clorgiline [Ligand Id: 6636] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8706 (Clorgiline, clorgyline, Clorgyline, M&B 9302) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Caspase 3/Caspase-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2334] [GtoPdb: 1619] [UniProtKB: P42574] | ||||||||
| ChEMBL | Inhibition of recombinant human caspase-3 using Ac-DEVD-AMC as substrate preincubated for 10 mins followed by substrate addition measured after 60 mins by fluorometric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Medchemcomm (2016) 7: 1628-1639 |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | Irreversible inhibition of recombinant human MAOA expressed in Pichia pastoris using varying levels of kynuramine as substrate measured after 5 mins by Michaelis-Menten equation analysis | B | 6.66 | pKi | 220 | nM | Ki | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| ChEMBL | Reversible inhibition of recombinant human MAOA expressed in Pichia pastoris using varying levels of kynuramine as substrate measured after 5 mins by Michaelis-Menten equation analysis | B | 7.4 | pKi | 40 | nM | Ki | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| ChEMBL | Irreversible inhibition of recombinant human MAO-A expressed in baculovirus infected BT1 cells using p-tyramine as substrate by Lineweaver-Burk plot analysis | B | 7.92 | pKi | 12 | nM | Ki | Eur J Med Chem (2013) 70: 88-101 [PMID:24140951] |
| ChEMBL | Inhibition of recombinant human MAOA using kynuramine as substrate assessed as decrease in formation of 4-hydroxyquinoline incubated for 20 mins by fluorescence assay | B | 9.52 | pKi | 0.3 | nM | Ki | Medchemcomm (2016) 7: 1628-1639 |
| ChEMBL | Inhibition of recombinant human MAO-A | B | 4.65 | pIC50 | 22600 | nM | IC50 | Eur J Med Chem (2020) 194: 112265-112265 [PMID:32240904] |
| ChEMBL | Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method | B | 5.35 | pIC50 | 4460 | nM | IC50 | Medchemcomm (2010) 1: 61-72 |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay | B | 5.35 | pIC50 | 4460 | nM | IC50 | Eur J Med Chem (2011) 46: 4846-4852 [PMID:21872365] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 5.35 | pIC50 | 4460 | nM | IC50 | J Med Chem (2008) 51: 4874-4880 [PMID:18666768] |
| ChEMBL | Inhibition of recombinant human MAOA using kynuramine as substrate measured for 30 mins by fluorescence spectrophotometric assay | B | 5.49 | pIC50 | 3200 | nM | IC50 | Eur J Med Chem (2021) 213: 113183-113183 [PMID:33493825] |
| ChEMBL | Inhibition of human recombinant MAO-A using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins prior to substrate addition measured after 20 mins by microplate fluorescence reader analysis | B | 5.56 | pIC50 | 2760 | nM | IC50 | Bioorg Med Chem (2015) 23: 515-525 [PMID:25541201] |
| ChEMBL | Inhibition of recombinant human MAOA using p-tyramine as substrate assessed as H2O2 production preincubated for 15 mins followed by substrate addition by fluorometric analysis | B | 5.57 | pIC50 | 2720 | nM | IC50 | Eur J Med Chem (2015) 103: 185-190 [PMID:26352677] |
| 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 | 6.72 | pIC50 | 189 | nM | IC50 | Eur J Med Chem (2018) 145: 588-593 [PMID:29339253] |
| ChEMBL | Inhibition of recombinant human microsomal MAO-A expressed in baculovirus-infected insect cells using p-tyramine as substrate assessed as H2O2 production pretreated for 15 mins followed by addition of Amplex Red, horseradish peroxidase and substrate measured for 15 mins by fluorimetric method | B | 6.72 | pIC50 | 189 | nM | IC50 | Bioorg Med Chem (2016) 24: 1741-1748 [PMID:26964672] |
| ChEMBL | Inhibition of human MAO-A preincubated for 5 mins followed by addition of Kynuramine substrate and measured after 30 mins by plate reader method | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2021) 211: 113112-113112 [PMID:33360800] |
| ChEMBL | Inhibition of human recombinant MAO-A using tyramine as substrate preincubated with enzyme for 30 mins followed by incubation with substrate for 30 mins by Amplex Red reagent based fluorometric method | B | 7.32 | pIC50 | 48 | nM | IC50 | RSC Med Chem (2020) 11: 1063-1074 [PMID:33479699] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 15 mins by resorufin dye-based fluorescence assay | B | 7.42 | pIC50 | 38 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1012-1018 [PMID:30792039] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in insect cells assessed as inhibition of kynuramine oxidation after 30 mins by fluorescence assay | B | 7.52 | pIC50 | 30.2 | nM | IC50 | J Med Chem (2011) 54: 7023-7029 [PMID:21923198] |
| ChEMBL | Activity Assay: Inhibitory activity of compounds was evaluated by a homogeneous luminescent method, the MAO-Glo Assay (Promega), measuring the monoamine oxidase activity (MAOs) from recombinant source (microsomes from baculovirus infected insect cells, Sigma). Experiments were performed according to the Supplier's procedure, incubating human recombinant MAO-A or MAO-B with a luminogenic substrate, a derivative of beetle luciferin ((4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid). MAOs converts this luciferin derivative to methyl ester luciferin and only compounds that interfere with the ability of the enzyme to use the pro-luminescent substrate will cause changes in the resulting luminescent signal. | B | 7.57 | pIC50 | 27 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| ChEMBL | Inhibition of human recombinant MAOA using kynuramine as substrate incubated for 10 mins by UPLC-ESI-MS/MS analysis | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2019) 27: 2027-2040 [PMID:30975503] |
