ic50 for UniProtKB: P47871   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glucagon receptor


(Homo sapiens (Human))
BDBM235136
PNG
(US9359339, 25)
Show SMILES CCC[C@@H](C(c1csc2c(cc(Cl)cc12)C#N)c1ccc(OC(F)(F)F)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H26ClF3N2O4S/c1-2-3-24(18-4-6-20(7-5-18)30(40)37-13-12-27(38)39)28(19-8-10-23(11-9-19)41-31(33,34)35)26-17-42-29-21(16-36)14-22(32)15-25(26)29/h4-11,14-15,17,24,28H,2-3,12-13H2,1H3,(H,37,40)(H,38,39)/t24-,28?/m1/s1
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n/an/a 0.100n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235135
PNG
(US9359339, 23)
Show SMILES CCC[C@@H](C(c1csc2c(cc(C)cc12)C#N)c1ccc(OC(F)(F)F)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C32H29F3N2O4S/c1-3-4-25(20-5-7-22(8-6-20)31(40)37-14-13-28(38)39)29(21-9-11-24(12-10-21)41-32(33,34)35)27-18-42-30-23(17-36)15-19(2)16-26(27)30/h5-12,15-16,18,25,29H,3-4,13-14H2,1-2H3,(H,37,40)(H,38,39)/t25-,29?/m1/s1
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n/an/a 0.200n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235137
PNG
(US9359339, 27)
Show SMILES OC(=O)CCNC(=O)c1ccc(cc1)[C@@H](CCC(F)(F)F)C(c1csc2c(cc(Cl)cc12)C#N)c1ccc(Cl)cc1
Show InChI InChI=1S/C30H23Cl2F3N2O3S/c31-21-7-5-18(6-8-21)27(25-16-41-28-20(15-36)13-22(32)14-24(25)28)23(9-11-30(33,34)35)17-1-3-19(4-2-17)29(40)37-12-10-26(38)39/h1-8,13-14,16,23,27H,9-12H2,(H,37,40)(H,38,39)/t23-,27?/m1/s1
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50119552
PNG
(CHEMBL3617565)
Show SMILES CCC[C@@H]([C@@H](c1c[nH]c2c(F)cc(Cl)cc12)c1ccc(OC(F)(F)F)cc1)c1ccc(cc1)C(=O)NCCC(O)=O |r|
Show InChI InChI=1S/C30H27ClF4N2O4/c1-2-3-22(17-4-6-19(7-5-17)29(40)36-13-12-26(38)39)27(18-8-10-21(11-9-18)41-30(33,34)35)24-16-37-28-23(24)14-20(31)15-25(28)32/h4-11,14-16,22,27,37H,2-3,12-13H2,1H3,(H,36,40)(H,38,39)/t22-,27+/m1/s1
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n/an/a 0.240n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Displacement of [125I]-glucagon from human glucagon receptor expressed in CHO cells after 4 to 12 hrs by liquid scintillation counting analysis


Bioorg Med Chem Lett 25: 4057-64 (2015)


Article DOI: 10.1016/j.bmcl.2015.07.092
BindingDB Entry DOI: 10.7270/Q2HM5B7N
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235138
PNG
(US9359339, 29)
Show SMILES CCCC[C@@H](C(c1csc2c(cc(Cl)cc12)C#N)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H28Cl2N2O3S/c1-2-3-4-25(19-5-7-21(8-6-19)31(38)35-14-13-28(36)37)29(20-9-11-23(32)12-10-20)27-18-39-30-22(17-34)15-24(33)16-26(27)30/h5-12,15-16,18,25,29H,2-4,13-14H2,1H3,(H,35,38)(H,36,37)/t25-,29?/m1/s1
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n/an/a 0.400n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50566470
PNG
(CHEMBL4857523)
Show SMILES 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(C)C)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@@H](C)O)C(N)=O)C(O)=O)C(O)=O |r|
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n/an/a 0.430n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at human GCGR expressed in HEK293 cells assessed as inhibition of glucogon-induced cAMP production


