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ChEMBL ligand: CHEMBL673 (Eutonyl, Eutron, Pargyline) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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aldehyde dehydrogenase 2 family member/Aldehyde dehydrogenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2812] [GtoPdb: 2595] [UniProtKB: P11884] | ||||||||
ChEMBL | Inhibition of Sprague-Dawley rat mitochondrial aldehyde dehydrogenase | B | 5.25 | pIC50 | 5600 | nM | IC50 | J Nat Prod (1997) 60: 1180-1182 |
ABCG2/ATP-binding cassette sub-family G member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0] | ||||||||
ChEMBL | Inhibition of BCRP (unknown origin) transfected in HEK293/R2 cells assessed as reversal of topotecan resistance after 5 days by MTS/PMS assay | B | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (2021) 64: 14311-14331 [PMID:34606270] |
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 20 mins by spectrophotometric analysis | B | 4.7 | pIC50 | >20000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 839-843 [PMID:30686752] |
ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate by fluorescence spectroscopy | B | 4.89 | pIC50 | 13000 | nM | IC50 | Eur J Med Chem (2017) 135: 196-203 [PMID:28456030] |
ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 20 mins | B | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4599-4605 [PMID:27578245] |
ChEMBL | Inhibition of human recombinant monoamine oxidase-A assessed as kynuramine conversion to 6-hydroxyquinoline after 20 mins by fluorescence spectrophotometric analysis | B | 4.89 | pIC50 | 12970 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1269-1273 [PMID:23374869] |
ChEMBL | Inhibition of human recombinant MAOA expressed in microsomes of baculovirus-infected insect cell using kynuramine as substrate preincubated for 20 mins followed by protein addition measured after 30 mins by fluorescence assay | B | 4.96 | pIC50 | 10900 | nM | IC50 | J Med Chem (2016) 59: 6791-6806 [PMID:27347731] |
ChEMBL | Inhibition of human recombinant MAO-A using pargyline as incubated for 20 mins measuring increase in emission signal at 310 nm multimode plate reader assay | B | 5.34 | pIC50 | 4600 | nM | IC50 | Bioorg Med Chem (2021) 42: 116255-116255 [PMID:34119696] |
ChEMBL | Inhibition of human recombinant MAO-A using kynuramine substrate by spectrophotometric assay | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2015) 58: 5561-5578 [PMID:26107513] |
ChEMBL | Inhibition of recombinant human microsomal MAOA expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by amplex red reagent-based horseradish peroxidase-coupled fluorometric assay | B | 5.4 | pIC50 | 3967.9 | nM | IC50 | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
ChEMBL | Inhibition of human MAO-A using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by fluorescence-based Amplex Red MAO assay | B | 5.45 | pIC50 | 3520 | nM | IC50 | Bioorg Med Chem (2017) 25: 5917-5928 [PMID:28988627] |
ChEMBL | Inhibition of MAOA (unknown origin) using kynuramine as substrate after 1 hr by fluorescence assay | B | 5.47 | pIC50 | 3390 | nM | IC50 | J Med Chem (2013) 56: 7334-7342 [PMID:24007511] |
ChEMBL | Inhibition of human recombinant microsomal MAO-A expressed in baculovirus-infected insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by amplex red assay | B | 5.47 | pIC50 | 3368 | nM | IC50 | Bioorg Med Chem (2017) 25: 633-645 [PMID:27908752] |
ChEMBL | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of kynuramine as substrate | B | 5.7 | pIC50 | >2000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4714-4719 [PMID:27575476] |
ChEMBL | Inhibition of human recombinant MAOA using kynuramine as substrate preincubated for 30 mins followed by substrate addition | B | 5.7 | pIC50 | >2000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 584-588 [PMID:29395970] |
ChEMBL | Inhibition of MAOA (unknown origin) using kynuramine as substrate preincubated for 30 mins followed by substrate addition | B | 5.88 | pIC50 | 1310 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
ChEMBL | Inhibition of recombinant human MAO-A assessed as reduction in H2O2 production using p-tyramine as substrate preincubated for 15 mins followed by substrate addition by Amplex red reagent based fluorescence assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Medchemcomm (2017) 8: 1459-1467 [PMID:30108857] |
