General Information of the Drug (ID: M6APDG00823)
Name
GSK461364
Synonyms
GSK461364; 929095-18-1; GSK-461364; 5-[6-[(4-Methyl-1-piperazinyl)methyl]-1h-benzimidazol-1-yl]-3-[(1r)-1-[2-(trifluoromethyl)phenyl]ethoxy]-2-thiophenecarboxamide; GSK 461364; UNII-8QO27TK6Q4; GSK-461364A; (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide; 8QO27TK6Q4; CHEMBL1908394; GSK461364A; ZHJGWYRLJUCMRT-QGZVFWFLSA-N; SCHEMBL310080; GTPL5684; C27H28F3N5O2S; CTK8B7590; CHEBI:91333; DTXSID60239197; MolPort-016-633-304; BCP01720; GSK 461364A
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Status
Phase 1
Structure
Formula
C27H28F3N5O2S
InChI
1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1
InChIKey
ZHJGWYRLJUCMRT-QGZVFWFLSA-N
PubChem CID
15983966
TTD Drug ID
D08RMJ
Target Gene(s) and Their Upstream m6A Regulator, Together with the Effect of Target Gene(s) in Drug Response
The target genes involved in drug-target interaction (such as drug-metabolizing enzymes, drug transporters and therapeutic targets) and drug-mediated cell death signaling (including modulating DNA damage and repair capacity, escaping from drug-induced apoptosis, autophagy, cellular metabolic reprogramming, oncogenic bypass signaling, cell microenvironment, cell stemness, etc.) could be regulated by m6A regulator(s) and affected their corresponding drug response. You can browse detailed information on drug-related target gene(s) mediated by m6A regulators.
Polo-like kinase 1 (PLK1)
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Polo-like kinase 1 (PLK1) is a therapeutic target for GSK461364. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of GSK461364 through regulating the expression of Polo-like kinase 1 (PLK1). [1], [2]
References
Ref 1 METTL3-mediated m(6)A modification regulates cell cycle progression of dental pulp stem cells. Stem Cell Res Ther. 2021 Mar 1;12(1):159. doi: 10.1186/s13287-021-02223-x.
Ref 2 TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9. doi: 10.1158/1535-7163.MCT-11-0762. Epub 2011 Dec 21.