CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].

CK-2127107(CK-107, Reldesemtiv) is a novel orally active fast skeletal troponin activator, selectively activates fast skeletal myofibrils with EC50 of 3.4 uM.

Elenbecestat (E2609) is a novel potent, oral BACE1 inhibitor for treatment of Alzheimer's disease..

beta-secretase inhibitor.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

PC786 (PC-786) is a potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 2.1 nM and 0.5 nM in cell-free enzyme assay and mini-genome assay in HEp-2 cells, respectively.

Emtricitabine is a nucleoside analogue which inhibits the reverse nucleoside transcriptase enzyme. Structurally this antiviral agent is similar to Lamivudine. This agent is effective at targeting HIV and HBV viruses since these viruses replicate in a reve

BMS-986120 (BMS986120) is a potent, selective, orally bioavailable, and reversible PAR4 antagonist with Kd of 0.098 nM for human PAR4.

INCB13739 (INCB-13739) is a potent, selective, oral 11βHSD1 inhibitor (IC50=1.1 nM) with high seelctivity over other dehydrogenases, glucocorticoid and mineralocorticoid receptors..

Tenapanor is an inhibitor of the Na+/H+ exchanger NHE3 with IC50 values of 5 and 10 nM against human and Rat NHE3, respectively.

Imatinib Mesylate is orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively.

JNJ 2408068 is a potent RSV (respiratory syncytial virus) inhibitor. JNJ2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. The minimum protective dose of JNJ 2408068 appears to be approximately 0.39 mg/kg[1].

VX-765 is a novel Caspase-1 inhibitor with an IC 50 of 0.8nM being investigated for the treatment of epilepsy, currently being developed by Vertex.

YM155 is a potent IAP (inhibitor of apoptosis proteins) inhibitor for survivin with IC50 of 0.54 nM.

XL184 (Cabozantinib) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

VX-745 is a potent and selective inhibitor of p38α MAPK and p38β MAPK with IC50 of 10 nM and 220 nM, respectively.

Vorapaxar (SCH 530348) is a potent and orally active thrombin receptor (PAR-1) antagonist with Ki of 8.1 nM.

TAS-120 is a highly potent and selective irreversible FGFR inhibitor, effective in tumors harboring various FGFR gene abnormalities.

VTP-27999 is an alkyl amine Renin inhibitor; VTP-27999 is useful for Hypertension and End-Organ Diseases.

Voxtalisib (SAR245409, XL765) is a dual inhibitor of mTOR/PI3K, mostly for p110γ with IC50 of 9 nM; also inhibits DNA-PK and mTOR.

Vorinostat (SAHA) is an HDAC1/3 inhibitor with IC50 of ~10 nM.

Voriconazole is an ergosterol biosynthesis inhibitor, as well as systemic antifungal. This compound, like many antifungal agents, is an inhibitor of CYP2C9, an enzyme involved in the oxidative metabolism of many xenobiotics.

Voreloxin(SNS-595; AG 7352) is a small molecule and a naphthyridine analogue with antineoplastic activity; inhibitor of Topo II.

Volasertib(BI6727) is a highly potent PLK1 inhibitor with an IC50 of 0.87 nM; shows 6- and 65-fold greater selectivity against Plk2 and Plk3.

Vismodegib (formerly GDC-0449) is a hedgehog antagonist, is also an orally bioavailable small molecule with potential antineoplastic activity.

Vicriviroc Malate is a potent CKR-5 (CCR5) antagonist with IC50 of 0.91 nM.

Verdinexor (KPT-335) is an orally bioavailable, selective XPO1/CRM1 inhibitor.

Velpatasvir(GS-5816) is a potent and selective Hepatitis C virus NS5A inhibitor.

Veliparib is a potent inhibitor of both PARP-1 and PARP-2 by [3H]NAD+ with Kis of 5.2 and 2.9 nmol/L, respectively.