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Target
Glucagon receptor
Ligand
BDBM50007223
Substrate
n/a
Meas. Tech.
ChEMBL_1338727 (CHEMBL3242198)
IC50
100±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:
BDBM50007223
Synonyms:
CHEMBL3238215
Type:
Small organic molecule
Emp. Form.:
C34H41Cl2N7O2
Mol. Mass.:
650.641
SMILES:
CC(C)(C)[C@H]1CC[C@]2(CC1)N=C(C(=O)N2[C@H](CCC1(C)CC1)c1ccc(cc1)C(=O)NCc1nn[nH]n1)c1cc(Cl)cc(Cl)c1 |r,wU:4.3,15.17,wD:7.6,c:11,(1.56,-50.44,;2.75,-51.42,;1.3,-51.96,;2.49,-52.94,;4.19,-50.89,;4.45,-49.37,;5.9,-48.84,;7.08,-49.83,;6.82,-51.35,;5.37,-51.88,;7.5,-48.35,;9.04,-48.29,;9.57,-49.74,;11.05,-50.15,;8.36,-50.69,;8.42,-52.22,;7.09,-53.01,;7.11,-54.55,;5.79,-55.33,;4.44,-54.58,;6.55,-56.66,;5.02,-56.65,;9.74,-53.01,;9.72,-54.55,;11.04,-55.34,;12.39,-54.59,;12.41,-53.05,;11.09,-52.26,;13.72,-55.38,;13.69,-56.92,;15.05,-54.62,;16.38,-55.41,;17.72,-54.65,;19.12,-55.29,;20.16,-54.16,;19.41,-52.82,;17.9,-53.12,;9.82,-46.96,;9.06,-45.62,;9.83,-44.29,;9.07,-42.96,;11.37,-44.3,;12.14,-45.64,;13.68,-45.65,;11.36,-46.97,)|
Structure:
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