taranabant [Ligand Id: 9231] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL220360 (Mk-0364, Mk0364, MK-0364, MK-0634, Taranabant)
  • 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]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting. - 9.52 pKi 0.3 nM Ki Bioorg Med Chem Lett (2009) 19: 4183-90 [PMID:19520572]
ChEMBL Displacement of [3H]rimonabant from human CB1 receptor expressed in HEK293 cells by liquid scintillation counting B 9.52 pKi 0.3 nM Ki Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572]
ChEMBL Displacement of [3H]CP-55940 from human CB1R F170L mutant expressed in CHO cells B 7.66 pIC50 22 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]SR-141716 from human CBR1 S383A mutant expressed in CHO cells B 7.72 pIC50 19 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R F200L mutant expressed in CHO cells B 8.3 pIC50 5 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R W279A mutant expressed in CHO cells B 8.31 pIC50 4.9 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human CB1R K192L mutant expressed in CHO cells B 8.92 pIC50 1.2 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP-55940 from human wild type CB1R expressed in CHO cells B 9.13 pIC50 0.74 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Displacement of [3H]CP55490 from human recombinant cannabinoid CB1 receptor expressed in CHO cells B 9.13 pIC50 0.74 nM IC50 Bioorg Med Chem Lett (2010) 20: 4757-4761 [PMID:20643546]
ChEMBL Inhibition of radiolabeled CP5549 binding to human Cannabinoid receptor 1 expressed in CHO cells by competition assay B 9.52 pIC50 0.3 nM IC50 J Med Chem (2020) 63: 6276-6302 [PMID:31497963]
ChEMBL Displacement of [3H]CP-55940 from human recombinant CB1R expressed in CHO cells B 9.52 pIC50 0.3 nM IC50 J Med Chem (2007) 50: 3427-3430 [PMID:17608398]
ChEMBL Displacement of [3H]CP-55940 from human CB1R expressed in HEK293 cells B 9.52 pIC50 0.3 nM IC50 J Med Chem (2008) 51: 2115-2127 [PMID:18335976]
ChEMBL Inverse agonist activity at cannabinoid CB1 receptor F 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2009) 19: 2591-2594 [PMID:19328684]
ChEMBL Inhibition of CB1 receptor (unknown origin) B 9.52 pIC50 0.3 nM IC50 Medchemcomm (2013) 4: 631-652
ChEMBL Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells B 9.52 pIC50 0.3 nM IC50 J Med Chem (2006) 49: 7584-7587 [PMID:17181138]
ChEMBL Displacement of [3H]CP-55940 from recombinant human CB1 receptor expressed in CHO cells B 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2009) 19: 5195-5199 [PMID:19632830]
ChEMBL Inhibition of human CB1 receptor B 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2010) 20: 1448-1452 [PMID:20096577]
ChEMBL Inhibition of cannabinoid CB1 receptor B 9.52 pIC50 0.3 nM IC50 J Med Chem (2010) 53: 4028-4037 [PMID:20423086]
ChEMBL Binding affinity to human CB1 receptor B 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2010) 20: 3750-3754 [PMID:20483606]
ChEMBL Displacement of [3H]CP-55940 from human CB1 receptor expressed in CHO cells B 9.54 pIC50 0.29 nM IC50 J Med Chem (2008) 51: 4359-4369 [PMID:18570365]
ChEMBL Displacement of [3H]SR-141716 from human wild type CB1R expressed in CHO cells B 10.03 pIC50 0.09 nM IC50 J Med Chem (2008) 51: 2108-2114 [PMID:18333607]
ChEMBL Inverse agonist activity at human recombinant CB1 receptor assessed as inhibition of forskolin-induced cAMP production in CHO cells F 8.62 pEC50 2.4 nM EC50 J Med Chem (2006) 49: 7584-7587 [PMID:17181138]
ChEMBL Inverse agonist activity at human CB1 receptor assessed as forskolin-induced cAMP level by adenylyl cyclase activation flash plate assay F 8.62 pEC50 2.4 nM EC50 Bioorg Med Chem Lett (2009) 19: 5195-5199 [PMID:19632830]
CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272]
ChEMBL Displacement of [3H]CP-55940 from CB1 receptor in Sprague-Dawley rat cerebellum by liquid scintillation spectrometry B 9.07 pIC50 0.86 nM IC50 J Med Chem (2008) 51: 7216-7233 [PMID:18954042]
ChEMBL Displacement of [3H]SR141716A from rat brain CB1 receptor at pH 7.4 after 1 hr by liquid scintillation counting B 9.52 pIC50 0.3 nM IC50 Bioorg Med Chem Lett (2011) 21: 4913-4918 [PMID:21741835]
CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
ChEMBL Displacement of [3H]rimonabant from human CB2 receptor expressed in HEK293 cells by liquid scintillation counting B 6.54 pKi 290 nM Ki Bioorg Med Chem Lett (2009) 19: 4183-4190 [PMID:19520572]
GtoPdb - - 6.54 pKi 290 nM Ki Bioorg Med Chem Lett (2009) 19: 4183-90 [PMID:19520572]
ChEMBL Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry B 5.93 pIC50 1170 nM IC50 J Med Chem (2008) 51: 7216-7233 [PMID:18954042]
ChEMBL Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells B 6.54 pIC50 290 nM IC50 J Med Chem (2006) 49: 7584-7587 [PMID:17181138]
ChEMBL Inhibition of cannabinoid CB2 receptor B 6.54 pIC50 290 nM IC50 J Med Chem (2010) 53: 4028-4037 [PMID:20423086]
ChEMBL Displacement of [3H]CP-55940 from recombinant human CB2 receptor expressed in CHO cell B 6.55 pIC50 285 nM IC50 Bioorg Med Chem Lett (2009) 19: 5195-5199 [PMID:19632830]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human ERG at holding potential of -80 mV to +40 mV B 4.85 pIC50 14200 nM IC50 Bioorg Med Chem (2010) 18: 6377-6388 [PMID:20673729]

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]