ASK1 Inhibitors

RESEARCH

ASK1 Inhibitors

We have identified three classes of ATP-competitive small-molecular inhibitors of protein kinase ASK1 (apoptosis signal-regulating kinase 1) using computer-based rational design approach.

ASK1 has recently emerged as an attractive therapeutic target for treatment of several human diseases.

It is ground for the search of potential ASK1 inhibitors which can be used in medical practice.

ASK1 overactivity scheme

In order to discover novel ASK1 inhibitors we have performed screening program, using both in silico and in vitro approaches. The virtual screening experiments were carried out targeting the ATP binding site of ASK1 by browsing the Otava Ltd. compound library of 156,000 organic compounds. The best-scored compounds have been selected and taken for the kinase assay study.

We have identified two classes of human ASK1 ATP-competitive inhibitors:

Title Filter Display #

#	Article Title
1	Identification of ASK1 inhibitors among the derivatives of Benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one
2	Identification of 3H-naphtho[1,2,3-de]quinoline-2,7-diones as Inhibitors of ASK1
3	Evaluation of 2-Thioxo-thiazolidin-4-ones Derivatives as Inhibitors of ASK1

Other kinase inhibitors research:

ASK1 Inhibitors

Identification of ASK1 inhibitors among the derivatives of Benzothiazol-2-yl-3-hydroxy-5-phenyl-1,5-dihydro-pyrrol-2-one

We have identified novel chemical class of ASK1 inhibitors, namely...

FGFR1 Inhibitors

Flavones

One of the first discovered in the screening of inhibitors of FGFR1 classes are...

CK2 Inhibitors

3-carboxy-4(1H)-quinolones

This CK2 inhibitors were revealed and evaluated to be a CK2 inhibitors after...