rasagiline [Ligand Id: 6641] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL887 (AGN-1135, Azilect, NSC-759639, Rasagiline, TV-1030)
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 7.72 pIC50 19 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibition of human serum BChE using butyrylthiocholine chloride as substrate incubated for 15 mins by Ellman's method B 5.32 pIC50 4760 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397]
ChEMBL Binding affinity towards monoamine oxidase A activity was measured using a kynuramine assay B 5.01 pKi 9700 nM Ki J Med Chem (2004) 47: 1760-1766 [PMID:15027867]
ChEMBL Inhibition of human recombinant microsomal MAOA expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production by amplex red-based fluorescence assay B 4.28 pIC50 53000 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of human recombinant microsomal MAOA expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production after 15 mins by amplex red-based fluorescence assay B 4.28 pIC50 52974 nM IC50 J Med Chem (2017) 60: 7206-7212 [PMID:28753307]
ChEMBL Inhibition of human microsomal MAO-A expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay B 4.28 pIC50 52974 nM IC50 J Med Chem (2016) 59: 5879-5893 [PMID:27244485]
ChEMBL Inhibition of recombinant human MAO-A using p-tyramine as substrate assessed as decrease in H2O2 production incubated for 15 mins by fluorimetric method B 4.29 pIC50 50710 nM IC50 Bioorg Med Chem (2016) 24: 5929-5940 [PMID:27692996]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate pretreated for 15 mins followed by substrate addition after 20 mins by Amplex red reagent based fluorimetric method B 4.3 pIC50 49700 nM IC50 Bioorg Med Chem (2017) 25: 3815-3826 [PMID:28549891]
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 4.53 pIC50 29520 nM IC50 J Med Chem (2020) 63: 1361-1387 [PMID:31917923]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by horse-radish peroxidase/Amplex Red coupled fluorimetric analysis B 4.53 pIC50 29500 nM IC50 Eur J Med Chem (2021) 209: 112911-112911 [PMID:33071056]
ChEMBL Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric analysis B 4.78 pIC50 16440 nM IC50 Eur J Med Chem (2013) 63: 151-161 [PMID:23474901]
ChEMBL Inhibition of human microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectrophotometric analysis B 5.44 pIC50 3650 nM IC50 Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorimetric method B 5.58 pIC50 2610 nM IC50 Bioorg Med Chem (2017) 25: 1997-2009 [PMID:28237559]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI-TN- 5B1-4 insect cells using kynuramine as substrate preincubated for 10 mins in presence of substrate followed by enzyme addition and measured every minute for 30 mins by spectrophotometry analysis B 5.63 pIC50 2340 nM IC50 J Med Chem (2021) 64: 11169-11182 [PMID:34269579]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 5.67 pIC50 2130 nM IC50 Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125]
ChEMBL Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence method B 5.67 pIC50 2130 nM IC50 Bioorg Med Chem Lett (2017) 27: 5046-5052 [PMID:29033233]
ChEMBL Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 5.81 pIC50 1560 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected High 5 insect cells using kynuramine as substrate incubated for 30 mins by spectrofluorometric method B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem (2017) 25: 1030-1041 [PMID:28011206]
ChEMBL Inhibition of human recombinant MAO-A using kynuramine as substrate after 30 mins by fluorescence spectrophotometry B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem (2016) 24: 2342-2351 [PMID:27079124]
