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Target
Glucagon receptor
Ligand
BDBM50122160
Substrate
n/a
Meas. Tech.
ChEMBL_72875 (CHEMBL684126)
IC50
4.9±n/a nM
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 Chem 45:5755-75 (2002) [PubMed] Article
More Info.:
Target
Name:
Glucagon receptor
Synonyms:
GCGR | GL-R | GLR_HUMAN | Glucagon Receptor (GCGR) | Glucagon receptor (GlucR)
Type:
Enzyme
Mol. Mass.:
54026.92
Organism:
Human
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Inhibitor
Name:
BDBM50122160
Synonyms:
3-Cyano-4-hydroxy-benzoic acid {4-[4-(4-chloro-benzyl)-piperazine-1-carbonyl]-naphthalen-1-ylmethylene}-hydrazide | CHEMBL154149
Type:
Small organic molecule
Emp. Form.:
C31H26ClN5O3
Mol. Mass.:
552.023
SMILES:
Oc1ccc(cc1C#N)C(=O)N\N=C\c1ccc(C(=O)N2CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc12