ART5537

ART5537 : Inhibitor of EXO1

Structure

Information

  • EXO1
  • Inhibitor
  • 1µM

In Vitro Validations

Uniprot ID: Q9UQ84
Target Class: Enzyme
Target SubClass: Endonuclease
Potency: IC50
Potency Value: 3.4 nM
Potency Assay: Biochemical assay
PDB ID for probe-target interaction (3D structure): 9SMO
Target aliases:
Exonuclease 1, HEX1, EXOI, EXO1, EXO1_HUMAN, hExoI ...

DOI Reference: 10.1021/acs.jmedchem.5c02593

Uniprot ID: Q9UQ84
Target Class: Enzyme
Target SubClass: Endonuclease
Potency: Kd
Potency Value: 6.8 nM
Potency Assay: SPR
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Exonuclease 1, HEX1, EXOI, EXO1, EXO1_HUMAN, hExoI ...

DOI Reference: 10.1021/acs.jmedchem.5c02593

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): ART5537 was found not to be broadly cytotoxic in a panel of 93 cancer cell lines, or in two additional noncancer lines.
Potency assay (off target): The broader nuclease selectivity profile of ART5537 is also supportive of EXO1-driven phenotypes, with ≥200-fold selectivity over a panel of the wider nuclease superfamily.
I have extra information to add

SERP ratings and comments


SERP Ratings

In Cell Rating

SERP Comments:

ART5537 is a promising and highly selective chemical probe for EXO1, demonstrating excellent performance in biochemical and cellular assays. However, its current pharmacokinetic limitations (high clearance, short half-life, low bioavailability) restrict its use as an in vivo tool.

(last updated: 1 Jan 2026 )