ChEMBL Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem (2018) 26: 1885-1895 [PMID:29500132]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence assay B 5.85 pIC50 1420 nM IC50 Eur J Med Chem (2017) 126: 762-775 [PMID:27951485]
ChEMBL Inhibition of human recombinant MAO-A using kynuramine as substrate measured after 30 mins by fluorescence assay B 5.85 pIC50 1420 nM IC50 Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535]
ChEMBL Inhibition of recombinant human MAOA expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay B 5.99 pIC50 1020 nM IC50 Bioorg Med Chem (2020) 28: 115374-115374 [PMID:32089390]
ChEMBL Inhibition of recombinant human MAO-A using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured over 15 mins by Amplex red reagent-based fluorimetric method B 6 pIC50 1010 nM IC50 Eur J Med Chem (2018) 145: 588-593 [PMID:29339253]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by horse-radish peroxidase-coupled amplex red reagent-based fluorescence spectrophotometric method B 6.12 pIC50 750 nM IC50 Eur J Med Chem (2019) 173: 203-212 [PMID:31005056]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay B 6.15 pIC50 712 nM IC50 Bioorg Med Chem (2020) 28: 115400-115400 [PMID:32146060]
ChEMBL Irreversible inhibition of human cerebral cortex MAO-A using [14C]-5-hydroxytryptamine creatinine disulphate as substrate pretreated for 60 mins followed by substrate addition after 30 mins by liquid scintillation counting method B 6.15 pIC50 710 nM IC50 Eur J Med Chem (2017) 130: 365-378 [PMID:28273563]
ChEMBL Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay B 6.15 pIC50 710 nM IC50 Bioorg Med Chem Lett (2017) 27: 718-722 [PMID:28131710]
ChEMBL Inhibition of human recombinant MAOA assessed as H2O2 production by Amplex Red reagent-based assay B 6.15 pIC50 700 nM IC50 J Med Chem (2012) 55: 8483-8492 [PMID:22978824]
ChEMBL Inhibitory concentration towards in human monoamine oxidase A was measured B 6.15 pIC50 700 nM IC50 J Med Chem (2004) 47: 1760-1766 [PMID:15027867]
ChEMBL Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method B 6.17 pIC50 680 nM IC50 Eur J Med Chem (2019) 179: 404-422 [PMID:31265934]
ChEMBL Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay B 6.17 pIC50 680 nM IC50 Eur J Med Chem (2019) 162: 793-809 [PMID:30522087]
ChEMBL Inhibition of human recombinant MAO-A using kynuramine as substrate measured after 30 mins by fluorimetric assay B 6.2 pIC50 630 nM IC50 Bioorg Med Chem Lett (2019) 29: 126625-126625 [PMID:31444085]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay B 6.21 pIC50 620 nM IC50 Eur J Med Chem (2019) 178: 726-739 [PMID:31229875]
ChEMBL Inhibition of human recombinant MAO-A by multimode plate reader assay B 6.23 pIC50 587 nM IC50 Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 6.23 pIC50 587 nM IC50 Bioorg Med Chem (2018) 26: 1102-1115 [PMID:29409707]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay B 6.23 pIC50 587 nM IC50 Eur J Med Chem (2019) 183: 111737-111737 [PMID:31581002]
ChEMBL Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay B 6.23 pIC50 587 nM IC50 Eur J Med Chem (2019) 180: 238-252 [PMID:31310916]
ChEMBL Inhibition Assay: MAO-A and MAO-B activity was measured using radioactive substrates. The substrate for MAO-A was 5 HT and for MAO-B was PEA. When measuring the activity of MAO-A, the MAO-B activity was inhibited with deprenyl and when measuring the activity of MAO-B the activity of MAO-A was inhibited with clorgylin. Blank samples were produced using TCP to inhibit both of the enzymes. The metabolites were extracted to toluene and read in a β -counter. The results are expressed in relative activity and normalized to the amount of protein in the tissue. Figs. 1 and 2 show MAO-A/MAO-B activity of compounds 3, 4 and of 0-Methyl-M3O at various concentrations (10 -"5 -10 -"8 ). As presented in Figs. 1 and 2, it can be seen that compounds 3, 4 and 0-Methyl-M3O were all potent inhibitors of MAO-A and MAO-B extracted from rat brain, compound 3 clearly the most potent inhibitor of the three compounds. B 6.39 pIC50 410 nM IC50 US-9034303-B2. Neuroprotective and neuro-restorative iron chelators and monoamine oxidase inhibitors and uses thereof (2015)
