Table 1.

Representative 2-aminobenzothiazole derivatives and their molecular targets.

Compd.	Chemical structure	Target	Bioactivity	Reference
1 (BLZ945)		CSF1R	IC50 = 1.0 nM	[27]
8 (IACS-9439)		CSF1R	IC50 = 1.7 nM Kd = 1.0 nM	[29]
12		EGFR	IC50 = 96 nM	[33]
23		VEGFR-2	IC50 = 97 nM	[45]
24		FAK	IC50 = 19.5 μM	[48]
34 (SAR125844)		MET	IC50 = 4 nM	[55]
35		Aurora B	IC50 = 0.09 μM	[58]
39		CDK2	IC50 = 15.4 nM	[63]
44		CK1δ	IC50 = 0.09 μM	[69]
45		CK2	IC50 = 0.08 μM	[72]
46 (TAK632)		BRAFV600E	IC50 = 2.4 nM	[78]
47		BRAFV600E	IC50 = 0.095 μM	[79]
50 (YK-2-69)		DYRK2	IC50 = 9 nM Kd = 92 nM	[81]
52		PI3Kγ	IC50 = 2 nM	[87]
54		PI3Kα	IC50 = 1.03 nM	[90]
57		Topoisomerase I	-	[95]
63		Topoisomerase IIα	-	[97]
67 (A-1331852)		BCL-XL	Ki < 0.01 nM	[103]
69 (A-1293102)		BCL-XL	Ki = 0.43 nM	[104]
73		HSP90	-	[114]
74		HSP90-CDC37	IC50 = 0.14 μM	[115]
78 (MB725)		Mutant p53	-	[120]
79		Mutant p53	Kzn = 119 nM	[121]
84		HDAC6	IC50 = 12 nM	[126]
93 (BT5)		NSD1	IC50 = 5.8 μM	[135]
95		LSD1	IC50 = 18.4 μM	[139]
96 (FTO-04)		FTO	IC50 = 3.39 μM	[144]
99		mPGES-1	IC50 = 0.7 μM	[145]
102		SCD	IC50 = 54 nM	[150]
109		hCA IX/XII	Ki = 48.9/57.5 nM	[159]
110		CXCR2	IC50 = 0.3 μM	[163]
111		CXCR1/2	-	[164]