otenabant [Ligand Id: 9232] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL562668 (Cp-945598, CP-945,598, CP-945598, CP-945598-01, Otenabant, Otenabant hydrochloride)
  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
  • 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]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
GtoPdb Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells - 9.15 pKi 0.7 nM Ki J Med Chem (2009) 52: 234-7 [PMID:19102698]
ChEMBL Displacement of [3H]SR141716A from human CB1 receptor expressed in HEK293 cells B 9.15 pKi 0.7 nM Ki J Med Chem (2009) 52: 234-237 [PMID:19102698]
ChEMBL Displacement of [3H]CP55940 from human CB1 expressed in CHOK1 cell membranes B 9.15 pKi 0.7 nM Ki J Med Chem (2018) 61: 4370-4385 [PMID:29688015]
ChEMBL Antagonist activity against human CB1 receptor expressed in CHO-K1 cells by [35S]GTPgamma binding assay F 9.92 pKi 0.12 nM Ki J Med Chem (2009) 52: 234-237 [PMID:19102698]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
GtoPdb Displacement of [3H]SR141716A from CB1 receptor in rat brain - 8.55 pKi 2.8 nM Ki J Med Chem (2009) 52: 234-7 [PMID:19102698]
ChEMBL Displacement of [3H]SR141716A from CB1 receptor in rat brain B 8.55 pKi 2.8 nM Ki J Med Chem (2009) 52: 234-237 [PMID:19102698]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]CP55940 from human CB2 expressed in CHOK1 cell membranes B 5.11 pKi 7700 nM Ki J Med Chem (2018) 61: 4370-4385 [PMID:29688015]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG B 5.52 pIC50 >3000 nM IC50 J Med Chem (2009) 52: 234-237 [PMID:19102698]

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]