Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | pyruvate dehydrogenase kinase, isozyme 2 | References | |
Homo sapiens | pyruvate dehydrogenase kinase, isozyme 4 | References | |
Homo sapiens | pyruvate dehydrogenase kinase, isozyme 1 | References | |
Homo sapiens | pyruvate dehydrogenase kinase, isozyme 3 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | pyruvate dehydrogenase (lipoamide) kinase, putative | pyruvate dehydrogenase kinase, isozyme 4 | 411 aa | 354 aa | 24.3 % |
Trypanosoma brucei | pyruvate dehydrogenase (lipoamide) kinase, putative | pyruvate dehydrogenase kinase, isozyme 3 | 415 aa | 360 aa | 23.1 % |
Leishmania major | pyruvate dehydrogenase (lipoamide) kinase, putative | pyruvate dehydrogenase kinase, isozyme 1 | 456 aa | 397 aa | 22.7 % |
Trypanosoma brucei | pyruvate dehydrogenase (lipoamide) kinase, putative | pyruvate dehydrogenase kinase, isozyme 2 | 343 aa | 321 aa | 22.7 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | uM | In vitro effective concentration in normal human dermal fibroblasts; Inactive | ChEMBL. | 10465550 |
EC50 (functional) | 0 uM | In vitro effective concentration in normal human dermal fibroblasts; Inactive | ChEMBL. | 10465550 |
Efficacy (functional) | = -2 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 4 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = -2 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 4 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 4 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 2 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 4 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 2 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 9 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 4 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 9 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 4 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 13 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 2 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 13 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 2 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 16 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 6 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 16 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 6 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 16 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day1 after 6 hr | ChEMBL. | 10465550 |
Efficacy (functional) | = 16 % | In vivo activity of the compound in a diabetic mouse at a dose of 200 umol/kg/day on day 3 after 6 hr | ChEMBL. | 10465550 |
IC50 (binding) | = 6.7 uM | In vitro inhibitory activity against pyruvate dehydrogenase kinase was determined | ChEMBL. | 10465550 |
IC50 (binding) | = 6.7 uM | In vitro inhibitory activity against pyruvate dehydrogenase kinase was determined | ChEMBL. | 10465550 |
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.