- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: THAL-SNS-032 is a cereblon (CRBN)-engaging degrader of the CDK9 kinase protein . It is a bifunctional molecule that uses PROTAC technology to promote degradation of the CDK9 protein. Degradation is achieved through co-engagement of CDK9 (via the multi-targeting kinase inhibitor BMS-387032, a.k.a. SNS-032) and cereblon (via a thalidomide derivative) to promote E3 ligase-mediated ubiquitination and proteasomal degradation of CDK9.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL et al.. (2018)
Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.
Nat Chem Biol, 14 (2): 163-170. [PMID:29251720]