Reaction Details |
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Target | Glucagon receptor |
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Ligand | BDBM50122138 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_72875 (CHEMBL684126) |
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IC50 | 33.5±n/a nM |
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Citation | Madsen, P; Ling, A; Plewe, M; Sams, CK; Knudsen, LB; Sidelmann, UG; Ynddal, L; Brand, CL; Andersen, B; Murphy, D; Teng, M; Truesdale, L; Kiel, D; May, J; Kuki, A; Shi, S; Johnson, MD; Teston, KA; Feng, J; Lakis, J; Anderes, K; Gregor, V; Lau, J Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. J Med Chem45:5755-75 (2002) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Glucagon receptor |
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Name: | Glucagon receptor |
Synonyms: | GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR) |
Type: | Enzyme |
Mol. Mass.: | 54026.92 |
Organism: | Homo sapiens (Human) |
Description: | P47871 |
Residue: | 477 |
Sequence: | MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNR
TFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQ
CQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANL
FASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYC
WLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDN
MGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGV
HEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRL
GKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
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BDBM50122138 |
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n/a |
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Name | BDBM50122138 |
Synonyms: | CHEMBL152103 | CHEMBL2111214 | N-{4-[(3-Chloro-4-hydroxy-benzoyl)-hydrazonomethyl]-3-methoxy-phenyl}-3-(4-trifluoromethyl-phenyl)-propionamide |
Type | Small organic molecule |
Emp. Form. | C25H21ClF3N3O4 |
Mol. Mass. | 519.9 |
SMILES | COc1cc(NC(=O)CCc2ccc(cc2)C(F)(F)F)ccc1\C=N\NC(=O)c1ccc(O)c(Cl)c1 |
Structure |
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