Details of the Drug Combination

General Information of Drug Combination (ID: DCKDRPS)

Drug Combination Name
PFK-158 Dichlorphenamide
Indication
Disease Entry Status REF
Chronic myelogenous leukemia Investigative [1]
Component Drugs PFK-158   DMIR21F Dichlorphenamide   DMH7IDQ
N.A. Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL
High-throughput Screening Result Testing Cell Line: KBM-7
Zero Interaction Potency (ZIP) Score: 2.01
Bliss Independence Score: 2.01
Loewe Additivity Score: 17.12
LHighest Single Agent (HSA) Score: 17.13

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of PFK-158
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [2]
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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Indication(s) of Dichlorphenamide
Disease Entry ICD 11 Status REF
Chronic glaucoma 9C61.0Z Approved [3]
Dichlorphenamide Interacts with 2 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Carbonic anhydrase I (CA-I) TTHQPL7 CAH1_HUMAN Modulator [5]
Carbonic anhydrase II (CA-II) TTANPDJ CAH2_HUMAN Inhibitor [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 ClinicalTrials.gov (NCT02044861) Phase 1 Safety Study of ACT-PFK-158, 2HCl in Patients With Advanced Solid Malignancies. U.S. National Institutes of Health.
3 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: 6807).
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.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
6 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.