Table 1. Cellular and Enzymatic Activities of Oxindole Amides and Ureas.

IC50 (μM)
	cellular Ba/F3 assaysa					biochemical assaysc
	TRK					TRK
compd	A	B	C	KDR	WTb	A	B	C
1	2.3	1.3	1.2	1.0	1.3	NA	NA	1.9
2	0.91	0.68	0.69	0.60	0.93	0.16	NA	NA
3	0.85	0.66	0.57	NA	2.2	NA	NA	NA
4	0.059	0.037	0.023	0.50	4.8	0.007	NA	0.029
5	0.015	0.005	0.007	0.50	>10	0.007	0.054	NA
6	0.39	0.22	0.27	2.8	4.7	0.016	NA	0.097
7	0.013	0.012	0.012	0.50	4.5	0.007,	0.007	NA
8	0.36	0.55	0.44	0.70	2.1	0.027	NA	NA
9	0.034	0.019	0.029	0.61	4.9	0.003	0.06	NA
10	0.19	0.079	0.15	4.9	>10	0.068	0.035	NA
11	0.022	0.020	NA	0.20	4.3	NA	NA	NA
12	>10	>10	>10	>10	>10	NA	NA	>10
13	0.36	0.12	0.19	2.2	>10	0.049	NA	NA
14	0.014	0.005	0.008	0.60	1.3	NA	0.027	NA
15	>10	>10	>10	>10	>10	NA	NA	NA
16	0.01	0.003	0.006	1.5	>10	NA	0.017	NA
17	0.009	0.006	0.022	0.23	5.2	0.004	0.019	NA
18	0.012	0.004	0.004	1.3	4.6	0.009	NA	NA
19	0.013	0.011	0.027	NA	1.4	NA	0.015	NA
20	0.004	0.005	0.004	0.52	2.4	0.007	NA	0.04
21	0.05	0.017	0.018	3.3	3.3	0.009	NA	NA
22	0.011	0.009	0.007	3.0	5.6	0.008	0.012	NA

^aProliferation assays with Tel-TRK or Tel-KDR fusions.

^bProliferation assay using parental Ba/F3 cells.

^cHTRF or Caliper assays with recombinant TRKA, -B, and -C kinase domains.