| ChEMBL | Inhibition of human MAOA | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Inhibition of human recombinant MAO-A preincubated for 30 mins followed by p-tyramine hydrochloride addition measured after 30 mins by Amplex red fluorescence based spectrophotometry | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2016) 24: 4835-4854 [PMID:27396685] |
| ChEMBL | Inhibition of human recombinant MAOA using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by horse-radish peroxidase/amplex red-based fluorometric method | B | 7.8 | pIC50 | 16 | nM | IC50 | Eur J Med Chem (2016) 121: 864-879 [PMID:26471320] |
| ChEMBL | Inhibition of recombinant human MAOA using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured after 15 mins by Amplex red reagent based fluorescence assay | B | 7.89 | pIC50 | 12.85 | nM | IC50 | Eur J Med Chem (2018) 143: 33-47 [PMID:29172081] |
| ChEMBL | Inhibition of human MAOA after 1 hr by luminescence assay | B | 7.91 | pIC50 | 12.4 | nM | IC50 | J Med Chem (2013) 56: 1247-1261 [PMID:23281824] |
| ChEMBL | Reversible inhibition of recombinant human MAO-A assessed as residual activity using kynuramine as substrate preincubated for 30 mins followed by dialysis for 6 hrs by spectrophotometric method | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2403-2407 [PMID:29925480] |
| ChEMBL | Inhibition of recombinant human MAOA using p-tyramine as substrate after 30 mins by Amplex red based spectrophotometric analysis | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2015) 23: 6486-6496 [PMID:26337020] |
| ChEMBL | Inhibition of recombinant human MAO-A using p-tyramine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by amplex red reagent based spectrophotometric assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2018) 26: 232-244 [PMID:29198609] |
| 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 | 8.1 | pIC50 | 7.91 | nM | IC50 | Bioorg Med Chem (2020) 28: 115400-115400 [PMID:32146060] |
| ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay | B | 8.1 | pIC50 | 7.9 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 718-722 [PMID:28131710] |
| ChEMBL | Inhibition of human MAOA using p-tyramine as substrate after 15 mins by Amplex Red MAO assay | B | 8.14 | pIC50 | 7.31 | nM | IC50 | Medchemcomm (2015) 6: 2146-2157 |
| ChEMBL | Inhibition of MAOA (unknown origin) using kynuramine as substrate preincubated for 30 mins followed by substrate addition | B | 8.15 | pIC50 | 7.1 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
| ChEMBL | Inhibition of human recombinant MAO-A using kynuramine as substrate preincubated with compound for 15 mins measured after 20 mins by fluorometric analysis | B | 8.17 | pIC50 | 6.7 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4926-4929 [PMID:22781190] |
| ChEMBL | Inhibition of human recombinant MAOA using kynuramine as substrate preincubated for 30 mins followed by substrate addition | B | 8.21 | pIC50 | 6.2 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 584-588 [PMID:29395970] |
| ChEMBL | Inhibition of recombinant human MAO-A 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 | 8.27 | pIC50 | 5.4 | nM | IC50 | Eur J Med Chem (2017) 131: 92-106 [PMID:28301816] |
| ChEMBL | Inhibition of human recombinant MAO-A assessed as inhibition of production of hydrogen peroxide after 15 mins by Amplex Red fluorimetric method | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2709-2712 [PMID:20382016] |
| ChEMBL | Inhibition of recombinant human MAO-A expressed in baculovirus infected insect cells assessed as reduction in H2O2 production using p-tyramine as substrate pretreated for 15 mins followed by substrate addition and measured over 15 mins by Amplex red reagent based fluorimetric assay | B | 8.28 | pIC50 | 5.2 | nM | IC50 | Medchemcomm (2017) 8: 1788-1796 [PMID:30108888] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay | B | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem (2010) 18: 5063-5070 [PMID:20579890] |
| ChEMBL | Inhibition of human recombinant MAO-A using kynuramine substrate by spectrophotometric assay | B | 8.31 | pIC50 | 4.9 | nM | IC50 | J Med Chem (2015) 58: 5561-5578 [PMID:26107513] |
| 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 | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4714-4719 [PMID:27575476] |
| 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 | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 839-843 [PMID:30686752] |
| 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 | 8.31 | pIC50 | 4.9 | nM | IC50 | Bioorg Med Chem (2021) 42: 116255-116255 [PMID:34119696] |
