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Target
Glucagon receptor
Ligand
BDBM50007389
Substrate
n/a
Meas. Tech.
ChEMBL_1338728 (CHEMBL3242199)
IC50
6.0±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:
BDBM50007389
Synonyms:
CHEMBL3237900
Type:
Small organic molecule
Emp. Form.:
C30H35ClFN3O4
Mol. Mass.:
556.068
SMILES:
C[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(F)cc(Cl)c1)c1ccc(cc1)C(=O)NCCC(O)=O |r,wU:10.14,1.0,wD:7.8,c:5,(20.39,-28.33,;21.71,-27.55,;21.66,-26.01,;22.87,-25.06,;24.35,-25.48,;22.34,-23.62,;20.79,-23.68,;20.38,-25.15,;19.19,-24.17,;17.74,-24.7,;17.48,-26.22,;18.67,-27.2,;20.12,-26.67,;16.04,-26.75,;14.86,-25.76,;14.6,-27.28,;15.78,-28.27,;23.11,-22.29,;24.66,-22.3,;25.43,-20.97,;26.97,-20.98,;24.67,-19.63,;23.13,-19.62,;22.36,-18.28,;22.35,-20.95,;23.04,-28.33,;23.01,-29.88,;24.34,-30.66,;25.69,-29.91,;25.71,-28.37,;24.38,-27.59,;27.01,-30.7,;26.99,-32.24,;28.35,-29.95,;29.67,-30.73,;31.02,-29.98,;32.34,-30.76,;33.68,-30,;32.32,-32.3,)|