selegiline [Ligand Id: 6639] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL972 (Eldepryl, Emsam, L-selegiline, Selegiline, Zelapar) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 6.17 | pKi | 674 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) | B | 5.75 | pIC50 | 1798 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.76 | pKi | 172 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.42 | pIC50 | 376 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [UniProtKB: P37840] | ||||||||
| ChEMBL | Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 6 days by thioflavin S based fluorescence assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| 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] | ||||||||
| GtoPdb | - | - | 4.17 | pKi | 67250 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1969-73 [PMID:21377879] |
| ChEMBL | Competitive inhibition of human recombinant MAO-A after 60 mins using p-tyramine as substrate by spectrophotometry | B | 4.17 | pKi | 67250 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1969-1973 [PMID:21377879] |
| ChEMBL | Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | B | 4.55 | pKi | 28060 | nM | Ki | J Med Chem (2021) 64: 1989-2009 [PMID:33533632] |
| 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 | 4.62 | pKi | 24060 | nM | Ki | Medchemcomm (2016) 7: 1628-1639 |
| ChEMBL | Inhibition of recombinant human MAO-A using p-tyramine as substrate assessed as H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins by amplex red assay | B | 4.77 | pKi | 16890 | nM | Ki | ACS Med Chem Lett (2016) 7: 56-61 [PMID:26819666] |
| ChEMBL | Competitive reversible inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 insect cells using p-tyramine as substrate assessed as H2O2 production after 15 mins by fluorimetric analysis | B | 5.04 | pKi | 9060 | nM | Ki | Eur J Med Chem (2013) 69: 762-767 [PMID:24099995] |
| ChEMBL | Inhibition of human MAO-A expressed in BTI insect cells using p-tyramine as substrate after 60 mins | B | 5.04 | pKi | 9060 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4296-4300 [PMID:21680183] |
| ChEMBL | Inhibition of recombinant human MAO-A assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay | B | 5.44 | pKi | 3600 | nM | Ki | Medchemcomm (2018) 9: 1164-1171 [PMID:30109004] |
| ChEMBL | Inhibition of human MAOA using p-tyramine as substrate after 15 mins by Amplex Red MAO assay | B | 4.09 | pIC50 | 81500 | nM | IC50 | Medchemcomm (2015) 6: 2146-2157 |
| 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 | 4.15 | pIC50 | 70200 | nM | IC50 | Bioorg Med Chem (2015) 23: 3722-3729 [PMID:25934229] |
| ChEMBL | Inhibition of human recombinant MAOA assessed as H2O2 production by Amplex Red reagent-based assay | B | 4.15 | pIC50 | 70200 | nM | IC50 | J Med Chem (2012) 55: 8483-8492 [PMID:22978824] |
| ChEMBL | Inhibition of human MAO-A assessed as inhibition of p-tyramine oxidation to p-hydroxyphenyl-acetaldehyde after 15 mins by fluorimetric method | B | 4.16 | pIC50 | 68730 | nM | IC50 | J Med Chem (2011) 54: 5165-5173 [PMID:21696156] |
| 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 | 4.16 | pIC50 | 68730 | nM | IC50 | Eur J Med Chem (2011) 46: 5838-5851 [PMID:22005185] |
| ChEMBL | Inhibition of human recombinant MAO-A assessed as inhibition of production of hydrogen peroxide after 15 mins by Amplex Red fluorimetric method | B | 4.16 | pIC50 | 68730 | 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 | 4.16 | pIC50 | 68730 | nM | IC50 | Medchemcomm (2017) 8: 1788-1796 [PMID:30108888] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in baculovirus-infected BTI insect cells assessed as conversion of p-tyramine into p-hydroxyphenyl-acetaldehyde after 15 mins by fluorimetric assay | B | 4.16 | pIC50 | 68730 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 258-261 [PMID:22137786] |
| 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 | 4.16 | pIC50 | 68730 | nM | IC50 | J Med Chem (2017) 60: 7206-7212 [PMID:28753307] |
| 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 by horse-radish peroxidase/amplex red-based fluorescence method | B | 4.16 | pIC50 | 68700 | nM | IC50 | Eur J Med Chem (2018) 156: 534-553 [PMID:30025348] |
| 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 | 4.16 | pIC50 | 68700 | nM | IC50 | Eur J Med Chem (2018) 158: 781-800 [PMID:30245401] |
| ChEMBL | Inhibition of human recombinant MAOA using p-tyramine as substrate incubated for 15 mins by fluorimetric method | B | 4.16 | pIC50 | 68700 | nM | IC50 | Eur J Med Chem (2016) 121: 376-386 [PMID:27267007] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in baculovirus infected BT1 cells | B | 4.17 | pIC50 | 67608.3 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6479-6482 [PMID:20934874] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method | B | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2011) 46: 1147-1152 [PMID:21316817] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2011) 54: 2155-2164 [PMID:21405131] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI insect cells using p-tyramine substrate by fluorometric method | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3268-3270 [PMID:19423346] |
| ChEMBL | Inhibition of human recombinant MAO-A using p-tyramine substrate by fluorometric method | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4224-4227 [PMID:21684743] |