| ChEMBL | Inhibition of human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 15 mins | B | 8.33 | pIC50 | 4.7 | nM | IC50 | J Med Chem (2014) 57: 10455-10463 [PMID:25418133] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2012) 48: 284-295 [PMID:22222137] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI cells using p-tyramine as substrate after 15 mins by Amplex Red-based fluorescence assay | B | 8.34 | pIC50 | 4.6 | nM | IC50 | Eur J Med Chem (2016) 108: 542-552 [PMID:26717204] |
| ChEMBL | Inhibition of human MAOA pre-incubated for 10 mins before p-tyramine substrate addition and measured after 10 mins by amplex red reagent-based microplate fluorescence reader analysis | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Medchemcomm (2017) 8: 452-464 [PMID:30108763] |
| 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 | 8.35 | pIC50 | 4.5 | nM | IC50 | Eur J Med Chem (2018) 158: 781-800 [PMID:30245401] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-A expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5128-5130 [PMID:23927971] |
| ChEMBL | Inhibition of human recombinant MAO-A assessed as hydrogen peroxide production | B | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2009) 52: 2818-2824 [PMID:19378991] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 cells | B | 8.35 | pIC50 | 4.47 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6479-6482 [PMID:20934874] |
| ChEMBL | Inhibition of human recombinant MAOA by fluorimetric method | B | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2008) 51: 6740-6751 [PMID:18834112] |
| ChEMBL | Inhibition of human MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2012) 58: 405-417 [PMID:23153812] |
| ChEMBL | Inhibition of recombinant human MAO-A expressed in baculovirus infected BT1-TN-5B1-4 cells assessed as inhibition of production of hydrogen peroxide from p-tyramine after 15 mins by Amplex Red assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2013) 59: 91-100 [PMID:23207410] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Bioorg Med Chem (2014) 22: 2887-2895 [PMID:24746464] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method | B | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2011) 54: 2155-2164 [PMID:21405131] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Amplex red dye based fluorimetric method | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2016) 117: 292-300 [PMID:27135371] |
| 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 | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2017) 60: 7206-7212 [PMID:28753307] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in baculovirus infected BTI insect cells assessed as hydrogen peroxide production after 15 mins by Amplex red assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2010) 45: 4490-4498 [PMID:20702005] |
| ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 20 mins by fluorescence assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2018) 143: 1543-1552 [PMID:29126727] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay | B | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2010) 53: 6516-6520 [PMID:20715818] |
| ChEMBL | Inhibition of human MAOA by fluorimetry | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Bioorg Med Chem (2010) 18: 5715-5723 [PMID:20615716] |
| 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 | 8.35 | pIC50 | 4.46 | nM | IC50 | J Med Chem (2016) 59: 5879-5893 [PMID:27244485] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 8.35 | pIC50 | 4.46 | nM | IC50 | Eur J Med Chem (2010) 45: 800-804 [PMID:19926363] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-A 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 | 8.36 | pIC50 | 4.39 | nM | IC50 | Eur J Med Chem (2019) 177: 221-234 [PMID:31151057] |
| ChEMBL | Inhibition of human recombinant MAOA assessed as H2O2 production by Amplex Red reagent-based assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2012) 55: 8483-8492 [PMID:22978824] |
| ChEMBL | Inhibition of recombinant human MAO-A using p-tyramine substrate preincubated for 15 mins before substrate addition measured after 20 mins by fluorescence assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Eur J Med Chem (2013) 62: 745-753 [PMID:23454517] |
| ChEMBL | Inhibition of human recombinant MAO-A using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured after 20 mins by fluorescence plate reader analysis | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Bioorg Med Chem (2015) 23: 3722-3729 [PMID:25934229] |
| ChEMBL | Inhibition of human recombinant MAO-A using p-tyramine as substrate assessed as formation of H2O2 preincubated for 15 mins under dark condition followed by substrate addition measured after 20 mins by fluorescence assay | B | 8.39 | pIC50 | 4.1 | nM | IC50 | Bioorg Med Chem (2013) 21: 7406-7417 [PMID:24128814] |
| ChEMBL | Inhibition of human recombinant MAOA using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured after 20 mins by fluorescence plate reader analysis | B | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2013) 56: 5843-5859 [PMID:23799643] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2009) 52: 1935-1942 [PMID:19267475] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem (2010) 18: 1273-1279 [PMID:20045650] |
