Protein Kinase Inhibitor Development

"Kinome" is a depository of promising drug targets - protein kinases, which control vast diversity of molecular interactions in cell life. Indeed, numerous reports describing the discovery of new pharmaceutical substances targeting protein kinases have been published during last few years. Some of these substances are being tested in clinical trials, some of them are already on the market.

Our Department has been involved in extensive research and development of inhibitors for various protein kinases:

Quinazolines

Figure 1. Quinazoline inhibitor of FGFR1.

Quinazolines is another known class of RTK inhibitors that is widely represented in the department chemical collection. We investigated the relationship between the substituents at...

Oxindoles

Oxindoles are known class of inhibitors of RTK, including FGFR1. We perform searching of FGFR1 inhibitors among available in department collection oxindole compounds. The result has found...

Phenylbenzisoxazoles and aminopyrimidines

Figure 1. Phenylbenzisoxazole and aminopyrimidine inhibitors of FGFR1.

Phenylbenzisoxazoles and aminopyrimidines were also found from virtual screening. Search for analogues of these inhibitors reveal the most active compounds with an IC50 of 5 and...

Flavones

Figure 1. The binding mode of flavone inhibitor of FGFR1 in the ATP-binding site. Hydrogen bonds are shown by the dashed lines.

One of the first discovered in the screening of inhibitors of FGFR1 classes are flavones. These compounds belong to a class of chromones which are widely represented in nature. They and...

4,5,6,7-tetrahalogeno-1H-isoindole-1,3(2H)-diones (TID)

Figure 1. The binding mode of TID46 in the CK2 active site. Hydrogen bonds are shown by the dotted lines.

The novel potent and specific CK2 inhibitors - 4,5,6,7-tetrahalogeno-1H-isoindole-1,3(2H)-diones (TID) was identified by high-throughput docking of OTAVA compound collection containing...

Protein Kinase Inhibitor Development

Quinazolines

Oxindoles

Phenylbenzisoxazoles and aminopyrimidines

Flavones

4,5,6,7-tetrahalogeno-1H-isoindole-1,3(2H)-diones (TID)

More Articles...

Other kinase inhibitors research:

ASK1 Inhibitors

CK2 Inhibitors

FGFR1 Inhibitors