ChEMBL Inhibition of MAOA B 6.39 pIC50 410 nM IC50 J Med Chem (2008) 51: 347-372 [PMID:18181565]
ChEMBL Inhibition of recombinant human MAO-A B 7.49 pIC50 32 nM IC50 Eur J Med Chem (2020) 194: 112265-112265 [PMID:32240904]
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
ChEMBL Inhibition of Sprague-Dawley rat liver MAO-A using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay B 6.37 pIC50 422 nM IC50 Eur J Med Chem (2019) 162: 793-809 [PMID:30522087]
ChEMBL In vitro inhibitory concentration against Monoamine oxidase A of rat brain homogenates; value ranges from 0.28-0.54 B 6.39 pIC50 410 nM IC50 J Med Chem (2002) 45: 5260-5279 [PMID:12431053]
ChEMBL Inhibition of MAO-A in rat brain using [14C]-5-hydroxytryptamine creatinine disulfate as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by liquid scintillation counting method B 6.39 pIC50 410 nM IC50 J Med Chem (2019) 62: 8881-8914 [PMID:31082225]
ChEMBL Inhibition of rat brain MAO-A in nuclei-free homogenates using [14C]hydroxytryptamine substrate after 20 mins by liquid scintillation counting B 9 pIC50 1 nM IC50 J Med Chem (2015) 58: 1400-1419 [PMID:25627172]
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338]
ChEMBL Binding affinity towards monoamine oxidase B activity was measured using a benzylamine assay B 6.15 pKi 700 nM Ki J Med Chem (2004) 47: 1760-1766 [PMID:15027867]
ChEMBL Inhibition constant against human recombinant Monoamine oxidase-B B 6.15 pKi 700 nM Ki Bioorg Med Chem Lett (2005) 15: 4438-4446 [PMID:16137882]
ChEMBL Binding affinity to human recombinant MAOB B 6.15 pKi 700 nM Ki Medchemcomm (2011) 2: 1099-1103
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 7.85 pKi 14.2 nM Ki Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407]
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 8.12 pKi 7.6 nM Ki Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407]
ChEMBL Inhibition of recombinant human MAOB using kynuramine as substrate measured for 30 mins by fluorescence spectrophotometric assay B 4.34 pIC50 45700 nM IC50 Eur J Med Chem (2021) 213: 113183-113183 [PMID:33493825]
ChEMBL Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured over 45 mins by horseradish peroxidase-Amplex Red-coupled fluorometric assay B 4.81 pIC50 15400 nM IC50 Bioorg Med Chem (2019) 27: 1195-1210 [PMID:30808606]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate pretreated for 15 mins followed by substrate addition after 20 mins by Amplex red reagent based fluorimetric method B 5.13 pIC50 7470 nM IC50 Bioorg Med Chem (2017) 25: 3815-3826 [PMID:28549891]
ChEMBL Inhibition of recombinant human MAO-B B 6.28 pIC50 530 nM IC50 Eur J Med Chem (2020) 194: 112265-112265 [PMID:32240904]
ChEMBL Inhibition of recombinant human MAOB expressed in baculovirus infected BTI insect cells using p-tyramine as substrate measured after 15 mins by Amplex red reagent based fluorescence assay B 6.85 pIC50 141.7 nM IC50 Eur J Med Chem (2020) 202: 112475-112475 [PMID:32652406]
ChEMBL Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 7.06 pIC50 87.6 nM IC50 Bioorg Med Chem Lett (2017) 27: 5053-5059 [PMID:29033232]