Citation and Details

Article DOI: 10.1021/acs.jmedchem.0c02069
BindingDB Entry DOI: 10.7270/Q23J3HQT
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235134
PNG
(US9359339, 21)
Show SMILES CCC[C@@H](C(c1csc2c(cc(Cl)cc12)C#N)c1ccc(Cl)c(Cl)c1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C30H25Cl3N2O3S/c1-2-3-22(17-4-6-18(7-5-17)30(38)35-11-10-27(36)37)28(19-8-9-25(32)26(33)13-19)24-16-39-29-20(15-34)12-21(31)14-23(24)29/h4-9,12-14,16,22,28H,2-3,10-11H2,1H3,(H,35,38)(H,36,37)/t22-,28?/m1/s1
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n/an/a 0.700n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120365
PNG
(CHEMBL3616693)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C37H33F6N3O5/c1-3-4-5-30(23-6-8-24(9-7-23)35(49)44-19-18-33(47)48)46-31-20-25(22-10-14-27(15-11-22)51-37(41,42)43)12-16-28(31)34(45-46)29-21-26(36(38,39)40)13-17-32(29)50-2/h6-17,20-21,30H,3-5,18-19H2,1-2H3,(H,44,49)(H,47,48)
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n/an/a 0.800n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235139
PNG
(US9359339, 32)
Show SMILES CC(C)C[C@@H](C(c1csc2c(cc(Cl)cc12)C#N)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H28Cl2N2O3S/c1-18(2)13-25(19-3-5-21(6-4-19)31(38)35-12-11-28(36)37)29(20-7-9-23(32)10-8-20)27-17-39-30-22(16-34)14-24(33)15-26(27)30/h3-10,14-15,17-18,25,29H,11-13H2,1-2H3,(H,35,38)(H,36,37)/t25-,29?/m1/s1
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Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244265
PNG
(CHEMBL480113 | trans-4-((4-tert-butylcyclohexyl)(1...)
Show SMILES CCCOc1ccc2nc(N(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)[C@H]3CC[C@@H](CC3)C(C)(C)C)n(C)c2c1 |r,wU:26.27,wD:29.34,(9.13,-42.84,;9.87,-44.19,;11.41,-44.22,;12.15,-45.57,;13.69,-45.6,;14.49,-44.28,;16.03,-44.32,;16.76,-45.67,;18.26,-46.03,;18.38,-47.56,;19.71,-48.34,;19.71,-49.88,;21.04,-50.66,;22.37,-49.89,;23.7,-50.67,;23.69,-52.21,;22.34,-52.97,;21.02,-52.19,;25.02,-52.99,;25.01,-54.53,;26.36,-52.22,;27.68,-53,;28.2,-54.45,;29.74,-54.42,;30.18,-52.94,;28.91,-52.06,;21.04,-47.58,;21.05,-46.04,;22.39,-45.28,;23.72,-46.06,;23.71,-47.6,;22.37,-48.36,;25.06,-45.3,;26.39,-44.52,;25.83,-46.64,;24.3,-43.97,;16.96,-48.15,;16.19,-49.49,;15.96,-46.98,;14.43,-46.95,)|
Show InChI InChI=1S/C30H40N8O2/c1-6-17-40-24-15-16-25-26(18-24)37(5)29(31-25)38(23-13-11-22(12-14-23)30(2,3)4)19-20-7-9-21(10-8-20)27(39)32-28-33-35-36-34-28/h7-10,15-16,18,22-23H,6,11-14,17,19H2,1-5H3,(H2,32,33,34,35,36,39)/t22-,23-
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n/an/a 1n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244238
PNG
(CHEMBL499372 | trans-4-(((5-(benzyloxy)-1-methyl-1...)
Show SMILES Cn1c(nc2cc(OCc3ccccc3)ccc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:34.38,wD:37.45,(-7.9,-48.6,;-7.12,-47.26,;-5.7,-46.67,;-5.82,-45.14,;-7.32,-44.78,;-8.06,-43.43,;-9.59,-43.39,;-10.33,-42.04,;-9.53,-40.73,;-10.27,-39.37,;-9.47,-38.06,;-10.21,-36.71,;-11.75,-36.67,;-12.55,-37.99,;-11.81,-39.34,;-10.4,-44.71,;-9.66,-46.06,;-8.13,-46.09,;-4.37,-47.45,;-4.38,-48.99,;-3.05,-49.77,;-1.72,-49,;-.39,-49.78,;-.4,-51.32,;-1.74,-52.08,;-3.07,-51.3,;.93,-52.1,;.92,-53.64,;2.27,-51.33,;3.6,-52.11,;4.12,-53.56,;5.66,-53.52,;6.1,-52.05,;4.83,-51.17,;-3.04,-46.69,;-3.04,-45.15,;-1.69,-44.39,;-.36,-45.17,;-.38,-46.71,;-1.71,-47.47,;.98,-44.41,;2.3,-43.63,;1.75,-45.75,;.21,-43.08,)|
Show InChI InChI=1S/C34H40N8O2/c1-34(2,3)26-14-16-27(17-15-26)42(21-23-10-12-25(13-11-23)31(43)36-32-37-39-40-38-32)33-35-29-20-28(18-19-30(29)41(33)4)44-22-24-8-6-5-7-9-24/h5-13,18-20,26-27H,14-17,21-22H2,1-4H3,(H2,36,37,38,39,40,43)/t26-,27-
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Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244236
PNG
(CHEMBL500315 | trans-4-(((4-tert-butylcyclohexyl)(...)
Show SMILES Cn1c(nc2cc(OC3CCCC3)ccc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:32.36,wD:35.43,(16.18,-49.49,;16.96,-48.15,;18.38,-47.56,;18.26,-46.02,;16.76,-45.67,;16.03,-44.32,;14.49,-44.28,;13.75,-42.93,;14.55,-41.62,;16.09,-41.49,;16.44,-39.99,;15.13,-39.19,;13.96,-40.19,;13.69,-45.6,;14.43,-46.95,;15.96,-46.98,;19.71,-48.34,;19.71,-49.88,;21.04,-50.66,;22.37,-49.89,;23.69,-50.66,;23.69,-52.21,;22.34,-52.97,;21.02,-52.19,;25.02,-52.98,;25.01,-54.52,;26.36,-52.22,;27.68,-53,;28.2,-54.45,;29.74,-54.41,;30.18,-52.94,;28.91,-52.06,;21.04,-47.58,;21.05,-46.04,;22.39,-45.28,;23.72,-46.06,;23.71,-47.6,;22.37,-48.36,;25.06,-45.3,;26.39,-44.52,;25.83,-46.64,;24.3,-43.97,)|
Show InChI InChI=1S/C32H42N8O2/c1-32(2,3)23-13-15-24(16-14-23)40(20-21-9-11-22(12-10-21)29(41)34-30-35-37-38-36-30)31-33-27-19-26(17-18-28(27)39(31)4)42-25-7-5-6-8-25/h9-12,17-19,23-25H,5-8,13-16,20H2,1-4H3,(H2,34,35,36,37,38,41)/t23-,24-
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Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120319
PNG
(CHEMBL3616588)
Show SMILES CCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C36H31F6N3O5/c1-3-4-29(22-5-7-23(8-6-22)34(48)43-18-17-32(46)47)45-30-19-24(21-9-13-26(14-10-21)50-36(40,41)42)11-15-27(30)33(44-45)28-20-25(35(37,38)39)12-16-31(28)49-2/h5-16,19-20,29H,3-4,17-18H2,1-2H3,(H,43,48)(H,46,47)
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Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235130
PNG
(US9359339, 13)
Show SMILES CCC[C@@H](C(c1csc2c(cc(F)cc12)C#N)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C30H26ClFN2O3S/c1-2-3-24(18-4-6-20(7-5-18)30(37)34-13-12-27(35)36)28(19-8-10-22(31)11-9-19)26-17-38-29-21(16-33)14-23(32)15-25(26)29/h4-11,14-15,17,24,28H,2-3,12-13H2,1H3,(H,34,37)(H,35,36)/t24-,28?/m1/s1
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n/an/a 1.10n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50358368
PNG
(CHEMBL1922834)
Show SMILES CCCOc1cc(cc2n(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)c(=Nc3ccc(OC(F)(F)F)cc3)n(C)c12)C(F)(F)F |w:26.28|
Show InChI InChI=1S/C28H24F6N8O3/c1-3-12-44-22-14-18(27(29,30)31)13-21-23(22)41(2)26(35-19-8-10-20(11-9-19)45-28(32,33)34)42(21)15-16-4-6-17(7-5-16)24(43)36-25-37-39-40-38-25/h4-11,13-14H,3,12,15H2,1-2H3,(H2,36,37,38,39,40,43)
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n/an/a 1.30n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting


Bioorg Med Chem Lett 21: 7131-6 (2011)


Article DOI: 10.1016/j.bmcl.2011.09.085
BindingDB Entry DOI: 10.7270/Q2C829QP
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235131
PNG
(US9359339, 14)
Show SMILES CCC[C@@H](C(c1csc2c(cc(C)cc12)C#N)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H29ClN2O3S/c1-3-4-25(20-5-7-22(8-6-20)31(37)34-14-13-28(35)36)29(21-9-11-24(32)12-10-21)27-18-38-30-23(17-33)15-19(2)16-26(27)30/h5-12,15-16,18,25,29H,3-4,13-14H2,1-2H3,(H,34,37)(H,35,36)/t25-,29?/m1/s1
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US Patent
n/an/a 1.30n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120342
PNG
(CHEMBL3616689)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(SC)cc1
Show InChI InChI=1S/C37H36F3N3O4S/c1-4-5-6-31(24-7-9-25(10-8-24)36(46)41-20-19-34(44)45)43-32-21-26(23-11-15-28(48-3)16-12-23)13-17-29(32)35(42-43)30-22-27(37(38,39)40)14-18-33(30)47-2/h7-18,21-22,31H,4-6,19-20H2,1-3H3,(H,41,46)(H,44,45)
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n/an/a 1.5n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120364
PNG
(CHEMBL3616692)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(OC)c(F)c1
Show InChI InChI=1S/C37H35F4N3O5/c1-4-5-6-30(22-7-9-23(10-8-22)36(47)42-18-17-34(45)46)44-31-20-25(24-12-15-33(49-3)29(38)19-24)11-14-27(31)35(43-44)28-21-26(37(39,40)41)13-16-32(28)48-2/h7-16,19-21,30H,4-6,17-18H2,1-3H3,(H,42,47)(H,45,46)
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n/an/a 1.5n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120366
PNG
(CHEMBL3616694)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C37H33F6N3O4/c1-3-4-5-30(23-6-8-24(9-7-23)35(49)44-19-18-33(47)48)46-31-20-25(22-10-13-26(14-11-22)36(38,39)40)12-16-28(31)34(45-46)29-21-27(37(41,42)43)15-17-32(29)50-2/h6-17,20-21,30H,3-5,18-19H2,1-2H3,(H,44,49)(H,47,48)
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n/an/a 1.60n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50358360
PNG
(CHEMBL1922708)
Show SMILES CCCCc1cc(cc2n(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)c(=Nc3ccc(OC(F)(F)F)cc3)n(C)c12)C(F)(F)F |w:26.28|
Show InChI InChI=1S/C29H26F6N8O2/c1-3-4-5-19-14-20(28(30,31)32)15-23-24(19)42(2)27(36-21-10-12-22(13-11-21)45-29(33,34)35)43(23)16-17-6-8-18(9-7-17)25(44)37-26-38-40-41-39-26/h6-15H,3-5,16H2,1-2H3,(H2,37,38,39,40,41,44)
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n/an/a 1.70n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting


Bioorg Med Chem Lett 21: 7131-6 (2011)


