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Compile Data Set for Download or QSAR

Found 246 hits with Last Name = 'rentzeperis' and Initial = 'd'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Glucagon receptor


(Homo sapiens (Human))
BDBM50525881
PNG
(CHEMBL4513792)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(c(C)cc12)-c1ccc(cc1C)C(F)(F)F |r|
Show InChI InChI=1S/C31H32F3N3O3/c1-18(2)13-27(21-5-7-22(8-6-21)30(40)35-12-11-29(38)39)37-28-15-20(4)26(16-23(28)17-36-37)25-10-9-24(14-19(25)3)31(32,33)34/h5-10,14-18,27H,11-13H2,1-4H3,(H,35,40)(H,38,39)/t27-/m0/s1
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14n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522731
PNG
(CHEMBL4441980)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2c(Cl)c(ccc2n1)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-26(19-4-6-20(7-5-19)29(40)35-13-12-27(38)39)37-16-24-25(36-37)11-10-23(28(24)31)22-9-8-21(15-18(22)3)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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19n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525882
PNG
(CHEMBL4472098)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2c(C)c(ccc2n1)-c1ccc(cc1C)C(F)(F)F |r|
Show InChI InChI=1S/C31H32F3N3O3/c1-18(2)15-28(21-5-7-22(8-6-21)30(40)35-14-13-29(38)39)37-17-26-20(4)25(11-12-27(26)36-37)24-10-9-23(16-19(24)3)31(32,33)34/h5-12,16-18,28H,13-15H2,1-4H3,(H,35,40)(H,38,39)/t28-/m0/s1
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22n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525891
PNG
(CHEMBL4463908)
Show SMILES COc1c(ccc2n(ncc12)[C@@H](CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1C)C(F)(F)F |r|
Show InChI InChI=1S/C31H32F3N3O4/c1-18(2)15-27(20-5-7-21(8-6-20)30(40)35-14-13-28(38)39)37-26-12-11-24(29(41-4)25(26)17-36-37)23-10-9-22(16-19(23)3)31(32,33)34/h5-12,16-18,27H,13-15H2,1-4H3,(H,35,40)(H,38,39)/t27-/m0/s1
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22n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522737
PNG
(CHEMBL4469925)
Show SMILES COc1c(ccc2nn(cc12)C(CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O4/c1-17(2)14-26(18-4-6-19(7-5-18)29(40)35-13-12-27(38)39)37-16-23-25(36-37)11-10-22(28(23)41-3)21-9-8-20(15-24(21)31)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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22n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525890
PNG
(CHEMBL4582082)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2c(C)c(ccc2n1)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-27(19-4-6-20(7-5-19)29(40)35-13-12-28(38)39)37-16-24-18(3)22(10-11-26(24)36-37)23-9-8-21(15-25(23)31)30(32,33)34/h4-11,15-17,27H,12-14H2,1-3H3,(H,35,40)(H,38,39)/t27-/m0/s1
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23n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525884
PNG
(CHEMBL4589676)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2cc(c(C)cc2n1)-c1ccc(cc1C)C(F)(F)F |r|
Show InChI InChI=1S/C31H32F3N3O3/c1-18(2)13-28(21-5-7-22(8-6-21)30(40)35-12-11-29(38)39)37-17-23-16-26(20(4)15-27(23)36-37)25-10-9-24(14-19(25)3)31(32,33)34/h5-10,14-18,28H,11-13H2,1-4H3,(H,35,40)(H,38,39)/t28-/m0/s1
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25n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522734
PNG
(CHEMBL4444819)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2c(C)c(ccc2n1)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-27(19-4-6-20(7-5-19)29(40)35-13-12-28(38)39)37-16-24-18(3)22(10-11-26(24)36-37)23-9-8-21(15-25(23)31)30(32,33)34/h4-11,15-17,27H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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29n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525893
