Page last updated: 2024-11-13
gsk2830371
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
GSK2830371: inhibits Wip1 phosphatase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 70983932 |
| CHEMBL ID | 3613749 |
| SCHEMBL ID | 13739288 |
| MeSH ID | M0593217 |
Synonyms (28)
| Synonym |
|---|
| bdbm50118478 |
| chembl3613749 , |
| S7573 , |
| HY-15832 |
| gsk 2830371 |
| (s)-5-(((5-chloro-2-methylpyridin-3-yl)amino)methyl)-n-(3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl)thiophene-2-carboxamide |
| AKOS024458513 |
| SCHEMBL13739288 |
| 1404456-53-6 |
| gsk2830371 |
| 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cycloprpylamino)-2-oxoethyl]-2-thiophenecarboxamide |
| gsk-2830371 |
| compound 8 [pmid: 24390428] |
| gtpl11103 |
| 5-[[(5-chloro-2-methylpyridin-3-yl)amino]methyl]-n-[(2s)-3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl]thiophene-2-carboxamide |
| 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]-2-thiophenecarboxamide |
| EX-A2687 |
| AS-16421 |
| BCP27848 |
| CCG-269347 |
| 2-thiophenecarboxamide, 5-[[(5-chloro-2-methyl-3-pyridinyl)amino]methyl]-n-[(1s)-1-(cyclopentylmethyl)-2-(cyclopropylamino)-2-oxoethyl]- |
| (s)-5-{[(5-chloro-2-methylpyridin-3-yl)amino]methyl}-n-[3-cyclopentyl-1-(cyclopropylamino)-1-oxopropan-2-yl]thiophene-2-carboxamide |
| A899200 |
| NCGC00378628-07 |
| (2s)-2-[(5-{[(5-chloro-2-methylpyridin-3-yl)amino]methyl}thiophen-2-yl)formamido]-3-cyclopentyl-n-cyclopropylpropanamide |
| EN300-179507 |
| Z1791350440 |
| AC-36606 |
Research Excerpts
Overview
GSK2830371 is a potent and selective allosteric inhibitor of PPM1D. Its mechanism of binding and inhibition of catalytic activity are unknown.
| Excerpt | Reference | Relevance |
|---|---|---|
| "GSK2830371 is a potent and selective allosteric inhibitor of PPM1D, but its mechanism of binding and inhibition of catalytic activity are unknown." | ( Allosteric inhibition of PPM1D serine/threonine phosphatase via an altered conformational state. Bajrami, B; Brousseau, M; Caliman, A; Campbell, AJ; Ebert, BL; Fischer, ES; Garvie, CW; Giacomelli, AO; Gibson, CJ; Guo, Q; Iqbal, S; Jiang, W; Jin, C; Kahn, J; Lintner, R; Miller, PG; Moroco, JA; Piccioni, F; Qian, Y; Raffier, C; Ranaghan, M; Root, DE; Sathappa, M; Shaw, S; Sperling, AS; Vernier, C; Yang, X, 2022) | 1.44 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (8)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 2.3919 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 8.4866 | 0.0033 | 9.1582 | 39.8107 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 8.4866 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Protein phosphatase 1D | Homo sapiens (human) | IC50 (µMol) | 0.0328 | 0.0060 | 0.0328 | 0.0863 | AID1245781; AID1625400; AID1674043 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (56)
Molecular Functions (23)
Ceullar Components (23)
Bioassays (6)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1674043 | Allosteric inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus infected sf9 cells using FDP as substrate by fluorescence method | 2020 | Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20 | Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application. |
| AID1245781 | 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 | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation. |
| AID1245780 | Inhibition of cell proliferation of human MCF7 cells incubated for 24 hrs | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation. |
| AID1245788 | Inhibition of cell proliferation of human H1299 cells at 5 to 20 incubated for 24 hrs | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation. |
| AID1625400 | Inhibition of human Wip1 (2 to 420 residues) expressed in baculovirus-infected insect SF9 cells assessed as fluorescein diphosphate hydrolysis after 5 mins by fluorescence assay | 2016 | Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14 | Chemical Space of DNA-Encoded Libraries. |
| AID1245787 | Inhibition of cell proliferation of human H1299 cells overexpressing HA-PPM1D at 5 to 20 incubated for 24 hrs | 2015 | Bioorganic & medicinal chemistry, Oct-01, Volume: 23, Issue:19 | Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (16)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 12 (75.00) | 24.3611 |
| 2020's | 4 (25.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 23.36
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (23.36) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (6.25%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 15 (93.75%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||