Details of the Drug Combination

General Information of Drug Combination (ID: DCF6B76)

Drug Combination Name
GSK2194069 PFK-158
Indication
Disease Entry Status REF
Chronic myelogenous leukemia Investigative [1]
Component Drugs GSK2194069   DMZ2TD9 PFK-158   DMIR21F
Small molecular drug N.A.
2D MOL 2D MOL
3D MOL is unavailable 3D MOL
High-throughput Screening Result Testing Cell Line: KBM-7
Zero Interaction Potency (ZIP) Score: 32.02
Bliss Independence Score: 32.02
Loewe Additivity Score: 46.04
LHighest Single Agent (HSA) Score: 46.05

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of GSK2194069
Disease Entry ICD 11 Status REF
Discovery agent N.A. Investigative [2]
GSK2194069 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Fatty acid synthase (FASN) TT7AOUD FAS_HUMAN Inhibitor [2]
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Indication(s) of PFK-158
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [3]
PFK-158 Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Renal carcinoma antigen NY-REN-56 (PFKFB3) TTTHMQJ F263_HUMAN Inhibitor [4]
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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 A human fatty acid synthase inhibitor binds beta-ketoacyl reductase in the keto-substrate site. Nat Chem Biol. 2014 Sep;10(9):774-9.
3 ClinicalTrials.gov (NCT02044861) Phase 1 Safety Study of ACT-PFK-158, 2HCl in Patients With Advanced Solid Malignancies. U.S. National Institutes of Health.
4 Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.