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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 2.

Structure-activity of the N-(3-aminophenyl)propionamide series of 3-cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines 8–15.

graphic file with name nihpp-2022.01.03.474779v3-t0010.jpg
Compound R1 CSNK2A1 nanoBRET (pIC50)a CSNK2A2 nanoBRET (pIC50)a MHV replication (pIC50)b
SGC-CK2–1 graphic file with name nihpp-2022.01.03.474779v3-t0011.jpg 7.4 7.8 6.9
8 graphic file with name nihpp-2022.01.03.474779v3-t0012.jpg 8.2 8.6 7.2
9 graphic file with name nihpp-2022.01.03.474779v3-t0013.jpg 8.4 8.7 7.0
10 graphic file with name nihpp-2022.01.03.474779v3-t0014.jpg 7.7 6.9 6.6
11 graphic file with name nihpp-2022.01.03.474779v3-t0015.jpg 7.0 7.0 6.1
12 graphic file with name nihpp-2022.01.03.474779v3-t0016.jpg 6.6 6.6 5.7
13 graphic file with name nihpp-2022.01.03.474779v3-t0017.jpg 8.1 7.8 6.5
14 graphic file with name nihpp-2022.01.03.474779v3-t0018.jpg 6.8 6.7 5.7
15 graphic file with name nihpp-2022.01.03.474779v3-t0019.jpg 8.7 7.8 6.6
a

In cell target engagement of CSNK2A2-nLuc in HEK293 cells.

b

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