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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]