| ChEMBL | Inhibition of human recombinant MAO-A expressed in insect BT1-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine up to 15 mins by amplex red-based fluorometric assay | B | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2011) 54: 7127-7137 [PMID:21923181] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2012) 48: 284-295 [PMID:22222137] |
| 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 | 4.17 | pIC50 | 67250 | 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2013) 59: 91-100 [PMID:23207410] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2013) 63: 151-161 [PMID:23474901] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Medchemcomm (2010) 1: 61-72 |
| ChEMBL | Inhibition of recombinant human MAO-A assessed as production of hydrogen peroxide from p-tyramine after 15 mins by Amplex Red assay | B | 4.17 | pIC50 | 67250 | nM | IC50 | Medchemcomm (2012) 3: 213-218 |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem (2014) 22: 2887-2895 [PMID:24746464] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 642-648 [PMID:25532905] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5128-5130 [PMID:23927971] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2008) 51: 4874-4880 [PMID:18666768] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2009) 52: 1935-1942 [PMID:19267475] |
| ChEMBL | Inhibition of human recombinant MAO-A assessed as hydrogen peroxide production | B | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2009) 52: 2818-2824 [PMID:19378991] |
| ChEMBL | Inhibition of human recombinant MAOA by fluorimetric method | B | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2008) 51: 6740-6751 [PMID:18834112] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI cells | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 5053-5055 [PMID:19628387] |
| ChEMBL | Inhibition of human recombinant MAOA expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem (2010) 18: 1273-1279 [PMID:20045650] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2010) 45: 800-804 [PMID:19926363] |
| ChEMBL | Inhibition of human MAOA by fluorimetry | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem (2010) 18: 5715-5723 [PMID:20615716] |
| ChEMBL | Inhibition of human MAOA expressed in BTI insect cells | B | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5157-5160 [PMID:20659799] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | J Med Chem (2010) 53: 6516-6520 [PMID:20715818] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Bioorg Med Chem (2010) 18: 5063-5070 [PMID:20579890] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2010) 45: 4490-4498 [PMID:20702005] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2016) 117: 292-300 [PMID:27135371] |
| 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 | 4.17 | pIC50 | 67250 | nM | IC50 | Medchemcomm (2016) 7: 1628-1639 |
| ChEMBL | Inhibition of human recombinant MAOA assessed as reduction in H2O2 production from p-tyramine incubated for 15 mins by Amplex red reagent based fluorimetric method | B | 4.17 | pIC50 | 67250 | nM | IC50 | J Nat Prod (2017) 80: 798-804 [PMID:28368606] |
| ChEMBL | Inhibition of recombinant human MAO-A using kynuramine as substrate after 20 mins by fluorescence assay | B | 4.17 | pIC50 | 67250 | nM | IC50 | Eur J Med Chem (2018) 143: 1543-1552 [PMID:29126727] |
| ChEMBL | Inhibition of human MAO-A expressed in baculovirus infected BTI insect cells preincubated for 15 mins | B | 4.2 | pIC50 | 63600 | nM | IC50 | J Med Chem (2014) 57: 10455-10463 [PMID:25418133] |
| 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 | 4.2 | pIC50 | 62663.8 | nM | IC50 | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| 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 | 4.22 | pIC50 | >60000 | nM | IC50 | Eur J Med Chem (2015) 103: 185-190 [PMID:26352677] |
| 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 | 4.26 | pIC50 | 55400 | nM | IC50 | Eur J Med Chem (2016) 121: 864-879 [PMID:26471320] |
| 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 | 4.26 | pIC50 | 54350 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1012-1018 [PMID:30792039] |
| ChEMBL | Inhibition of human recombinant MAOA | B | 4.32 | pIC50 | 47900 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| ChEMBL | Inhibition of human MAO-A expressed in baculovirus infected insect cell membranes using kynuramine as substrate after 15 to 20 mins by discontinuous fluorimetric method | B | 4.52 | pIC50 | >30000 | nM | IC50 | Eur J Med Chem (2018) 148: 487-497 [PMID:29477889] |
| 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 | 4.7 | pIC50 | 20100 | nM | IC50 | Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793] |
| 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 | 4.72 | pIC50 | 19100 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| ChEMBL | DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) | B | 5.53 | pIC50 | 2984 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| 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 | 5.68 | pIC50 | 2089 | nM | IC50 | J Med Chem (2018) 61: 7043-7064 [PMID:30016860] |
| 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 | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem (2016) 24: 4835-4854 [PMID:27396685] |
| 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 | 5.77 | pIC50 | 1700 | nM | IC50 | Eur J Med Chem (2017) 130: 365-378 [PMID:28273563] |
| 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 | 5.82 | pIC50 | 1500 | nM | IC50 | Bioorg Med Chem (2018) 26: 232-244 [PMID:29198609] |
