Target
Glucagon receptor
Ligand
BDBM50007214
Substrate
n/a
Meas. Tech.
ChEMBL_1338727 (CHEMBL3242198)
IC50
130±n/a nM
Citation
 DeMong, DDai, XHwa, JMiller, MLin, SIKang, LStamford, AGreenlee, WYu, WWong, MLavey, BKozlowski, JZhou, GYang, DYPatel, BSoriano, AZhai, YSondey, CZhang, HLachowicz, JGrotz, DCox, KMorrison, RAndreani, TCao, YLiang, MMeng, TMcNamara, PWong, JBradley, PFeng, KIBelani, JChen, PDai, PGauuan, JLin, PZhao, 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:
BDBM50007214
Synonyms:
CHEMBL3237925
Type:
Small organic molecule
Emp. Form.:
C33H41Cl2N7O2
Mol. Mass.:
638.63
SMILES:
CCCCC[C@@H](N1C(=O)C(=N[C@@]11CC[C@@H](CC1)C(C)(C)C)c1cc(Cl)cc(Cl)c1)c1ccc(cc1)C(=O)NCc1nn[nH]n1 |r,wU:14.18,5.4,wD:11.12,c:9,(26.77,-29.67,;28.09,-28.88,;28.07,-27.34,;29.4,-26.56,;29.38,-25.02,;30.7,-24.23,;30.65,-22.69,;31.86,-21.74,;33.34,-22.16,;31.33,-20.3,;29.78,-20.36,;29.37,-21.83,;28.18,-20.85,;26.74,-21.38,;26.47,-22.9,;27.66,-23.88,;29.11,-23.35,;25.03,-23.43,;23.85,-22.45,;23.59,-23.96,;24.77,-24.95,;32.1,-18.97,;31.34,-17.63,;32.12,-16.3,;31.35,-14.97,;33.66,-16.31,;34.42,-17.65,;35.96,-17.66,;33.65,-18.98,;32.03,-25.02,;32.01,-26.56,;33.33,-27.35,;34.68,-26.59,;34.7,-25.06,;33.37,-24.27,;36,-27.39,;35.98,-28.92,;37.34,-26.63,;38.67,-27.42,;40.01,-26.66,;41.4,-27.3,;42.45,-26.17,;41.69,-24.82,;40.18,-25.13,)|
Structure:
Search PDB for entries with ligand similarity: