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. Author manuscript; available in PMC: 2023 Aug 11.
Published in final edited form as: J Med Chem. 2022 Jul 26;65(15):10251–10284. doi: 10.1021/acs.jmedchem.2c00552

Table 6.

Potency and selectivity of bicyclic pyrrolopyrazine analogs

graphic file with name nihms-1859502-t0035.jpg
R1 R2 PKMYT1 cell assay IC50 (μM) PKMYT1 nanoBRET IC50 (μM) EPHB3 selectivity ratio
39 n.a. n.a. 0.020 0.009 3.3
45 H H 0.626 0.012 168
46 Me Me 0.073 0.005 31
47 H Me 0.488 - -
48 Me H 0.108 - -
49 cPr H 0.042 0.001 15
50 tBuOH H 0.026 0.023 2.2
51 graphic file with name nihms-1859502-t0036.jpg H 0.025 - -
52 graphic file with name nihms-1859502-t0037.jpg H 0.050 - -
53 graphic file with name nihms-1859502-t0038.jpg H 0.034 - -