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 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 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]
