A highly potent, selective mutant p53 (R175H, R249S, R273H, R273C) reactivator.

A novel small molecule that overcomes HdmX-mediated p53 repression, binds directly to HdmX (Kd=450 nM) to prevent p53-HdmX complex formation.

CB-002 is a novel small molecule that restores p53 function in mutant p53-expressing colorectal cancer cells without toxicity to normal human fibroblasts; increases expression of endogenous p53 target genes NOXA, DR5, and p21 and cell death; decreases the stability of mutant p53 in RXF393 cancer cells and an exogenously expressed R175H p53 mutant in HCT116 p53-null cells.

A potent and orally active p53-MDM2 interaction inhibitor with IC50 of 2.4 nM.

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.1 nM), cellular potency (SJSA-1 EdU IC50=16 nM), and favorable pharmacokinetic properties.

A potent MDM2-p53 interaction inhibitor with remarkable biochemical (HTRF IC50=0.4 nM), cellular potency (SJSA-1 EdU IC50=25 nM), and favorable pharmacokinetic properties.

A potent small molecule inhibitor that binds and disrupts the MDM2/MDMX-p53 interaction with IC50 of 0.19 uM and 19.7 uM, respectively..

RO-5963 is an inhibitor of the interaction of both MDM2 and MDMX with p53.

A potent, highly selective, orally active MDM2-p53 interaction inhibitor with IC50 of 4 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 6 nM.

A potent, selective, and orally active p53-MDM2 antagonist with IC50 of 7 nM.

A potent, selective, orally bioavailable MDM2-p53 interaction inhibitor with HTRF IC50 of 1.1 nM, SJSA-1 EdU IC50 of 68 nM.

A small molecule inhibitor of HDM2-p53 interaction with FP IC50 of 0.7 uM.

A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 16 uM..

A small molecule inhibitor of MDM2-p53 protein-protein interaction with IC50 of 5.3 uM in ELISA assay.

AMG232 is a potent, selective and orally bioavailable inhibitor of MDM2−p53 interaction with IC50 value of 9.1 nM in EdU cells .

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.

DS-3032b is a potent, selective, orally available MDM2-p53 inhibitor with potential antineoplastic activity.

HDM201 is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.

JNJ-26854165 (Serdemetan) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53.

MB710 is a small-molecule p53 mutant Y220C stabilizer, binds tightly to the Y220C pocket and stabilizes p53-Y220C in vitro..

MB725 is a small-molecule p53 mutant Y220C stabilizer, induces selective viability reduction in several p53-Y220C cancer cell lines (Huh7 cell IC50=10 uM).