Table 3.

Fluor-KI conjugates in this review, their targets, specificities, potencies, cell membrane permeability and whether the probe was applied in vivo.

conjugate	KI	target	dye	binding and kinase inhibition (cell-free, nM, unless otherwise noted)	potencies relative to parent KI	cell membrane permeable	applied in vivo
1 23	dasatinib	Src, Abl	BODIPY	Kd: Src 0.5; Abl 0.15	N/A	yes	no
2 23	dasatinib (DFG-out)			Kd: Src 2.8; Abl 0.75	ligand induced different binding conformation	N/A	N/A
3 23	dasatinib (αC-helix-out)			Kd: Src 4.6; Abl 0.58.		N/A	N/A
4 26	a type II KI	Src, p38		IC50:Src 25.4; p38 25.5	N/A	N/A	N/A
5 30–32	HS-133	PI3Kα	intrinsically fluorescent	IC50: 68 nM	N/A	yes	yes
6 33	gefitinib	ERBB2		Ki (in cell): 3,100	N/A	yes	no
7a-b 34				Ki (in cell): 7a N/A, 7b 9 μM	reporter of type I or II binding mode	yes	no
8a 37 , 8c 38				Ki (in cell): 8a 71; 8c N/A		yes	no
8b 37	lapatinib			Ki (in cell): 27		yes	no
9b 39	type I KI	Aurora-A, Blk, LCK	intrinsically fluorescent	IC50:222 nM (Arora-A), 554 nM (Blk), 124 nM (LCK)	N/A	yes	no
10a43, 10b44	ibrutinib	Btk	BODIPY	IC50: 10a N/A: 10b ~200	100x inferior	yes	yes
11 13	BI2536	PLK1–3		IC50: PLK1 5.01; PLK2 19.4; PLK3 9.37	comparable	yes	no
12 49	nilotinib	BCR-Abl		N/A	inferior	yes	no
13a 7	ibrutinib	Btk	SiRh	IC50: 122	200~300x inferior	yes	yes
13b 7	spebrutinib	Btk	SiRh	IC50: 283		yes	no
14 19	vemurafenib	BRAFV600E	BODIPY	EC50: 380	3x inferior	yes	yes
15 11	UNC2025	MERTK	SiRh	IC50 (in cell): 19.7 μM	inferior	yes	yes
16 54	gefitinib	EGFR	aza-BODIPY	IC50 (in cell): PC9, 50 H1650, 780	superior	yes	yes
17 61,79	dasatinib	Src, Lyn	NIR Cy7 (MHI-148)	IC50 (Src, cell-free): 184 IC50 (in cell): 5380	less potent in cell-free than in cell-based assays	yes	yes
18 8	crizotinib	ALK	NIR Cy7 (IR-786)	EC50: (average of 3 GBM cell lines): 50 ± 20	100x superior	yes	no
19 20	afatinib	EGFR, HER2	Cy3 and Cy5	IC50 (three cell lines average): Cy3-AFTN 1480 Cy5-AFTN 2460	inferior	yes	yes
20 83	dasatinib	Src	Cy5	IC50 (in cell): 46 ± 30 nM	similar but inferior (used for PET)	yes	yes
21, 22 9	erlotinib	EGFR	porphyrin	N/A	used as PDT photosensitizer	yes	yes