General Information of the Drug (ID: M6APDG00728)
Name
KO-947
Synonyms
ODIUJYZERXVGEI-UHFFFAOYSA-N; KO947; 1695533-89-1; GTPL9976; SCHEMBL16619993; EX-A1980; BCP25116; HY-112181; CS-0043627; 6-benzyl-3-pyridin-4-yl-2,5-dihydro-1H-pyrazolo[4,3-g]quinazolin-7-one; 6-benzyl-3-(pyridin-4-yl)-1,5,6,8-tetrahydro-7H-pyrazolo[4,3-g]quinazolin-7-one; KO947,1695533-89-1,1,5,6,8-Tetrahydro-6-(phenylmethyl)-3-(4-pyridinyl)-7H-pyrazolo[4,3-g]quinazolin-7-one,KO947,KO-947,KO 947
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Status
Phase 1
Structure
Formula
C21H17N5O
InChI
1S/C21H17N5O/c27-21-23-18-11-19-17(20(25-24-19)15-6-8-22-9-7-15)10-16(18)13-26(21)12-14-4-2-1-3-5-14/h1-11H,12-13H2,(H,23,27)(H,24,25)
InChIKey
ODIUJYZERXVGEI-UHFFFAOYSA-N
PubChem CID
136653617
TTD Drug ID
D0A1DG
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.
Ephrin type-B receptor 2 (EPHB2)
Fat mass and obesity-associated protein (FTO)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The Fat mass and obesity-associated protein (FTO) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [1], [2]
Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The Heterogeneous nuclear ribonucleoproteins A2/B1 (HNRNPA2B1) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [2], [3]
Methyltransferase-like 14 (METTL14)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The Methyltransferase-like 14 (METTL14) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [2], [4]
Methyltransferase-like 3 (METTL3)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The Methyltransferase-like 3 (METTL3) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [2], [4]
RNA demethylase ALKBH5 (ALKBH5)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The RNA demethylase ALKBH5 (ALKBH5) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [2], [5]
YTH domain-containing family protein 1 (YTHDF1)
In total 1 mechanisms lead to this potential drug response
Response Summary Ephrin type-B receptor 2 (EPHB2) is a therapeutic target for KO-947. The YTH domain-containing family protein 1 (YTHDF1) has potential in affecting the response of KO-947 through regulating the expression of Ephrin type-B receptor 2 (EPHB2). [2], [4]
References
Ref 1 Mutant NPM1-Regulated FTO-Mediated m(6)A Demethylation Promotes Leukemic Cell Survival via PDGFRB/ERK Signaling Axis. Front Oncol. 2022 Feb 8;12:817584. doi: 10.3389/fonc.2022.817584. eCollection 2022.
Ref 2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 3 hnRNPA2B1 Promotes Colon Cancer Progression via the MAPK Pathway. Front Genet. 2021 Sep 22;12:666451. doi: 10.3389/fgene.2021.666451. eCollection 2021.
Ref 4 Dynamic m(6)A mRNA Methylation Reveals the Role of METTL3/14-m(6)A-MNK2-ERK Signaling Axis in Skeletal Muscle Differentiation and Regeneration. Front Cell Dev Biol. 2021 Oct 1;9:744171. doi: 10.3389/fcell.2021.744171. eCollection 2021.
Ref 5 Post-translational modification of RNA m6A demethylase ALKBH5 regulates ROS-induced DNA damage response. Nucleic Acids Res. 2021 Jun 4;49(10):5779-5797. doi: 10.1093/nar/gkab415.