Details of the Drug Combination

General Information of Drug Combination (ID: DCDC56N)

Drug Combination Name
BGT226 BIX-01294
Indication
Disease Entry Status REF
DD2 Investigative [1]
Component Drugs BGT226   DMXKDUL BIX-01294   DM5CBNY
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL is unavailable
High-throughput Screening Result Testing Cell Line: DD2
Zero Interaction Potency (ZIP) Score: 6.925
Bliss Independence Score: 8.298
Loewe Additivity Score: 0.814
LHighest Single Agent (HSA) Score: 4.388

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of BGT226
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
BGT226 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Serine/threonine-protein kinase mTOR (mTOR) TTCJG29 MTOR_HUMAN Modulator [4]
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Modulator [4]
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Indication(s) of BIX-01294
Disease Entry ICD 11 Status REF
Breast cancer 2C60-2C65 Preclinical [3]
BIX-01294 Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Euchromatic histone-lysine N-methyltransferase 1 (EHMT1) TTOFXD7 EHMT1_HUMAN Inhibitor [5]
Histone-lysine N-methyltransferase EHMT2 (EHMT2) TTS6RZT EHMT2_HUMAN Inhibitor [5]
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BIX-01294 Interacts with 2 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Interferon alpha-2 (IFNA2) OT4GII73 IFNA2_HUMAN Increases Response To Substance [6]
Interferon regulatory factor 7 (IRF7) OTC1A2PQ IRF7_HUMAN Increases Expression [6]
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References

1 Recurrent recessive mutation in deoxyguanosine kinase causes idiopathic noncirrhotic portal hypertension.Hepatology. 2016 Jun;63(6):1977-86. doi: 10.1002/hep.28499. Epub 2016 Mar 31.
2 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7951).
3 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286.
4 Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs. 2012 Jan;23(1):131-8.
5 Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25(3):473-81.
6 Inhibition of euchromatic histone methyltransferase 1 and 2 sensitizes chronic myeloid leukemia cells to interferon treatment. PLoS One. 2014 Jul 31;9(7):e103915. doi: 10.1371/journal.pone.0103915. eCollection 2014.