Tyroserleutide is a tripeptide consisting of tyrosine, serine, and leucine with potential antineoplastic activity.

Tyrphostin AG 528 is an inhibitor of EGFR and ErbB2 with IC50s of 4.9 and 2.1 μM, respectively.

U-0126 is a selective MAP Kinase Kinase inhibitor, displaying a preference for MEK-1 (IC50 = 72 nM) and MEK-2 (IC50 58nM).

U0126-EtOH(U-0126) is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059.

U93631 is a GABAA receptor ligand of novel chemical structure with IC50 of 100 nM,and has been shown to induce a rapid, time-dependent decay of GABA-induced whole-cell Cl-currents in recombinant GABAA receptors.

UK-371804 is a potent and selective uPA inhibitor with excellent enzyme potency (Ki 10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).

Ulipristal is a selective SPRM for emergency contraception after an unprotected intercourse or contraceptive failure.

UM-164 is a Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer.

Umeclidinium bromide(GSK573719A) is a muscarinic receptor antagonist which is useful in treatment of chronic obstructive pulmonary disease (COPD).

UNC-0224 is a potent inhibitor of G9a histone lysine methyltransferase (IC50 = 15 nM).

UNC1079 is the piperidine analog of UNC1021, as a structurally similar but significantly less potent inhibitor for use as a negative control in cellular studies.

UNC2881 is a potent and specific Mer kinase inhibitor; inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM.

Uprosertib is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

URB602 is a selective inhibitor of monoglycerol lipase (MGL), exhibiting an IC50 of 28 µM for the rat brain enzyme.

Urolithin A is an intestinal metabolite of ellagic acid with antioxidant and antiproliferative effects; inhibits T24 and Caco-2 cell growth with IC50 values of 43.9 and 49 μM, respectively.

UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.

V-9302 is a competitive antagonist of transmembrane glutamine flux, selectively and potently targeting the amino acid transporter ASCT2.

Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia.

Valbenazine(NBI-98854) is a potent and selective VMAT2 inhibitor..

Valspodar(PSC833) is a P-glycoprotein (P-gp) inhibitor widely used in preclinical and clinical studies for overcoming multidrug resistance (MDR).

VEGFR2 kinase inhibitor I(SU-5408)is a potent, cell-permeable inhibitor of mouse VEGFR2 kinase (IC50 = 70 nM).

Velaresol, also known as BW12C or BW12C79, is a oxyhaemoglobin stabilizer.

Veliparib (ABT-888) is a potent inhibitor of PARP1 and PARP2 with Ki of 5.2 nM and 2.9 nM, respectively.

Verdiperstat is a selective, irreversible and orally active myeloperoxidase inhibitor, with an IC50 of 630 nM, and is used in the research of neurodegenerative brain disorders.

Verinurad is an urate transporter inhibitor with EC50 value of 0.05 μM.Verinurad is useful in the modulation of blood or serum uric acid levels, reducing serum uric acid levels in a human.

Verucerfont(GSK561679) is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000 nM for CRF1, CRF2, and CRF-BP, respectively.

Vilanterol trifenatate (GW642444)is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.

Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.

Vortioxetine (Lu AA21004) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.

Vortioxetine Hcl (Lu AA21004 Hcl) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.