Page last updated: 2024-11-13
gsk2256098
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
GSK2256098: a focal adhesion kinase-1 antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 46214930 |
| CHEMBL ID | 4742157 |
| SCHEMBL ID | 691518 |
| MeSH ID | M000609321 |
Synonyms (39)
| Synonym |
|---|
| S8523 |
| gtpl7939 |
| 2-[(5-chloro-2-{[3-methyl-1-(propan-2-yl)-1h-pyrazol-5-yl]amino}pyridin-4-yl)amino]-n-methoxybenzamide |
| gsk2256098 |
| gsk-2256098 |
| SCHEMBL691518 |
| BVAHPPKGOOJSPU-UHFFFAOYSA-N , |
| 2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino}-4-pyridiny)amino]-n-(methyloxy)benzamide |
| 2-[(5-chloro-2-{[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino}-4-pyridinyl)amino]-n-(methyloxy)benzamide |
| AC-29885 |
| 1224887-10-8 |
| gsk 2256098 |
| CS-6083 |
| HY-100498 |
| EX-A671 |
| AS-74894 |
| 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino]-4-pyridinyl]amino]-n-methoxybenzamide |
| mfcd30502650 |
| 2-((5-chloro-2-((1-isopropyl-3-methyl-1h-pyrazol-5-yl)amino)pyridin-4-yl)amino)-n-methoxybenzamide |
| gsk2256098 [who-dd] |
| 2-((5-chloro-2-((3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl)amino)-4-pyridinyl)amino)-n-methoxybenzamide |
| benzamide, 2-((5-chloro-2-((3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl)amino)-4-pyridinyl)amino)-n-methoxy- |
| R7O0O4110G , |
| gtpl7939;2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-n-methoxybenzamide |
| unii-r7o0o4110g |
| A903443 |
| AKOS030627136 |
| BCP18311 |
| Q27077884 |
| AMY16729 |
| 2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-n-methoxybenzamide |
| benzamide, 2-[[5-chloro-2-[[3-methyl-1-(1-methylethyl)-1h-pyrazol-5-yl]amino]-4-pyridinyl]amino]-n-methoxy- |
| CCG-268826 |
| B0084-470953 |
| 2-(5-chloro-2-(1-isopropyl-3-methyl-1h-pyrazol-5-ylamino)pyridin-4-ylamino)-n-methoxybenzamide |
| nsc-800999 |
| nsc800999 |
| CHEMBL4742157 , |
| bdbm50568532 |
Research Excerpts
Overview
GSK2256098 is a novel oral focal adhesion kinase (FAK) inhibitor.
| Excerpt | Reference | Relevance |
|---|---|---|
| "GSK2256098 is a novel oral focal adhesion kinase (FAK) inhibitor. " | ( A study of the focal adhesion kinase inhibitor GSK2256098 in patients with recurrent glioblastoma with evaluation of tumor penetration of [11C]GSK2256098. Arkenau, HT; Auger, KR; Blagden, S; Brown, NF; Cox, D; Fleming, RA; Lenox, L; Lewis, Y; Mulholland, P; Plisson, C; Saleem, A; Searle, G; Singh, R; Tolson, J; Williams, M; Yan, L; Zhang, J, 2018) | 2.18 |
Effects
| Excerpt | Reference | Relevance |
|---|---|---|
| "GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD, and has clinical activity in patients with mesothelioma, particularly those with merlin loss." | ( A phase I, pharmacokinetic and pharmacodynamic study of GSK2256098, a focal adhesion kinase inhibitor, in patients with advanced solid tumors. Arkenau, HT; Auger, KR; Bahleda, R; Blagden, SP; Brown, J; Dean, E; Evans, TR; Fleming, RA; Gan, HK; Gibson, D; Hollebecque, A; Lemech, C; Mazumdar, J; Millward, M; Murray, S; Nebot, N; Peddareddigari, V; Plummer, R; Ranson, M; Singh, R; Soria, JC; Swartz, L; Zalcman, G, 2016) | 2.12 |
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Treatment with GSK2256098 resulted in greater inhibition of pFAK(Y397) in PTEN-mutated (Ishikawa) than in PTEN-wild-type (Hec1A) cells." | ( PTEN Expression as a Predictor of Response to Focal Adhesion Kinase Inhibition in Uterine Cancer. Ali-Fehmi, R; Armaiz-Pena, GN; Coleman, RL; Dalton, HJ; Dorniak, PL; Hansen, JM; Hu, W; Huang, J; Ivan, C; Previs, RA; Rupaimoole, R; Sood, AK; Thanapprapasr, D, 2015) | 0.76 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "Thirteen patients were treated in 3 dose cohorts (1000 mg, 750 mg, 500 mg; all dosed twice daily)." | ( A study of the focal adhesion kinase inhibitor GSK2256098 in patients with recurrent glioblastoma with evaluation of tumor penetration of [11C]GSK2256098. Arkenau, HT; Auger, KR; Blagden, S; Brown, NF; Cox, D; Fleming, RA; Lenox, L; Lewis, Y; Mulholland, P; Plisson, C; Saleem, A; Searle, G; Singh, R; Tolson, J; Williams, M; Yan, L; Zhang, J, 2018) | 0.74 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (3)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 20.8212 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 20.8212 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [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) |
|---|---|---|---|---|---|---|---|
| Focal adhesion kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0090 | 0.0002 | 0.5416 | 8.3000 | AID1755623; AID1755624; AID1755625; AID1755626 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (77)
Molecular Functions (16)
Ceullar Components (15)
Bioassays (14)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1755625 | Inhibition of FAK in human OVCAR8 cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK). |
| AID1755623 | Inhibition of FAK in human U87MG cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK). |
| AID1755626 | Inhibition of FAK (unknown origin) | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK). |
| AID1675117 | Selectivity ratio of inhibition of Pyk2 (unknown origin) to inhibition of tracer 236 binding to recombinant human GST-tagged full length FAK expressed in baculovirus expression system incubated for 1 hr by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675123 | Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1755624 | Inhibition of FAK in human A549 cells assessed as reduction in phosphorylation at Y397 residue incubated for 30 mins by Western blot analysis | 2020 | Journal of medicinal chemistry, 12-10, Volume: 63, Issue:23 | Progress in the Development of Small Molecular Inhibitors of Focal Adhesion Kinase (FAK). |
| AID1675126 | Inhibition of FAK (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675121 | Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675124 | Inhibition of tracer 236 binding to recombinant human GST-tagged full length FAK expressed in baculovirus expression system incubated for 1 hr by Lanthascreen TR-FRET assay | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675119 | Antiproliferative activity against human 786-O cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675118 | Inhibition of FAK autophosphorylation assessed as decrease in ratio of Phospho-Tyr397-FAK to total FAK in human MDA-MB-231 cells ast 0.1 uM incubated for 1 hr by ELISA | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675120 | Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1675122 | Antiproliferative activity against human BXPC-3 cells assessed as reduction in cell viability | 2020 | Bioorganic & medicinal chemistry letters, 11-01, Volume: 30, Issue:21 | Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (11)
| 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 | 6 (54.55) | 24.3611 |
| 2020's | 5 (45.45) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 29.43
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 (29.43) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 4 (36.36%) | 5.53% |
| Reviews | 2 (18.18%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (45.45%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||