| 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 | 5.85 | pIC50 | 1424 | nM | IC50 | Eur J Med Chem (2019) 162: 793-809 [PMID:30522087] |
| 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 | 5.85 | pIC50 | 1424 | nM | IC50 | Eur J Med Chem (2019) 179: 404-422 [PMID:31265934] |
| ChEMBL | Inhibition of MAOA | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2008) 51: 347-372 [PMID:18181565] |
| 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 | 7.17 | pIC50 | 67.25 | nM | IC50 | Eur J Med Chem (2011) 46: 4846-4852 [PMID:21872365] |
| 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 | 4.42 | pKi | 38000 | nM | Ki | J Med Chem (2003) 46: 917-920 [PMID:12620068] |
| ChEMBL | Inhibition of bovine brain mitochondria MAOA by fluorometric assay | B | 5.42 | pKi | 3800 | nM | Ki | J Med Chem (2007) 50: 922-931 [PMID:17256833] |
| ChEMBL | Inhibition of bovine brain mitochondrial MAO-A by fluorometric assay | B | 5.42 | pKi | 3800 | 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 | 5.42 | pKi | 3800 | nM | Ki | J Med Chem (2012) 55: 10424-10436 [PMID:23153282] |
| ChEMBL | Inhibition of MAO-A in bovine brain mitochondria by fluorimetric method | B | 4.42 | pIC50 | 38018.94 | nM | IC50 | J Med Chem (2007) 50: 425-428 [PMID:17266193] |
| ChEMBL | Inhibition of bovine mitochondrial MAOA | B | 4.42 | pIC50 | 38018.94 | nM | IC50 | Eur J Med Chem (2008) 43: 2262-2267 [PMID:18281126] |
| Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396] | ||||||||
| ChEMBL | Competitive inhibition of MAOA in rat liver homogenate after 60 mins by Lineweaver-Burke plot analysis | B | 3.98 | pKi | 105660 | nM | Kic | Bioorg Med Chem (2010) 18: 1875-1881 [PMID:20149663] |
| ChEMBL | Inhibitory concentration for rat Monoamine oxidase A | B | 4.42 | pKi | 38000 | nM | Ki | J Med Chem (2005) 48: 4220-4223 [PMID:15974574] |
| ChEMBL | Inhibition of MAO-A in rat liver homogenate after 60 mins by Lineweaver-Burke plot | B | 4.8 | pKi | 15700 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Competitive inhibition of rat liver MAO-A after 60 mins using p-tyramine as substrate by spectrophotometry | B | 4.98 | pKi | 10566 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1969-1973 [PMID:21377879] |
| ChEMBL | Inhibition of MAO-A in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| ChEMBL | Competitive inhibition of MAOA in rat liver homogenate by spectrophotometrically | B | 4.04 | pIC50 | 90550 | nM | IC50 | Bioorg Med Chem (2009) 17: 6761-6772 [PMID:19682910] |
| ChEMBL | Inhibition of Monoamine oxidase A of rat liver mitochondrial membranes | B | 5.42 | pIC50 | 3800 | nM | IC50 | J Med Chem (1992) 35: 3705-3713 [PMID:1433183] |
| ChEMBL | Displacement of [3H]-Ro 41-1049 from MAO-A receptor in rat cerebral cortex | B | 5.92 | pIC50 | 1202.26 | nM | IC50 | J Med Chem (2012) 55: 3242-3249 [PMID:22385498] |
| ChEMBL | In vitro inhibitory concentration against Monoamine oxidase A of rat brain homogenates; value ranges from 1.1-1.3 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2002) 45: 5260-5279 [PMID:12431053] |
| 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 | 6.01 | pIC50 | 969 | nM | IC50 | Eur J Med Chem (2019) 162: 793-809 [PMID:30522087] |
| ChEMBL | In vitro inhibitory activity on rat brain by monoamine oxidase A (MAO-A) | B | 6.1 | pIC50 | 800 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Compound was evaluated for the time-dependence inhibition of MAO-A at 60 minutes of preincubated period. values are same with or without pre-incubation | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | In vitro ability to inhibit Monoamine oxidase A activity in rat whole brain in vitro | B | 6.29 | pIC50 | 516 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2715-2717 [PMID:11591508] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2014) 80: 543-561 [PMID:24813882] |
| ChEMBL | Inhibition of MAO-A in rat whole brain homogenate in presence of selegiline | B | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Binding affinity to human recombinant microsomal MAO-B by ITC | B | 7.23 | pKd | 58.9 | nM | Kd | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| ChEMBL | Irreversible inhibition of recombinant human MAOB expressed in Pichia pastoris using varying levels of kynuramine as substrate measured after 5 mins by Michaelis-Menten equation analysis | B | 5.25 | pKi | 5680 | nM | Ki | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| ChEMBL | Competitive inhibition of human recombinant MAO-B after 60 mins using p-tyramine as substrate by spectrophotometry | B | 5.71 | pKi | 1960 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1969-1973 [PMID:21377879] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect cells using p-tyramine as substrate incubated for 30 mins by Amplex red reagent based fluorescence analysis | B | 5.71 | pKi | 1930 | nM | Ki | J Med Chem (2021) 64: 1989-2009 [PMID:33533632] |
| GtoPdb | - | - | 6 | pKi | 970 | nM | Ki |
J Med Chem (2005) 48: 4220-3 [PMID:15974574]; Bioorg Med Chem Lett (2011) 21: 1969-73 [PMID:21377879] |
| ChEMBL | Inhibitory concentration for human Monoamine oxidase B | B | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2005) 48: 4220-4223 [PMID:15974574] |
| ChEMBL | Inhibition constant against human recombinant Monoamine oxidase-B | B | 6.01 | pKi | 970 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4438-4446 [PMID:16137882] |
