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[Preprint]. 2022 Jan 26:2022.01.03.474779. Originally published 2022 Jan 4. [Version 3] doi: 10.1101/2022.01.03.474779

Table 1.

Structure-activity of the N-(3-aminophenyl)acetamide series of 3-cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines 1–7.

graphic file with name nihpp-2022.01.03.474779v3-t0002.jpg
Compound R CSNK2A1 nanoBRET (pIC50)a CSNK2A2 nanoBRET (pIC50)a MHV replication (pIC50)b
silmitasertib — 6.5 7.3 6.2
1 graphic file with name nihpp-2022.01.03.474779v3-t0003.jpg 8.5 8.7 8.1
2 graphic file with name nihpp-2022.01.03.474779v3-t0004.jpg 8.5 8.6 8.6
3 graphic file with name nihpp-2022.01.03.474779v3-t0005.jpg 8.3 8.4 8.1
4 graphic file with name nihpp-2022.01.03.474779v3-t0006.jpg 8.6 8.9 8.7
5 graphic file with name nihpp-2022.01.03.474779v3-t0007.jpg 7.8 8.1 7.6
6 graphic file with name nihpp-2022.01.03.474779v3-t0008.jpg 7.2 7.8 7.1
7 graphic file with name nihpp-2022.01.03.474779v3-t0009.jpg 6.6 6.9 5.2
a

In cell target engagement of CSNK2A-nLuc in HEK293 cells. Data from reference 24.

b

Inhibition of MHV-nLuc replication in DBT cells. Values are the mean of three assays with range ± 15%.