Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | lysine (K)-specific demethylase 1A | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.009 | 0.4923 | 0.5 | |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.0165 | 1 | 1 |
Mycobacterium ulcerans | protoporphyrinogen oxidase | 0.0017 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0083 | 0.4451 | 0.4451 |
Brugia malayi | amine oxidase, flavin-containing family protein | 0.0024 | 0.0473 | 0.0473 |
Mycobacterium ulcerans | monoamine oxidase | 0.0017 | 0 | 0.5 |
Plasmodium falciparum | conserved Plasmodium protein, unknown function | 0.0017 | 0 | 0.5 |
Plasmodium vivax | lysine-specific histone demethylase 1, putative | 0.0017 | 0 | 0.5 |
Mycobacterium tuberculosis | Conserved hypothetical protein | 0.0017 | 0 | 0.5 |
Echinococcus multilocularis | lysine specific histone demethylase 1A | 0.0083 | 0.4451 | 0.4451 |
Chlamydia trachomatis | protoporphyrinogen oxidase | 0.0017 | 0 | 0.5 |
Brugia malayi | SWIRM domain containing protein | 0.009 | 0.4923 | 0.4923 |
Mycobacterium leprae | PROBABLE PROTOPORPHYRINOGEN OXIDASE HEMY (PROTOPORPHYRINOGEN-IX OXIDASE) (PROTOPORPHYRINOGENASE) (PPO) | 0.0017 | 0 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase | 0.0165 | 1 | 1 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.0165 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0083 | 0.4451 | 0.4451 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0165 | 1 | 1 |
Mycobacterium ulcerans | flavin-containing monoamine oxidase AofH | 0.0017 | 0 | 0.5 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.0165 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.009 | 0.4923 | 0.4923 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 0.0165 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0024 | 0.0473 | 0.0473 |
Plasmodium vivax | hypothetical protein, conserved | 0.0017 | 0 | 0.5 |
Mycobacterium ulcerans | flavin-containing monoamine oxidase AofH | 0.0017 | 0 | 0.5 |
Mycobacterium ulcerans | oxidoreductase | 0.0017 | 0 | 0.5 |
Plasmodium vivax | hypothetical protein, conserved | 0.0017 | 0 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.0165 | 1 | 1 |
Schistosoma mansoni | Lysine-specific histone demethylase 1 | 0.0083 | 0.4451 | 0.4451 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0165 | 1 | 1 |
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.0165 | 1 | 1 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.0165 | 1 | 1 |
Echinococcus granulosus | lysine specific histone demethylase 1A | 0.0083 | 0.4451 | 0.4451 |
Toxoplasma gondii | CMGC kinase, MAPK family (ERK) MAPK-1 | 0.0165 | 1 | 1 |
Trypanosoma brucei | protein kinase, putative | 0.0165 | 1 | 0.5 |
Plasmodium falciparum | protoporphyrinogen oxidase | 0.0017 | 0 | 0.5 |
Mycobacterium tuberculosis | Possible oxidoreductase | 0.0017 | 0 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0165 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0165 | 1 | 0.5 |
Giardia lamblia | Kinase, CMGC MAPK | 0.0165 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0165 | 1 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0165 | 1 | 0.5 |
Plasmodium falciparum | lysine-specific histone demethylase 1, putative | 0.0017 | 0 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase | 0.0165 | 1 | 1 |
Plasmodium vivax | protoporphyrinogen oxidase, putative | 0.0017 | 0 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0165 | 1 | 1 |
Mycobacterium ulcerans | dehydrogenase | 0.0017 | 0 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.0165 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 291 nM | BindingDB_Patents: Inhibitor Screening Assay. The primary assay for compound inhibitory activity was the LSD1 Inhibitor Screening Assay Kit (Cayman Chemical Company, Ann Arbor, Mich.; Cayman Chemical Item Number 700120). Briefly, test compounds were diluted to 20.times. the desired test concentration in 100% DMSO and 2.5 .mu.L of the diluted drug sample was added to a black 384-well plate. The LSD1 enzyme stock was diluted 17-fold with assay buffer and 40 .mu.M of the diluted LSD1 enzyme was added to the appropriate wells. The reaction mixture comprised horseradish peroxidase, dimethyl K4 peptide (corresponding to the first 21 amino acids of the N-terminal tail of histone H3), and 10-acetyl-3,7-dihydroxyphenoxazine was then added to wells. Generation of resorufin (generated by reacting with H.sub.2O.sub.2 produced in the reaction) was analyzed on an Envision microplate reader with an excitation wavelength of 530 nm and an emission wavelength of 595 nm. | ChEMBL. | No reference |
IC50 (binding) | = 291 nM | BindingDB_Patents: Inhibitor Screening Assay. The primary assay for compound inhibitory activity was the LSD1 Inhibitor Screening Assay Kit (Cayman Chemical Company, Ann Arbor, Mich.; Cayman Chemical Item Number 700120). Briefly, test compounds were diluted to 20.times. the desired test concentration in 100% DMSO and 2.5 .mu.L of the diluted drug sample was added to a black 384-well plate. The LSD1 enzyme stock was diluted 17-fold with assay buffer and 40 .mu.M of the diluted LSD1 enzyme was added to the appropriate wells. The reaction mixture comprised horseradish peroxidase, dimethyl K4 peptide (corresponding to the first 21 amino acids of the N-terminal tail of histone H3), and 10-acetyl-3,7-dihydroxyphenoxazine was then added to wells. Generation of resorufin (generated by reacting with H.sub.2O.sub.2 produced in the reaction) was analyzed on an Envision microplate reader with an excitation wavelength of 530 nm and an emission wavelength of 595 nm. | ChEMBL. | No reference |
IC50 (binding) | = 0.291 uM | Inhibition of LSD1 (unknown origin) using dimethyl K4 peptide as substrate assessed as resorufin level by spectrophotometric analysis | ChEMBL. | 24237195 |
IC50 (functional) | = 0.971 uM | Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay | ChEMBL. | 24237195 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 24237195 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.