Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cytochrome P450, family 2, subfamily C, polypeptide 9 | Starlite/ChEMBL | References |
Homo sapiens | polo-like kinase 4 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 2, subfamily C, polypeptide 19 | Starlite/ChEMBL | References |
Homo sapiens | cytochrome P450, family 3, subfamily A, polypeptide 4 | Starlite/ChEMBL | 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 % |
Mycobacterium tuberculosis | Probable cytochrome P450 136 Cyp136 | cytochrome P450, family 2, subfamily C, polypeptide 9 | 490 aa | 441 aa | 21.8 % |
Leishmania major | cytochrome p450-like protein | cytochrome P450, family 2, subfamily C, polypeptide 19 | 490 aa | 411 aa | 23.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | Serine:threonine protein kinase PLK4 | 0.0135 | 0.5473 | 1 |
Echinococcus multilocularis | serine:threonine protein kinase PLK1 | 0.0058 | 0.17 | 0.2286 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0058 | 0.17 | 0.1448 |
Echinococcus granulosus | serine:threonine protein kinase PLK1 | 0.0058 | 0.17 | 0.2286 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Trypanosoma cruzi | polo-like protein kinase, putative | 0.0058 | 0.17 | 1 |
Onchocerca volvulus | Serine\/threonine kinase homolog | 0.0058 | 0.17 | 0.5 |
Brugia malayi | hypothetical protein | 0.0035 | 0.0581 | 0.0581 |
Loa Loa (eye worm) | PLK/PLK1 protein kinase | 0.0058 | 0.17 | 0.17 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0059 | 0.1746 | 0.1746 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Leishmania major | protein kinase, putative,polo-like protein kinase, putative | 0.0058 | 0.17 | 1 |
Giardia lamblia | Kinase, PLK | 0.0058 | 0.17 | 0.5 |
Schistosoma mansoni | kinase | 0.0192 | 0.8306 | 1 |
Loa Loa (eye worm) | follicle stimulating hormone receptor | 0.0227 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0023 | 0 | 0.5 |
Trypanosoma brucei | polo-like protein kinase | 0.0058 | 0.17 | 1 |
Trypanosoma cruzi | polo-like protein kinase, putative | 0.0058 | 0.17 | 1 |
Entamoeba histolytica | serine/threonine protein kinase, putative | 0.0058 | 0.17 | 1 |
Trichomonas vaginalis | CAMK family protein kinase | 0.0058 | 0.17 | 0.5 |
Brugia malayi | serine/threonine-protein kinase plk-2 | 0.0058 | 0.17 | 0.17 |
Brugia malayi | Cytochrome P450 family protein | 0.0059 | 0.1746 | 0.1746 |
Echinococcus granulosus | Serine:threonine protein kinase PLK4 | 0.0135 | 0.5473 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
GI50 (functional) | = 0.013 uM | Growth inhibition of human MDA-MB-468 cells after 5 days by SRB assay | ChEMBL. | 25723005 |
GI50 (functional) | = 0.08 uM | Cytotoxicity against human MCF7 cells after 5 days by SRB assay | ChEMBL. | 24867403 |
IC50 (binding) | = 3.1 nM | Inhibition of PLK4 (unknown origin) by ELISA | ChEMBL. | 25723005 |
IC50 (binding) | = 7.2 nM | Inhibition of human N-terminal GST-tagged PLK4 (1 to 391 residues) expressed in Escherichia coli incubated for 30 mins by ELISA method | ChEMBL. | 24867403 |
IC50 (ADMET) | = 1 uM | Inhibition of CYP2C9 (unknown origin) by fluorescence assay | ChEMBL. | 25723005 |
IC50 (ADMET) | = 1.2 uM | Inhibition of CYP2C19 (unknown origin) by fluorescence assay | ChEMBL. | 25723005 |
IC50 (ADMET) | = 3 uM | Inhibition of CYP3A4 (unknown origin) using BFC as substrate by fluorescence assay | ChEMBL. | 25723005 |
IC50 (ADMET) | = 6.2 uM | Inhibition of CYP3A4 (unknown origin) using DBF as substrate by fluorescence assay | ChEMBL. | 25723005 |
Inhibition (ADMET) | Inhibition of CYP1A2 (unknown origin) by fluorescence assay | ChEMBL. | 25723005 | |
Inhibition (ADMET) | Inhibition of CYP2D6 (unknown origin) by fluorescence assay | ChEMBL. | 25723005 | |
T1/2 (ADMET) | = 13 min | Half life in mouse liver microsomes | ChEMBL. | 25723005 |
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.
2 literature references were collected for this gene.