Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50122102
Substrate
n/a
Meas. Tech.
ChEMBL_219264 (CHEMBL822374)
IC50
0.43±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:
GL-R | GLR_RAT | Gcgr
Type:
PROTEIN
Mol. Mass.:
55053.40
Organism:
Rattus norvegicus
Description:
ChEMBL_1450588
Residue:
485
Sequence:
MLLTQLHCPYLLLLLVVLSCLPKAPSAQVMDFLFEKWKLYSDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPPNTTANISCPWYLPWYHKVQHRLVFKRCGPDGQWVRGPRGQSWRDASQCQMDDDEIEVQKGVAKMYSSYQVMYTVGYSLSLGALLLALVILLGLRKLHCTRNYIHGNLFASFVLKAGSVLVIDWLLKTRYSQKIGDDLSVSVWLSDGAVAGCRVATVIMQYGIIANYCWLLVEGVYLYSLLSITTFSEKSFFSLYLCIGWGSPLLFVIPWVVVKCLFENVQCWTSNDNMGFWWILRIPVLLAILINFFIFVRIIHLLVAKLRAHQMHYADYKFRLARSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSTKLFFDLFFSSFQGLLVAVLYCFLNKEVQAELLRRWRRWQEGKALQEERMASSHGSHMAPAGTCHGDPCEKLQLMSAGSSSGTGCEPSAKTSLASSLPRLADSPT
Inhibitor
Name:
BDBM50122102
Synonyms:
3-Cyano-4-hydroxy-benzoic acid [1-(2,3,5,6-tetramethyl-benzyl)-1H-indol-4-ylmethylene]-hydrazide | CHEMBL152640 | N'-((1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-yl)methylene)-3-cyano-4-hydroxybenzohydrazide
Type:
Small organic molecule
Emp. Form.:
C28H26N4O2
Mol. Mass.:
450.5316
SMILES:
Cc1cc(C)c(C)c(Cn2ccc3c(\C=N\NC(=O)c4ccc(O)c(c4)C#N)cccc23)c1C