TPPU is a potent inhibitor of both human and mouse sEH (IC50 = 3.7 and 2.8 nM, respectively).

TPT-260 2Hcl (TPU260 2Hcl) is a thiophene thiourea derivative with molecule weight 260.00 in free base form; There is no formal name yet, we temporally call this molecule as TPT-260.

TR-14035 is a a dual alpha4beta7(IC50=7 nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .

Trabectedin (Ecteinascidin-743 or ET-743) is a novel antitumour agent of marine origin with potent antitumour activity both in vitro and in vivo.

TRAM-34 is a highly selective blocker of intermediate conductance Ca2+-activated K+ channels (KCa3.1) (Kd = 20 nM).

Trametinib is a highly specific and potent MEK1 and MEK2 inhibitor with IC50 of 0.92 nM and 1.8 nM, respectively.

Tranilast (SB 252218)

Transcrocetin (trans-Crocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with high affinity.

trans-Tranilast (trans-MK-341) is an antiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.

Tranylcypromine HCl is an inhibitor of monoamine oxidase (MAO) and prostacyclin synthase, potently suppresses the enzymatic activity of Lysine-Specific Demethylase 1 (LSD1) (IC50 <2 μM for BHC110/LSD1).

Traxoprodil is an NMDA ε 2 (NR2B) antagonist that has been studied as an alternative to serotonin selective reuptake inhibitors.

TRC051384 is a heat shock protein 70 (HSP70) inducer.

Trelagliptin(SYR-472) is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).

Treprostinil is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.

Treprostinil sodium is a potent DP1 and EP2 agonist with EC50 values of 0.6±0.1 and 6.2±1.2 nM, respectively.

TRi-1 (TXNRD1 inhibitor 1) is a potent, specific and irreversible inhibitor of cytosolic thioredoxin reductase 1 (TXNRD1) with anticancer potential, 5- to 10-fold higher specificity for TXNRD1 over TXNRD2.

Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.

Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis. Phase 2.

Triazavirin is a guanine nucleotide analog antiviral originally developed in Russia that has shown efficacy against influenza A and B, including the H5N1 strain. It appears that Triazavirin has shown promise in reducing influenza disease severity and associated complications.5 Given the similarities between SARS-CoV-2 and H5N1, health officials are investigating Triazavirin as an option to combat SARS-CoV-2, the coronavirus responsible for COVID-19.

Trichostatin A (TSA) is a selective and potent HDAC inhibitor with IC50 of ~1.8 nM; HDAC8 is the only known member of the HDAC-family that is not affected by TSA.

TRIF agonist AV-C is a novel TRIF pathway agonist that activates innate and interferon-associated responses, strongly inhibits replication of ZIKV, CHIKV, and DENV (IC90~5 uM).

Trifluridine (Viroptic)

Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.

TRIM24 inhibitor X is a potent TRIM24 bromodomain inhibitor for synthesis dTRIM24..

Triptolide is the major bioactive constituent of T. wilfordii Hook F., also known as thunder god vine, a traditional Chinese medicinal herb with known antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and anti-polycystic kidney disea

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH), shows greater potency than endogenous LHRH, triptorelin reversibly represses gonadotropin secretion..

TrkA inhibitor compound 23 is an allosteric, potent, Subtype Selective and Peripherally Restricted TrkA Kinase Inhibitor， with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays.

Trk-IN-3 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

TRO19622, a small cholesterol-like molecule, is a neuroregenerative and neuroprotective compound.

Trofinetide (NNZ-2566) is an analog of a molecule which is derived from IGF-1 and occurs naturally in the brain. IGF-1 is a growth factor stimulated by growth hormone.

Tropifexor (LJN452) is a highly potent non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate.

TRPC6 inhibitor is a potent TRPC6(Transient receptor potential cation channel, subfamily C, member 6) inhibitor.

TRPM4 inhibitor 5 is a potent and selective inhibitor of TRPM4 with IC50 of 1.5 uM (Na+ influx).

TRPM8 Antagonist is a potent and selective TRPM8 antagonist, with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

TRx 0237 (LMTX™) mesylate is a second-generation tau protein aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia.