| ChEMBL | Reversible inhibition of recombinant human MAOB expressed in Pichia pastoris using varying levels of kynuramine as substrate measured after 5 mins by Michaelis-Menten equation analysis | B | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| ChEMBL | Inhibition of recombinant human MAO-B using p-tyramine as substrate assessed as H2O2 production preincubated for 15 mins followed by substrate addition measured for 15 mins by amplex red assay | B | 6.42 | pKi | 380 | nM | Ki | ACS Med Chem Lett (2016) 7: 56-61 [PMID:26819666] |
| ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in H2O2 production preincubated for 30 mins followed by p-tyramine substrate addition measured after 30 mins by amplex red reagent based fluorescence assay | B | 6.59 | pKi | 255 | nM | Ki | Medchemcomm (2018) 9: 1164-1171 [PMID:30109004] |
| ChEMBL | Inhibition of human MAO-B expressed in BTI insect cells using p-tyramine as substrate after 60 mins | B | 7.04 | pKi | 91 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 4296-4300 [PMID:21680183] |
| ChEMBL | Competitive reversible inhibition of human recombinant MAO-B expressed in baculovirus infected BT1 insect cells using p-tyramine as substrate assessed as H2O2 production after 15 mins by fluorimetric analysis | B | 7.05 | pKi | 90 | nM | Ki | Eur J Med Chem (2013) 69: 762-767 [PMID:24099995] |
| ChEMBL | Irreversible inhibition of recombinant human MAO-B expressed in baculovirus infected BT1 cells using benzylamine as substrate at 200 uM preincubated for 30 mins by Lineweaver-Burk plot analysis | B | 7.26 | pKi | 55 | nM | Ki | Eur J Med Chem (2013) 70: 88-101 [PMID:24140951] |
| ChEMBL | Inhibition of recombinant human MAOB using kynuramine as substrate assessed as decrease in formation of 4-hydroxyquinoline incubated for 20 mins by fluorescence assay | B | 8.05 | pKi | 9 | nM | Ki | Medchemcomm (2016) 7: 1628-1639 |
| 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 | 8.41 | pKi | 3.9 | 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 | 8.48 | pKi | 3.3 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| ChEMBL | Inhibition of human MAOB by fluorimetry | B | 4.71 | pIC50 | 19600 | nM | IC50 | Bioorg Med Chem (2010) 18: 5715-5723 [PMID:20615716] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 4.71 | pIC50 | 19600 | nM | IC50 | Eur J Med Chem (2010) 45: 800-804 [PMID:19926363] |
| ChEMBL | Inhibition of human MAOB expressed in BTI insect cells | B | 4.71 | pIC50 | 19600 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5157-5160 [PMID:20659799] |
| ChEMBL | Inhibition of recombinant human MAO-B assessed as production of hydrogen peroxide from p-tyramine after 15 mins by Amplex Red assay | B | 4.83 | pIC50 | 14800 | nM | IC50 | Medchemcomm (2012) 3: 213-218 |
| ChEMBL | Inhibition of MAO-B (unknown origin) using p-tyramine substrate by HPLC method | B | 4.96 | pIC50 | 10960 | nM | IC50 | Bioorg Med Chem (2013) 21: 7890-7897 [PMID:24169316] |
| ChEMBL | Inhibition Assay: A stock solution was prepared using a human MAO-B enzyme (purchased from Aldrich) and a Amplex Red monoamine oxidase assay kit according to a preparation manual. The kit includes a 5x reaction buffer, an Amplex red reagent (1 mg), HRP, DMSO, H2O2, p-tyramine (substrate of MAO-A, B), benzylamine (substrate of MAO-B), clorgiline (inhibitor of MAO-A), and pargyline (inhibitor of MAO-B). Among these reagents in the kit, benzylamine was used as a substrate for MAO-B, and pargyline was used as an MAO-B inhibitor. A solution as overall substrates was prepared as follows. 200 ul of a solution of 1 mg of Amplex red sufficiently dissolved in 200 ul of DMSO, 100 ul of a mixed solution of HRP and 1 ml of a 1x buffer, 200 ul of a solution of benzylamine dissolved in 1.2 ml of dH2O were added to 9.5 ml of a 1x buffer to reach a total volume of 10 mL, which is sufficient for 100 wells. 0.5 ul of a mixture of MAO-B inhibitor pargyline and 1 ml of dH2O was put into each well. First, the activity of MAO-B was determined using 10 uM of the synthesized compound. 96 wells were injected with positive and negative types, and the wile type. The positive type included only substrate and hydrogen peroxide, and the negative type included only substrate. For the wild type, corresponding wells were injected with the enzyme, substrate, and MAO-B inhibitor, but with no synthesized compound. Afterward, 2 ul of the synthesized compound (1 mM) was added into each well, and the human MAO-B enzyme was put only into the 1st row of wells. 0.5 ug of the human MAO-B was put into each well along with 100 ul of a 1x buffer. The human MAO-B enzyme was put into the 2nd row of the wells along with 0.5 ul of a pargyline, the MAO-B inhibitor. To reduce an experimental error for accuracy, the test was repeated three times for each compound. After 30 minutes, 100 ul of the substrate solution was added into each well in a darkroom. The test was performed in the darkroom due to light sensitivity of the Amplex reagent. Finally, a total volume of the reaction solution per well reached 200 ul. After about 2 to 3 hours, chromophoric degrees of the samples were measured. A variation in data values for the 1st and 2nd rows of the wells indicates the pure reaction activity of the MAO-B enzyme with the substrate. Using the samples with the synthesized compound the remaining activity of MAO-B after inhibited by the synthesized compound may be determined. This is because the activities of the other enzymes excluding the MAO-B enzyme may be excluded through this method. Compounds with high inhibitory activity at a concentration of 10 uM were screened from among the synthesized compounds at a compound concentration of 10 uM. Afterward, concentration-dependent IC50 values of these compounds may be obtained through an activity assay at different concentrations of 0.001 uM, 0.01 uM, 0.1 uM, 1 uM, and 10 uM. | B | 5.01 | pIC50 | 9700 | nM | IC50 | US-9469653-B2. Pharmaceutical compositions for preventing or treating degenerative brain disease and method of screening the same (2016) |
