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Target
Cannabinoid receptor 1
Ligand
BDBM21278
Substrate
n/a
Meas. Tech.
ChEMBL_545298 (CHEMBL1020744)
EC50
15.7±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:
BDBM21278
Synonyms:
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide | Acomplia | CHEMBL111 | CHEMBL558598 | RIMONABANT HYDROCHLORIDE | Rimonabant | SR 141716A | SR141716 | SR141716A | [3H]Rimonabant | [3H]SR141716A
Type:
Small organic molecule
Emp. Form.:
C22H21Cl3N4O
Mol. Mass.:
463.787
SMILES:
Cc1c(nn(c1-c1ccc(Cl)cc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
Structure:
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