tranylcypromine [Ligand Id: 5281] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL313833
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  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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  • lysine demethylase 1B/Lysine-specific histone demethylase 1B in Human [ChEMBL: CHEMBL1938208] [GtoPdb: 2670] [UniProtKB: Q8NB78]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP2B6/Cytochrome P450 2B6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4729] [GtoPdb: 1324] [UniProtKB: P20813]
ChEMBL Fluorescent High Throughput P450 Assay: The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds was calculated on isoenzymes (CYP1A2, CYP2C9, CYP2C19, CYP2C8, CYP2B6, CYP2D6, CYP2E1, CYP3A4 and CYP3A5). Inhibition of the P450 isoforms was measured in specific assays using specific substrates that become fluorescent upon CYP metabolism. Compounds, dissolved in ACN (acetonitrile) (CYP2E1, CYP2C8, CYP2B6, CYP3A5) or DMSO (all remaining isoforms), were tested in duplicate (n=2) in concentration-response curves (eight concentrations) in a 96-well plate containing incubation/NADPH regenerating buffer. Specific isoenzymes and substrates were added and incubated at 37° C. Reactions were terminated at different times, depending on the assays, and plates read on a Fluoroskan Ascent at the appropriate emission/excitation wavelengths. Concentration-response curves performed in duplicate for known inhibitors for each isoenzyme were tested in ever B 5.16 pIC50 6900 nM IC50 US-9173935-B2. Phospholipid drug analogs (2015)
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261]
ChEMBL Fluorescent High Throughput P450 Assay: The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds was calculated on isoenzymes (CYP1A2, CYP2C9, CYP2C19, CYP2C8, CYP2B6, CYP2D6, CYP2E1, CYP3A4 and CYP3A5). Inhibition of the P450 isoforms was measured in specific assays using specific substrates that become fluorescent upon CYP metabolism. Compounds, dissolved in ACN (acetonitrile) (CYP2E1, CYP2C8, CYP2B6, CYP3A5) or DMSO (all remaining isoforms), were tested in duplicate (n=2) in concentration-response curves (eight concentrations) in a 96-well plate containing incubation/NADPH regenerating buffer. Specific isoenzymes and substrates were added and incubated at 37° C. Reactions were terminated at different times, depending on the assays, and plates read on a Fluoroskan Ascent at the appropriate emission/excitation wavelengths. Concentration-response curves performed in duplicate for known inhibitors for each isoenzyme were tested in ever B 5.3 pIC50 5000 nM IC50 US-9173935-B2. Phospholipid drug analogs (2015)
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
GtoPdb In vitro KDM1A demethylation assay using purified human KDM1A protein and dimethylated H3K4 peptide as substrate. - 4.4 pIC50 39660 nM IC50 MBio (2013) 4: e00558-12 [PMID:23386436]
ChEMBL Inhibition of recombinant LSD1 (157 to 852 amino acids) (unknown origin) expressed in Escherichia coli BL21(DE) using H3K4me2 substrate by amplex red and horseradish peroxidase based fluorescence assay B 4.53 pIC50 29310 nM IC50 Eur J Med Chem (2017) 140: 392-402 [PMID:28987602]
ChEMBL Inhibition of human recombinant N-terminal His/GST-tagged LSD1 (172 to 852 residues) expressed in baculovirus infected insect cells using biotin-labeled H3K4me2 (1 to 24 residues) as substrate after 1 hr by TR-FRET assay B 4.65 pIC50 22300 nM IC50 Eur J Med Chem (2017) 141: 101-112 [PMID:29031059]
lysine demethylase 1B/Lysine-specific histone demethylase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1938208] [GtoPdb: 2670] [UniProtKB: Q8NB78]
ChEMBL Inhibition of human full length LSD2 using biotin-labeled H3K4me2 (1 to 24 residues) as substrate after 1 hr by TR-FRET assay B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2017) 141: 101-112 [PMID:29031059]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
GtoPdb - - 4.7 pIC50 20000 nM IC50 Bioorg Med Chem (2004) 12: 2645-52 [PMID:15110846]
ChEMBL Inhibition of human recombinant MAO-A expressed in baculovirus infected insect cells by luminescence assay B 4.94 pIC50 11500 nM IC50 Eur J Med Chem (2017) 141: 101-112 [PMID:29031059]
ChEMBL Inhibition of MAOA (unknown origin) using beetle luciferin as substrate by MAO-Glo assay B 5.33 pIC50 4720 nM IC50 Eur J Med Chem (2017) 140: 392-402 [PMID:28987602]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
GtoPdb - - 4.72 pIC50 19000 nM IC50 Bioorg Med Chem (2004) 12: 2645-52 [PMID:15110846]
ChEMBL Inhibition of human recombinant MAO-B expressed in baculovirus infected insect cells by luminescence assay B 5.15 pIC50 7000 nM IC50 Eur J Med Chem (2017) 141: 101-112 [PMID:29031059]
ChEMBL Inhibition of MAOB (unknown origin) using beetle luciferin as substrate by MAO-Glo assay B 5.53 pIC50 2950 nM IC50 Eur J Med Chem (2017) 140: 392-402 [PMID:28987602]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]