| 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 | 5.54 | pIC50 | 2890 | nM | IC50 | Eur J Med Chem (2015) 103: 185-190 [PMID:26352677] |
| ChEMBL | Inhibition of human recombinant MAO-B 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 | 5.55 | pIC50 | 2820 | nM | IC50 | Bioorg Med Chem (2015) 23: 515-525 [PMID:25541201] |
| 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 | 6.32 | pIC50 | 480 | nM | IC50 | US-8633208-B2. 6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands (2014) |
| ChEMBL | Inhibition of human MAOB after 1 hr by luminescence assay | B | 6.48 | pIC50 | 334 | nM | IC50 | J Med Chem (2013) 56: 1247-1261 [PMID:23281824] |
| ChEMBL | Inhibition of recombinant human microsomal MAO-B 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 | 6.49 | pIC50 | 321 | nM | IC50 | Bioorg Med Chem (2016) 24: 1741-1748 [PMID:26964672] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 6.57 | pIC50 | 270 | nM | IC50 | J Med Chem (2015) 58: 6710-6715 [PMID:26278660] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in Sf9 cells using benzylamine as substrate preincubated for 15 mins followed by substrate addition for 60 mins by Luminex assay | B | 6.66 | pIC50 | 221 | nM | IC50 | J Med Chem (2020) 63: 15021-15036 [PMID:33210537] |
| ChEMBL | Inhibition of MAOB (unknown origin) using beetle luciferin as substrate by MAO-Glo assay | B | 7.03 | pIC50 | 94 | nM | IC50 | Eur J Med Chem (2017) 140: 392-402 [PMID:28987602] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells assessed as inhibition of kynuramine oxidation after 30 mins by fluorescence assay | B | 7.07 | pIC50 | 85.2 | nM | IC50 | J Med Chem (2011) 54: 7023-7029 [PMID:21923198] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence spectrophotometric analysis | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem (2018) 26: 5531-5537 [PMID:30279044] |
| ChEMBL | Inhibition of human recombinant monoamine oxidase-B assessed as kynuramine conversion to 6-hydroxyquinoline after 20 mins by fluorescence spectrophotometric analysis | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1269-1273 [PMID:23374869] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate by fluorescence spectroscopy | B | 7.1 | pIC50 | 79 | nM | IC50 | Eur J Med Chem (2017) 135: 196-203 [PMID:28456030] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in insect cell microsomes using kynuramine as substrate after 20 mins by fluorescence spectrophotometric analysis | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 7367-7370 [PMID:23122857] |
| ChEMBL | Inhibition of MAO-B (unknown origin) | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5498-5502 [PMID:24012182] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells microsomes assessed as inhibition of 4-hydroxyquinoline formation using kynuramine as substrate incubated for 20 mins by fluorescence spectrophotometry analysis | B | 7.1 | pIC50 | 79 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126677-126677 [PMID:31537422] |
| ChEMBL | Inhibition of MAO-B (unknown origin) using (4S)-4,5-dihydro-2-(6-hydroxybenzothiazolyl)-4-thiazolecarboxylic acid as substrate by MAO-Glo assay | B | 7.15 | pIC50 | 71 | nM | IC50 | Bioorg Med Chem (2018) 26: 6000-6014 [PMID:30448189] |
| ChEMBL | Inhibition of MAO-B (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2021) 41: 127993-127993 [PMID:33775841] |
| 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 | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1090-1093 [PMID:30833108] |
| ChEMBL | Inhibition of recombinant human MAO-B assessed as inhibition of kynuramine oxidation by spectrophotometry | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem (2013) 21: 186-195 [PMID:23211968] |
| ChEMBL | Inhibition of MAOB | B | 7.32 | pIC50 | 48 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Inhibition of human recombinant MAO-B using kynuramine as substrate preincubated with compound for 15 mins measured after 20 mins by fluorometric analysis | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 4926-4929 [PMID:22781190] |
| ChEMBL | Inhibition of human MAO-B using tyramine hydrochloride as substrate after 30 mins by Amplex Red reagent based horseradish peroxidase enzyme-coupled fluorescence assay | B | 7.36 | pIC50 | 44 | nM | IC50 | Eur J Med Chem (2018) 144: 68-81 [PMID:29248751] |
| ChEMBL | Inhibition of MAO-B (unknown origin) by fluorometric assay | B | 7.37 | pIC50 | 42.84 | nM | IC50 | Eur J Med Chem (2021) 222: 113558-113558 [PMID:34116327] |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate after 15 to 20 mins by discontinuous fluorimetric method | B | 7.38 | pIC50 | 42 | nM | IC50 | Eur J Med Chem (2018) 148: 487-497 [PMID:29477889] |
| 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 | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2017) 131: 92-106 [PMID:28301816] |
