Supplementary Table 1. The current clinical success of the phase III targets reported in the 2009 paper (J Pharmacol Exp Ther. 330(1):304-15, 2009) together with their previous prediction resultsat the time of evaluation in the 2009 paper.

Target Name / Drug of the Highest Clinical Status / Drug Status (approval year, or clinical trial ID and period) / Predicted as Promising by Methods inthe 2009 Paper / Target Status at the Time of Evaluation in the 2009 Paper (clinical status of target’s corresponding drugs)
Somatostatin receptor 1 / Pasireotide / Approved (Dec, 2014) / Combination of A, C, D / Phase III (pasireotide); Phase II (CAP-232)
Orexin-OX1/OX2 receptor* / Suvorexant / Approved (Aug, 2014) / Combination of A, C, D / Phase III (almorexant)
Thrombin receptor* / Vorapaxar / Approved (Aug, 2014) / Combination of A, B, C / Phase III (SCH-530348)
B2 bradykinin receptor* / Icatibant / Approved (Aug, 2011) / Combination of A, B, C / Phase III (icatibant); Phase II (anatibant)
Coagulation factor IIa* / Dabigatran / Approved (Oct, 2010) / Combination of A, B, C, D / Phase II/III (SR-123781A)
S1P receptor 1* / Fingolimod / Approved (Sep, 2010) / Combination of A, B, D / Phase III (FTY720)
Plasma kallikrein* / Ecallantide / Approved (Nov, 2009) / Combination of A, B, D / Phase III (DX-88)
C-X-C chemokine receptor 4 / Plerixafor / Approved (Dec, 2008) / Combination of A, B, D / Phase III (AMD-3100); Phase I/II (AMD-070); Phase I (MSX-122)
C1 esterase* / Cinryze / Approved (Oct, 2008) / Combination of A, B, D / Phase III (C1-INH)
5-HT 3 receptor / Granisetron / Approved (Sep, 2008) / Combination of A, C, D / Phase III (cilansetron)
NK-2 receptor* / Ibodutant / Phase 3 (NCT02320318; 2015-2016) / Combination of A, C, D / Phase III (saredutant)
Tropomyosin receptor kinase A* / MIM-D3 / Phase 3 (NCT02634853; 2015-2017) / Combination of A, B, C, D / Phase II/III (lestaurtinib)
Cholecystokinin A receptor* / Dexloxiglumide / Phase 2 (EudraCT 2013-004469-15; 2013-2016) / Combination of A, B, C, D / Phase III (dexloxiglumide)
Heparanase* / Suramin / Phase 1 (NCT02508259; 2015-2016) / Combination of A, C, D / Phase III (PI-88)
Multidrug resistance protein 3 / LY335979 / Discontinued in Phase 3 / Combination of A, C, D / Phase III (LY335979)
Neuropeptide Y receptor 5 / CGP71683A / Discontinued in Phase 3 / Combination of A, B, D / Phase III (CGP71683A)
Neutral endopeptidase / Sacubitril/valsartan / Approved (Jul, 2015) / Only D / Phase II/III (Ilepatril); Phase II (SLV 306)
Alpha-glucosidase / Deoxynojirimycin / Phase 3 (NCT02969070; 2016-2017) / Combination of A, D / Phase III (acarbose); Phase II(celgosivir)
MMP-2/MMP-9 / Curcumin / Phase 3 (NCT02255370; 2014-2017) / None / Phase III (neovastat); Phase II (PG-530742)
Cyclin-dependent kinase 2 / PHA848125 / Phase 2 (NCT01011439; 2009-2017) / Combination of A, B / Phase III (flavopiridol); Phase II completed (seliciclib)
Farnesyl protein transferase / Zarnestra / Phase 2 (NCT02210858; 2000-2017) / Only D / Phase III (R115777)
Heat shock protein 90 / AUY922 / Phase 2 (NCT01854034; 2013-2017) / Only C / Phase III (tanespimycin); Phase II (alvespimycin HCl, IPI-504)
Heme oxygenase / Stannsoporfin / Phase 2 (NCT01887327; 2013-2016) / Only D / Phase III (stannsoporfin)
Protein kinase B / CMX-2043 / Phase 2 (NCT02103959; 2014-2015) / Combination of A, B / Phase III (enzastaurin); Phase II (perifosine); Phase II (XL880)
Sphingosine kinase / ABC294640 / Phase 2 (NCT02939807; 2016-2021) / Only D / Phase III (phenoxodiol)
Cathepsin K / Odanacatib / Phase 1 (NCT01630616; 2013-2016) / None / Phase III (odanacatib); Phase II (relacatib); Phase I/II (MIV-701)
Lipoprotein-associated phospholipase A2 / Rilapladib / Phase 1 (NCT02130661; 2017-2018) / Only D / Phase II/III (darapladib); Phase I (659032)
MMP-12 / FP-025 / Phase 1 (NCT02238834; 2015-2018) / Only D / Phase III (AE-941)
Arachidonate 5-lipoxygenaseactivating protein / Veliflapon / Discontinued in Phase 3 / Only D / Phase III (DG031); Phase I (AM803, AM103)
Myophosphorylase / Flavopiridol / Discontinued in Phase 3 / Only D / Phase III (flavopiridol); Phase IIa (PSN357)
Squalene synthetase / Lapaquistat acetate / Discontinued in Phase 3 / Combination of C, D / Phase III (TAK-475)