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Target
Glucagon receptor
Ligand
BDBM50007224
Substrate
n/a
Meas. Tech.
ChEMBL_1338727 (CHEMBL3242198)
IC50
42±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:
BDBM50007224
Synonyms:
CHEMBL3238216
Type:
Small organic molecule
Emp. Form.:
C34H43ClFN7O2
Mol. Mass.:
636.202
SMILES:
CC(C)(C)CC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(F)cc(Cl)c1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:15.19,6.5,wD:12.13,c:10,(7.31,-14.38,;7.3,-12.84,;5.95,-12.09,;5.96,-13.59,;8.62,-12.05,;8.6,-10.51,;9.93,-9.73,;9.87,-8.19,;11.08,-7.24,;12.56,-7.66,;10.55,-5.79,;9.01,-5.85,;8.59,-7.33,;7.4,-6.35,;5.96,-6.88,;5.7,-8.4,;6.88,-9.38,;8.33,-8.85,;4.26,-8.93,;3.07,-7.94,;2.81,-9.46,;3.99,-10.45,;11.33,-4.46,;12.87,-4.48,;13.64,-3.15,;15.18,-3.15,;12.88,-1.8,;11.34,-1.8,;10.57,-.46,;10.56,-3.13,;11.25,-10.51,;11.23,-12.06,;12.55,-12.84,;13.9,-12.09,;13.92,-10.55,;12.6,-9.77,;15.22,-12.88,;15.2,-14.42,;16.56,-12.13,;17.89,-12.91,;19.23,-12.16,;20.63,-12.8,;21.67,-11.66,;20.91,-10.32,;19.4,-10.62,)|
Structure:
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