ChEMBL Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence method B 7.07 pIC50 86 nM IC50 Bioorg Med Chem Lett (2017) 27: 5046-5052 [PMID:29033233]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 7.07 pIC50 86 nM IC50 Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected High 5 insect cells using kynuramine as substrate incubated for 30 mins by spectrofluorometric method B 7.08 pIC50 83 nM IC50 Bioorg Med Chem (2017) 25: 1030-1041 [PMID:28011206]
ChEMBL Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay B 7.08 pIC50 83 nM IC50 Bioorg Med Chem (2018) 26: 1885-1895 [PMID:29500132]
ChEMBL Inhibition of human recombinant MAO-B using kynuramine as substrate after 30 mins by fluorescence spectrophotometry B 7.08 pIC50 82.5 nM IC50 Bioorg Med Chem (2016) 24: 2342-2351 [PMID:27079124]
ChEMBL Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorescence assay B 7.08 pIC50 82.5 nM IC50 Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence assay B 7.08 pIC50 82.5 nM IC50 Eur J Med Chem (2017) 126: 762-775 [PMID:27951485]
ChEMBL Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric analysis B 7.16 pIC50 69 nM IC50 Eur J Med Chem (2013) 63: 151-161 [PMID:23474901]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using tyramine as substrate pretreated for 30 mins followed by substrate addition incubated for 30 mins measured at 5 mins interval by horse-radish peroxidase/amplex red-based fluorometric method B 7.18 pIC50 66 nM IC50 Eur J Med Chem (2017) 131: 92-106 [PMID:28301816]
ChEMBL Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay B 7.3 pIC50 50.12 nM IC50 J Med Chem (2016) 59: 5879-5893 [PMID:27244485]
ChEMBL Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production by amplex red-based fluorescence assay B 7.3 pIC50 50 nM IC50 Eur J Med Chem (2018) 158: 781-800 [PMID:30245401]
ChEMBL Inhibition of human recombinant microsomal MAOB expressed in baculovirus infected BTI-TN-5B1- 4 cells using p-tyramine as substrate assessed as decrease in H2O2 production after 15 mins by amplex red-based fluorescence assay B 7.3 pIC50 49.66 nM IC50 J Med Chem (2017) 60: 7206-7212 [PMID:28753307]
ChEMBL Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay B 7.3 pIC50 49.66 nM IC50 J Med Chem (2016) 59: 5879-5893 [PMID:27244485]
ChEMBL Inhibition of recombinant human MAO-B expressed in insect cells using kynuramine as substrate assessed as formation of 4-hydroxyquinoline measured every 5 mins for 30 mins B 7.34 pIC50 46 nM IC50 Bioorg Med Chem (2013) 21: 6634-6641 [PMID:24012376]
ChEMBL Inhibition of human recombinant MAO-B expressed in insect cells assessed as kynuramine hydrobromide oxidation after 20 mins by spectrophotometric analysis B 7.34 pIC50 46 nM IC50 Bioorg Med Chem (2012) 20: 3065-3071 [PMID:22436387]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI-TN- 5B1-4 insect cells using kynuramine as substrate preincubated for 10 mins in presence of substrate followed by enzyme addition and measured every minute for 30 mins by spectrophotometry analysis B 7.34 pIC50 45.7 nM IC50 J Med Chem (2021) 64: 11169-11182 [PMID:34269579]
ChEMBL Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay B 7.36 pIC50 44 nM IC50 Bioorg Med Chem Lett (2017) 27: 718-722 [PMID:28131710]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay B 7.36 pIC50 43.7 nM IC50 Bioorg Med Chem (2020) 28: 115400-115400 [PMID:32146060]
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 7.44 pIC50 36 nM IC50 J Med Chem (2020) 63: 1361-1387 [PMID:31917923]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition and measured over 20 mins by horse-radish peroxidase/Amplex Red coupled fluorimetric analysis B 7.44 pIC50 36 nM IC50 Eur J Med Chem (2021) 209: 112911-112911 [PMID:33071056]
