. 2016 Jun 1;26(11):2724–2729. doi: 10.1016/j.bmcl.2016.03.100

Table 1.

Biological data for exemplar bioisosteric replacements

Compound	Ar	RET IC₅₀^a (μM)	Enzymatic selectivity versus KDR	RET cellular IC₅₀^a (μM)	KDR cellular IC₅₀^a (μM)
7	2-Me-3-OH-6-F-Ph	0.044 (0.006)	130	2.10 (1.0)	>10
8	Ph	1.7 (0.29)	>5	n/d	n/d
9	3-MeSO₂NH-Ph	7.7 (10)	n/d	>10	>10
10	3-CHF₂-Ph	2.9 (0.3)	2	>10	>10
11	6-Indolyl	1.7 (0.48)	2	>10	>10
12	4-Indolyl	9.1 (1.1)	n/d	>10	>10
13	6-Benzimidazolyl	>30	n/d	>10	>10
14	4-Benzimidazolyl	4.3 (0.6)	3	n/d	n/d
15	7-Indazoloy	3.3 (0.19)	>30	n/d	n/d
16	6-Indazolyl	0.28 (0.01)	2	>10	5.2 (1.4)
17	5-Indazolyl	0.60 (0.18)	5	>10	>10
18	4-Indazolyl	0.14 (0.06)	38	4.6 (0.26)	>10

Biological data are stated as the geometric mean of at least four independent determinations. Standard deviations are given in parentheses. n/d = not determined.