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Target
Cannabinoid receptor 1
Ligand
BDBM50279126
Substrate
n/a
Meas. Tech.
ChEMBL_545298 (CHEMBL1020744)
EC50
8.5±n/a nM
Citation
 Wu, CH; Hung, MS; Song, JS; Yeh, TK; Chou, MC; Chu, CM; Jan, JJ; Hsieh, MT; Tseng, SL; Chang, CP; Hsieh, WP; Lin, Y; Yeh, YN; Chung, WL; Kuo, CW; Lin, CY; Shy, HS; Chao, YS; Shia, KS Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesity efficacy in DIO mice. J Med Chem 52:4496-510 (2009) [PubMed]  Article
Target
Name:
Cannabinoid receptor 1
Synonyms:
CANN6 | CANNABINOID CB1 | CB-R | CB1 | CNR | CNR1 | CNR1_HUMAN | Cannabinoid CB1 receptor | Cannabinoid receptor | Cannabinoid receptor 1 (CB1) | Cannabinoid receptor 1 (brain)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
52868.96
Organism:
Homo sapiens (Human)
Description:
P21554
Residue:
472
Sequence:
MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQEKMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIAVLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVFHRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLMWTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWKAHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLLAIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQPLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
  
Inhibitor
Name:
BDBM50279126
Synonyms:
2-[5-(4-Chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-methyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazole-4-thio | CHEMBL524634
Type:
Small organic molecule
Emp. Form.:
C22H19Cl3N4S
Mol. Mass.:
477.837
SMILES:
CN1C(=NC(=S)C1(C)C)c1nn(c(c1C)-c1ccc(Cl)cc1)-c1ccc(Cl)cc1Cl |c:2|
Structure:
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