Article DOI: 10.1016/j.bmcl.2011.09.085
BindingDB Entry DOI: 10.7270/Q2C829QP
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235132
PNG
(US9359339, 15)
Show SMILES CCC[C@@H](C(c1csc2c(cc(cc12)C(F)(F)F)C#N)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C31H26ClF3N2O3S/c1-2-3-24(18-4-6-20(7-5-18)30(40)37-13-12-27(38)39)28(19-8-10-23(32)11-9-19)26-17-41-29-21(16-36)14-22(15-25(26)29)31(33,34)35/h4-11,14-15,17,24,28H,2-3,12-13H2,1H3,(H,37,40)(H,38,39)/t24-,28?/m1/s1
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n/an/a 1.70n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50199486
PNG
(3-(1-(N-((1r,4r)-4-tert-butylcyclohexyl)-2-(4-(tri...)
Show SMILES CC(C)(C)[C@H]1CC[C@@H](CC1)N(C1CCc2cc(ccc12)C(=O)NCCC(O)=O)C(=O)Cc1ccc(OC(F)(F)F)cc1 |w:11.11,wU:7.10,wD:4.3,(-1.44,-41.26,;-1.43,-39.72,;.11,-39.73,;-2.97,-39.72,;-1.42,-38.18,;-.09,-37.41,;-.08,-35.87,;-1.4,-35.1,;-2.75,-35.87,;-2.75,-37.4,;-1.41,-33.56,;-.07,-32.8,;.25,-31.29,;2.11,-31.33,;2.58,-32.79,;3.92,-33.55,;3.92,-35.09,;2.59,-35.87,;1.25,-35.1,;1.26,-33.56,;5.26,-35.86,;5.26,-37.4,;6.59,-35.09,;7.92,-35.86,;9.26,-35.08,;10.59,-35.85,;11.92,-35.08,;10.6,-37.39,;-2.74,-32.79,;-2.74,-31.25,;-4.07,-33.57,;-5.41,-32.8,;-6.75,-33.57,;-8.08,-32.8,;-8.08,-31.25,;-9.41,-30.48,;-9.41,-28.94,;-9.43,-27.4,;-7.87,-28.94,;-10.95,-28.95,;-6.75,-30.48,;-5.41,-31.25,)|
Show InChI InChI=1S/C32H39F3N2O5/c1-31(2,3)23-8-10-24(11-9-23)37(28(38)18-20-4-12-25(13-5-20)42-32(33,34)35)27-15-7-21-19-22(6-14-26(21)27)30(41)36-17-16-29(39)40/h4-6,12-14,19,23-24,27H,7-11,15-18H2,1-3H3,(H,36,41)(H,39,40)/t23-,24-,27?
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n/an/a 1.80n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125]glucagon from human glucagon receptor expressed in CHO cells


Bioorg Med Chem Lett 17: 587-92 (2007)


Article DOI: 10.1016/j.bmcl.2006.11.014
BindingDB Entry DOI: 10.7270/Q2N58M0Q
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235142
PNG
(US9359339, 45)
Show SMILES CCC[C@@H](C(c1sc2ccccc2c1C)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C30H30ClNO3S/c1-3-6-25(20-9-11-22(12-10-20)30(35)32-18-17-27(33)34)28(21-13-15-23(31)16-14-21)29-19(2)24-7-4-5-8-26(24)36-29/h4-5,7-16,25,28H,3,6,17-18H2,1-2H3,(H,32,35)(H,33,34)/t25-,28?/m1/s1
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n/an/a 1.80n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50393776
PNG
(CHEMBL2159349)
Show SMILES COc1ccc2cc(ccc2c1)-c1cc(nn1[C@@H](C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1cc(Cl)cc(c1)C(F)(F)F |r|
Show InChI InChI=1S/C33H27ClF3N3O4/c1-19(20-3-5-21(6-4-20)32(43)38-12-11-31(41)42)40-30(24-8-7-23-16-28(44-2)10-9-22(23)13-24)18-29(39-40)25-14-26(33(35,36)37)17-27(34)15-25/h3-10,13-19H,11-12H2,1-2H3,(H,38,43)(H,41,42)/t19-/m0/s1
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n/an/a 1.90n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay


J Med Chem 55: 6137-48 (2012)


Article DOI: 10.1021/jm300579z
BindingDB Entry DOI: 10.7270/Q2X63P2C
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120339
PNG
(CHEMBL3616687)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(OC)cc1
Show InChI InChI=1S/C37H36F3N3O5/c1-4-5-6-31(24-7-9-25(10-8-24)36(46)41-20-19-34(44)45)43-32-21-26(23-11-15-28(47-2)16-12-23)13-17-29(32)35(42-43)30-22-27(37(38,39)40)14-18-33(30)48-3/h7-18,21-22,31H,4-6,19-20H2,1-3H3,(H,41,46)(H,44,45)
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n/an/a 1.90n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244199
PNG
(CHEMBL458145 | trans-4-(((4-tert-butylcyclohexyl)(...)
Show SMILES Cn1c(nc2cc(O)ccc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:27.30,wD:30.37,(-7.23,-33.1,;-6.46,-31.77,;-5.03,-31.18,;-5.16,-29.64,;-6.66,-29.29,;-7.39,-27.94,;-8.93,-27.9,;-9.67,-26.55,;-9.73,-29.22,;-8.99,-30.57,;-7.46,-30.6,;-3.7,-31.96,;-3.71,-33.5,;-2.38,-34.28,;-1.05,-33.51,;.28,-34.28,;.27,-35.83,;-1.08,-36.59,;-2.4,-35.81,;1.6,-36.6,;1.59,-38.14,;2.94,-35.84,;4.27,-36.62,;4.79,-38.07,;6.32,-38.03,;6.76,-36.56,;5.5,-35.68,;-2.37,-31.2,;-2.37,-29.66,;-1.02,-28.9,;.31,-29.68,;.29,-31.22,;-1.04,-31.98,;1.65,-28.92,;2.97,-28.14,;2.42,-30.26,;.88,-27.59,)|
Show InChI InChI=1S/C27H34N8O2/c1-27(2,3)19-9-11-20(12-10-19)35(26-28-22-15-21(36)13-14-23(22)34(26)4)16-17-5-7-18(8-6-17)24(37)29-25-30-32-33-31-25/h5-8,13-15,19-20,36H,9-12,16H2,1-4H3,(H2,29,30,31,32,33,37)/t19-,20-
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120327
PNG
(CHEMBL3616675)
Show SMILES CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(Cl)ccc2C(N)=O)c2ccc(cc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C33H26ClF3N4O5/c1-18(19-2-4-21(5-3-19)32(45)39-15-14-29(42)43)41-28-16-22(20-6-10-24(11-7-20)46-33(35,36)37)8-12-26(28)30(40-41)27-17-23(34)9-13-25(27)31(38)44/h2-13,16-18H,14-15H2,1H3,(H2,38,44)(H,39,45)(H,42,43)
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120281
PNG
(CHEMBL3616584)
Show SMILES CCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(C)cc1
Show InChI InChI=1S/C36H34F3N3O4/c1-4-5-30(24-10-12-25(13-11-24)35(45)40-19-18-33(43)44)42-31-20-26(23-8-6-22(2)7-9-23)14-16-28(31)34(41-42)29-21-27(36(37,38)39)15-17-32(29)46-3/h6-17,20-21,30H,4-5,18-19H2,1-3H3,(H,40,45)(H,43,44)
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244237
PNG
(CHEMBL448921 | trans-4-(((4-tert-butylcyclohexyl)(...)
Show SMILES Cn1c(nc2cc(OCC3CCCC3)ccc12)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:33.37,wD:36.44,(-7.9,-48.6,;-7.12,-47.26,;-5.7,-46.67,;-5.82,-45.13,;-7.32,-44.78,;-8.06,-43.43,;-9.59,-43.39,;-10.33,-42.04,;-9.53,-40.73,;-10.27,-39.37,;-9.61,-37.98,;-10.73,-36.92,;-12.08,-37.66,;-11.8,-39.17,;-10.4,-44.71,;-9.66,-46.06,;-8.13,-46.09,;-4.37,-47.45,;-4.38,-48.99,;-3.05,-49.77,;-1.72,-49,;-.39,-49.77,;-.4,-51.32,;-1.74,-52.08,;-3.07,-51.3,;.93,-52.09,;.92,-53.63,;2.27,-51.33,;3.6,-52.11,;4.12,-53.56,;5.66,-53.52,;6.1,-52.05,;4.83,-51.17,;-3.04,-46.69,;-3.04,-45.15,;-1.69,-44.39,;-.36,-45.17,;-.38,-46.71,;-1.71,-47.47,;.98,-44.41,;2.3,-43.63,;1.75,-45.75,;.21,-43.08,)|
Show InChI InChI=1S/C33H44N8O2/c1-33(2,3)25-13-15-26(16-14-25)41(20-22-9-11-24(12-10-22)30(42)35-31-36-38-39-37-31)32-34-28-19-27(17-18-29(28)40(32)4)43-21-23-7-5-6-8-23/h9-12,17-19,23,25-26H,5-8,13-16,20-21H2,1-4H3,(H2,35,36,37,38,39,42)/t25-,26-
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244235
PNG
(CHEMBL480692 | trans-4-(((4-tert-butylcyclohexyl)(...)
Show SMILES CCCOc1ccc2n(C)c(nc2c1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:30.33,wD:33.40,(15,-40.17,;14.2,-41.49,;14.94,-42.84,;14.14,-44.16,;14.88,-45.51,;14.07,-46.83,;14.81,-48.17,;16.34,-48.21,;17.35,-49.38,;16.57,-50.71,;18.77,-48.79,;18.65,-47.25,;17.15,-46.9,;16.41,-45.55,;20.1,-49.57,;20.09,-51.11,;21.42,-51.88,;22.75,-51.12,;24.08,-51.89,;24.07,-53.43,;22.73,-54.2,;21.4,-53.42,;25.4,-54.21,;25.39,-55.75,;26.74,-53.45,;28.07,-54.23,;28.59,-55.68,;30.13,-55.64,;30.57,-54.16,;29.3,-53.29,;21.43,-48.8,;21.43,-47.27,;22.78,-46.51,;24.11,-47.29,;24.09,-48.83,;22.76,-49.58,;25.45,-46.53,;26.77,-45.75,;26.22,-47.86,;24.68,-45.19,)|
Show InChI InChI=1S/C30H40N8O2/c1-6-17-40-24-15-16-26-25(18-24)31-29(37(26)5)38(23-13-11-22(12-14-23)30(2,3)4)19-20-7-9-21(10-8-20)27(39)32-28-33-35-36-34-28/h7-10,15-16,18,22-23H,6,11-14,17,19H2,1-5H3,(H2,32,33,34,35,36,39)/t22-,23-
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50244234
PNG
(CHEMBL518939 | trans-4-(((4-tert-butylcyclohexyl)(...)
Show SMILES CCOc1ccc2n(C)c(nc2c1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)[C@H]1CC[C@@H](CC1)C(C)(C)C |r,wU:29.32,wD:32.39,(-10.27,-39.37,;-9.53,-40.73,;-10.33,-42.04,;-9.59,-43.39,;-10.4,-44.71,;-9.66,-46.06,;-8.13,-46.09,;-7.12,-47.26,;-7.9,-48.6,;-5.7,-46.67,;-5.82,-45.14,;-7.32,-44.78,;-8.06,-43.43,;-4.37,-47.45,;-4.38,-48.99,;-3.05,-49.77,;-1.72,-49,;-.39,-49.78,;-.4,-51.32,;-1.74,-52.08,;-3.07,-51.3,;.93,-52.1,;.92,-53.64,;2.27,-51.33,;3.6,-52.11,;4.12,-53.56,;5.66,-53.52,;6.1,-52.05,;4.83,-51.17,;-3.04,-46.69,;-3.04,-45.15,;-1.69,-44.39,;-.36,-45.17,;-.38,-46.71,;-1.71,-47.47,;.98,-44.41,;2.3,-43.63,;1.75,-45.75,;.21,-43.08,)|
Show InChI InChI=1S/C29H38N8O2/c1-6-39-23-15-16-25-24(17-23)30-28(36(25)5)37(22-13-11-21(12-14-22)29(2,3)4)18-19-7-9-20(10-8-19)26(38)31-27-32-34-35-33-27/h7-10,15-17,21-22H,6,11-14,18H2,1-5H3,(H2,31,32,33,34,35,38)/t21-,22-
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n/an/a 2n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 18: 3701-5 (2008)


