Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | checkpoint kinase 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Schistosoma japonicum | Serine/threonine-protein kinase Chk1, putative | Get druggable targets OG5_130454 | All targets in OG5_130454 |
Schistosoma mansoni | serine/threonine protein kinase | Get druggable targets OG5_130454 | All targets in OG5_130454 |
Brugia malayi | Protein kinase domain containing protein | Get druggable targets OG5_130454 | All targets in OG5_130454 |
Loa Loa (eye worm) | CAMK/CAMKL/CHK1 protein kinase | Get druggable targets OG5_130454 | All targets in OG5_130454 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 3.8 micromol.hr/L | AUC in mouse plasma at 10 mg/kg | ChEMBL. | 17935989 |
AUC (ADMET) | = 3.8 micromol.hr/L | AUC in mouse plasma at 10 mg/kg | ChEMBL. | 17935989 |
EC2 (functional) | = 57.6 uM | Cytotoxicity against HeLa cells by MTS assay | ChEMBL. | 17352464 |
EC2 (functional) | = 57.6 uM | Cytotoxicity against HeLa cells by MTS assay | ChEMBL. | 17352464 |
EC50 (functional) | = 1.3 uM | Inhibition of accumulation of H1299 cells in G2/M phase in presence of doxorubicin by FACS assay | ChEMBL. | 17352464 |
EC50 (functional) | = 1.3 uM | Inhibition of doxorubicin-induced cell cycle arrest in H1299 cells at G2/M phase by FACS assay | ChEMBL. | 17935989 |
EC50 (functional) | = 1.3 uM | Inhibition of accumulation of H1299 cells in G2/M phase in presence of doxorubicin by FACS assay | ChEMBL. | 17352464 |
EC50 (functional) | = 3.08 uM | Cytotoxicity against HeLa cells in presence of doxorubicin by MTS assay | ChEMBL. | 17352464 |
EC50 (functional) | = 3.08 uM | Cytotoxicity against HeLa cells in presence of doxorubicin by MTS assay | ChEMBL. | 17352464 |
EC50 (functional) | > 10 uM | Accumulation of H1299 cells in G2/M phase measured as cell cylce arrest by FACS assay | ChEMBL. | 17352464 |
EC50 (functional) | > 10 uM | Cell cycle arrest in human NCI-H1299 cells assessed as accumulation at G2/M phase by FACS | ChEMBL. | 17931867 |
EC50 (functional) | > 10 uM | Cell cycle arrest in H1299 cells by accumulation at G2/M phase by FACS assay | ChEMBL. | 17935989 |
EC50 (functional) | > 10 uM | Accumulation of H1299 cells in G2/M phase measured as cell cylce arrest by FACS assay | ChEMBL. | 17352464 |
EC50 (functional) | > 10 uM | Cell cycle arrest in human NCI-H1299 cells assessed as accumulation at G2/M phase by FACS | ChEMBL. | 17931867 |
EC50 (functional) | = 57.6 uM | Cytotoxicity against HeLa cells by MTS assay | ChEMBL. | 17935989 |
EC50 (functional) | = 57.6 uM | Cytotoxicity against HeLa cells by MTS assay | ChEMBL. | 17935989 |
EC50 (functional) | > 59.29 uM | Antiproliferative activity against human HeLa cells by MTS assay | ChEMBL. | 17931867 |
EC50 (functional) | > 59.29 uM | Antiproliferative activity against human HeLa cells by MTS assay | ChEMBL. | 17931867 |
IC50 (binding) | = 6 nM | Inhibition of recombinant Chk1 | ChEMBL. | 17352464 |
IC50 (binding) | = 6 nM | Inhibition of Chk1 enzyme by radiometric assay | ChEMBL. | 17931867 |
IC50 (binding) | = 6 nM | Inhibition of Chk1 | ChEMBL. | 17935989 |
IC50 (binding) | = 6 nM | Inhibition of recombinant Chk1 | ChEMBL. | 17352464 |
IC50 (binding) | = 6 nM | Inhibition of Chk1 enzyme by radiometric assay | ChEMBL. | 17931867 |
IC50 (binding) | = 6 nM | Inhibition of Chk1 | ChEMBL. | 17935989 |
Ratio EC50 (functional) | 0 | Ratio of EC50 against HeLa cells in presence of camptothecin over EC50 of camptothecin for HeLa cells | ChEMBL. | 17352464 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 17352464 |
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.
3 literature references were collected for this gene.