Reaction Details |
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Target | Cannabinoid receptor 1 |
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Ligand | BDBM29076 |
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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 | 1.4±n/a nM |
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EC50 | 0.7±n/a 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 |
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: | MKSILDGLADTTFRTITTDLLYVGSNDIQYEDIKGDMASKLGYFPQKFPLTSFRGSPFQE
KMTAGDNPQLVPADQVNITEFYNKSLSSFKENEENIQCGENFMDIECFMVLNPSQQLAIA
VLSLTLGTFTVLENLLVLCVILHSRSLRCRPSYHFIGSLAVADLLGSVIFVYSFIDFHVF
HRKDSRNVFLFKLGGVTASFTASVGSLFLTAIDRYISIHRPLAYKRIVTRPKAVVAFCLM
WTIAIVIAVLPLLGWNCEKLQSVCSDIFPHIDETYLMFWIGVTSVLLLFIVYAYMYILWK
AHSHAVRMIQRGTQKSIIIHTSEDGKVQVTRPDQARMDIRLAKTLVLILVVLIICWGPLL
AIMVYDVFGKMNKLIKTVFAFCSMLCLLNSTVNPIIYALRSKDLRHAFRSMFPSCEGTAQ
PLDNSMGDSDCLHKHANNAASVHRAAESCIKSTVKIAKVTMSVSTDTSAEAL
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BDBM29076 |
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BDBM21278 |
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Name | BDBM29076 |
Synonyms: | ether-based lactam, 19e |
Type | Small organic molecule |
Emp. Form. | C22H19Cl2F2N3O2 |
Mol. Mass. | 466.308 |
SMILES | CCC(F)(F)CN1CCOc2c(nn(c2-c2ccc(Cl)cc2)-c2ccccc2Cl)C1=O |
Structure |
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