Article DOI: 10.1016/j.bmcl.2008.05.072
BindingDB Entry DOI: 10.7270/Q26Q1X25
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235129
PNG
(US9359339, 8)
Show SMILES CCC[C@@H](C(c1c(C)sc2ccccc12)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C30H30ClNO3S/c1-3-6-24(20-9-11-22(12-10-20)30(35)32-18-17-27(33)34)29(21-13-15-23(31)16-14-21)28-19(2)36-26-8-5-4-7-25(26)28/h4-5,7-16,24,29H,3,6,17-18H2,1-2H3,(H,32,35)(H,33,34)/t24-,29?/m1/s1
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n/an/a 2.20n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50358373
PNG
(CHEMBL1922839)
Show SMILES CCCOc1cc(cc2n(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)c(=Nc3ccc(cc3)C(C)(C)C)n(C)c12)C(F)(F)F |w:26.28|
Show InChI InChI=1S/C31H33F3N8O2/c1-6-15-44-25-17-22(31(32,33)34)16-24-26(25)41(5)29(35-23-13-11-21(12-14-23)30(2,3)4)42(24)18-19-7-9-20(10-8-19)27(43)36-28-37-39-40-38-28/h7-14,16-17H,6,15,18H2,1-5H3,(H2,36,37,38,39,40,43)
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n/an/a 2.20n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting


Bioorg Med Chem Lett 21: 7131-6 (2011)


Article DOI: 10.1016/j.bmcl.2011.09.085
BindingDB Entry DOI: 10.7270/Q2C829QP
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50122102
PNG
(3-Cyano-4-hydroxy-benzoic acid [1-(2,3,5,6-tetrame...)
Show SMILES Cc1cc(C)c(C)c(Cn2ccc3c(\C=N\NC(=O)c4ccc(O)c(c4)C#N)cccc23)c1C
Show InChI InChI=1S/C28H26N4O2/c1-17-12-18(2)20(4)25(19(17)3)16-32-11-10-24-22(6-5-7-26(24)32)15-30-31-28(34)21-8-9-27(33)23(13-21)14-29/h5-13,15,33H,16H2,1-4H3,(H,31,34)/b30-15+
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n/an/a 2.30n/an/an/an/an/an/a



Novo Nordisk A/S

Curated by ChEMBL


Assay Description
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells


J Med Chem 45: 5755-75 (2002)


BindingDB Entry DOI: 10.7270/Q26W99FD
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235126
PNG
(US9359339, 3)
Show SMILES CCC[C@@H](C(c1csc2c(Br)cc(C)cc12)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)Nc1nnn[nH]1 |r|
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n/an/a 2.30n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50122102
PNG
(3-Cyano-4-hydroxy-benzoic acid [1-(2,3,5,6-tetrame...)
Show SMILES Cc1cc(C)c(C)c(Cn2ccc3c(\C=N\NC(=O)c4ccc(O)c(c4)C#N)cccc23)c1C
Show InChI InChI=1S/C28H26N4O2/c1-17-12-18(2)20(4)25(19(17)3)16-32-11-10-24-22(6-5-7-26(24)32)15-30-31-28(34)21-8-9-27(33)23(13-21)14-29/h5-13,15,33H,16H2,1-4H3,(H,31,34)/b30-15+
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n/an/a 2.30n/an/an/an/an/an/a



Dainippon Sumitomo Pharma. Co. Ltd

Curated by ChEMBL


Assay Description
Antagonist activity against human glucagon receptor


Bioorg Med Chem Lett 24: 4266-70 (2014)


Article DOI: 10.1016/j.bmcl.2014.07.025
BindingDB Entry DOI: 10.7270/Q2ZW1NK4
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM235127
PNG
(US9359339, 4)
Show SMILES CCC[C@@H](C(c1csc2c(Br)cc(C)cc12)c1ccc(Cl)cc1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r|
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n/an/a 2.5n/an/an/an/a7.525



Merck Sharp & Dohme Corp.

US Patent


Assay Description
A stable CHO (Chinese hamster ovary) cell line expressing cloned human glucagon receptor was maintained as described (Chicchi, et. al. J Biol Chem 27...


US Patent US9359339 (2016)


BindingDB Entry DOI: 10.7270/Q2FQ9VHC
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50393781
PNG
(CHEMBL2159337)
Show SMILES C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(cc1-c1ccc2cc(OC(F)(F)F)ccc2c1)-c1cc(Cl)cc(Cl)c1 |r|
Show InChI InChI=1S/C32H24Cl2F3N3O4/c1-18(19-2-4-20(5-3-19)31(43)38-11-10-30(41)42)40-29(17-28(39-40)24-13-25(33)16-26(34)14-24)23-7-6-22-15-27(44-32(35,36)37)9-8-21(22)12-23/h2-9,12-18H,10-11H2,1H3,(H,38,43)(H,41,42)/t18-/m0/s1
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n/an/a 2.5n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay


J Med Chem 55: 6137-48 (2012)