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
ChEMBL | Inhibition of MAO-A in rat liver homogenate after 60 mins by Lineweaver-Burke plot | B | 5.07 | pKi | 8500 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
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 | 6.56 | pKd | 275.4 | nM | Kd | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
ChEMBL | Inhibition constant against human recombinant Monoamine oxidase-B | B | 5.74 | pKi | 1800 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4438-4446 [PMID:16137882] |
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 | 7.31 | pKi | 49.5 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
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 | 7.69 | pKi | 20.3 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
ChEMBL | Inhibition of human recombinant MAOB using kynuramine as substrate incubated for 10 mins by UPLC-ESI-MS/MS analysis | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2019) 27: 2027-2040 [PMID:30975503] |
ChEMBL | Inhibition of human recombinant MAOB expressed in microsomes of baculovirus-infected insect cell using kynuramine as substrate preincubated for 20 mins followed by protein addition measured after 30 mins by fluorescence assay | B | 5.57 | pIC50 | 2690 | nM | IC50 | J Med Chem (2016) 59: 6791-6806 [PMID:27347731] |
ChEMBL | Inhibition of MAOB | B | 5.59 | pIC50 | 2600 | nM | IC50 | Eur J Med Chem (2009) 44: 3584-3590 [PMID:19321235] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells assessed as reduction in formation of 4-quinolinol using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition and measured after 20 mins by fluorescence based microplate reader assay | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem (2020) 28: 115156-115156 [PMID:31740200] |
ChEMBL | Inhibition of human recombinant MAO-B using kynuramine as substrate incubated for 20 mins measuring increase in emission signal at 400 nm multimode plate reader assay | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem (2021) 42: 116255-116255 [PMID:34119696] |
ChEMBL | Inhibition of human MAO-B using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by fluorescence-based Amplex Red MAO assay | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2017) 25: 5917-5928 [PMID:28988627] |
ChEMBL | Inhibition of human MAO-B using p-tyramine as substrate assessed as production of H2O2 from p-tyramine incubated for 15 mins by Amplex Red MAO assay | B | 6.7 | pIC50 | 198.5 | nM | IC50 | Medchemcomm (2015) 6: 1293-1302 |
ChEMBL | Inhibition of recombinant human microsomal MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by amplex red reagent-based horseradish peroxidase-coupled fluorometric assay | B | 6.71 | pIC50 | 195.5 | nM | IC50 | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus-infected insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured for 20 mins by amplex red assay | B | 6.71 | pIC50 | 195 | nM | IC50 | Bioorg Med Chem (2017) 25: 633-645 [PMID:27908752] |
ChEMBL | Inhibition of recombinant human MAO-B using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by amplex red reagent based fluorescence assay | B | 6.71 | pIC50 | 194 | nM | IC50 | Eur J Med Chem (2017) 138: 715-728 [PMID:28728104] |
ChEMBL | Inhibition of human recombinant MAO-B using p-tyramine as substrate assessed as H2O2 production after 15 mins by fluorescence assay | B | 6.72 | pIC50 | 192 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 508-513 [PMID:25542589] |
ChEMBL | Inhibition of recombinant human MAO-B using p-benzylamine substrate preincubated for 15 mins before substrate addition measured after 20 mins by fluorescence assay | B | 6.73 | pIC50 | 188 | nM | IC50 | Eur J Med Chem (2013) 62: 745-753 [PMID:23454517] |
ChEMBL | Inhibition of human recombinant MAO-B using benzylamine as substrate incubated for 15 mins prior to substrate addition measured after 20 mins by fluorescence plate reader analysis | B | 6.73 | pIC50 | 188 | nM | IC50 | Bioorg Med Chem (2015) 23: 3722-3729 [PMID:25934229] |
ChEMBL | Inhibition of recombinant human MAOB using benzylamine as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by Amplex red reagent based fluorescence assay | B | 6.73 | pIC50 | 188 | nM | IC50 | Eur J Med Chem (2018) 143: 33-47 [PMID:29172081] |