TT-10 is a novel multifaceted fluorinated compound with promising features of CM proliferative, antioxidant, and antiapoptotic activities in vitro.

TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM.

TTNPB (Arotinoid Acid) is a potent RAR agonist, and inhibits binding of [3H]tRA with IC50 of 5.1 nM, 4.5 nM, and 9.3 nM for human RARα, β, and γ, respectively.

TTP 22 is a high affinity, ATP-competitive casein kinase 2 (CK2) inhibitor with IC50/Ki of 0.1 uM/40 nM; shows selectivity for CK2 over JNK3, ROCK1, and MET(IC50> 10 uM).

Tubacin is a selective inhibitor of HDAC6 via inhibition of the second deacetylase domain (DD2).

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).

Tubercidin, an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

Tubulysin A is a novel antibiotic, which is anti-microtubule, anti-mitotic, an apoptosis inducer, anticancer, anti-angiogenic, and antiproliferative.

TUG-1375 (TUG1375, TUG 1375) is a potent, selective free fatty acid receptor 2 (FFA2/GPR43) agonist with β-arrestin-2 pEC50 of 6.1 and cAMP pEC50 of 7.11.

TUG-770 is a highly potent free fatty acid receptor 1 (FFA1/GPR40) agonist with EC50 of 6 nM for hFFA1.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.

TVB-3166 is an orally-available, reversible, potent, and selective fatty acid synthase (FASN) inhibitor with biochemical IC50 of 42 nM.

TW-37 is a novel nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29 μM, 1.11 μM and 0.26 μM, respectively.

TWS119 is a GSK-3β inhibitor with IC50 of 30 nM.

TX1-85-1 is a potent, selective, ATP-competitive Her3 (ErbB3) inhibitor with IC50 of 23 nM, forms a covalent bond with Cys721 located in the ATP-binding site of Her3.

TY-52156 is a potent and selective inhibitor of S1P3 receptor (Ki=110 nM).

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.

Tyrphostin AG 555 is a potent epidermal growth factor receptor kinase inhibitor.

Tyrphostin AG 879 is a protein tyrosine kinase inhibitor with potent effects on TrkA.

TZ9 is a novel inhibitor of Rad6 ubiquitin conjugating enzyme(E2 enzyme); inhibits MDA-MB-231 cell proliferation with IC50 of ~6 uM.

U 19963 is a bioactive compound.

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.

U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.

U18666A, a cell permeable drug, is a cholesterol synthesis and transport inhibitor.

U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO (5-lipoxygenase).

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.

UAMC00039 dihydrochloride is a potent inhibitor of dipeptidyl peptidase II (DPP-II) (IC50 = 0.48 nM).

UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.

Bestatin is a natural, broad-spectrum, and competitive aminopeptidase inhibitor.

UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver.

UC-514321 is a more effective analog of NSC-370284 that directly binds to STAT3/5, significantly and selectively suppresses the viability of AML cells with high level of TET1 expression both in vitro and in vivo.

UCB9608 is a Potent, Orally Bioavailable PI4KIIIβ Inhibitor.

UCPH-101 is a selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor.

UF010 is a potent and selective HADC inhibitor with IC50 ~0.06 μM, 0.1 μM, 0.5 μM and 1.5 μM for HDACs 3, 2, 1 and 8, respectively. It has > 6-fold selectivity over other HDACs.

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).

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).

UK5099 is an inhibitor of plasma membrane monocarboxylate transporters (MCTs) and the mitochondrial pyruvate carrier (MPC).

UKH-1114 (UKH1114) is a potent, sigma 2 receptor/Tmem97 agonist with Ki of 46 nM.

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

Ulixertinib, also known as BVD-523 and VRT752271, is an inhibitors of ERK protein kinase.

ULK-101 is a potent and selective ULK1 inhibitor with in vitro IC50 of 8.3 nM.

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).

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.

UNBS5162 is a novel naphthalimide that decreases CXCL chemokine expression in experimental prostate cancers; the mean antiproliferative activity IC50 value is 17.9 uM for 9 cancer cell lines; hydrolysis product of UNBS3157.

UNC 669 is a potent antagonist of L3MBTL1(IC50=4.2 uM) and L3MBTL3(IC50=3.1 uM).

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

UNC0321 is a potent and selective G9a inhibitor with Ki of 63 pM, UNC0321 is the first G9a inhibitor with picomolar potency and the most potent G9a inhibitor to date.IC50 value: 63 pM(Ki); 9 nM (ECSD assay) [1]Target: G9aIt was found that replacing the 5-

UNC0379 is a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8 with IC50 of 7.3±1.0 uM; selective over 15 other methyltransferases.

UNC-0631 is a novel G9a inhibitor with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.

UNC0638 is an inhibitor of protein lysine methyltransferases G9a(IC50<15 nM) and GLP(IC50=19 nM) with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.

UNC0642 is a novel highly potent, selective and cell permeable inhibitor of the homologous protein lysine methyltransferases, G9a and GLP, with IC50 < 2.5 nM.

UNC0646 is a potent and selective inhibitor of the homologous protein lysine methyltransferases, G9a and GLP (IC50 values are 6 nM and 15 nM for G9a and GLP, respectively).

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.

UNC1215 is a potent and selective chemical probe for the methyllysine (Kme) reading function of L3MBTL3 with Kd value of 120 nM.

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.

UNC-2025 is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.

UNC2025 is a potent and orally bioavailable Mer/Flt3 dual inhibitor with IC50 of 0.8/0.74 nM for Mer/Flt3.

UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.

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

UNC3866 is a potent and selective antagonist of CBX4 and CBX7 chromodomains with (Kd ≈ 100 nM). It is 6- to 63-fold selective for these chromodomains over the other CBX and CDY chromodomains.

UNC569 is a novel small-molecule MER inhibitor with efficacy against acute lymphoblastic leukemia in vitro and in vivo.

UNC-926 is a methyl-lysine (Kme) reader domain inhibitor; inhibits L3MBTL1 with an IC50 of 3.9 μM.

UoS12258 (UoS-12258) is a selective, positive allosteric modulator of the AMPA receptor with pEC50 of 5.6.

Upadacitinib (ABT-494) is a potent and selective Janus kinase (JAK) 1 inhibitor being developed for the treatment of several autoimmune disorders with an IC50 of 43 nM.

UPCDC30245 is an allosteric inhibitor of AAA ATPase p97 with IC50 of 27 nM, binds at the junction between the D1 and D2 domains of p97..

UPF 1069 is a selective PARP2 inhibitor with IC50 of 0.3 μM; ~27-fold selective against PARP1.

UPGL00004 is a potent glutaminase C (GAC) inhibitor with an IC50 of 29 nM, showing high selectivity for GAC over GLS2.

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.

URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM.

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.

USP10-IN-3 is a HBX19818 analog, potent and selective USP10 inhibitor, but does not inhibit USP7 (IC50>100 uM).

UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.

UTL-5g (GBL-5g) is a novel potential chemoprotective agent, TNF-α inhibitor that reduces cisplatin-induced side effects including nephrotoxicity, hepatotoxicity and hematotoxicity.

UU-T03 is the ethyl ester derivative of UU-T02, which is a potent, selective inhibitor of β-catenin/Tcf4 interaction with Ki of 1.36 uM; exhibits growth inhibition of SW480 cells with IC50 of 10.77 uM; downregulates the transcription of AXIN2, LGR5, cyclin D1, and c-Myc in dose-dependent manners in SW480 cells.

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.

Vaborbactam is a cyclic boronic acid pharmacophore β-lactamase inhibitor.

Vacquinol-1 is an activator of MKK4-dependent macropinocytotic cell death in glioblastoma cells.

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..

Val-cit-PAB-OH is a peptide prodrug linker.

Valerylcarnitine is an endogenous metabolite, belonging to the short-chain acylcarnitines.

Valrocemide (TV1901,VGD)) has a broad spectrum of anticonvulsant activity and promising potential as a new AED.

Valrubicin (AD-32) is a chemotherapy drug used to treat bladder cancer.