Article DOI: 10.1021/jm300579z
BindingDB Entry DOI: 10.7270/Q2X63P2C
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120374
PNG
(CHEMBL3616701)
Show SMILES COc1ccc(cc1-c1nn(C(C)c2ccc(cc2)C(=O)NCCC(O)=O)c2cc(ccc12)-c1ccc(C)cc1)C(F)(F)F
Show InChI InChI=1S/C34H30F3N3O4/c1-20-4-6-23(7-5-20)25-12-14-27-29(18-25)40(39-32(27)28-19-26(34(35,36)37)13-15-30(28)44-3)21(2)22-8-10-24(11-9-22)33(43)38-17-16-31(41)42/h4-15,18-19,21H,16-17H2,1-3H3,(H,38,43)(H,41,42)
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n/an/a 2.60n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120341
PNG
(CHEMBL3616688)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccc(C)cc1
Show InChI InChI=1S/C37H36F3N3O4/c1-4-5-6-31(25-11-13-26(14-12-25)36(46)41-20-19-34(44)45)43-32-21-27(24-9-7-23(2)8-10-24)15-17-29(32)35(42-43)30-22-28(37(38,39)40)16-18-33(30)47-3/h7-18,21-22,31H,4-6,19-20H2,1-3H3,(H,41,46)(H,44,45)
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n/an/a 2.60n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50122159
PNG
(CHEMBL152477 | Cyclopentanecarboxylic acid {4-[(3-...)
Show SMILES Oc1ccc(cc1C#N)C(=O)NN=Cc1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12 |w:12.12|
Show InChI InChI=1S/C31H30N4O4/c32-18-24-17-22(14-16-28(24)36)29(37)34-33-19-23-13-15-27(26-12-6-5-11-25(23)26)35(30(38)20-7-1-2-8-20)31(39)21-9-3-4-10-21/h5-6,11-17,19-21,36H,1-4,7-10H2,(H,34,37)
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n/an/a 2.80n/an/an/an/an/an/a



Novo Nordisk A/S

Curated by ChEMBL


Assay Description
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells


J Med Chem 45: 5755-75 (2002)


BindingDB Entry DOI: 10.7270/Q26W99FD
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50358366
PNG
(CHEMBL1922714)
Show SMILES CCOc1cc(cc2n(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)c(=Nc3ccc(OC(F)(F)F)cc3)n(C)c12)C(F)(F)F |w:25.27|
Show InChI InChI=1S/C27H22F6N8O3/c1-3-43-21-13-17(26(28,29)30)12-20-22(21)40(2)25(34-18-8-10-19(11-9-18)44-27(31,32)33)41(20)14-15-4-6-16(7-5-15)23(42)35-24-36-38-39-37-24/h4-13H,3,14H2,1-2H3,(H2,35,36,37,38,39,42)
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n/an/a 2.80n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting


Bioorg Med Chem Lett 21: 7131-6 (2011)


Article DOI: 10.1016/j.bmcl.2011.09.085
BindingDB Entry DOI: 10.7270/Q2C829QP
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120322
PNG
(CHEMBL3616591)
Show SMILES COc1ccc(Cl)cc1-c1nn(C(C)c2ccc(cc2)C(=O)NCCC(O)=O)c2cc(ccc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C33H27ClF3N3O5/c1-19(20-3-5-22(6-4-20)32(43)38-16-15-30(41)42)40-28-17-23(21-7-11-25(12-8-21)45-33(35,36)37)9-13-26(28)31(39-40)27-18-24(34)10-14-29(27)44-2/h3-14,17-19H,15-16H2,1-2H3,(H,38,43)(H,41,42)
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n/an/a 3n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120333
PNG
(CHEMBL3616681)
Show SMILES CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(Cl)cc(c2)C(F)(F)F)c2ccc(cc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C33H24ClF6N3O4/c1-18(19-2-4-21(5-3-19)31(46)41-13-12-29(44)45)43-28-16-22(20-6-9-26(10-7-20)47-33(38,39)40)8-11-27(28)30(42-43)23-14-24(32(35,36)37)17-25(34)15-23/h2-11,14-18H,12-13H2,1H3,(H,41,46)(H,44,45)
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n/an/a 3n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50120362
PNG
(CHEMBL3616690)
Show SMILES CCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1nc(-c2cc(ccc2OC)C(F)(F)F)c2ccc(cc12)-c1ccccc1
Show InChI InChI=1S/C36H34F3N3O4/c1-3-4-10-30(24-11-13-25(14-12-24)35(45)40-20-19-33(43)44)42-31-21-26(23-8-6-5-7-9-23)15-17-28(31)34(41-42)29-22-27(36(37,38)39)16-18-32(29)46-2/h5-9,11-18,21-22,30H,3-4,10,19-20H2,1-2H3,(H,40,45)(H,43,44)
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n/an/a 3n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human glucagon receptor expressed in CHO cell membranes


Bioorg Med Chem Lett 25: 4143-7 (2015)


Article DOI: 10.1016/j.bmcl.2015.08.015
BindingDB Entry DOI: 10.7270/Q23F4RGX
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50075752
PNG
(4-[5-(4-Chloro-phenyl)-3-(2-isobutoxy-phenyl)-1H-p...)
Show SMILES CC(C)COc1ccccc1-c1cc([nH]c1-c1ccncc1)-c1ccc(Cl)cc1
Show InChI InChI=1S/C25H23ClN2O/c1-17(2)16-29-24-6-4-3-5-21(24)22-15-23(18-7-9-20(26)10-8-18)28-25(22)19-11-13-27-14-12-19/h3-15,17,28H,16H2,1-2H3
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n/an/a 3n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Binding affinity determined by reduction in binding of 125 I-glucagon to the human glucagon receptor expressed on CHO cells in absence of Mg+2


Bioorg Med Chem Lett 9: 641-6 (1999)


