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. Author manuscript; available in PMC: 2021 Dec 10.
Published in final edited form as: J Med Chem. 2020 Nov 20;63(23):14626–14646. doi: 10.1021/acs.jmedchem.0c01174

Table 1.

Thieno[3,2-d]pyrimidines with STK17B activity

graphic file with name nihms-1655834-t0010.jpg
DiscoverX a
Entry Compound X R1 R2 scanMAX
S10(1 μM)		 STK17A
KD (nM)		 STK17B
KD (nM)		 Tpl2 b
IC50 (nM)
1 PFE-PKIS 43 (4) S SCH3 H 0.005 230 3.8 3400
2 PFE-PKIS 14 (5) S CONH2 H 0.020 270 11 1500
3 PFE-PKIS 9 (6) O ─NHN=C─ 0.012 250 30 1000
a

DiscoverX KINOMEscan. scanMAX, S10(1 μM) = number of kinases with 10 % or less of control activity remaining at 1 μM / number of wild type kinases tested (403), n = 1. KD, determined by dose response, n = 2.

b

Reported by Ni et al (reference 19).