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Target
Glucagon receptor
Ligand
BDBM50007426
Substrate
n/a
Meas. Tech.
ChEMBL_1338727 (CHEMBL3242198)
IC50
550±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
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:
Homo sapiens (Human)
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Inhibitor
Name:
BDBM50007426
Synonyms:
CHEMBL3237908
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)c1ccc(Cl)c(Cl)c1)c1ccc(cc1)C(=O)NCCC(O)=O |r,wU:10.14,1.0,wD:7.8,c:5,(38.24,-55.26,;39.57,-54.47,;39.51,-52.93,;40.72,-51.98,;42.2,-52.4,;40.19,-50.54,;38.65,-50.6,;38.23,-52.07,;37.05,-51.09,;35.6,-51.62,;35.34,-53.14,;36.52,-54.12,;37.97,-53.59,;33.9,-53.67,;32.71,-52.68,;32.45,-54.2,;33.64,-55.19,;40.97,-49.21,;42.51,-49.22,;43.28,-47.89,;42.52,-46.55,;43.3,-45.22,;40.98,-46.54,;40.21,-45.2,;40.21,-47.87,;40.89,-55.25,;40.87,-56.8,;42.19,-57.58,;43.54,-56.83,;43.56,-55.29,;42.24,-54.51,;44.86,-57.62,;44.84,-59.16,;46.2,-56.87,;47.53,-57.65,;48.87,-56.9,;50.19,-57.68,;51.54,-56.93,;50.18,-59.22,)|