BindingDB Entry DOI: 10.7270/Q2VD6XM1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50358370
PNG
(CHEMBL1922836)
Show SMILES CCCCOc1cc(cc2n(Cc3ccc(cc3)C(=O)Nc3nnn[nH]3)c(=Nc3ccc(OC(F)(F)F)cc3)n(C)c12)C(F)(F)F |w:27.29|
Show InChI InChI=1S/C29H26F6N8O3/c1-3-4-13-45-23-15-19(28(30,31)32)14-22-24(23)42(2)27(36-20-9-11-21(12-10-20)46-29(33,34)35)43(22)16-17-5-7-18(8-6-17)25(44)37-26-38-40-41-39-26/h5-12,14-15H,3-4,13,16H2,1-2H3,(H2,37,38,39,40,41,44)
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n/an/a 3.10n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 4 to 12 hrs by scintillation counting


Bioorg Med Chem Lett 21: 7131-6 (2011)


Article DOI: 10.1016/j.bmcl.2011.09.085
BindingDB Entry DOI: 10.7270/Q2C829QP
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50334486
PNG
(CHEMBL1643951 | trans-4-((1-(4-tert-butylcyclohexy...)
Show SMILES CC(C)(C)[C@H]1CC[C@@H](CC1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)C(=O)Nc1ccc(OC(F)(F)F)cc1 |r,wU:7.10,wD:4.3,(26.38,-4.09,;27.72,-3.32,;29.05,-4.09,;27.7,-4.85,;27.72,-1.78,;29.05,-1.01,;29.05,.54,;27.72,1.29,;26.38,.53,;26.38,-1.01,;27.71,2.83,;26.38,3.6,;25.05,2.82,;25.05,1.27,;23.71,.5,;22.38,1.27,;22.38,2.82,;23.71,3.59,;21.05,.5,;21.04,-1.04,;19.71,1.27,;18.38,.5,;16.98,1.14,;15.95,-.01,;16.72,-1.34,;18.23,-1.02,;29.04,3.61,;29.04,5.15,;30.38,2.84,;31.71,3.62,;33.04,2.85,;34.37,3.62,;34.37,5.16,;35.7,5.94,;37.03,5.18,;38.36,5.96,;37.04,3.64,;38.36,4.41,;33.02,5.93,;31.7,5.15,)|
Show InChI InChI=1S/C27H32F3N7O3/c1-26(2,3)19-8-12-21(13-9-19)37(25(39)31-20-10-14-22(15-11-20)40-27(28,29)30)16-17-4-6-18(7-5-17)23(38)32-24-33-35-36-34-24/h4-7,10-11,14-15,19,21H,8-9,12-13,16H2,1-3H3,(H,31,39)(H2,32,33,34,35,36,38)/t19-,21-
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n/an/a 3.20n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Displacement of [125I]glucagon from human GCGR expressed in CHO cells


Bioorg Med Chem Lett 21: 76-81 (2010)


Article DOI: 10.1016/j.bmcl.2010.11.074
BindingDB Entry DOI: 10.7270/Q2R211PW
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50171818
PNG
(4-[1-(4-tert-Butyl-cyclohexyl)-3-(4-trifluorometho...)
Show SMILES CC(C)(C)C1CCC(CC1)N(Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)C(=O)Nc1ccc(OC(F)(F)F)cc1 |(-1.28,-4.62,;-2.05,-3.29,;-2.82,-1.94,;-3.4,-4.04,;-.72,-2.5,;.17,-.87,;1.62,-1.75,;4.02,-1.82,;2.92,-2.9,;2.08,-2.5,;5.35,-2.59,;5.35,-4.13,;6.68,-4.88,;6.68,-6.44,;8.01,-7.21,;9.34,-6.44,;9.34,-4.88,;8.01,-4.11,;10.69,-7.21,;10.69,-8.75,;12.02,-6.42,;13.35,-7.19,;14.85,-6.84,;15.64,-8.14,;14.66,-9.32,;13.24,-8.73,;6.68,-1.8,;6.68,-.26,;8.01,-2.57,;9.34,-1.8,;9.34,-.28,;10.67,.49,;12,-.28,;13.33,.49,;14.68,-.26,;13.89,-1.59,;16.01,-1.03,;15.43,1.07,;12,-1.82,;10.67,-2.59,)|
Show InChI InChI=1S/C27H32F3N7O3/c1-26(2,3)19-8-12-21(13-9-19)37(25(39)31-20-10-14-22(15-11-20)40-27(28,29)30)16-17-4-6-18(7-5-17)23(38)32-24-33-35-36-34-24/h4-7,10-11,14-15,19,21H,8-9,12-13,16H2,1-3H3,(H,31,39)(H2,32,33,34,35,36,38)
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n/an/a 3.20n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Antagonist activity against human glucagon receptor expressed in CHO cell membranes using [125I]glucagon


Bioorg Med Chem Lett 15: 4564-9 (2005)


Article DOI: 10.1016/j.bmcl.2005.06.101
BindingDB Entry DOI: 10.7270/Q26T0M5F
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50122153
PNG
(CHEMBL156724 | Cyclopentanecarboxylic acid {4-[(3-...)
Show SMILES Oc1ccc(cc1Cl)C(=O)NN=Cc1ccc(N(C(=O)C2CCCC2)C(=O)C2CCCC2)c2ccccc12 |w:11.11|
Show InChI InChI=1S/C30H30ClN3O4/c31-25-17-21(14-16-27(25)35)28(36)33-32-18-22-13-15-26(24-12-6-5-11-23(22)24)34(29(37)19-7-1-2-8-19)30(38)20-9-3-4-10-20/h5-6,11-20,35H,1-4,7-10H2,(H,33,36)
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n/an/a 3.40n/an/an/an/an/an/a



Novo Nordisk A/S

Curated by ChEMBL


Assay Description
In vitro binding affinity for recombinant human glucagon receptor (hGGR) in BHK cells


J Med Chem 45: 5755-75 (2002)


BindingDB Entry DOI: 10.7270/Q26W99FD
More data for this
Ligand-Target Pair
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