Table 2.

Target-based hit assessment.

Rank	Antagonist	Target(s)	IMin (% Luminescence)	Z-score	IC50 (µM)
1	Sorafenib	RAF, PDGFR, VEGFR2/3	5.98	−7.62	3.98
2	H-89	PKA	16.07	−6.81	12.16
3	Staurosporine	PKC, PKA, PKG	18.86	−6.58	0.54
4	GSK 269962 A	ROCK1	28.81	−5.77	24.66
5	LY 333531	PKCβ	34.34	−5.33	12.19
6	Crizotinib	ALK	34.72	−5.29	12.19
7	PLX4720	B-RafV600E	36.71	−5.13	2.14
8	BX 912	PDK1	37.84	−5.04	9.23
9	PIK 75	PI3Kα	38.11	−5.01	1.63
10	BI 2536	PLK1, BRD4	43.68	−4.57	8.71
11	Lestaurtinib	FLT3, JAK2	45.45	−4.42	1.22
12	CI 1040	MEK1/2	46.49	−4.34	14.85
Rank	Agonist	Target(s)	EMax (% Luminescence)	Z-score	EC50 (µM)
1	Chlorambucil	Alkylating agent	252.88	12.39	16.41
2	Vinorelbine	Microtubules	208.53	8.79	1.55
3	Vincristine	Microtubules	198.49	7.99	0.27
4	Vinblastine	Microtubules	191.58	7.42	20.56
5	Decitabine	DNA synthesis inhibitor	191.40	7.41	28.77
6	Vismodegib	SMO	161.54	4.99	1.91
7	SB 203580	p38 MAPK	152.42	4.25	3.56
8	Floxuridine	Antimetabolite	146.01	3.73	2.46

Hits are ranked by average Z-score from the primary screening (n = 2). Estimated IC₅₀ and EC₅₀s are calculated from data represented in Fig. 5.