ART5537

ART5537 : Inhibitor of EXO1

Structure

SERP Rating

Probe ART5537 is in the process of SERP review.

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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.

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