arachidonyl-2-chloroethylamide [Ligand Id: 738] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL151167
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • CB1 receptor/Cannabinoid CB1 receptor in Mouse [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
  • CB1 receptor/Cannabinoid CB1 receptor in Rat [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
  • CB2 receptor/Cannabinoid CB2 receptor in Mouse [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
  • CB2 receptor/Cannabinoid CB2 receptor in Rat [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of FAAH B 6.05 pIC50 900 nM IC50 J Med Chem (2008) 51: 7327-7343 [PMID:18983142]
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK293 cells B 8.28 pKi 5.3 nM Ki Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
CB1 receptor/Cannabinoid CB1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3037] [GtoPdb: 56] [UniProtKB: P47746]
ChEMBL Displacement of [3H]CP-55940 from CB1 receptor in DBA/J2 mouse brain B 8.41 pKi 3.9 nM Ki J Med Chem (2006) 49: 5947-5957 [PMID:17004710]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the absence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 5.47 pKi 3400 nM Ki J Med Chem (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Binding affinity towards cannabinoid receptor 1 from rat forebrain membranes in the presence of phenylmethanesulfonylfluoride (PMSF) using 0.8 nM [3H]CP-55940 as radioligand B 8.28 pKi 5.29 nM Ki J Med Chem (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Displacement of [3H]-CP55940 from CB1 receptor of rat cerebellar membranes by liquid scintillation counting in presence of serine protease inhibitor PMSF B 8.85 pKi 1.4 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]
GtoPdb - - 8.9 pKi - - - J Pharmacol Exp Ther (1999) 289: 1427-33 [PMID:10336536]
ChEMBL Displacement of [35S]GTP-gamma-S from rat cerebellar CB1 receptor F 6.5 pEC50 316.23 nM EC50 J Med Chem (2006) 49: 554-566 [PMID:16420041]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells B 7.02 pKi 95 nM Ki Bioorg Med Chem Lett (2007) 17: 6505-6510 [PMID:17942307]
CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936]
ChEMBL Binding affinity towards Cannabinoid receptor 2 from mouse spleen membranes using 0.8 nM [3H]CP-55940 as radioligand B 6.71 pKi 195 nM Ki J Med Chem (1998) 41: 5353-5361 [PMID:9876105]
ChEMBL Displacement of [3H]CP-55940 from CB2 receptor in DBA/J2 mouse spleen B 6.92 pKi 120.8 nM Ki J Med Chem (2006) 49: 5947-5957 [PMID:17004710]
CB2 receptor/Cannabinoid CB2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2470] [GtoPdb: 57] [UniProtKB: Q9QZN9]
ChEMBL Displacement of [3H]-CP55940 from CB2 receptor of rat spleen membranes by liquid scintillation counting in presence of serine protease inhibitor PMSF B 5.7 pKi >2000 nM Ki J Med Chem (2013) 56: 8224-8256 [PMID:23865723]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]