| ChEMBL | Inhibition of recombinant human MAO-A incubated for 30 mins by fluorescence-based method | B | 8.4 | pIC50 | 4 | nM | IC50 | J Nat Prod (2020) 83: 852-863 [PMID:32150413] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2011) 46: 5838-5851 [PMID:22005185] |
| ChEMBL | Inhibition of recombinant human MAO-A expressed in baculovirus infected insect cell microsomes using kynuramine as substrate measured after 30 mins by fluorescence based assay | B | 8.42 | pIC50 | 3.8 | nM | IC50 | Eur J Med Chem (2019) 161: 292-309 [PMID:30366255] |
| ChEMBL | Inhibition of MAOA (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | B | 8.44 | pIC50 | 3.6 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| 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 | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem (2017) 25: 633-645 [PMID:27908752] |
| 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 | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence method | B | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 5046-5052 [PMID:29033233] |
| 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 | 8.47 | pIC50 | 3.4 | nM | IC50 | Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125] |
| 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 | 8.47 | pIC50 | 3.4 | nM | IC50 | Eur J Med Chem (2021) 209: 112911-112911 [PMID:33071056] |
| 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 | 8.49 | pIC50 | 3.21 | nM | IC50 | J Med Chem (2021) 64: 11169-11182 [PMID:34269579] |
| ChEMBL | Inhibition of MAOA by spectrophotometry | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2010) 45: 4479-4489 [PMID:20708306] |
| ChEMBL | Inhibition of MAO-A (unknown origin) using (4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid as substrate by MAO-Glo assay | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Bioorg Med Chem (2018) 26: 6000-6014 [PMID:30448189] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| 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 | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem (2020) 28: 115374-115374 [PMID:32089390] |
| 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 | 8.56 | pIC50 | 2.74 | nM | IC50 | Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793] |
| ChEMBL | Inhibition of human recombinant MAO-A by multimode plate reader assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2021) 216: 113310-113310 [PMID:33667847] |
| ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 30 mins by fluorescence assay | B | 8.57 | pIC50 | 2.7 | 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 after 30 mins by fluorescence assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2018) 26: 1102-1115 [PMID:29409707] |
| ChEMBL | Inhibition of human recombinant MAO-A using kynuramine as substrate after 30 mins by fluorescence spectrophotometry | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2016) 24: 2342-2351 [PMID:27079124] |
| ChEMBL | Inhibition of human recombinant MAO-A using kynuramine as substrate measured after 30 mins by fluorescence assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535] |
| 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 | 8.57 | pIC50 | 2.7 | nM | IC50 | Eur J Med Chem (2017) 126: 762-775 [PMID:27951485] |
| 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 | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2017) 25: 1997-2009 [PMID:28237559] |
| 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 | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2017) 25: 1030-1041 [PMID:28011206] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in insect cell microsomes using kynuramine as substrate after 20 mins by fluorescence spectrophotometric analysis | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7367-7370 [PMID:23122857] |
| 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 | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (2016) 59: 6791-6806 [PMID:27347731] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using tyramine as substrate preincubated for 1 hr followed by substrate addition and measured after 30 mins by resazurin dye-based fluorescence assay | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2018) 61: 7043-7064 [PMID:30016860] |
| ChEMBL | Inhibition of recombinant human MAO-A expressed in Sf9 cells using p-tyramine as substrate preincubated for 15 mins followed by substrate addition for 60 mins by Luminex assay | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2020) 63: 15021-15036 [PMID:33210537] |
| ChEMBL | Inhibition of MAO-A (unknown origin) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| ChEMBL | Inhibition of MAO-A (unknown origin) | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2021) 41: 127993-127993 [PMID:33775841] |
| ChEMBL | Inhibition of human recombinant MAOA using kynuramine as substrate preincubated for 10 mins followed by substrate addition at 10 secs intervals measured after 20 mins by fluorescence assay | B | 8.97 | pIC50 | 1.06 | nM | IC50 | Medchemcomm (2018) 9: 357-370 [PMID:30108930] |
| ChEMBL | Inhibition of recombinant human MAOA using kynuramine as substrate assessed as decrease in formation of 4-hydroxyquinoline incubated for 20 mins by fluorescence assay | B | 9 | pIC50 | 1 | nM | IC50 | Medchemcomm (2016) 7: 1628-1639 |
