CCT251921

Potency assay (off target): CCT-251921 was tested at 1 µM across a panel of 279 kinases (Millipore Panel: data expressed as percentage effect versus control for each kinase tested at its respective Km for ATP). Where >50% inhibition was observed at a single 1 µM concentration an IC50 was obtained.

Potency assay (off target): CCT-251921 was tested at 10 µM across a panel of 29 enzymes (CEREP) and tested at 10 µM across a panel of 59 receptors and ion channels (CEREP) showing a clear profile.

Potency assay (off target): CCT-251921 was profiled for inhibitory activity in enzymatic activity assays covering 32 human CDK/cyclin pairs, representing 20 of the 21 human CDKs demonstrating the expected potent low-nanomolar IC50 selectivity for CDK8/cyclin C and CDK19/cyclin C and no significant activity (IC50 > 1 μM) against the remaining CDK/cyclin pairs in the panel, confirming their high selectivity for CDK8 and CDK19 within the CDK-family of protein kinases. (DOI: 10.1021/acschembio.5c00338)

Potency assay, off target (cells): CDK8, CDK19 and CDK8/19 Double Knockout Cells were used to assess the selectivity of compound CCT-251921 (DOI: 10.1021/acschembio.5c00338)