| 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 | 7.41 | pIC50 | 38.6 | nM | IC50 | Eur J Med Chem (2020) 185: 111770-111770 [PMID:31711793] |
| ChEMBL | Inhibition of human MAOB using p-tyramine as substrate after 15 mins by Amplex Red MAO assay | B | 7.45 | pIC50 | 35.6 | nM | IC50 | Medchemcomm (2015) 6: 2146-2157 |
| 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 | 7.48 | pIC50 | 33 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1012-1018 [PMID:30792039] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2010) 18: 5063-5070 [PMID:20579890] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2009) 52: 1935-1942 [PMID:19267475] |
| ChEMBL | Inhibition of human recombinant MAO-B assessed as hydrogen peroxide production | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2009) 52: 2818-2824 [PMID:19378991] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2010) 53: 6516-6520 [PMID:20715818] |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2013) 63: 151-161 [PMID:23474901] |
| ChEMBL | Inhibition of recombinant human MAOB using kynuramine as substrate assessed as decrease in formation of 4-hydroxyquinoline incubated for 20 mins by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Medchemcomm (2016) 7: 1628-1639 |
| 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 | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2016) 121: 864-879 [PMID:26471320] |
| ChEMBL | Inhibition of human recombinant MAOB using kynuramine as substrate preincubated for 10 mins followed by substrate addition at 10 secs intervals measured after 20 mins by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Medchemcomm (2018) 9: 357-370 [PMID:30108930] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BT1 cells | B | 7.7 | pIC50 | 19.95 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 6479-6482 [PMID:20934874] |
| ChEMBL | Inhibition of human recombinant MAOB by fluorimetric method | B | 7.71 | pIC50 | 19.6 | nM | IC50 | J Med Chem (2008) 51: 6740-6751 [PMID:18834112] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2013) 59: 91-100 [PMID:23207410] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2010) 45: 4490-4498 [PMID:20702005] |
| 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 | 7.71 | pIC50 | 19.6 | 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem (2014) 22: 2887-2895 [PMID:24746464] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells using p-tyramine substrate assessed as reduction in H2O2 production | B | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 642-648 [PMID:25532905] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2012) 58: 405-417 [PMID:23153812] |
| ChEMBL | Inhibition of human recombinant MAOB | B | 7.71 | pIC50 | 19.6 | nM | IC50 | J Med Chem (2008) 51: 4874-4880 [PMID:18666768] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | J Med Chem (2011) 54: 2155-2164 [PMID:21405131] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence assay | B | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2018) 143: 1543-1552 [PMID:29126727] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in BTI insect cells using p-tyramine substrate by fluorometric method | B | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3268-3270 [PMID:19423346] |
| ChEMBL | Inhibition of human MAO-B using p-tyramine as substrate after 15 mins by amplex red reagent based assay | B | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112] |
| ChEMBL | Inhibition of human recombinant MAO-B using p-tyramine substrate by fluorometric method | B | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4224-4227 [PMID:21684743] |
| ChEMBL | Inhibition of human recombinant MAOB assessed as reduction in H2O2 production from p-tyramine incubated for 15 mins by Amplex red reagent based fluorimetric method | B | 7.71 | pIC50 | 19.6 | nM | IC50 | J Nat Prod (2017) 80: 798-804 [PMID:28368606] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect BT1-TN-5B1-4 cells assessed as production of hydrogen peroxide from p-tyramine up to 15 mins by amplex red-based fluorometric assay | B | 7.71 | pIC50 | 19.6 | nM | IC50 | J Med Chem (2011) 54: 7127-7137 [PMID:21923181] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Eur J Med Chem (2016) 117: 292-300 [PMID:27135371] |
| 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 | 7.71 | pIC50 | 19.6 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5128-5130 [PMID:23927971] |
| 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 | 7.71 | pIC50 | 19.6 | 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 | 7.72 | pIC50 | 19 | nM | IC50 | Eur J Med Chem (2012) 48: 284-295 [PMID:22222137] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in BTI-TN-5B1-4 cells by para-tyramine oxidation assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem (2010) 18: 1273-1279 [PMID:20045650] |
| 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 | 7.73 | pIC50 | 18.5 | nM | IC50 | Bioorg Med Chem (2015) 23: 3722-3729 [PMID:25934229] |
| ChEMBL | Inhibition of human recombinant MAOB assessed as H2O2 production by Amplex Red reagent-based assay | B | 7.73 | pIC50 | 18.5 | nM | IC50 | J Med Chem (2012) 55: 8483-8492 [PMID:22978824] |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected BTI insect cells preincubated for 15 mins | B | 7.74 | pIC50 | 18.2 | 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 | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem (2016) 24: 4835-4854 [PMID:27396685] |