| ChEMBL | Inhibition of human monoamine oxidase A | B | 11.31 | pIC50 | 0 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| Monoamine oxidase A in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3254] [UniProtKB: P21398] | ||||||||
| ChEMBL | Inhibitory activity against monoamine oxidase A in isolated bovine brain mitochondria | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2003) 46: 917-920 [PMID:12620068] |
| ChEMBL | Inhibition of bovine brain mitochondria MAOA by fluorometric assay | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2007) 50: 922-931 [PMID:17256833] |
| ChEMBL | Inhibition of bovine brain mitochondrial MAO-A by fluorometric assay | B | 7.27 | pKi | 54 | nM | Ki | Bioorg Med Chem (2008) 16: 9729-9740 [PMID:18951803] |
| ChEMBL | Inhibition of bovine brain MAOA using kinuramine as substrate preincubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric assay | B | 7.27 | pKi | 54 | nM | Ki | J Med Chem (2012) 55: 10424-10436 [PMID:23153282] |
| ChEMBL | Inhibition of MAO-A in bovine brain mitochondria using serotonin as substrate preincubated for 30 mins measured after 30 mins by spectrofluorimetric analysis | B | 8.44 | pIC50 | 3.65 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5281-5285 [PMID:26428872] |
| ChEMBL | Inhibition of bovine brain MAO-A preincubated for 60 mins before substrate addition by fluorimetric method | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2015) 93: 308-320 [PMID:25707011] |
| ChEMBL | Inhibition of bovine brain mitochondria MAO-A by spectrofluorimetry | B | 8.51 | pIC50 | 3.1 | nM | IC50 | Eur J Med Chem (2015) 93: 481-491 [PMID:25732770] |
| ChEMBL | Inhibition of bovine brain mitochondria MAO-A using serotonin substrate after 60 mins by fluorimetric method | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem (2015) 23: 3574-3585 [PMID:25922182] |
| 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 | 5.92 | pKi | 1200 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Inhibition of rat liver MAOA after 60 mins pre-incubation | B | 5.57 | pIC50 | 2720 | nM | IC50 | Bioorg Med Chem (2007) 15: 5775-5786 [PMID:17611112] |
| ChEMBL | Inhibition of MAO-A in rat liver homogenate after 60 mins by residual activity plot | B | 5.69 | pIC50 | 2050 | nM | IC50 | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Inhibition of MAOA in rat liver homogenates preincubated for 60 mins | B | 5.69 | pIC50 | 2050 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6362-6368 [PMID:18980841] |
| ChEMBL | Inhibition of MAO-A in rat liver homogenate using [14C]-5HT as substrate preincubated for 30 mins followed by substrate addition measured after 20 mins by liquid scintillation counting analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2014) 80: 543-561 [PMID:24813882] |
| ChEMBL | Inhibition of Wistar rat brain MAOA using kynuramine as substrate preincubated for 15 mins followed by substrate addition and measured after 15 mins by fluorescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | J Nat Prod (2019) 82: 785-791 [PMID:30920216] |
| ChEMBL | Inhibition of MAO-A in rat liver mitochondria using p-tyramine as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of MAO-B inhibitor deprenyl by Amplex red dye-based fluorescence assay | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Eur J Med Chem (2018) 143: 1373-1386 [PMID:29126721] |
| ChEMBL | Inhibition of MAO-A in rat liver mitochondria using serotonin as substrate preincubated with enzyme for 60 mins prior to substrate addition | B | 8.54 | pIC50 | 2.9 | nM | IC50 | Bioorg Med Chem Lett (2014) 25: 70-74 [PMID:25466194] |
| ChEMBL | In vitro inhibitory activity on rat brain by monoamine oxidase A (MAO-A) | B | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Inhibition of MAO-A in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 9.38 | pIC50 | 0.42 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Inhibition of human MAOB using p-tyramine as substrate after 15 mins by Amplex Red MAO assay | B | 4.15 | pIC50 | 71500 | nM | IC50 | Medchemcomm (2015) 6: 2146-2157 |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 15 mins | B | 4.18 | pIC50 | 65800 | nM | IC50 | J Med Chem (2014) 57: 10455-10463 [PMID:25418133] |
| ChEMBL | Inhibition of human recombinant MAO-B preincubated for 30 mins followed by p-tyramine hydrochloride addition measured after 30 mins by Amplex red fluorescence based spectrophotometry | B | 4.18 | pIC50 | 65500 | nM | IC50 | Bioorg Med Chem (2016) 24: 4835-4854 [PMID:27396685] |
| ChEMBL | Inhibition of human recombinant MAOB using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 1 hr by horse-radish peroxidase/amplex red-based fluorometric method | B | 4.18 | pIC50 | 65500 | nM | IC50 | Eur J Med Chem (2016) 121: 864-879 [PMID:26471320] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine after 15 mins by amplex red assay | B | 4.2 | pIC50 | 63410 | nM | IC50 | Eur J Med Chem (2011) 46: 5838-5851 [PMID:22005185] |
| 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 | 4.2 | pIC50 | 63410 | nM | IC50 | J Med Chem (2016) 59: 5879-5893 [PMID:27244485] |
