Table 1.

Compounds tested in this study

CompoundaMain targetClinical phasebCompoundaMain targetClinical phaseb
ABT-737BCL2Phase ILapatinibEGFRMarketed
Actinomycin-DTranscriptionMarketedLGK-974PORCNPhase I
AfatinibEGFRMarketedMasitinibKITPhase III
All-trans retinoic acidRARMarketedMelphalanDNA alkylatingMarketed
AlpelisibPI3KPhase IIMercaptopurineNucleoside analogueMarketed
AMG-900Aurora kinasesPhase IMethotrexateFolate synthesisMarketed
ApitolisibPI3KPhase IIMitomycin-CDNA crosslinkingMarketed
AT-7519CDKPhase IMitoxantroneTopoisomerase IIMarketed
AxitinibVEGFR/PDGFRMarketedMK-1775WEE1Phase II
AZD-8055mTORPhase IMK-2206AKTPhase II
BGJ-398FGFRPhase IIMK-5108Aurora kinasesPhase I
BI-2536PLK1Phase IIMLN-8054Aurora kinasesPhase I
BIIB021HSP90Phase IMomelotinibTBK-1Phase II
BLU-9931FGFR4PreclinicalMPI-0479605TTKPreclinical
BortezomibProteasomeMarketedMps1-IN-1TTKPreclinical
BosutinibABLMarketedMubritinibERBB2Phase I
BuparlisibPI3KPhase IIINavitoclaxBCL2Phase II
BusulfanDNA alkylatingMarketedNeratinibEGFRPhase II
CabozantinibMET/VEGFRMarketedNilotinibABLMarketed
CarboplatinDNA damageMarketedNintedanibVEGFR/FGFRPhase III
CarfilzomibProteasomeMarketedNMS-P715TTKPreclinical
CeritinibALKMarketedNutlin 3aMDM2Preclinical
CHIR-124CHK1PreclinicalNVP-ADW742IGF1RPreclinical
CisplatinDNA damageMarketedOlaparibPARPMarketed
CrizotinibALK/METMarketedPaclitaxelTubulinMarketed
CytarabineNucleoside analogMarketedPalbociclibCDK4/6Marketed
DabrafenibRAFMarketedPanobinostatHDACMarketed
DacarbazineDNA alkylatingMarketedPazopanibVEGFR/PDGFRMarketed
DactolisibPI3K/mTORPhase IIPD-0325901MEKPhase II
DanusertibAurora kinasesPhase IIPelitinibEGFRPhase II
DasatinibABL/VEGFRMarketedPHA-793887CDKPhase I
DaunorubicinTopoisomerase IIMarketedPictilisibPI3KPhase I
DinaciclibCDKPhase IIIPonatinibABLMarketed
DocetaxelTubulinMarketedPrednisoloneGRMarketed
DoxorubicinTopoisomerase IIMarketedQuizartinibFLT3Phase II
DuvelisibPI3KPhase IIRegorafenibVEGFR/PDGFRMarketed
EntinostatHDACPhase IIIRoscovitineCDKPhase II
EpirubicinTopoisomerase IIMarketedRuxolitinibJAK2/JAK3Marketed
Epothilone BTubulinPhase IISCH-900776CHK1Phase II
EPZ-005687EZH2PreclinicalSelumetinibMEKPhase III
EPZ-5676DOT1LPhase ISN-38Topoisomerase IMarketed
EPZ-6438EZH2Phase IISorafenibVEGFR/PDGFRMarketed
ErlotinibEGFRMarketedSunitinibVEGFR/PDGFRMarketed
EtoposideTopoisomerase IIMarketedTemozolomideDNA alkylatingMarketed
EverolimusmTORMarketedTemsirolimusmTORMarketed
FluorouracilNucleoside analogueMarketedTGX-221PI3KPreclinical
GefitinibEGFRMarketedTH-588MTH1Preclinical
GemcitabineNucleoside analogueMarketedThioguanineNucleoside analogMarketed
GSK-1070916Aurora kinasesPhase ITopotecanTopoisomerase IMarketed
GSK-126EZH2PreclinicalTozasertibAurora kinasesPhase II
GSK-1838705AIGF1RPreclinicalTrametinibMEKMarketed
GSK-343EZH2PreclinicalUNC1999EZH1/EZH2Preclinical
GSK-461364PLK1Phase IVandetanibVEGFR/PDGFRMarketed
I-BET-762BETPreclinicalVatalanibVEGFRMarketed
IbrutinibBTKMarketedVemurafenibRAFMarketed
ICG-001Wnt pathwayPreclinicalVenetoclaxBCL2Marketed
IdelalisibPI3KMarketedVincristineTubulinMarketed
ImatinibABLMarketedVinflunineTubulinMarketed
IrinotecanTopoisomerase IMarketedVolasertibPLK1Phase II
JQ1BETPreclinicalVorinostatHDACMarketed
KU-60019ATMPreclinicalXAV-939TNKS (tankyrase)Preclinical
  • aCompounds also tested, but found inactive, were XL147, SGX-523, fasudil, NVP-LDE225 (erismodegib), tofacitinib, streptozocin, and macitentan.

  • bHighest clinical phase reached (status May 2016, source: clinicaltrials.gov).