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 |
