phenelzine [Ligand Id: 7266] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1089 (Nardil, Phenelzine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| amine oxidase copper containing 3/Amine oxidase, copper containing in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3437] [GtoPdb: 2767] [UniProtKB: Q16853] | ||||||||
| GtoPdb | - | - | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2010) 53: 6301-15 [PMID:20690686] |
| ChEMBL | Inhibition of human recombinant VAP-1 expressed in CHO cells after 30 mins by coupled colorimetric method | B | 7.7 | pIC50 | 19.95 | nM | IC50 | J Med Chem (2010) 53: 6301-6315 [PMID:20690686] |
| CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6.1 | pIC50 | 800 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2C9 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 5.4 | pIC50 | 4000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| indoleamine 2,3-dioxygenase 1/Indoleamine 2,3-dioxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4685] [GtoPdb: 2829] [UniProtKB: P14902] | ||||||||
| ChEMBL | Inhibition of IDO1 (unknown origin) using L-tryptophan substrate incubated for 60 mins by HPLC | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2014) 84: 284-301 [PMID:25036789] |
| lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341] | ||||||||
| ChEMBL | Inhibition of LSD1 | B | 4.74 | pKi | 18000 | nM | Ki | J Med Chem (2011) 54: 8236-8250 [PMID:21955276] |
| ChEMBL | Inhibition of LSD1 | B | 4.75 | pKi | 17600 | nM | Ki | Bioorg Med Chem (2011) 19: 3625-3636 [PMID:21596573] |
| ChEMBL | Inhibition of human recombinant LSD1 using H3K4me2 as substrate preincubated for 15 mins followed by substrate addition and measured after 30 mins by Amplex Red reagent based fluorescence microplate reader analysis | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (2021) 64: 13980-14010 [PMID:34591474] |
| ChEMBL | Inhibition of LSD1 (unknown origin) | B | 5.25 | pKi | 5600 | nM | Ki | Eur J Med Chem (2017) 125: 940-951 [PMID:27769034] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Mixed-type inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinoline formation using varying levels of kynuramine as substrate after 20 mins by Lineweaver-Burk plot analysis | B | 6.79 | pKi | 163 | nM | Ki | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| GtoPdb | - | - | 7.33 | pKi | 47 | nM | Ki | Biochemistry (2008) 47: 5616-25 [PMID:18426226] |
| ChEMBL | Inhibition of recombinant human MAO-A assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay | B | 6.62 | pIC50 | 238 | nM | IC50 | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| ChEMBL | DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) | B | 6.84 | pIC50 | 146 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
| ChEMBL | In vitro ability to inhibit Monoamine oxidase A activity in rat whole brain in vitro | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2715-2717 [PMID:11591508] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Mixed-type inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinoline formation using varying levels of kynuramine as substrate after 20 mins by Lineweaver-Burk plot analysis | B | 6.91 | pKi | 124 | nM | Ki | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| ChEMBL | Inhibition of human recombinant soluble MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay | B | 7.03 | pKi | 94 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| GtoPdb | - | - | 7.82 | pKi | 15 | nM | Ki | Biochemistry (2008) 47: 5616-25 [PMID:18426226] |
| ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorometric assay | B | 6.84 | pIC50 | 143 | nM | IC50 | J Nat Prod (2016) 79: 2538-2544 [PMID:27754693] |
| Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | In vitro ability to inhibit Monoamine oxidase B activity in rat whole brain in vitro | B | 7.12 | pIC50 | 76.3 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2715-2717 [PMID:11591508] |
| NET in Human [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
| DAT in Human [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| GtoPdb | - | - | 5.08 | pKi | 8400 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
| SERT in Human [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | Eur J Pharmacol (1997) 340: 249-58 [PMID:9537821] |
| CYP2C8 in Human [GtoPdb: 1325] [UniProtKB: P10632] | ||||||||
| GtoPdb | - | - | 5.14 | pKi | 7266 | nM | Ki | Curr Drug Metab (2005) 6: 413-54 [PMID:16248836] |
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]