PNG
(CHEMBL4567272)
Show SMILES COc1c(ccc2n(ncc12)[C@@H](CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O4/c1-17(2)14-26(18-4-6-19(7-5-18)29(40)35-13-12-27(38)39)37-25-11-10-22(28(41-3)23(25)16-36-37)21-9-8-20(15-24(21)31)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)/t26-/m0/s1
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30n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525883
PNG
(CHEMBL4468579)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(c(C)cc12)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)12-26(19-4-6-20(7-5-19)29(40)35-11-10-28(38)39)37-27-13-18(3)24(14-21(27)16-36-37)23-9-8-22(15-25(23)31)30(32,33)34/h4-9,13-17,26H,10-12H2,1-3H3,(H,35,40)(H,38,39)/t26-/m0/s1
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32n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522721
PNG
(CHEMBL4558340)
Show SMILES CC(C)CC(c1ccc(nc1)C(=O)NCCC(O)=O)n1ncc2cc(c(C)cc12)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C30H31F3N4O3/c1-17(2)11-26(20-5-8-25(35-15-20)29(40)34-10-9-28(38)39)37-27-13-19(4)24(14-21(27)16-36-37)23-7-6-22(12-18(23)3)30(31,32)33/h5-8,12-17,26H,9-11H2,1-4H3,(H,34,40)(H,38,39)
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32n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525888
PNG
(CHEMBL4460982)
Show SMILES COc1c(ccc2nn(cc12)[C@H](CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O4/c1-17(2)14-26(18-4-6-19(7-5-18)29(40)35-13-12-27(38)39)37-16-23-25(36-37)11-10-22(28(23)41-3)21-9-8-20(15-24(21)31)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)/t26-/m1/s1
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35n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525887
PNG
(CHEMBL4444605)
Show SMILES COc1c(ccc2nn(cc12)[C@@H](CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O4/c1-17(2)14-26(18-4-6-19(7-5-18)29(40)35-13-12-27(38)39)37-16-23-25(36-37)11-10-22(28(23)41-3)21-9-8-20(15-24(21)31)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)/t26-/m0/s1
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35n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522707
PNG
(CHEMBL4436021)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(c(C)cc12)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C31H32F3N3O3/c1-18(2)13-27(21-5-7-22(8-6-21)30(40)35-12-11-29(38)39)37-28-15-20(4)26(16-23(28)17-36-37)25-10-9-24(14-19(25)3)31(32,33)34/h5-10,14-18,27H,11-13H2,1-4H3,(H,35,40)(H,38,39)
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36n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525889
PNG
(CHEMBL4536588)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2c(C)c(ccc12)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-27(19-4-6-20(7-5-19)29(40)35-13-12-28(38)39)37-26-11-10-22(18(3)24(26)16-36-37)23-9-8-21(15-25(23)31)30(32,33)34/h4-11,15-17,27H,12-14H2,1-3H3,(H,35,40)(H,38,39)/t27-/m0/s1
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42n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522722
PNG
(CHEMBL4540172)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2cc(c(Cl)cc2n1)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)12-27(19-4-6-20(7-5-19)29(40)35-11-10-28(38)39)37-16-21-14-24(25(31)15-26(21)36-37)23-9-8-22(13-18(23)3)30(32,33)34/h4-9,13-17,27H,10-12H2,1-3H3,(H,35,40)(H,38,39)
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44n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522720
PNG
(CHEMBL4456601)
Show SMILES CCOc1c(ccc2nn(cc12)C(CC(C)C)c1ccc(nc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C30H30ClF3N4O4/c1-4-42-28-21(20-7-6-19(14-23(20)31)30(32,33)34)8-10-24-22(28)16-38(37-24)26(13-17(2)3)18-5-9-25(36-15-18)29(41)35-12-11-27(39)40/h5-10,14-17,26H,4,11-13H2,1-3H3,(H,35,41)(H,39,40)
