Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | protein phosphatase, Mg2+/Mn2+ dependent, 1D | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Brugia malayi | Protein phosphatase 2C containing protein | Get druggable targets OG5_133255 | All targets in OG5_133255 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_133255 | All targets in OG5_133255 |
Onchocerca volvulus | Protein phosphatase 1D homolog | Get druggable targets OG5_133255 | All targets in OG5_133255 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | Protein phosphatase 1D homolog | 0.026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.026 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 5.3 % | Induction of cell cycle arrest in human MCF7 cells assessed as increase in accumulation at Sub-G1 phase at 40 uM after 1 day by propidium iodide staining-based flow cytometry | ChEMBL. | 22115592 |
Activity (functional) | = 12.9 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 40 uM after 5 days by propidium iodide staining-based flow cytometry (Rvb = 21.2 %) | ChEMBL. | 22115592 |
Activity (functional) | = 15 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S1 phase at 40 uM after 5 days by propidium iodide staining-based flow cytometry (Rvb = 13.8 %) | ChEMBL. | 22115592 |
Activity (functional) | = 16 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S1 phase at 40 uM after 3 days by propidium iodide staining-based flow cytometry (Rvb = 29.3 %) | ChEMBL. | 22115592 |
Activity (functional) | = 16.4 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at Sub-G1 phase at 40 uM after 3 days by propidium iodide staining-based flow cytometry (Rvb = 9.4 %) | ChEMBL. | 22115592 |
Activity (functional) | = 16.8 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 40 uM after 1 day by propidium iodide staining-based flow cytometry (Rvb = 21.4 %) | ChEMBL. | 22115592 |
Activity (functional) | = 25.3 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at Sub-G1 phase at 40 uM after 5 days by propidium iodide staining-based flow cytometry (Rvb = 8.1 %) | ChEMBL. | 22115592 |
Activity (functional) | = 28.2 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G2/M phase at 40 uM after 3 days by propidium iodide staining-based flow cytometry (Rvb = 22.9 %) | ChEMBL. | 22115592 |
Activity (functional) | = 29.8 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at S1 phase at 40 uM after 1 day by propidium iodide staining-based flow cytometry (Rvb = 24 %) | ChEMBL. | 22115592 |
Activity (functional) | = 39 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 40 uM after 1 day by propidium iodide staining-based flow cytometry (Rvb = 45.6 %) | ChEMBL. | 22115592 |
Activity (functional) | = 39.3 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 40 uM after 3 days by propidium iodide staining-based flow cytometry (Rvb = 38.5 %) | ChEMBL. | 22115592 |
Activity (functional) | = 46.8 % | Induction of cell cycle arrest in human MCF7 cells assessed as accumulation at G1 phase at 40 uM after 5 days by propidium iodide staining-based flow cytometry (Rvb = 57 %) | ChEMBL. | 22115592 |
Activity (functional) | > 60 % | Antiproliferative activity against human MCF7 cells overexpressing PPM1D at 40 uM after 1 to 5 days by trypan blue assay | ChEMBL. | 22115592 |
IC50 (binding) | = 86.9 nM | Inhibition of His-tagged PPM1D (1 to 420 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) pLysS cells using Ac-VEPPLS(P)QETFSDLW-NH2 substrate | ChEMBL. | 26358280 |
IC50 (binding) | = 0.48 uM | Inhibition of N-terminal histidine-tagged PPM1Dc after 10 mins using BIOMOL GREEN assay | ChEMBL. | 22115592 |
IC50 (functional) | = 26.9 uM | Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs | ChEMBL. | 26358280 |
Inhibition (binding) | Inhibition of C-terminal truncated PPM1D in human HCT116 cells assessed as increase in Ser15 phosphorylated p53 level at 40 uM after 24 to 48 hrs by western blotting in presence of doxorubicin | ChEMBL. | 25466181 | |
Inhibition (binding) | Inhibition of C-terminal truncated PPM1D in human HCT116 cells assessed as increase in p21 level at 40 uM after 24 to 48 hrs by western blotting in presence of doxorubicin | ChEMBL. | 25466181 | |
Inhibition (binding) | = 68 % | Inhibition of wild-type PPM1A expressed in BL21(DE3)pLysS cells at 40 uM after 10 mins by BIOMOL GREEN assay | ChEMBL. | 22115592 |
Inhibition (binding) | = 97.1 % | Inhibition of N-terminal histidine-tagged PPM1Dc at 4 uM after 10 mins by BIOMOL GREEN assay | ChEMBL. | 22115592 |
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.