ChEMBL Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorimetric assay B 7.44 pIC50 36 nM IC50 Bioorg Med Chem Lett (2019) 29: 126625-126625 [PMID:31444085]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate measured after 30 mins by fluorescence based assay B 7.51 pIC50 31 nM IC50 Eur J Med Chem (2019) 178: 726-739 [PMID:31229875]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence based assay B 7.55 pIC50 28.1 nM IC50 Eur J Med Chem (2019) 183: 111737-111737 [PMID:31581002]
ChEMBL Inhibition of human recombinant MAO-B by multimode plate reader assay B 7.55 pIC50 28.1 nM IC50 Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorescence assay B 7.55 pIC50 28.1 nM IC50 Bioorg Med Chem (2018) 26: 1102-1115 [PMID:29409707]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate incubated for 30 mins by fluorescence based assay B 7.55 pIC50 28.1 nM IC50 Eur J Med Chem (2019) 180: 238-252 [PMID:31310916]
ChEMBL Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorescence-based Amplex Red MAO assay B 7.6 pIC50 25 nM IC50 Bioorg Med Chem Lett (2018) 28: 3596-3600 [PMID:30404719]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI cells using p-tyramine as substrate by fluorometric assay B 7.6 pIC50 25 nM IC50 Eur J Med Chem (2020) 207: 112743-112743 [PMID:32882609]
ChEMBL Inhibition of recombinant human MAOB using kynuramine as substrate preincubated for 30 mins followed by substrate addition and measured after 30 mins by fluorescence assay B 7.64 pIC50 23 nM IC50 Bioorg Med Chem (2021) 35: 116074-116074 [PMID:33640707]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition and measured after 1 hr by fluorimetric analysis B 7.81 pIC50 15.4 nM IC50 Eur J Med Chem (2020) 208: 112765-112765 [PMID:32949963]
GtoPdb - - 7.85 pIC50 14 nM IC50 Br J Pharmacol (2001) 132: 500-6 [PMID:11159700]
ChEMBL Irreversible inhibition of human cerebral cortex MAO-B using [14C]-phenylethylamin as substrate pretreated for 60 mins followed by substrate addition after 20 mins by liquid scintillation counting method B 7.85 pIC50 14 nM IC50 Eur J Med Chem (2017) 130: 365-378 [PMID:28273563]
ChEMBL Inhibitory concentration towards in human monoamine oxidase B was measured B 7.85 pIC50 14 nM IC50 J Med Chem (2004) 47: 1760-1766 [PMID:15027867]
ChEMBL Irreversible inhibition of human MAOB B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (2018) 28: 3596-3600 [PMID:30404719]
ChEMBL Irreversible inhibition of human recombinant MAOB B 7.85 pIC50 14 nM IC50 Medchemcomm (2011) 2: 1099-1103
ChEMBL Inhibition of human recombinant MAOB assessed as H2O2 production by Amplex Red reagent-based assay B 7.85 pIC50 14 nM IC50 J Med Chem (2012) 55: 8483-8492 [PMID:22978824]
ChEMBL Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2019) 162: 793-809 [PMID:30522087]
ChEMBL Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method B 7.89 pIC50 13 nM IC50 Eur J Med Chem (2019) 179: 404-422 [PMID:31265934]
ChEMBL Inhibition of recombinant human MAOB expressed in baculovirus infected in BTI cells using kynuramine as substrate after 30 mins by fluorescence based assay B 7.94 pIC50 11.6 nM IC50 Bioorg Med Chem (2020) 28: 115374-115374 [PMID:32089390]
ChEMBL Inhibition of recombinant human MAO-B using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured over 15 mins by Amplex red reagent-based fluorimetric method B 8 pIC50 10 nM IC50 Eur J Med Chem (2018) 145: 588-593 [PMID:29339253]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using kynuramine as substrate after 30 mins by fluorimetric method B 8 pIC50 9.97 nM IC50 Bioorg Med Chem (2017) 25: 1997-2009 [PMID:28237559]
ChEMBL Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by horse-radish peroxidase-coupled amplex red reagent-based fluorescence spectrophotometric method B 8.08 pIC50 8.4 nM IC50 Eur J Med Chem (2019) 173: 203-212 [PMID:31005056]
