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. 2024 Oct 23;15(11):1925–1932. doi: 10.1021/acsmedchemlett.4c00374

Table 2. Hinge Binder Exploration in the Pyridazine Core.

graphic file with name ml4c00374_0008.jpg

compound R ALK5 pKia
2A 7.1 ± 0.65
4 2-NH2 8.5 ± 0.10
5 3-NH2 7.3 ± 0.24
6 2-CONH2 6.5 ± 0.02
7 3-CONH2 8.3 ± 0.27
8 2-OMe 6.1 ± 0.09
9 3-OMe 7.8 ± 0.09
a

Potency values are reported as arithmetic mean ± standard deviation from at least two independent experiments; all data were obtained as described in Table 1.