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Target
Glucagon receptor
Ligand
BDBM50007384
Substrate
n/a
Meas. Tech.
ChEMBL_1338728 (CHEMBL3242199)
IC50
96±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:
BDBM50007384
Synonyms:
CHEMBL3237895
Type:
Small organic molecule
Emp. Form.:
C30H35Cl2N3O4
Mol. Mass.:
572.523
SMILES:
C[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(Cl)cc(Cl)c1)c1ccc(cc1)C(=O)NCCC(O)=O |r,wU:10.14,1.0,wD:7.8,c:5,(6.68,-10.11,;8,-9.32,;7.95,-7.79,;9.16,-6.84,;10.64,-7.25,;8.63,-5.39,;7.08,-5.45,;6.67,-6.93,;5.48,-5.94,;4.04,-6.47,;3.77,-7.99,;4.96,-8.98,;6.41,-8.44,;2.33,-8.52,;1.15,-7.54,;.89,-9.05,;2.07,-10.04,;9.4,-4.06,;8.64,-2.72,;9.42,-1.39,;8.66,-.05,;10.96,-1.4,;11.72,-2.74,;13.26,-2.75,;10.95,-4.07,;9.33,-10.11,;9.31,-11.65,;10.63,-12.44,;11.98,-11.68,;12,-10.15,;10.67,-9.36,;13.3,-12.48,;13.28,-14.01,;14.64,-11.72,;15.96,-12.51,;17.31,-11.75,;18.63,-12.54,;19.97,-11.78,;18.61,-14.07,)|
Structure:
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