ChEMBL Inhibition of recombinant human MAO-B using p-tyramine as substrate assessed as decrease in H2O2 production incubated for 15 mins by fluorimetric method B 8.1 pIC50 7.87 nM IC50 Bioorg Med Chem (2016) 24: 5929-5940 [PMID:27692996]
ChEMBL Inhibition of human MAO-B B 8.22 pIC50 6 nM IC50 Bioorg Med Chem Lett (2021) 43: 128051-128051 [PMID:33887441]
ChEMBL Inhibition of MAOB B 8.36 pIC50 4.4 nM IC50 J Med Chem (2008) 51: 347-372 [PMID:18181565]
ChEMBL Inhibition Assay: MAO-A and MAO-B activity was measured using radioactive substrates. The substrate for MAO-A was 5 HT and for MAO-B was PEA. When measuring the activity of MAO-A, the MAO-B activity was inhibited with deprenyl and when measuring the activity of MAO-B the activity of MAO-A was inhibited with clorgylin. Blank samples were produced using TCP to inhibit both of the enzymes. The metabolites were extracted to toluene and read in a β -counter. The results are expressed in relative activity and normalized to the amount of protein in the tissue. Figs. 1 and 2 show MAO-A/MAO-B activity of compounds 3, 4 and of 0-Methyl-M3O at various concentrations (10 -"5 -10 -"8 ). As presented in Figs. 1 and 2, it can be seen that compounds 3, 4 and 0-Methyl-M3O were all potent inhibitors of MAO-A and MAO-B extracted from rat brain, compound 3 clearly the most potent inhibitor of the three compounds. B 8.4 pIC50 4 nM IC50 US-9034303-B2. Neuroprotective and neuro-restorative iron chelators and monoamine oxidase inhibitors and uses thereof (2015)
Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643]
ChEMBL Inhibition of rat MAOB using benzylamine as substrate pretreated for 1200 secs followed by substrate addition and measured after 3600 secs B 4.98 pIC50 10360 nM IC50 Bioorg Med Chem (2018) 26: 4863-4870 [PMID:30143367]
ChEMBL Inhibition of rat brain MAO-B in nuclei-free homogenates using [14C]phenylacetaldehyde substrate after 20 mins by liquid scintillation counting B 5.52 pIC50 3000 nM IC50 J Med Chem (2015) 58: 1400-1419 [PMID:25627172]
ChEMBL Inhibition of MAO-B in Wistar rat liver using 4-trifluoromethyl benzylamine as substrate preincubated for 20 mins followed by substrate addition measured after 90 mins by microplate reader assay B 6.64 pIC50 230 nM IC50 Bioorg Med Chem Lett (2020) 30: 126900-126900 [PMID:31882295]
ChEMBL Inhibition of MAO-B in rat brain using [14C]-phenylethylamine as substrate preincubated for 60 mins followed by substrate addition and measured after 30 mins by liquid scintillation counting method B 8.36 pIC50 4.4 nM IC50 J Med Chem (2019) 62: 8881-8914 [PMID:31082225]
ChEMBL In vitro inhibitory concentration against Monoamine oxidase B of rat brain homogenates; value ranges from 0.0035-0.053 B 8.36 pIC50 4.4 nM IC50 J Med Chem (2002) 45: 5260-5279 [PMID:12431053]
ChEMBL Inhibition of rat brain MAO-B using [14C]-phenylethylamine as substrate preincubated for 60 mins followed by substrate addition and measured after 20 mins by liquid scintillation counting method B 8.36 pIC50 4.4 nM IC50 Bioorg Med Chem Lett (2019) 29: 126612-126612 [PMID:31421966]
ChEMBL Inhibition of Sprague-Dawley rat liver MAO-B using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay B 8.37 pIC50 4.31 nM IC50 Eur J Med Chem (2019) 162: 793-809 [PMID:30522087]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]-LSD from human 5HT6 receptor expressed in HEK293 cells measured after 1 hr by microbeta plate reader method B 8.85 pKi 1.4 nM Ki Eur J Med Chem (2020) 208: 112765-112765 [PMID:32949963]

ChEMBL data shown on this page come from version 32:

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]