| ChEMBL | Inhibition of human recombinant MAO-B assessed as inhibition of production of hydrogen peroxide after 15 mins by the Amplex Red fluorimetric method | B | 4.2 | pIC50 | 63410 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2709-2712 [PMID:20382016] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected insect cells assessed as reduction in H2O2 production using p-tyramine as substrate pretreated for 15 mins followed by substrate addition and measured over 15 mins by Amplex red reagent based fluorimetric assay | B | 4.2 | pIC50 | 63410 | nM | IC50 | Medchemcomm (2017) 8: 1788-1796 [PMID:30108888] |
| 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 | 4.2 | pIC50 | 63400 | nM | IC50 | Eur J Med Chem (2018) 158: 781-800 [PMID:30245401] |
| 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 | 4.21 | pIC50 | 62010 | nM | IC50 | Eur J Med Chem (2020) 202: 112475-112475 [PMID:32652406] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BT1 cells | B | 4.21 | pIC50 | 61659.5 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6479-6482 [PMID:20934874] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as hydrogen peroxide production from p-tyramine by amplex red assay | B | 4.21 | pIC50 | 61356 | nM | IC50 | Bioorg Med Chem (2010) 18: 5063-5070 [PMID:20579890] |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate incubated for 15 mins prior to substrate addition measured for 15 mins by Amplex red assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2012) 58: 405-417 [PMID:23153812] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BT1-TN-5B1-4 cells assessed as inhibition of production of hydrogen peroxide from p-tyramine after 15 mins by Amplex Red assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2013) 59: 91-100 [PMID:23207410] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus-infected insect BTI-TN-5B1-4 cells assessed as p-tyramine conversion to H2O2 by fluorescence assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5128-5130 [PMID:23927971] |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate assessed as hydrogen peroxide production by fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | Medchemcomm (2010) 1: 61-72 |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus-infected BTI-TN-5B1-4 cell microsomes assessed as decrease in H2O2 production using p-tyramine as substrate preincubated for 15 mins by Amplex Red reagent based fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | Bioorg Med Chem (2014) 22: 2887-2895 [PMID:24746464] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI cells using p-tyramine as substrate after 15 mins by Amplex Red-based fluorescence assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2016) 108: 542-552 [PMID:26717204] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins Amplex red dye based fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2016) 117: 292-300 [PMID:27135371] |
| ChEMBL | Inhibition of human MAOB pre-incubated for 10 mins before p-tyramine substrate addition and measured after 10 mins by amplex red reagent-based microplate fluorescence reader analysis | B | 4.21 | pIC50 | 61350 | nM | IC50 | Medchemcomm (2017) 8: 452-464 [PMID:30108763] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells assessed as effect on H2O2 production from para-tyramine by fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2009) 52: 1935-1942 [PMID:19267475] |
| ChEMBL | Inhibition of human recombinant MAO-B assessed as hydrogen peroxide production | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2009) 52: 2818-2824 [PMID:19378991] |
| ChEMBL | Inhibition of human recombinant MAOB by fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2008) 51: 6740-6751 [PMID:18834112] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Bioorg Med Chem (2010) 18: 1273-1279 [PMID:20045650] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2010) 45: 800-804 [PMID:19926363] |
| ChEMBL | Inhibition of human MAOB by fluorimetry | B | 4.21 | pIC50 | 61350 | nM | IC50 | Bioorg Med Chem (2010) 18: 5715-5723 [PMID:20615716] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus infected insect BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine by amplex red assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2010) 53: 6516-6520 [PMID:20715818] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus infected BTI insect cells assessed as hydrogen peroxide production after 15 mins by Amplex red assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2010) 45: 4490-4498 [PMID:20702005] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect sells assessed as hydrogen peroxide production by fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2011) 54: 2155-2164 [PMID:21405131] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine after 15 mins by microplate fluorescence assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2011) 46: 4846-4852 [PMID:21872365] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as inhibition of hydrogen peroxide production from p-tryptamine after 15 mins by fluorimetric method | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2012) 48: 284-295 [PMID:22222137] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2018) 143: 1543-1552 [PMID:29126727] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 4.21 | pIC50 | 61350 | nM | IC50 | J Med Chem (2008) 51: 4874-4880 [PMID:18666768] |
