TABLE 1

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 NameFDA-ApprovedTargetCmax (µM)Average EC50 (µM)Maximum ResponseReference
JFD00244NoSIRT2 inhibitorN.D.7.5154 ± 5.6
6-Bromo-indirubin-3′-monoximeNoGSK3-β inhibitorN.D.1.9115 ± 7.3
Indirubin-3′-monoximeNoGSK3-β inhibitor, CDk5/1, 5-lipoxygenaseN.D.4292.9 ± 10
SB 216763NoGSK3-α,β inhibitorN.D.5.849.1 ± 4.2
StaurosporineNoPKC inhibitor0.0350.7465.6 ± 6.1Edelman et al., 2007
CP-154526NoCRF1 antagonistN.D.1.2127 ± 3.8
PapaverineYesPDE4/10 inhibitor, increased cAMP0.161142 ± 1.5Kiessling et al., 2013
DipyridamoleYesPDE4/10 and adenosine deaminase inhibitor, increased cAMP7.41640.2 ± 8.2Offman et al., 2013
Tyrophostin-A9NoPDGFR and CRAC inhibitorN.D.1.171.7 ± 3.6
SunitinibYesPDGFR/VEGFR inhibitor0.0950.4766.3 ± 4.3Kim et al., 2009
AMG 9810NoCompetitive vanilloid TRPV1 receptor antagonistN.D.3.186.6 ± 4.2
S-(p-Azidophenacyl)glutathioneNoantioxidantN.D.2.354.5 ± 4.4
SB 242084No5-HT2c receptor inhibitorN.D.∼3.057.7 ± 4.2
DiphenyleneiodoniumNoNitric oxide synthetase inhibitor, NADPH oxidase inhibitorN.D.0.008245.5 ± 6.6
Cl-IB-MECANoA3 adenosine receptor agonist0.359.238.7 ± 10van Troostenburg et al., 2004
RotenoneNoMitochondrial uncouplingN.D.0.1344.2 ± 5.5
NiclosamideYesMitochondrial uncoupling0.0018∼0.7590.6 ± 3.4Burock 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.