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ChEMBL ligand: CHEMBL279390 (Lazabemide, RO-196327, RO 19-6327/000) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
ChEMBL | Inhibition of MAOA (unknown origin) using kynuramine as substrate preincubated for 30 mins followed by substrate addition | B | 4.1 | pIC50 | >80000 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
ChEMBL | In vitro inhibitory against monoamine oxidase A (MAO-A) in rat brain homogenate. | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1195-1198 |
ChEMBL | In vitro inhibitory activity against rat brain Monoamine oxidase A | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1995) 38: 4786-4792 [PMID:7490728] |
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
ChEMBL | Binding affinity to human recombinant microsomal MAO-B by ITC | B | 7.18 | pKd | 66 | nM | Kd | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
ChEMBL | Inhibition constant against human recombinant Monoamine oxidase-B | B | 7.08 | pKi | 84 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4438-4446 [PMID:16137882] |
GtoPdb | - | - | 7.08 | pKi | 84 | nM | Ki |
Adv Neurol (1990) 53: 505-12 [PMID:2122653]; Bioorg Med Chem Lett (2005) 15: 4438-46 [PMID:16137882] |
ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay | B | 7.14 | pKi | 72.2 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay | B | 8.22 | pKi | 6 | nM | Ki | Medchemcomm (2018) 9: 1164-1171 [PMID:30109004] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2021) 64: 1989-2009 [PMID:33533632] |
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 | 8.41 | pKi | 3.9 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
ChEMBL | Inhibition of recombinant human MAO-B using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1136-1140 [PMID:28188065] |
ChEMBL | Inhibition of human recombinant monoamine oxidase-B assessed as kynuramine conversion to 6-hydroxyquinoline after 20 mins by fluorescence spectrophotometric analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1269-1273 [PMID:23374869] |
ChEMBL | Reversible inhibition of recombinant human MAO-B assessed as inhibition of kynuramine conversion to fluorescent metabolite 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5498-5502 [PMID:24012182] |
ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate assessed as 4-hydroxyquinoline production after 30 mins by fluorescence spectrophotometry analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2758-2763 [PMID:24794105] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in insect cells assessed as inhibition of oxidation of kynuramine to 4-hydroxyquinoline after 20 mins by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2014) 82: 164-171 [PMID:24904963] |
ChEMBL | Inhibition of human recombinant MAO-B assessed as kynuramine oxidation to 4-hydroxyquinoline formation by spectrofluorometric analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1206-1211 [PMID:25701250] |
ChEMBL | Inhibition of human recombinant MAOB using kynuramine substrate assessed as reduction in MAO-generated 4-hydroxyquinoline level by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1896-1900 [PMID:25857942] |
ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected BT1 cells microsome fraction by fluorescence spectrometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5270-5276 [PMID:26432037] |
ChEMBL | Inhibition of recombinant human MAO-B after 20 mins using 50 uM kynuramine as substrate by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1200-1204 [PMID:26821818] |
ChEMBL | Inhibition of human recombinant MAO-B using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometric analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2214-2219 [PMID:27020523] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cell microsomes using kynuramine as substrate after 20 mins by fluorescence spectroscopy | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2017) 135: 196-203 [PMID:28456030] |
ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cell microsome assessed as 4-hydroxyquinoline formation using kynuramine as substrate after 20 mins by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem (2012) 20: 7040-7050 [PMID:23122934] |
ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence spectrophotometric analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem (2018) 26: 5531-5537 [PMID:30279044] |
ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells microsomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometry analysis | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126677-126677 [PMID:31537422] |
ChEMBL | Inhibition of recombinant human MAOB expressed in insect cell microsomes using kynuramine as substrate measured after 20 mins by fluorescence spectrophotometry | B | 7.04 | pIC50 | 91 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 40-46 [PMID:30455149] |
ChEMBL | Inhibition of MAOB (unknown origin) using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 7.38 | pIC50 | 42 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
ChEMBL | Inhibition of recombinant human MAO-B using benzylamine as substrate incubated for 30 mins by spectrophotometric method | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480] |
ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using benzylamine as substrate after 30 mins by spectrophotometric analysis | B | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 839-843 [PMID:30686752] |
ChEMBL | Inhibition of human recombinant MAOB using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 584-588 [PMID:29395970] |
ChEMBL | Inhibition of human recombinant soluble MAO-B assessed as thermal shift after 20 mins by SYPRO orange staining-based fluorescence assay | B | 5.15 | pEC50 | 7100 | nM | EC50 | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
ChEMBL | In vitro inhibitory activity against rat brain Monoamine oxidase B | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (1995) 38: 4786-4792 [PMID:7490728] |
ChEMBL | In vitro inhibitory activity against monoamine oxidase B (MAO-B) in rat brain homogenate. | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 1195-1198 |
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]