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ChEMBL ligand: CHEMBL279390 (Lazabemida, 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 MAO-B | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2018) 145: 445-497 [PMID:29335210] |
ChEMBL | Inhibition of MAO-B (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2021) 64: 17656-17689 [PMID:34905377] |
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 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]