Table 5.

Advanced investigation of amide derivatives.

Name	R1	X1	X2	TLK2 IC50 (nM)a	FLT3 (%)b	TRKC (%)b
88 c	4-CN	N	C-H	12	39	47
89 c	3-CN	N	C-H	95	56	52
90		C-H	N	48	60	46
91	2-CN	C-H	N	4000	75	33
92	4-OMe	N	C-H	88	36	45
93		C-H	N	110	44	50
94	3-OMe	N	C-H	100	42	48
95 c		C-H	N	2800	84	80
96	2-OMe	N	C-H	9.1	25	43
97		C-H	N	67	40	34
98	4-F	N	C-H	190	41	39
99		C-H	N	140	46	53
100	3-F	N	C-H	200	34	33
101 c		C-H	N	490	70	60
102	2-F	C-H	N	110	26	24
103	4-CF3	N	C-H	330	58	57
104 c		C-H	N	6100	88	83
105 c	2-CF3	N	C-H	400	60	17
106 c		C-H	N	190	62	20

^a.8-point dose response (n=1);

^b.percentage inhibition at 0.5 μM (n=2);

^c.E:Z ratio: 88 (50:50); 89 (43:57); 95 (37:63); 101 (35:65); 104 (34:66); 105 (38:62); 106 (34:66).³⁹