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57n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525886
PNG
(CHEMBL4476825)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C29H27ClF3N3O3/c1-17(2)13-26(18-3-5-19(6-4-18)28(39)34-12-11-27(37)38)36-25-10-7-20(14-21(25)16-35-36)23-9-8-22(15-24(23)30)29(31,32)33/h3-10,14-17,26H,11-13H2,1-2H3,(H,34,39)(H,37,38)/t26-/m0/s1
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85n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522728
PNG
(CHEMBL4449022)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ccc2cc(ccc12)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C31H31F3N2O3/c1-19(2)16-28(21-4-6-22(7-5-21)30(39)35-14-12-29(37)38)36-15-13-24-18-23(8-11-27(24)36)26-10-9-25(17-20(26)3)31(32,33)34/h4-11,13,15,17-19,28H,12,14,16H2,1-3H3,(H,35,39)(H,37,38)
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85n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522713
PNG
(CHEMBL4473209)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H27ClF3N3O3/c1-17(2)13-26(18-3-5-19(6-4-18)28(39)34-12-11-27(37)38)36-25-10-7-20(14-21(25)16-35-36)23-9-8-22(15-24(23)30)29(31,32)33/h3-10,14-17,26H,11-13H2,1-2H3,(H,34,39)(H,37,38)
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86n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522725
PNG
(CHEMBL4445178)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2cc(ccc2n1)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C32H37N3O3/c1-21(2)18-29(23-6-8-24(9-7-23)31(38)33-17-16-30(36)37)35-20-26-19-25(12-15-28(26)34-35)22-10-13-27(14-11-22)32(3,4)5/h6-15,19-21,29H,16-18H2,1-5H3,(H,33,38)(H,36,37)
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86n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525892
PNG
(CHEMBL4540602)
Show SMILES CC(C)C[C@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C29H28F3N3O3/c1-18(2)15-26(20-3-5-21(6-4-20)28(38)33-14-13-27(36)37)35-25-12-9-22(16-23(25)17-34-35)19-7-10-24(11-8-19)29(30,31)32/h3-12,16-18,26H,13-15H2,1-2H3,(H,33,38)(H,36,37)/t26-/m1/s1
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96n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522730
PNG
(CHEMBL4437105)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2c(Cl)c(ccc12)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-26(19-4-6-20(7-5-19)29(40)35-13-12-27(38)39)37-25-11-10-23(28(31)24(25)16-36-37)22-9-8-21(15-18(22)3)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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100n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522739
PNG
(CHEMBL4557989)
Show SMILES COc1c(ccc2n(ncc12)C(CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O4/c1-17(2)14-26(18-4-6-19(7-5-18)29(40)35-13-12-27(38)39)37-25-11-10-22(28(41-3)23(25)16-36-37)21-9-8-20(15-24(21)31)30(32,33)34/h4-11,15-17,26H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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100n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522708
PNG
(CHEMBL4559572)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ccc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C33H38N2O3/c1-22(2)20-30(24-6-8-25(9-7-24)32(38)34-18-16-31(36)37)35-19-17-27-21-26(12-15-29(27)35)23-10-13-28(14-11-23)33(3,4)5/h6-15,17,19,21-22,30H,16,18,20H2,1-5H3,(H,34,38)(H,36,37)
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110n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522718
PNG
(CHEMBL4513964)
Show SMILES CC(C)(C)c1ccc(cc1)-c1ccc2n(ncc2c1)C(CC1CCCCC1)c1ccc(cc1)C(=O)NCCC(O)=O
