Reaction Details Report a problem with these data
Target
Glucagon receptor
Ligand
BDBM50007241
Substrate
n/a
Meas. Tech.
ChEMBL_1338728 (CHEMBL3242199)
IC50
31±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:
Human
Description:
P47871
Residue:
477
Sequence:
MPPCQPQRPLLLLLLLLACQPQVPSAQVMDFLFEKWKLYGDQCHHNLSLLPPPTELVCNRTFDKYSCWPDTPANTTANISCPWYLPWHHKVQHRFVFKRCGPDGQWVRGPRGQPWRDASQCQMDGEEIEVQKEVAKMYSSFQVMYTVGYSLSLGALLLALAILGGLSKLHCTRNAIHANLFASFVLKASSVLVIDGLLRTRYSQKIGDDLSVSTWLSDGAVAGCRVAAVFMQYGIVANYCWLLVEGLYLHNLLGLATLPERSFFSLYLGIGWGAPMLFVVPWAVVKCLFENVQCWTSNDNMGFWWILRFPVFLAILINFFIFVRIVQLLVAKLRARQMHHTDYKFRLAKSTLTLIPLLGVHEVVFAFVTDEHAQGTLRSAKLFFDLFLSSFQGLLVAVLYCFLNKEVQSELRRRWHRWRLGKVLWEERNTSNHRASSSPGHGPPSKELQFGRGGGSQDSSAETPLAGGLPRLAESPF
Inhibitor
Name:
BDBM50007241
Synonyms:
CHEMBL3238229
Type:
Small organic molecule
Emp. Form.:
C33H41Cl2N7O2
Mol. Mass.:
638.63
SMILES:
CC(C)[C@H]1CC[C@]2(CC1)N=C(C(=O)N2[C@H](CCC(C)(C)C)c1ccc(cc1)C(=O)NCc1nn[nH]n1)c1cc(Cl)cc(Cl)c1 |r,wU:14.16,3.2,wD:6.5,c:10,(22.68,-7.09,;24,-7.87,;23.99,-9.41,;25.34,-7.11,;25.6,-5.59,;27.05,-5.06,;28.24,-6.05,;27.98,-7.57,;26.53,-8.1,;28.65,-4.57,;30.2,-4.51,;30.73,-5.96,;32.21,-6.37,;29.52,-6.91,;29.57,-8.44,;28.25,-9.23,;28.27,-10.77,;26.94,-11.56,;26.96,-13.1,;25.6,-10.8,;25.6,-12.31,;30.9,-9.23,;30.87,-10.78,;32.2,-11.56,;33.55,-10.81,;33.57,-9.27,;32.24,-8.48,;34.87,-11.6,;34.85,-13.14,;36.21,-10.85,;37.53,-11.63,;38.88,-10.88,;40.27,-11.51,;41.32,-10.38,;40.56,-9.04,;39.05,-9.34,;30.97,-3.18,;30.21,-1.85,;30.99,-.51,;30.22,.83,;32.53,-.52,;33.29,-1.86,;34.83,-1.87,;32.52,-3.19,)|