Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | UDP-glucose ceramide glucosyltransferase | 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 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Leishmania major | cytochrome p450-like protein | 0.0015 | 0 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0015 | 0 | 0.5 |
Schistosoma mansoni | ceramide glucosyltransferase | 0.0288 | 1 | 0.5 |
Echinococcus multilocularis | ceramide glucosyltransferase | 0.0288 | 1 | 0.5 |
Giardia lamblia | Ceramide glucosyltransferase | 0.0131 | 0.4236 | 0.5 |
Echinococcus granulosus | ceramide glucosyltransferase | 0.0288 | 1 | 0.5 |
Schistosoma mansoni | ceramide glucosyltransferase | 0.0288 | 1 | 0.5 |
Loa Loa (eye worm) | ceramide glucosyltransferase | 0.0288 | 1 | 1 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0015 | 0 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.0015 | 0 | 0.5 |
Onchocerca volvulus | Ceramide glucosyltransferase homolog | 0.0288 | 1 | 0.5 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0015 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | Increase in insulin-stimulated AKT phosphorylation in DIO mouse muscle at 10 mg/kg, po qd for 28 days measured after 28 days | ChEMBL. | 22497444 | |
Activity (functional) | Increase in insulin-stimulated AKT phosphorylation in DIO mouse liver at 10 mg/kg, po qd for 28 days measured after 28 days | ChEMBL. | 22497444 | |
Activity (functional) | Increase in insulin-stimulated AKT phosphorylation in DIO mouse WAT at 10 mg/kg, po qd for 28 days measured after 28 days | ChEMBL. | 22497444 | |
Activity (functional) | Antidiabetic activity in DIO mouse assessed as increase in glucose tolerance at 10 mg/kg, po qd measured after 28 days by OGTT | ChEMBL. | 22497444 | |
Activity (functional) | Antidiabetic activity in DIO mouse assessed as increase in glucose tolerance at 10 mg/kg, po qd measured 2 hrs post last dose on day 14 by OGTT | ChEMBL. | 22497444 | |
Activity (functional) | Reduction in glycosphingolipid level in DIO mouse liver at 10 mg/kg, po qd for 28 days measured after 28 days | ChEMBL. | 22497444 | |
Activity (functional) | Reduction in fat accumulation in po dosed DIO mouse ZDF rat administered daily for 4 weeks by Oil Red O staining analysis | ChEMBL. | 22497444 | |
Activity (functional) | Effect on ceramide level C57/B6 mouse liver at 10 mg/kg, po qd for 4 days measured 4 hrs post last dose by HPLC analysis | ChEMBL. | 22497444 | |
Activity (functional) | Reduction in GM3 level in DIO mouse liver at 10 mg/kg, po qd for 28 days measured after 28 days | ChEMBL. | 22497444 | |
Activity (functional) | Reduction in fat accumulation in po dosed DIO mouse ZDF rat administered daily for 4 weeks by Hematoxylin-eosin staining analysis | ChEMBL. | 22497444 | |
Activity (functional) | Antidiabetic activity in DIO mouse assessed as decrease in body weight at 10 mg/kg, po qd for 28 days | ChEMBL. | 22497444 | |
IC50 (binding) | = 2 nM | Inhibition of GCS assessed as amount of UDP glucose after 3 hrs by Fluorometry analysis | ChEMBL. | 22497444 |
IC50 (binding) | = 15 nM | Inhibition of GCS in human A549 cells assessed as decrease in GM1 synthesis after 72 hrs by Fluorescence assay | ChEMBL. | 22497444 |
IC50 (ADMET) | = 2900 nM | Inhibition of human CYP3A4 using testosterone as substrate after 45 mins | ChEMBL. | 22497444 |
Inhibition (functional) | Inhibition of GCS in C57/B6 mouse assessed as decrease in liver GM3 level at 10 mg/kg, po qd for 4 days measured 4 hrs post last dose by HPLC analysis | ChEMBL. | 22497444 | |
Inhibition (functional) | Inhibition of GCS in C57/B6 mouse assessed as decrease in liver lactosylceramide level at 10 mg/kg, po qd for 4 days measured 4 hrs post last dose by HPLC analysis | ChEMBL. | 22497444 | |
Inhibition (functional) | Inhibition of GCS in C57/B6 mouse assessed as decrease in liver glucosylceramide level at 10 mg/kg, po qd for 4 days measured 4 hrs post last dose by HPLC analysis | ChEMBL. | 22497444 |
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.