ChEMBL | Inhibition of human recombinant MAO-B using benzylamine as substrate preincubated for 15 mins under dark condition followed by substrate addition measured after 20 mins by fluorescence assay | B | 6.73 | pIC50 | 188 | nM | IC50 | Bioorg Med Chem (2013) 21: 7406-7417 [PMID:24128814] |
ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in production of H202 using p-tyramine as substrate incubated for 30 mins followed by substrate addition by horse radish peroxidase/Amplex red reagent based fluorescence assay | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2019) 177: 221-234 [PMID:31151057] |
ChEMBL | Inhibition of MAOB (unknown origin) using kynuramine as substrate after 1 hr by fluorescence assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2013) 56: 7334-7342 [PMID:24007511] |
ChEMBL | Inhibition of human recombinant MAO-B using kynuramine substrate by spectrophotometric assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2015) 58: 5561-5578 [PMID:26107513] |
ChEMBL | Inhibition of recombinant human MAO-B using p-tyramine as substrate preincubated with enzyme for 15 mins followed incubation with substrate for 20 mins by Amplex red reagent based fluorescence based analysis | B | 6.92 | pIC50 | 120 | nM | IC50 | RSC Med Chem (2020) 11: 225-233 [PMID:33479629] |
ChEMBL | Inhibition of human recombinant MAOB using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 584-588 [PMID:29395970] |
ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 10 mins followed by substrate addition by fluorimetric analysis | B | 6.97 | pIC50 | 107.3 | nM | IC50 | Bioorg Med Chem (2020) 28: 115550-115550 [PMID:32503694] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 10 mins followed by addition of benzylamine as substrate | B | 6.99 | pIC50 | 103 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4714-4719 [PMID:27575476] |
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 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 839-843 [PMID:30686752] |
ChEMBL | Inhibition of MAOB (unknown origin) using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 7.04 | pIC50 | 91 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells incubated for 15 mins with substrate p-Tyramine by fluorescence assay | B | 7.07 | pIC50 | 85.8 | nM | IC50 | Eur J Med Chem (2019) 180: 367-382 [PMID:31325784] |
ChEMBL | Inhibition of human MAO-B preincubated for 5 mins followed by addition of Kynuramine substrate and measured after 30 mins by plate reader method | B | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2021) 211: 113112-113112 [PMID:33360800] |
ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in H2O2 production using p-tyramine as substrate preincubated for 15 mins followed by substrate addition by Amplex red reagent based fluorescence assay | B | 7.12 | pIC50 | 75.2 | nM | IC50 | Medchemcomm (2017) 8: 1459-1467 [PMID:30108857] |
ChEMBL | Inhibition of MAO-B (unknown origin) | B | 8.09 | pIC50 | 8.2 | nM | IC50 | Eur J Med Chem (2017) 138: 715-728 [PMID:28728104] |
Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
ChEMBL | Inhibition of MAO-B in rat liver homogenate after 60 mins by Lineweaver-Burke plot | B | 5.47 | pKi | 3360 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
ChEMBL | Inhibition of MAO-B in rat liver homogenate after 60 mins by residual activity plot | B | 5.41 | pIC50 | 3850 | nM | IC50 | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
ChEMBL | Inhibition of MAOB in rat liver homogenates preincubated for 60 mins | B | 5.41 | pIC50 | 3850 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6362-6368 [PMID:18980841] |
ChEMBL | Inhibition of rat liver MAOB after 60 mins pre-incubation | B | 5.55 | pIC50 | 2850 | nM | IC50 | Bioorg Med Chem (2007) 15: 5775-5786 [PMID:17611112] |
GtoPdb | - | - | 5.74 | pIC50 | 1800 | nM | IC50 | Biochem Pharmacol (1982) 31: 3555-61 [PMID:6817759] |
ChEMBL | Inhibition of Wistar rat brain MAOB using kynuramine as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by fluorescence assay | B | 6.66 | pIC50 | 220 | nM | IC50 | J Nat Prod (2019) 82: 785-791 [PMID:30920216] |
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]