Show InChI InChI=1S/C35H41N3O3/c1-35(2,3)30-16-13-25(14-17-30)28-15-18-31-29(22-28)23-37-38(31)32(21-24-7-5-4-6-8-24)26-9-11-27(12-10-26)34(41)36-20-19-33(39)40/h9-18,22-24,32H,4-8,19-21H2,1-3H3,(H,36,41)(H,39,40)
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114n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522738
PNG
(CHEMBL4576987)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ccc2cc(ccc12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C30H29F3N2O3/c1-19(2)17-27(21-3-5-22(6-4-21)29(38)34-15-13-28(36)37)35-16-14-24-18-23(9-12-26(24)35)20-7-10-25(11-8-20)30(31,32)33/h3-12,14,16,18-19,27H,13,15,17H2,1-2H3,(H,34,38)(H,36,37)
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115n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522719
PNG
(CHEMBL4465107)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2c(C)c(ccc12)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C30H29ClF3N3O3/c1-17(2)14-27(19-4-6-20(7-5-19)29(40)35-13-12-28(38)39)37-26-11-10-22(18(3)24(26)16-36-37)23-9-8-21(15-25(23)31)30(32,33)34/h4-11,15-17,27H,12-14H2,1-3H3,(H,35,40)(H,38,39)
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115n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522705
PNG
(CHEMBL4471941)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C29H28F3N3O3/c1-18(2)15-26(20-3-5-21(6-4-20)28(38)33-14-13-27(36)37)35-25-12-9-22(16-23(25)17-34-35)19-7-10-24(11-8-19)29(30,31)32/h3-12,16-18,26H,13-15H2,1-2H3,(H,33,38)(H,36,37)
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125n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522735
PNG
(CHEMBL4452109)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C32H37N3O3/c1-21(2)18-29(23-6-8-24(9-7-23)31(38)33-17-16-30(36)37)35-28-15-12-25(19-26(28)20-34-35)22-10-13-27(14-11-22)32(3,4)5/h6-15,19-21,29H,16-18H2,1-5H3,(H,33,38)(H,36,37)
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125n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522729
PNG
(CHEMBL4567337)
Show SMILES CC(C)CCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C33H39N3O3/c1-22(2)6-16-29(24-7-9-25(10-8-24)32(39)34-19-18-31(37)38)36-30-17-13-26(20-27(30)21-35-36)23-11-14-28(15-12-23)33(3,4)5/h7-15,17,20-22,29H,6,16,18-19H2,1-5H3,(H,34,39)(H,37,38)
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144n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522714
PNG
(CHEMBL4434750)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2cc(ccc2n1)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C29H27ClF3N3O3/c1-17(2)13-26(18-3-5-19(6-4-18)28(39)34-12-11-27(37)38)36-16-21-14-20(7-10-25(21)35-36)23-9-8-22(15-24(23)30)29(31,32)33/h3-10,14-17,26H,11-13H2,1-2H3,(H,34,39)(H,37,38)
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150n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522715
PNG
(CHEMBL4558907)
Show SMILES CC(C)CC(c1ccc(nc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C28H26ClF3N4O3/c1-16(2)11-25(18-3-7-23(34-14-18)27(39)33-10-9-26(37)38)36-24-8-4-17(12-19(24)15-35-36)21-6-5-20(13-22(21)29)28(30,31)32/h3-8,12-16,25H,9-11H2,1-2H3,(H,33,39)(H,37,38)
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175n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522706
PNG
(CHEMBL4464664)
Show SMILES CCCCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C34H41N3O3/c1-5-6-7-8-9-30(25-10-12-26(13-11-25)33(40)35-21-20-32(38)39)37-31-19-16-27(22-28(31)23-36-37)24-14-17-29(18-15-24)34(2,3)4/h10-19,22-23,30H,5-9,20-21H2,1-4H3,(H,35,40)(H,38,39)
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199n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522717
PNG
(CHEMBL4444404)
