Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | lysine (K)-specific demethylase 1A | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0083 | 0.8938 | 0.8938 |
Schistosoma mansoni | Lysine-specific histone demethylase 1 | 0.0083 | 0.8938 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0083 | 0.8938 | 0.8938 |
Echinococcus granulosus | lysine specific histone demethylase 1A | 0.0083 | 0.8938 | 0.5 |
Echinococcus multilocularis | lysine specific histone demethylase 1A | 0.0083 | 0.8938 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (ADMET) | Toxicity in BALB/C nude mouse xenografted with human MGC803 cells assessed as body weight loss at 20 mg/kg, iv after 21 days | ChEMBL. | 24131029 | |
IC50 (functional) | = 1.13 uM | Cytotoxicity against human HGC27 cells overexpressing LSD1 by MTT assay | ChEMBL. | 24131029 |
IC50 (binding) | = 2.1 uM | Inhibition of human recombinant LSD1 (157 to 852 aa) expressed in Escherichia coli BL21(DE) using H3K4me2 as substrate by fluorescence assay | ChEMBL. | 24131029 |
IC50 (functional) | = 17.25 uM | Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay | ChEMBL. | 23353743 |
IC50 (binding) | = 36.6 uM | Inhibition of recombinant LSD2 (22 to 822 aa) (unknown origin) expressed in Escherichia coli BL21(DE) by fluorescence assay | ChEMBL. | 24131029 |
IC50 (binding) | > 1250 uM | Inhibition of MAO-B (unknown origin) by fluorescence assay | ChEMBL. | 24131029 |
IC50 (binding) | > 1250 uM | Inhibition of MAO-A (unknown origin) by fluorescence assay | ChEMBL. | 24131029 |
Inhibition (binding) | Inhibition of human recombinant LSD1 (157 to 852 aa) expressed in Escherichia coli BL21(DE) using H3K4me2 as substrate at 0.5 to 12.5 uM after 60 mins | ChEMBL. | 24131029 | |
Inhibition (binding) | Competitive inhibition of human recombinant LSD1 (157 to 852 aa) expressed in Escherichia coli BL21(DE) after 24 hrs by dialysis assay in presence of FAD | ChEMBL. | 24131029 | |
Inhibition (binding) | Inhibition of LSD1 in human MGC803 cells using H3K4 as substrate assessed as H3K4me1 expression level after 48 hrs by Western blotting analysis | ChEMBL. | 24131029 | |
Kd (binding) | = 0.35 uM | Binding affinity to human recombinant LSD1 (157 to 852 aa) expressed in Escherichia coli BL21(DE) by microscale thermophoresis assay | ChEMBL. | 24131029 |
TGI (functional) | = 68.5 % | Antitumor activity against human MGC803 cells xenografted in BALB/C nude mouse assessed as inhibition of tumor growth at 20 mg/kg, iv after 21 days | ChEMBL. | 24131029 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 23353743 |
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.