pargyline [Ligand Id: 7262] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL673 (Eutonyl, Eutron, Pargyline)
  • aldehyde dehydrogenase 2 family member/Aldehyde dehydrogenase in Rat [ChEMBL: CHEMBL2812] [GtoPdb: 2595] [UniProtKB: P11884]
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  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]