Show SMILES CCCCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C33H39N3O3/c1-5-6-7-8-29(24-9-11-25(12-10-24)32(39)34-20-19-31(37)38)36-30-18-15-26(21-27(30)22-35-36)23-13-16-28(17-14-23)33(2,3)4/h9-18,21-22,29H,5-8,19-20H2,1-4H3,(H,34,39)(H,37,38)
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255n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522705
PNG
(CHEMBL4471941)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C29H28F3N3O3/c1-18(2)15-26(20-3-5-21(6-4-20)28(38)33-14-13-27(36)37)35-25-12-9-22(16-23(25)17-34-35)19-7-10-24(11-8-19)29(30,31)32/h3-12,16-18,26H,13-15H2,1-2H3,(H,33,38)(H,36,37)
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260n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522733
PNG
(CHEMBL4517914)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(OC(F)(F)F)cc1
Show InChI InChI=1S/C29H28F3N3O4/c1-18(2)15-26(20-3-5-21(6-4-20)28(38)33-14-13-27(36)37)35-25-12-9-22(16-23(25)17-34-35)19-7-10-24(11-8-19)39-29(30,31)32/h3-12,16-18,26H,13-15H2,1-2H3,(H,33,38)(H,36,37)
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285n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525885
PNG
(CHEMBL4473724)
Show SMILES CC(C)C[C@@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C29H28F3N3O3/c1-18(2)15-26(20-3-5-21(6-4-20)28(38)33-14-13-27(36)37)35-25-12-9-22(16-23(25)17-34-35)19-7-10-24(11-8-19)29(30,31)32/h3-12,16-18,26H,13-15H2,1-2H3,(H,33,38)(H,36,37)/t26-/m0/s1
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460n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522736
PNG
(CHEMBL4439846)
Show SMILES CCCC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C31H35N3O3/c1-5-6-27(22-7-9-23(10-8-22)30(37)32-18-17-29(35)36)34-28-16-13-24(19-25(28)20-33-34)21-11-14-26(15-12-21)31(2,3)4/h7-16,19-20,27H,5-6,17-18H2,1-4H3,(H,32,37)(H,35,36)
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650n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522723
PNG
(CHEMBL4584712)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ccc2c(C)c(cc(F)c12)-c1ccc(cc1C)C(F)(F)F
Show InChI InChI=1S/C32H32F4N2O3/c1-18(2)15-28(21-5-7-22(8-6-21)31(41)37-13-11-29(39)40)38-14-12-25-20(4)26(17-27(33)30(25)38)24-10-9-23(16-19(24)3)32(34,35)36/h5-10,12,14,16-18,28H,11,13,15H2,1-4H3,(H,37,41)(H,39,40)
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700n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522711
PNG
(CHEMBL4554170)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc2ncccc2c1
Show InChI InChI=1S/C31H30N4O3/c1-20(2)16-29(21-5-7-22(8-6-21)31(38)33-15-13-30(36)37)35-28-12-10-24(18-26(28)19-34-35)23-9-11-27-25(17-23)4-3-14-32-27/h3-12,14,17-20,29H,13,15-16H2,1-2H3,(H,33,38)(H,36,37)
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800n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522709
PNG
(CHEMBL4524978)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccccc1
Show InChI InChI=1S/C28H29N3O3/c1-19(2)16-26(21-8-10-22(11-9-21)28(34)29-15-14-27(32)33)31-25-13-12-23(17-24(25)18-30-31)20-6-4-3-5-7-20/h3-13,17-19,26H,14-16H2,1-2H3,(H,29,34)(H,32,33)
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1.10E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522727
PNG
(CHEMBL4441433)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)N1CCN(C)CC1
Show InChI InChI=1S/C33H39N5O3/c1-23(2)20-31(25-4-6-26(7-5-25)33(41)34-15-14-32(39)40)38-30-13-10-27(21-28(30)22-35-38)24-8-11-29(12-9-24)37-18-16-36(3)17-19-37/h4-13,21-23,31H,14-20H2,1-3H3,(H,34,41)(H,39,40)
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1.25E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525880
PNG
(CHEMBL4560114)
Show SMILES CC(C)C[C@H](c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1Cl)C(F)(F)F |r|
