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// Workers AI · dad joke modeWhat did SET2 say to SET1? Let's set things straight.

From Wikipedia, the free encyclopedia
SET2
Identifiers
  • N-(furan-2-ylmethyl)-3-({4-[methyl(propyl)amino]-6-(trifluoromethyl)pyrimidin-2-yl}sulfanyl)propanamide
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC17H21F3N4O2S
Molar mass402.44 g·mol−1
3D model (JSmol)
  • O=C(CCSc1nc(cc(n1)N(C)CCC)C(F)(F)F)NCc2ccco2
  • InChI=1S/C17H21F3N4O2S/c1-3-7-24(2)14-10-13(17(18,19)20)22-16(23-14)27-9-6-15(25)21-11-12-5-4-8-26-12/h4-5,8,10H,3,6-7,9,11H2,1-2H3,(H,21,25)
  • Key:LZHSWRWIMQRTOP-UHFFFAOYSA-N

SET2 is a drug which acts as a selective antagonist for the TRPV2 receptor. It is moderately potent with an IC50 of 460nM, but is highly selective for TRPV2 over the other subtypes of TRPV, and is the first such compound to be developed. A role has been suggested for TRPV2 in tumor metastasis, making this a target of interest in the treatment of cancer.[1]

See also

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References

[edit]
  1. Chai H, Cheng X, Zhou B, Zhao L, Lin X, Huang D, Lu W, Lv H, Tang F, Zhang Q, Huang W, Li Y, Yang H (February 2019). "Structure-Based Discovery of a Subtype-Selective Inhibitor Targeting a Transient Receptor Potential Vanilloid Channel". Journal of Medicinal Chemistry. 62 (3): 1373–1384. doi:10.1021/acs.jmedchem.8b01496. PMID 30620187. S2CID 58543255.