Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | diacylglycerol lipase, beta | References | |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | References | |
Homo sapiens | cytochrome P450, family 2, subfamily D, polypeptide 6 | References | |
Homo sapiens | cytochrome P450, family 2, subfamily C, polypeptide 19 | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | cytochrome P450 | cytochrome P450, family 3, subfamily A, polypeptide 4 | 502 aa | 492 aa | 24.2 % |
Leishmania major | cytochrome p450-like protein | cytochrome P450, family 2, subfamily C, polypeptide 19 | 490 aa | 411 aa | 23.1 % |
Brugia malayi | cytochrome P450 | cytochrome P450, family 2, subfamily D, polypeptide 6 | 497 aa | 425 aa | 32.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trichomonas vaginalis | lipase containing protein, putative | 0.0173 | 1 | 0.5 |
Echinococcus granulosus | sn1 specific diacylglycerol lipase beta | 0.0173 | 1 | 0.5 |
Brugia malayi | Cytochrome P450 family protein | 0.0036 | 0.0834 | 0.0834 |
Trypanosoma brucei | lipase domain protein, putative | 0.0173 | 1 | 1 |
Trichomonas vaginalis | lipase containing protein, putative | 0.0173 | 1 | 0.5 |
Echinococcus multilocularis | sn1 specific diacylglycerol lipase beta | 0.0173 | 1 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0173 | 1 | 1 |
Onchocerca volvulus | 0.0173 | 1 | 0.5 | |
Loa Loa (eye worm) | lipase | 0.0173 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0023 | 0 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0036 | 0.0834 | 0.0834 |
Leishmania major | hypothetical protein, conserved | 0.0173 | 1 | 1 |
Trypanosoma brucei | lipase domain protein, putative | 0.0173 | 1 | 1 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.0173 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (ADMET) | Transactivation of human PXR expressed in human HepG2 cells after 15 mins by luciferase reporter gene assay | ChEMBL. | 26917221 | |
IC50 (binding) | = 112 nM | Inhibition of DAGLbeta (unknown origin) | ChEMBL. | 26917221 |
IC50 (ADMET) | = 4 uM | Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate incubated for 7 mins by LC-MS analysis | ChEMBL. | 26917221 |
IC50 (ADMET) | = 6 uM | Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate incubated for 5 mins by LC-MS analysis | ChEMBL. | 26917221 |
IC50 (ADMET) | = 13 uM | Inhibition of CYP2C19 in human liver microsomes using (S)-mephenytoin as substrate incubated for 5 mins by LC-MS analysis | ChEMBL. | 26917221 |
IC50 (ADMET) | = 27 uM | Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate incubated for 10 mins by LC-MS analysis | ChEMBL. | 26917221 |
Inhibition (binding) | Inhibition of porcine pancreatic lipase at 30 uM | ChEMBL. | 26917221 | |
Inhibition (binding) | Inhibition of MAGL (unknown origin) at 30 uM | ChEMBL. | 26917221 | |
Ratio IC50 (binding) | = 4 | Ratio of IC50 for full length human C-terminal HA-tagged DAGLalpha expressed in HEK293 cells assessed as reduction in intracellular 2-AG level to IC50 for full length human C-terminal HA-tagged DAGLalpha expressed in HEK293 cell membrane | ChEMBL. | 26917221 |
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.