| ChEMBL | Inhibition of recombinant human MAOB using p-tyramine as substrate assessed as H2O2 production preincubated for 15 mins followed by substrate addition by fluorometric analysis | B | 4.22 | pIC50 | >60000 | nM | IC50 | Eur J Med Chem (2015) 103: 185-190 [PMID:26352677] |
| 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 | 4.22 | pIC50 | >60000 | nM | IC50 | Eur J Med Chem (2018) 145: 588-593 [PMID:29339253] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 4.27 | pIC50 | 54300 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| ChEMBL | Inhibition of human recombinant MAO-B by multimode plate reader assay | B | 4.68 | pIC50 | 20800 | 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 | 4.68 | pIC50 | 20800 | nM | IC50 | Bioorg Med Chem (2018) 26: 1102-1115 [PMID:29409707] |
| 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 15 mins by Amplex red reagent/horseradish peroxidase coupled fluorescence assay | B | 4.69 | pIC50 | 20300 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1090-1093 [PMID:30833108] |
| ChEMBL | Inhibition of human MAO-B | B | 4.69 | pIC50 | 20270 | nM | IC50 | Bioorg Med Chem Lett (2021) 43: 128051-128051 [PMID:33887441] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells using p-tyramine as substrate preincubated for 30 mins followed by substrate addition measured for 15 mins by resorufin dye-based fluorescence assay | B | 4.69 | pIC50 | 20270 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1012-1018 [PMID:30792039] |
| ChEMBL | Activity Assay: Inhibitory activity of compounds was evaluated by a homogeneous luminescent method, the MAO-Glo Assay (Promega), measuring the monoamine oxidase activity (MAOs) from recombinant source (microsomes from baculovirus infected insect cells, Sigma). Experiments were performed according to the Supplier's procedure, incubating human recombinant MAO-A or MAO-B with a luminogenic substrate, a derivative of beetle luciferin ((4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid). MAOs converts this luciferin derivative to methyl ester luciferin and only compounds that interfere with the ability of the enzyme to use the pro-luminescent substrate will cause changes in the resulting luminescent signal. | B | 4.84 | pIC50 | 14300 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| 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 | 4.85 | pIC50 | 14190 | nM | IC50 | Bioorg Med Chem (2021) 35: 116074-116074 [PMID:33640707] |
| 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 | 4.87 | pIC50 | 13600 | nM | IC50 | Eur J Med Chem (2021) 209: 112911-112911 [PMID:33071056] |
| 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 | 4.87 | pIC50 | 13568.4 | 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 | 4.87 | pIC50 | 13568 | nM | IC50 | Bioorg Med Chem (2017) 25: 633-645 [PMID:27908752] |
| ChEMBL | Inhibition of human recombinant MAO-B using kynuramine substrate by spectrophotometric assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (2015) 58: 5561-5578 [PMID:26107513] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay | B | 5.05 | pIC50 | 8850 | 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 | 5.05 | pIC50 | 8850 | nM | IC50 | Bioorg Med Chem (2020) 28: 115400-115400 [PMID:32146060] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells using benzylamine as substrate preincubated for 1 hr followed by substrate addition and measured after 30 mins by resazurin dye-based fluorescence assay | B | 5.12 | pIC50 | 7647 | nM | IC50 | J Med Chem (2018) 61: 7043-7064 [PMID:30016860] |
| 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 | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem (2021) 42: 116255-116255 [PMID:34119696] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence method | B | 5.3 | pIC50 | 5020 | 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 | 5.3 | pIC50 | 5020 | nM | IC50 | Bioorg Med Chem (2017) 25: 3006-3017 [PMID:28487125] |
| ChEMBL | Inhibition of human recombinant MAO-B using kynuramine as substrate after 30 mins by fluorescence spectrophotometry | B | 5.38 | pIC50 | 4190 | nM | IC50 | Bioorg Med Chem (2016) 24: 2342-2351 [PMID:27079124] |
| 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 | 5.38 | pIC50 | 4190 | nM | IC50 | Bioorg Med Chem (2017) 25: 1030-1041 [PMID:28011206] |
| ChEMBL | Inhibition of human recombinant MAO-B using kynuramine as substrate measured after 30 mins by fluorescence assay | B | 5.38 | pIC50 | 4190 | nM | IC50 | Bioorg Med Chem (2017) 25: 714-726 [PMID:27923535] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 30 mins by fluorescence assay | B | 5.38 | pIC50 | 4190 | nM | IC50 | Bioorg Med Chem (2018) 26: 1885-1895 [PMID:29500132] |
| 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 | 5.38 | pIC50 | 4190 | nM | IC50 | Eur J Med Chem (2017) 126: 762-775 [PMID:27951485] |
