| Reaction Details |
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 | Report a problem with these data |
| Target | Cannabinoid receptor 1 |
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| Ligand | BDBM21278 |
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| Substrate/Competitor | BDBM21278 |
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| Meas. Tech. | CB1 Radioligand Binding Assay (Ki) and GTP-gamma-[35S] Binding Assay (EC50) |
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| pH | 7.4±n/a |
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| Temperature | 303.15±n/a K |
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| Ki | 1.8±1.4 nM |
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| EC50 | 1.6±0.7 nM |
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| Citation |  Dow, RL; Carpino, PA; Hadcock, JR; Black, SC; Iredale, PA; DaSilva-Jardine, P; Schneider, SR; Paight, ES; Griffith, DA; Scott, DO; O'Connor, RE; Nduaka, CI Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity. J Med Chem52:2652-5 (2009) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Cannabinoid receptor 1 |
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| Name: | Cannabinoid receptor 1 |
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| Synonyms: | CANN6 | CANNABINOID CB1 | CB-R | CB1 | CNR | CNR1 | CNR1_HUMAN | Cannabinoid CB1 receptor | Cannabinoid receptor | Cannabinoid receptor 1 (CB1) | Cannabinoid receptor 1 (brain) |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 52868.96 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P21554 |
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| Residue: | 472 |
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| Sequence: | MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
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| BDBM21278 |
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| BDBM21278 |
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| Name | BDBM21278 |
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| 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 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H21Cl3N4O |
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| Mol. Mass. | 463.787 |
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| SMILES | Cc1c(nn(c1-c1ccc(Cl)cc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1 |
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| Structure | 
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