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TargetCannabinoid receptor 1
LigandBDBM50253587
Substrate/Competitorn/a
Meas. Tech.ChEMBL_510957 (CHEMBL1007291)
EC50 18.7±n/a nM
Citation Tseng, SLHung, MSChang, CPSong, JSTai, CLChiu, HHHsieh, WPLin, YChung, WLKuo, CWWu, CHChu, CMTung, YSChao, YSShia, KS Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagonists. J Med Chem51:5397-412 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Cannabinoid receptor 1
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50253587
n/a
NameBDBM50253587
Synonyms:1-(2,4-Dichlorophenyl)-4-methyl-5-[5-(3-phenoxyprop-1-ynyl)-thiophen-2-yl]-1H-pyrazole-3-carboxylic Acid Piperidin-1-ylamide | CHEMBL523872
TypeSmall organic molecule
Emp. Form.C29H26Cl2N4O2S
Mol. Mass.565.513
SMILESCc1c(nn(c1-c1ccc(s1)C#CCOc1ccccc1)-c1ccc(Cl)cc1Cl)C(=O)NN1CCCCC1
Structure
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