Reaction Details |
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Target | Cannabinoid receptor 1 |
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Ligand | BDBM21279 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_456127 (CHEMBL887035) |
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Ki | 3±n/a nM |
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Citation | Ellsworth, BA; Wang, Y; Zhu, Y; Pendri, A; Gerritz, SW; Sun, C; Carlson, KE; Kang, L; Baska, RA; Yang, Y; Huang, Q; Burford, NT; Cullen, MJ; Johnghar, S; Behnia, K; Pelleymounter, MA; Washburn, WN; Ewing, WR Discovery of pyrazine carboxamide CB1 antagonists: the introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series. Bioorg Med Chem Lett17:3978-82 (2007) [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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BDBM21279 |
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n/a |
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Name | BDBM21279 |
Synonyms: | 1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide | AM 251 | AM-251 | AM251 | CHEMBL285932 | N-(piperidin-1-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide |
Type | Small organic molecule |
Emp. Form. | C22H21Cl2IN4O |
Mol. Mass. | 555.239 |
SMILES | Cc1c(nn(c1-c1ccc(I)cc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1 |
Structure |
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