Hits from secondary follow-up screen with IC50, efficacy, and Cmax values
Table 1 shows the compound name, FDA status, the compound target, its reported Cmax (if any), the experimentally determined EC50, the experimentally determined maximum response with S.D., and the reference for the Cmax.
| Compound Name | FDA-Approved | Target | Cmax (µM) | Average EC50 (µM) | Maximum Response | Reference |
|---|---|---|---|---|---|---|
| JFD00244 | No | SIRT2 inhibitor | N.D. | 7.5 | 154 ± 5.6 | |
| 6-Bromo-indirubin-3′-monoxime | No | GSK3-β inhibitor | N.D. | 1.9 | 115 ± 7.3 | |
| Indirubin-3′-monoxime | No | GSK3-β inhibitor, CDk5/1, 5-lipoxygenase | N.D. | 42 | 92.9 ± 10 | |
| SB 216763 | No | GSK3-α,β inhibitor | N.D. | 5.8 | 49.1 ± 4.2 | |
| Staurosporine | No | PKC inhibitor | 0.035 | 0.74 | 65.6 ± 6.1 | Edelman et al., 2007 |
| CP-154526 | No | CRF1 antagonist | N.D. | 1.2 | 127 ± 3.8 | |
| Papaverine | Yes | PDE4/10 inhibitor, increased cAMP | 0.16 | 11 | 42 ± 1.5 | Kiessling et al., 2013 |
| Dipyridamole | Yes | PDE4/10 and adenosine deaminase inhibitor, increased cAMP | 7.4 | 16 | 40.2 ± 8.2 | Offman et al., 2013 |
| Tyrophostin-A9 | No | PDGFR and CRAC inhibitor | N.D. | 1.1 | 71.7 ± 3.6 | |
| Sunitinib | Yes | PDGFR/VEGFR inhibitor | 0.095 | 0.47 | 66.3 ± 4.3 | Kim et al., 2009 |
| AMG 9810 | No | Competitive vanilloid TRPV1 receptor antagonist | N.D. | 3.1 | 86.6 ± 4.2 | |
| S-(p-Azidophenacyl)glutathione | No | antioxidant | N.D. | 2.3 | 54.5 ± 4.4 | |
| SB 242084 | No | 5-HT2c receptor inhibitor | N.D. | ∼3.0 | 57.7 ± 4.2 | |
| Diphenyleneiodonium | No | Nitric oxide synthetase inhibitor, NADPH oxidase inhibitor | N.D. | 0.0082 | 45.5 ± 6.6 | |
| Cl-IB-MECA | No | A3 adenosine receptor agonist | 0.35 | 9.2 | 38.7 ± 10 | van Troostenburg et al., 2004 |
| Rotenone | No | Mitochondrial uncoupling | N.D. | 0.13 | 44.2 ± 5.5 | |
| Niclosamide | Yes | Mitochondrial uncoupling | 0.0018 | ∼0.75 | 90.6 ± 3.4 | Burock et al., 2018 |
N.D., not determined; PKC, protein kinase C. SIRT2 - NAD-dependent deacetylase sirtuin 2. CDk5/1 - cyclin-dependent kinase 5/1. CRF1 - Corticotropin-releasing hormone receptor 1. PDE4/10 - phosphodiesterase 4/10. CRAC - calcium release activated channel. VEGFR - vascular endothelial growth factor receptor. TRPV1 - transient receptor potential cation channel subfamily V member 1. 5-HT2c - 5-hydroxytryptamine receptor 2C.