Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor.

Zafirlukast(Accolate)

Remdesivir metabolite.Remdesivir blocks SARS-CoV and MERS-CoV in HAE cells with EC50s of both 74 Nm,and also showed potent activity blocking 2019-nCov(Coronavirus).

CVT-10216 is a potent and selective, reversible inhibitor of aldehyde dehydrogenase 2 (ALDH2) (IC50 values are 29 and 1300 nM for ALDH2 and ALDH1, respectively).

Decernotinib(VX-509; VRT-831509) is a potent and selective Janus kinase 3 (JAK3) inhibitor with Ki of 2.5 nM; IC50 is 50-170 nM in cellular assays.

Eribulin Mesylate (E7389 Mesylate), a synthetic analogue of halichondrin B in phase III clinical trials for breast cancer, binds to tubulin and microtubules.

GLPG-1690 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.

AMG9810 is a potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM).

GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).

Tavapadon is a potent, orally-bioavailable, selective partial agonist of the dopamine D1 and D5 receptors.

Lacosamide (Vimpat; Erlosamide) is a medication developed for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain.

BMS-708163 is a potent, selective γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, respectively.

Galicaftor (ABBV-2222/GLPG-2222) is an orally bioavailable small molecule that functions as a CFTR corrector, demonstrating potential for therapeutic development in cystic fibrosis research.

Sufugolix(TAK-013) is a non-peptide, orally-active, selective antagonist of the gonadotropin-releasing hormone receptor (GnRHR) (IC50 = 0.1 and 0.06 nM for affinity and in vitro inhibition, respectively).

CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1.

RX-3117 is an orally available and potent DNA synthesis inhibitor with potential antineoplastic activity.

​​Flavopiridol hydrochloride​​ is a potent pan-cyclin-dependent kinase (CDK) inhibitor with a unique ATP-competitive mechanism.

PF-00562271 is the benzenesulfonate salt of PF-562271, which is a potent, ATP-competitive, reversible inhibitor of FAK and Pyk2 with IC50 of 1.5 nM and 14 nM, respectively.

MK-571 is a selective, orally active CysLT1 receptor antagonist.

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

Dabigatran etexilate mesylate (BIBR 1048MS) serves as the ​orally bioavailable prodrug of the active anticoagulant dabigatran. Following absorption, this precursor compound undergoes ​enzymatic conversion to release dabigatran - a highly ​selective, reversible direct thrombin inhibitor (DTI) with exceptional potency (Ki = ​4.5 nM).

BIBR-1048 (Dabigatran) represents a breakthrough in anticoagulant therapy as a ​potent, selective direct thrombin inhibitor.

(E/Z)-4-hydroxy Tamoxifen is an active metabolite of tamoxifen that is formed by the action of cytochrome P450 2D6 in human liver.

Duvelisib (IPI-145) is a selective inhibitor of the p110δ isoform, exhibiting IC50 values of 2.5 nM, 27.4 nM, 85 nM, and 1602 nM for p110δ, p110γ, p110β, and p110α, respectively, highlighting its specificity and potency.

COTI-2 is a small molecule candidate anti-cancer drug which can convert mutant p53 to wild-type conformation.

NPS-2143(SB 262470A ) is a selective potent calcium ion-sensing receptor antagonist with IC50 of 43 and 41 nM for cytoplasmic Ca2+ concentrations and parathyroid hormone secretion, respectively.

AZD6244 (Selumetinib, ARRY-142886) is highly potent to inhibit MEK1 with IC50 of 14 nM.

17-AAG (17-N-Allylamino-17-demethoxygeldanamycin), also known by its NSC number 330507 and CP number 127374, is a well-studied inhibitor of Heat Shock Protein 90 (HSP90). HSP90 is a molecular chaperone that plays a critical role in the stabilization and activation of a wide range of client proteins, many of which are involved in oncogenic processes. By inhibiting HSP90, 17-AAG disrupts the function of these client proteins, leading to the degradation of oncogenic proteins and ultimately inhibiting cancer cell growth and survival.

TAK-901 is a non-selective Aurora kinase inhibitor (IC50s = 3.1, 10, and 4.2 nM for Aurora A, B, and C, respectively).