Table 2. Top 16 hits of the Tocriscreen™ Mini library screen.
| %Inhibition | Compound | Known Activity | Cellular TR-FRET Assay | Cytotoxicity Assay | Biochemical LRRK2 assay | |
| Initial screen | Max % Inhibition | IC50 (µM) +/−SD | IC50 (µM) | IC50 (µM) +/− SD | ||
| 97.5 | Bay 11-7085 | Irreversible inhibitor of TNFa-induced IkB phosphorylation | 100 | 5.3+/−2.8 | >20 | >100 |
| 90.1 | JTC 801 | ORL1 antagonist | 84 | 9.6+/−6.3 | 10 | >100 |
| 88.3 | SP 600125 | JNK and other kinase inhibitor | 103 | 1.0+/−0.4 | >20 | 0.22+/−0.16 |
| 85.5 | Bay 11-7821 | Irreversible inhibitor of TNFa-induced IkB phosphorylation | 94 | 4.0+/−2.1 | 20 | >100 |
| 81.7 | IKK 16 | Inhibitor of IKK | 82 | 1.3+/−0.8 | >20 | 0.05+/−0.03 |
| 76.1 | NSC 95397 | Selective Cdc25 dual specificity phosphatase inhibitor | 80 | 1.3+/−0.9 | 7.8 | 15+/−5.5 |
| 69.8 | Ro 106-9920 | Inhibitor of NFkB activation | 76 | 7.6+/−0.01 | 20 | >100 |
| 69.7 | GW 441756 | TrkA inhibitor | 72 | 2.2+/−0.3 | >20 | 0.32+/−0.18 |
| 69.7 | BNTX maleate | Standard d1 selective antagonist | 88 | 4.0+/−1.4 | >20 | >100 |
| 67.3 | PD 407824 | Inhibitor of Chk1 and Wee1 | 65 | 0.5+/−0.04 | 15 | 0.32+/−0.32 |
| 67.3 | Y-27632 | p160ROCK inhibitor | 69 | 10+/−4.7 | >20 | 0.57+/−0.27 |
| 63.5 | Indirubin-3-oxime | GSK-3b inhibitor. Also inhibits other protein kinases | 64 | 4.4+/−0.5 | >20 | >10 |
| 59.1 | NSC 663284 | Cdc25 phosphatase inhibitor | 45 | 5.8+/−1.2 | 2 | 0.48+/−0.32 |
| 56.2 | Aminopurvalanol A | Cyclin-dependent kinase inhibitor | 50 | 1.4+/−2.2 | >20 | ND |
| 55.3 | SB 218078 | Inhibitor of checkpoint kinase 1 (Chk1) | 54 | 9.5+/−0.4 | >20 | ND |
| 54.8 | TPCA-1 | Inhibitor of IKK-2 | 50 | 0.1+/−0.03 | >20 | ND |
| 100 | LRRK2 IN-1 | Positive Control Compound | 100 | 0.07+/−0.02 | >20 | 0.01+/−0.001 |
The IC50 values are the averaged numbers from three independent experiments for both cellular and biochemical TR-FRET assays and one representative data of two independent experiments for the cytotoxicity assay.