Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50334476
Substrate
n/a
Meas. Tech.
ChEMBL_701137 (CHEMBL1648235)
IC50
170±n/a nM
Citation
 Shen, DM; Brady, EJ; Candelore, MR; Dallas-Yang, Q; Ding, VD; Feeney, WP; Jiang, G; McCann, ME; Mock, S; Qureshi, SA; Saperstein, R; Shen, X; Tong, X; Tota, LM; Wright, MJ; Yang, X; Zheng, S; Chapman, KT; Zhang, BB; Tata, JR; Parmee, ER Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core. Bioorg Med Chem Lett 21:76-81 (2010) [PubMed]  Article 
Target
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:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
  
Inhibitor
Name:
BDBM50334476
Synonyms:
CHEMBL1644178 | trans-4-((5-(4-tert-butylcyclohexyl)-3-(4-(trifluoromethoxy)phenyl)-1H-pyrazol-1-yl)methyl)-N-(2H-tetrazol-5-yl)benzamide
Type:
Small organic molecule
Emp. Form.:
C29H32F3N7O2
Mol. Mass.:
567.6053
SMILES:
CC(C)(C)[C@H]1CC[C@@H](CC1)c1cc(nn1Cc1ccc(cc1)C(=O)Nc1nnn[nH]1)-c1ccc(OC(F)(F)F)cc1 |r,wU:7.10,wD:4.3,(27.54,-.77,;27.08,.69,;28.12,1.83,;28.56,.3,;25.58,1.03,;25.11,2.5,;23.61,2.84,;22.57,1.7,;23.04,.23,;24.54,-.1,;21.06,2.03,;19.91,1.01,;18.58,1.79,;18.91,3.29,;20.45,3.44,;21.23,4.76,;22.77,4.75,;23.54,6.08,;25.07,6.08,;25.84,4.75,;25.06,3.41,;23.53,3.42,;27.38,4.75,;28.15,6.08,;28.14,3.41,;29.68,3.41,;30.58,2.16,;32.05,2.64,;32.05,4.18,;30.59,4.65,;17.17,1.16,;15.93,2.08,;14.52,1.46,;14.35,-.07,;12.94,-.69,;11.7,.22,;10.29,-.4,;11.87,1.75,;10.36,1,;15.6,-.98,;17.01,-.36,)|
Structure:
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