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ChEMBL ligand: CHEMBL220360 (Mk-0364, Mk0364, MK-0364, MK-0634, Taranabant) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]