| 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 | 5.59 | pIC50 | 2550 | nM | IC50 | J Med Chem (2016) 59: 6791-6806 [PMID:27347731] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected insect cell microsomes using kynuramine as substrate measured after 30 mins by fluorescence based assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | Eur J Med Chem (2019) 161: 292-309 [PMID:30366255] |
| 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 | 5.61 | pIC50 | 2430 | nM | IC50 | Bioorg Med Chem (2017) 25: 1997-2009 [PMID:28237559] |
| 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 | 5.63 | pIC50 | 2340 | nM | IC50 | Bioorg Med Chem (2020) 28: 115374-115374 [PMID:32089390] |
| 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 | 5.66 | pIC50 | 2212 | nM | IC50 | J Med Chem (2021) 64: 11169-11182 [PMID:34269579] |
| ChEMBL | Inhibition of human microsomal MAO-B 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 | 5.66 | pIC50 | 2210 | nM | IC50 | Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793] |
| 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 | 5.7 | pIC50 | >2000 | 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 | 5.7 | pIC50 | >2000 | 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 | 5.7 | pIC50 | >2000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 584-588 [PMID:29395970] |
| ChEMBL | Inhibition of MAOB (unknown origin) using benzylamine as substrate preincubated for 30 mins followed by substrate addition | B | 5.77 | pIC50 | 1690 | nM | IC50 | Medchemcomm (2018) 9: 1871-1881 [PMID:30568755] |
| ChEMBL | Inhibition of recombinant human MAOB using benzylamine as substrate after 30 mins by Amplex red based spectrophotometric analysis | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2015) 23: 6486-6496 [PMID:26337020] |
| ChEMBL | Inhibition of recombinant human MAO-B using benzylamine as substrate preincubated for 15 mins followed by substrate addition measured after 20 mins by amplex red reagent based spectrophotometric assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2018) 26: 232-244 [PMID:29198609] |
| ChEMBL | Inhibition of recombinant human MAO-B | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Eur J Med Chem (2020) 194: 112265-112265 [PMID:32240904] |
| Monoamine oxidase B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2756] [UniProtKB: P56560] | ||||||||
| ChEMBL | Inhibitory activity against monoamine oxidase B in isolated bovine brain mitochondria | B | 4.24 | pKi | 58000 | nM | Ki | J Med Chem (2003) 46: 917-920 [PMID:12620068] |
| ChEMBL | Inhibition of bovine brain mitochondria MAOB by fluorometric assay | B | 4.24 | pKi | 58000 | nM | Ki | J Med Chem (2007) 50: 922-931 [PMID:17256833] |
| ChEMBL | Inhibition of bovine brain mitochondrial MAO-B by fluorometric assay | B | 4.24 | pKi | 58000 | nM | Ki | Bioorg Med Chem (2008) 16: 9729-9740 [PMID:18951803] |
| ChEMBL | Inhibition of bovine brain MAOB using kinuramine as substrate preincubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric assay | B | 4.24 | pKi | 58000 | nM | Ki | J Med Chem (2012) 55: 10424-10436 [PMID:23153282] |
| ChEMBL | Inhibition of MAO-B in bovine brain mitochondria using benzylamine as substrate | B | 4.01 | pIC50 | 98000 | nM | IC50 | Bioorg Med Chem Lett (2014) 25: 70-74 [PMID:25466194] |
| ChEMBL | Inhibition of bovine brain mitochondria MAO-B using benzylamine substrate after 60 mins by fluorimetric method | B | 4.01 | pIC50 | 98000 | nM | IC50 | Bioorg Med Chem (2015) 23: 3574-3585 [PMID:25922182] |
| 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 | 5.25 | pKi | 5600 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Inhibition of MAO-B in rat liver mitochondria using p-tyramine as substrate preincubated for 10 mins followed by substrate addition measured after 30 mins in presence of MAO-A inhibitor clorgyline by Amplex red dye-based fluorescence assay | B | 4.21 | pIC50 | 61350 | nM | IC50 | Eur J Med Chem (2018) 143: 1373-1386 [PMID:29126721] |
| ChEMBL | Inhibition of MAO-B in rat liver homogenate using [14C]-phenylethylamine as substrate preincubated for 30 mins followed by substrate addition measured after 4 mins by liquid scintillation counting analysis | B | 5.1 | pIC50 | 8000 | nM | IC50 | Eur J Med Chem (2014) 80: 543-561 [PMID:24813882] |
| ChEMBL | In vitro inhibitory activity on rat brain MAO-B. | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Inhibition of MAO-B in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| ChEMBL | Inhibition of MAO-B in rat whole brain homogenate in presence of clorgyline | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| σ2/Sigma intracellular receptor 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4802011] [GtoPdb: 2553] [UniProtKB: Q8VD00] | ||||||||
| ChEMBL | Inhibition of radioligand binding to sigma2 receptor in C57BL/6 mouse brain membranes | B | 6.3 | pKi | 505 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3465] [GtoPdb: 2552] [UniProtKB: O55242] | ||||||||
| ChEMBL | Inhibition of radioligand binding to sigma1 receptor in C57BL/6 mouse brain membranes | B | 8.54 | pKi | 2.9 | nM | Ki | J Med Chem (2020) 63: 15187-15217 [PMID:33111525] |
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]