Show InChI InChI=1S/C29H27ClF3N3O3/c1-17(2)13-26(18-3-5-19(6-4-18)28(39)34-12-11-27(37)38)36-25-10-7-20(14-21(25)16-35-36)23-9-8-22(15-24(23)30)29(31,32)33/h3-10,14-17,26H,11-13H2,1-2H3,(H,34,39)(H,37,38)/t26-/m1/s1
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1.27E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522724
PNG
(CHEMBL4456905)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1cc2cc(cc(C)c2n1)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C33H39N3O3/c1-21(2)17-29(24-7-9-25(10-8-24)32(39)34-16-15-30(37)38)36-20-27-19-26(18-22(3)31(27)35-36)23-11-13-28(14-12-23)33(4,5)6/h7-14,18-21,29H,15-17H2,1-6H3,(H,34,39)(H,37,38)
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1.35E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522710
PNG
(CHEMBL4515516)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1cccc2ccccc12
Show InChI InChI=1S/C32H31N3O3/c1-21(2)18-30(23-10-12-24(13-11-23)32(38)33-17-16-31(36)37)35-29-15-14-25(19-26(29)20-34-35)28-9-5-7-22-6-3-4-8-27(22)28/h3-15,19-21,30H,16-18H2,1-2H3,(H,33,38)(H,36,37)
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1.35E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522726
PNG
(CHEMBL4560433)
Show SMILES CC(C)CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1cc(Cl)cc(Cl)c1
Show InChI InChI=1S/C28H27Cl2N3O3/c1-17(2)11-26(18-3-5-19(6-4-18)28(36)31-10-9-27(34)35)33-25-8-7-20(12-22(25)16-32-33)21-13-23(29)15-24(30)14-21/h3-8,12-17,26H,9-11H2,1-2H3,(H,31,36)(H,34,35)
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1.65E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50525894
PNG
(CHEMBL4451707)
Show SMILES COc1c(ccc2n(ncc12)[C@H](CC(C)C)c1ccc(cc1)C(=O)NCCC(O)=O)-c1ccc(cc1C)C(F)(F)F |r|
Show InChI InChI=1S/C31H32F3N3O4/c1-18(2)15-27(20-5-7-21(8-6-20)30(40)35-14-13-28(38)39)37-26-12-11-24(29(41-4)25(26)17-36-37)23-10-9-22(16-19(23)3)31(32,33)34/h5-12,16-18,27H,13-15H2,1-4H3,(H,35,40)(H,38,39)/t27-/m1/s1
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1.85E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Inhibition of human full length GCGR transfected in HEK293 cells assessed as reduction in glucagon-induced cAMP response by LANCE TR-FRET assay


Bioorg Med Chem Lett 29: (2019)


Article DOI: 10.1016/j.bmcl.2019.126668
BindingDB Entry DOI: 10.7270/Q2902776
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522732
PNG
(CHEMBL4567763)
Show SMILES CC(C)CC(c1ccc(nc1)C(=O)NCCC(O)=O)n1ccc2cc(cc(C)c12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C33H39N3O3/c1-21(2)17-29(25-9-12-28(35-20-25)32(39)34-15-13-30(37)38)36-16-14-24-19-26(18-22(3)31(24)36)23-7-10-27(11-8-23)33(4,5)6/h7-12,14,16,18-21,29H,13,15,17H2,1-6H3,(H,34,39)(H,37,38)
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>2.60E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
Glucagon receptor


(Homo sapiens (Human))
BDBM50522716
PNG
(CHEMBL4483722)
Show SMILES CC(c1ccc(cc1)C(=O)NCCC(O)=O)n1ncc2cc(ccc12)-c1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C29H31N3O3/c1-19(20-5-7-22(8-6-20)28(35)30-16-15-27(33)34)32-26-14-11-23(17-24(26)18-31-32)21-9-12-25(13-10-21)29(2,3)4/h5-14,17-19H,15-16H2,1-4H3,(H,30,35)(H,33,34)
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2.80E+3n/an/an/an/an/an/an/an/a



Janssen Research & Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at full length human recombinant GCGR transfected in HEK293 cells assessed as inhibition of glucagon-stimulated cAMP by by LANCE ...


Bioorg Med Chem Lett 29: 1974-1980 (2019)


Article DOI: 10.1016/j.bmcl.2019.05.036
BindingDB Entry DOI: 10.7270/Q2KH0RR1
More data for this
Ligand-Target Pair
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