Details of the Drug Combination

General Information of Drug Combination (ID: DCKJSSQ)

• Drug Combination Name: 1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole + IT-141
• Indication: Chronic myelogenous leukemia; Status: Investigative [1]
• Component Drugs:
  1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole (DMQEJVU): Small molecular drug
  IT-141 (DMAYD7O): N.A.
• High-throughput Screening Result:
  Testing Cell Line: KBM-7
  Zero Interaction Potency (ZIP) Score: 2.78
  Bliss Independence Score: 2.78
  Loewe Additivity Score: 3.4
  LHighest Single Agent (HSA) Score: 3.41

Molecular Interaction Atlas of This Drug Combination

Indication(s) of 1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole

Disease Entry	ICD 11	Status	REF
Conjunctival fibrosis	9A61.3	Investigative	[2]

1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole Interacts with 2 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
Calcium-activated potassium channel (KCN)	TTMNI76	NOUNIPROTAC	Inhibitor	[4]
Calcium-activated potassium channel KCa3.1 (KCNN4)	TT7M9I6	KCNN4_HUMAN	Blocker (channel blocker)	[5]

1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole Interacts with 2 DOT Molecule(s)

DOT Name	DOT ID	UniProt ID	Mode of Action	REF
Estrogen receptor (ESR1)	OTKLU61J	ESR1_HUMAN	Decreases Expression	[6]
Progesterone receptor (PGR)	OT0FZ3QE	PRGR_HUMAN	Increases Expression	[6]

Indication(s) of IT-141

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[3]

IT-141 Interacts with 1 DTT Molecule(s)

DTT Name	DTT ID	UniProt ID	Mode of Action	REF
DNA topoisomerase I (TOP1)	TTGTQHC	TOP1_HUMAN	Inhibitor	[3]

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] Blockade of KCa3.1: A novel target to treat TGF-1 induced conjunctival fibrosis.Exp Eye Res. 2018 Feb;167:140-144.
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] Inhibitors of potassium channels KV1.3 and IK-1 as immunosuppressants. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2299-304.
• [5] Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis. Circulation. 2003 Sep 2;108(9):1119-25.
• [6] The intermediate conductance Ca2+-activated K+ channel inhibitor TRAM-34 stimulates proliferation of breast cancer cells via activation of oestrogen receptors. Br J Pharmacol. 2010 Feb 1;159(3):650-8. doi: 10.1111/j.1476-5381.2009.00557.x. Epub 2009 Dec 24.