Reaction Details |
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Target | Cannabinoid receptor 1 |
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Ligand | BDBM29097 |
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Substrate/Competitor | BDBM21278 |
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Meas. Tech. | CB Receptor Radioligand Binding Assay (Ki) |
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pH | 7.2±n/a |
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Temperature | 295.15±n/a K |
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Ki | 0.79±0.2 nM |
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Citation | Pettersson, H; Bülow, A; Ek, F; Jensen, J; Ottesen, LK; Fejzic, A; Ma, JN; Del Tredici, AL; Currier, EA; Gardell, LR; Tabatabaei, A; Craig, D; McFarland, K; Ott, TR; Piu, F; Burstein, ES; Olsson, R Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists. J Med Chem52:1975-82 (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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BDBM29097 |
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BDBM21278 |
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Name | BDBM29097 |
Synonyms: | dibenzothiazepine, 12c |
Type | Small organic molecule |
Emp. Form. | C26H22ClF2N3OS |
Mol. Mass. | 497.987 |
SMILES | FC1(F)CCN(CC1)C1=Nc2cc(ccc2Sc2ccccc12)C(=O)NCc1cccc(Cl)c1 |t:9| |
Structure |
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