| ChEMBL | Inhibition of human recombinant MAOB using p-tyramine as substrate incubated for 15 mins by fluorimetric method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2016) 121: 376-386 [PMID:27267007] |
| ChEMBL | Inhibition of human MAO-B assessed as inhibition of p-tyramine oxidation to p-hydroxyphenyl-acetaldehyde after 15 mins by fluorimetric method | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2011) 54: 5165-5173 [PMID:21696156] |
| 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 | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2011) 46: 5838-5851 [PMID:22005185] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus-infected BTI insect cells assessed as using transformed p-tyramine after 15 mins by fluorimetric assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 258-261 [PMID:22137786] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN5B1-4 cells using p-tyramine as substrate assessed as reduction in H2O2 production preincubated for 15 mins followed by substrate addition measured after 15 mins by Amplex red dye based fluorescence assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2017) 139: 1-11 [PMID:28797881] |
| 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 | 7.77 | pIC50 | 17 | 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 | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2018) 158: 781-800 [PMID:30245401] |
| 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 by horse-radish peroxidase/amplex red-based fluorescence method | B | 7.77 | pIC50 | 17 | nM | IC50 | Eur J Med Chem (2018) 156: 534-553 [PMID:30025348] |
| ChEMBL | Inhibition of human recombinant MAOB expressed in baculovirus-infected BTI insect cells after 15 mins by fluorimetric assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 707-709 [PMID:21194943] |
| 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 | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2709-2712 [PMID:20382016] |
| 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 | 7.78 | pIC50 | 16.73 | nM | IC50 | J Med Chem (2017) 60: 7206-7212 [PMID:28753307] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in BTI-TN-5B1-4 cells assessed as H2O2 production using para-tyramine substrate by fluorimetric method | B | 7.83 | pIC50 | 14.8 | nM | IC50 | Eur J Med Chem (2011) 46: 1147-1152 [PMID:21316817] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells assessed as kynuramine hydrobromide oxidation after 20 mins by spectrophotometric analysis | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2012) 20: 3065-3071 [PMID:22436387] |
| 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 | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2013) 21: 6634-6641 [PMID:24012376] |
| 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 | 7.92 | pIC50 | 12.1 | nM | IC50 | J Med Chem (2020) 63: 1361-1387 [PMID:31917923] |
| 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 | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem (2018) 26: 232-244 [PMID:29198609] |
| ChEMBL | Inhibition of recombinant human MAO-B using kynuramine as substrate after 20 mins by fluorescence assay | B | 8 | pIC50 | <10 | nM | IC50 | Eur J Med Chem (2019) 163: 83-94 [PMID:30503945] |
| ChEMBL | Inhibition of recombinant human MAOB using benzylamine as substrate after 30 mins by Amplex red based spectrophotometric analysis | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem (2015) 23: 6486-6496 [PMID:26337020] |
| ChEMBL | Inhibition of recombinant human MAO-B assessed as reduction in 4-hydroxyquinolone production using kynuramine as substrate after 20 mins by fluorescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2017) 125: 853-864 [PMID:27744252] |
| ChEMBL | Inhibition of MAOB | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2008) 51: 347-372 [PMID:18181565] |
| 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 | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2018) 61: 7043-7064 [PMID:30016860] |
| 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 | 8.15 | pIC50 | 7 | nM | IC50 | Eur J Med Chem (2017) 130: 365-378 [PMID:28273563] |
| ChEMBL | Irreversible inhibition of human MAOB | B | 8.17 | pIC50 | 6.8 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 3596-3600 [PMID:30404719] |
| ChEMBL | Inhibition of recombinant human MAO-B expressed in baculovirus-infected insect cells using p-tyramine as substrate incubated for 30 mins prior to substrate addition measured for 45 mins by amplex red reagent-based microplate fluorescence reader analysis | B | 8.21 | pIC50 | 6.13 | nM | IC50 | J Med Chem (2013) 56: 4580-4596 [PMID:23631427] |
| ChEMBL | Inhibition of human MAO-B | B | 8.21 | pIC50 | 6.13 | nM | IC50 | Bioorg Med Chem (2013) 21: 7435-7452 [PMID:24139167] |
| 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 | 8.26 | pIC50 | 5.5 | 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 | 8.26 | pIC50 | 5.5 | nM | IC50 | Eur J Med Chem (2019) 179: 404-422 [PMID:31265934] |
| ChEMBL | Inhibition of human MAO-B expressed in baculovirus infected insect cell membranes using kynuramine as substrate preincubated for 30 mins followed by substrate addition measured after 15 to 20 mins by discontinuous fluorimetric method | B | 8.41 | pIC50 | 3.9 | nM | IC50 | Eur J Med Chem (2018) 148: 487-497 [PMID:29477889] |
| ChEMBL | Inhibition of human recombinant MAO-B expressed in insect cells by Amplex Red assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem (2013) 21: 7890-7897 [PMID:24169316] |
