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Target
Glucagon receptor
Ligand
BDBM50007288
Substrate
n/a
Meas. Tech.
ChEMBL_1338728 (CHEMBL3242199)
IC50
65±n/a nM
Citation
 DeMong, D; Dai, X; Hwa, J; Miller, M; Lin, SI; Kang, L; Stamford, A; Greenlee, W; Yu, W; Wong, M; Lavey, B; Kozlowski, J; Zhou, G; Yang, DY; Patel, B; Soriano, A; Zhai, Y; Sondey, C; Zhang, H; Lachowicz, J; Grotz, D; Cox, K; Morrison, R; Andreani, T; Cao, Y; Liang, M; Meng, T; McNamara, P; Wong, J; Bradley, P; Feng, KI; Belani, J; Chen, P; Dai, P; Gauuan, J; Lin, P; Zhao, H The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist. J Med Chem 57:2601-10 (2014) [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:
BDBM50007288
Synonyms:
CHEMBL3238243
Type:
Small organic molecule
Emp. Form.:
C35H47Cl2N7O2
Mol. Mass.:
668.699
SMILES:
CC(C)(C)CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(Cl)cc(Cl)c1)c1ccc(cc1)C(=O)NCCC1=NNNN1 |r,wU:6.5,15.19,wD:12.13,c:10,t:45,(52.53,-14.67,;52.51,-13.13,;51.17,-12.38,;51.17,-13.89,;53.84,-12.35,;53.82,-10.81,;55.14,-10.02,;55.09,-8.49,;56.3,-7.54,;57.78,-7.95,;55.77,-6.09,;54.22,-6.15,;53.81,-7.63,;52.62,-6.64,;51.17,-7.17,;50.91,-8.69,;52.1,-9.68,;53.55,-9.14,;49.57,-9.45,;48.25,-8.67,;49.56,-10.99,;48.23,-10.21,;56.54,-4.76,;55.78,-3.42,;56.56,-2.09,;55.79,-.76,;58.1,-2.1,;58.86,-3.44,;60.4,-3.45,;58.09,-4.77,;56.47,-10.81,;56.44,-12.35,;57.77,-13.14,;59.12,-12.39,;59.14,-10.85,;57.81,-10.06,;60.44,-13.18,;60.42,-14.72,;61.78,-12.42,;63.1,-13.21,;63.09,-14.75,;64.41,-15.53,;64.56,-17.06,;66.06,-17.4,;66.85,-16.08,;65.83,-14.92,)|
Structure:
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