Reaction Details |
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Target | Cannabinoid receptor 1 |
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Ligand | BDBM50211843 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_597135 (CHEMBL1048890) |
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EC50 | >30000±n/a nM |
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Citation | Giblin, GM; Billinton, A; Briggs, M; Brown, AJ; Chessell, IP; Clayton, NM; Eatherton, AJ; Goldsmith, P; Haslam, C; Johnson, MR; Mitchell, WL; Naylor, A; Perboni, A; Slingsby, BP; Wilson, AW Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain. J Med Chem52:5785-8 (2009) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM50211843 |
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n/a |
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Name | BDBM50211843 |
Synonyms: | 2-(2,4-dichlorophenylamino)-4-trifluoromethyl-pyrimidine-5-carboxylic acid N-(tetrahydropyran-4-ylmethyl)amide | 2-(2,4-dichlorophenylamino)-N-((tetrahydro-2H-pyran-4-yl)methyl)-4-(trifluoromethyl)pyrimidine-5-carboxamide | CHEMBL225411 | GW-842166 | GW-842166X |
Type | Small organic molecule |
Emp. Form. | C18H17Cl2F3N4O2 |
Mol. Mass. | 449.254 |
SMILES | FC(F)(F)c1nc(Nc2ccc(Cl)cc2Cl)ncc1C(=O)NCC1CCOCC1 |
Structure |
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