| ChEMBL | Inhibition of human recombinant MAO-B using benzylamine hydrochloride as substrate assessed as H2O2 synthesis after 1 hr by fluorescence assay | B | 8.89 | pIC50 | 1.3 | nM | IC50 | Bioorg Med Chem (2013) 21: 5480-5487 [PMID:23810676] |
| ChEMBL | Inhibition of human monoamine oxidase B | B | 10.77 | pIC50 | 0.02 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| 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 | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2003) 46: 917-920 [PMID:12620068] |
| ChEMBL | Inhibition of bovine brain mitochondria MAOB by fluorometric assay | B | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2007) 50: 922-931 [PMID:17256833] |
| ChEMBL | Inhibition of bovine brain mitochondrial MAO-B by fluorometric assay | B | 6.01 | pKi | 970 | 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 | 6.01 | pKi | 970 | nM | Ki | J Med Chem (2012) 55: 10424-10436 [PMID:23153282] |
| ChEMBL | Inhibition of MAO-B in bovine brain mitochondria fluorimetric method | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2007) 50: 425-428 [PMID:17266193] |
| ChEMBL | Inhibition of bovine mitochondrial MAOB | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2008) 43: 2262-2267 [PMID:18281126] |
| 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 | 5.87 | pKi | 1350 | nM | Ki | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Competitive inhibition of MAOB in rat liver homogenate by spectrophotometrically | B | 5.87 | pKi | 1350 | nM | Ki | Bioorg Med Chem (2009) 17: 6761-6772 [PMID:19682910] |
| ChEMBL | Inhibition of MAO-B in rat liver homogenate by spectrophotometry-based Holt method | B | 5.87 | pKi | 1350 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 132-136 [PMID:19945874] |
| ChEMBL | Competitive inhibition of MAOB in rat liver homogenate after 60 mins by Lineweaver-Burke plot analysis | B | 5.87 | pKi | 1350 | nM | Kic | Bioorg Med Chem (2010) 18: 1875-1881 [PMID:20149663] |
| ChEMBL | Competitive inhibition of rat liver MAO-B after 60 mins using p-tyramine as substrate by spectrophotometry | B | 5.87 | pKi | 1350 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1969-1973 [PMID:21377879] |
| ChEMBL | Inhibition of MAO-B in rat liver homogenate after 60 mins by residual activity plot | B | 5.7 | pIC50 | 2010 | nM | IC50 | Bioorg Med Chem (2009) 17: 675-689 [PMID:19091581] |
| ChEMBL | Inhibition of MAOB in rat liver homogenates preincubated for 60 mins | B | 5.7 | pIC50 | 2010 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6362-6368 [PMID:18980841] |
| ChEMBL | Inhibition of rat mitochondrial MAO-B using DAB as substrate incubated for 30 mins by HPLC analysis | B | 5.73 | pIC50 | 1860 | nM | IC50 | J Med Chem (2016) 59: 6169-6186 [PMID:27341519] |
| ChEMBL | Competitive inhibition of MAOB in rat liver homogenate by spectrophotometrically | B | 5.8 | pIC50 | 1600 | nM | IC50 | Bioorg Med Chem (2009) 17: 6761-6772 [PMID:19682910] |
| ChEMBL | Compound was evaluated for the time-dependence inhibition of MAO-B at 0 minute pre-incubation periods | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Inhibition of Monoamine oxidase B of rat liver mitochondrial membranes | B | 7.28 | pIC50 | 52 | nM | IC50 | J Med Chem (1992) 35: 3705-3713 [PMID:1433183] |
| ChEMBL | Inhibition of MAO-B in Sprague-Dawley rat brain homogenate using kynuramine as substrate preincubated for 10 mins measured by fluorimetric assay | B | 7.86 | pIC50 | 13.91 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3343-3348 [PMID:22475561] |
| ChEMBL | Compound was evaluated for the time-dependence inhibition of MAO-B at 20 minutes pre-incubation periods | B | 8 | pIC50 | 9.9 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Compound was evaluated for the time-dependence inhibition of MAO-B at 30 minutes pre-incubation periods | B | 8.03 | pIC50 | 9.4 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | In vitro inhibitory activity on rat brain MAO-B. | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | Displacement of [3H]-Ro 16-6491 from MAO-B receptor in rat cerebral cortex | B | 8.15 | pIC50 | 7.08 | nM | IC50 | J Med Chem (2012) 55: 3242-3249 [PMID:22385498] |
| ChEMBL | Compound was evaluated for the time-dependence inhibition of MAO-B at 60 minutes preincubation periods | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (1993) 36: 1157-1167 [PMID:8487255] |
| ChEMBL | In vitro inhibitory concentration against Monoamine oxidase B of rat brain homogenates; value ranges from 0.004-0.014 | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2002) 45: 5260-5279 [PMID:12431053] |
| ChEMBL | Inhibition of MAO-B in mitochondria-enriched Sprague-Dawley rat liver fractions using p-tyramine as substrate incubated for 30 mins prior to substrate addition measured for 45 mins by amplex red reagent-based microplate fluorescence reader analysis | B | 8.17 | pIC50 | 6.74 | nM | IC50 | J Med Chem (2013) 56: 4580-4596 [PMID:23631427] |
| 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 | 8.17 | pIC50 | 6.7 | nM | IC50 | Eur J Med Chem (2014) 80: 543-561 [PMID:24813882] |
| 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 | 8.21 | pIC50 | 6.11 | nM | IC50 | Eur J Med Chem (2019) 162: 793-809 [PMID:30522087] |
| ChEMBL | In vitro ability to inhibit Monoamine oxidase B activity in rat whole brain in vitro | B | 8.56 | pIC50 | 2.76 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2715-2717 [PMID:11591508] |
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]