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

Vamorolone (VBP-15) is a dissociative steroidal compound, reduces NF-κB-mediated cytokine expression in vitro, alsp reduecs glucocorticoid-mediated side-effects when compared to dexamethasone in vivo.

Vandetanib (Zactima, ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM.

Vanoxerine 2 Hcl(GBR12909) is a potent and selective DRI (Dopamine reuptake inhibitor).

Vardenafil is a PDE5 inhibitor used for treating erectile dysfunction.

Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.

Varenicline(CP 526555;Champix) is a selective α4β2 nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.

VAS2870 is a selective inhibitor of the NADPH oxidases.

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.

VCH-222(Lomibuvir) is a novel, potent and selective inhibitor of HCV polymerase with IC50 of 0.94-1.2 μM, 15.3-fold less effective for mutant M423T, and 108-fold less effective for mutant I482L.

VCMMAE-(PEG)4-DBCO is made by MMAE conjugated to DBCO-(PEG)4-vc-PAB linker. Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate.

VE-821 is a potent and selective ATP competitive inhibitor of ATR with Ki and IC50 of 13 nM and 26 nM, respectively.

VE-822 is a selective ATR inhibitor with an Ki value of 0.2 nM, >150 fold selectivity over ATM (Ki=34 nM), DNA-PK (Ki >4 uM) and mTOR (Ki >1 uM).

Vecuronium Bromide

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.

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.

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

VER-155008 is a novel, small molecule inhibitor of Hsc70/Hsp70 with GI50 of 5.3-14.4 uM in human breast and colon cancer cell lines.

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

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.

Vericiguat (BAY 1021189) is a novel potent, selective, orally available soluble guanylate cyclase (sGC) stimulator (MEC=0.3 uM), stimulating sGC NO-independently and in synergy with NO.

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.

Verteporfin(CL 318952; Visudyne), a benzoporphyrin derivative monoacid ring A, is a photosensitising drug for photodynamic therapy (PDT) activated by low-intensity, nonheat-generating light of 689nm wavelength.

VERU-111 (Sabizabulin) is a novel potent colchicine binding site inhibitor (CBSI) in tubulin with potential anticancer activities. Sabizabulin is a novel oral agent with both anti-viral and anti-inflammatory activities.Sabizabulin is a cytoskeleton disruptor which by causing microtubule depolymerization has both anti-viral and anti-inflammatory activity and could be effective against the SARS-CoV-2 virus by disrupting its intracellular transport along the microtubules. Microtubule trafficking is critical for viruses to be transported, replicated, assembled, and released from the cell. In addition, microtubule depolymerization drugs that target the “colchicine binding site” of microtubules, like sabizabulin, also have strong anti-inflammatory effects, including the potential to treat the cytokine release syndrome (cytokine storm) and septic shock induced by the SARS-CoV-2 viral infection that is associated with high COVID-19 mortality rates.

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.

Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.

VGX-1027(GIT27) is an isoxazole compound that exhibits various immunomodulatory properties; reduce the secretion of IL-1beta, TNF-alpha and IL-10 from purified murine macrophages.

VH-032 (VHL ligand 1) is a VHL ligand for PROTAC and potent, small molecule inhibitor of the VHL/HIF-1α interaction with Kd of 185 nM..

VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.

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

Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive drug that inhibits DHODH; inhibits IL-17 secretion in vitro independently of effects on lymphocyte proliferation.

Vigabatrin(γ-Vinyl-GABA; Sabril) is a structural analog of the inhibitory neurotransmitter γ-aminobutyric acid (GABA) that irreversibly inhibits the catabolism of GABA by GABA transaminase. IC50 value: Target: GABA transaminase Clinical studies have sh

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.

Vinorelbine (Navelbine) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.

Vinorelbine is a semi-synthetic Vinca alkaloid which is currently used in treatment of different cancer types mainly advanced breast cancer (ABC) and advanced/metastatic non-small cell lung cancer (NSCLC). Vinorelbine-loaded SSM can be developed as a new,

Vipadenant(BIIB-014) is an adenosine A2a antagonist with Ki of 1.3 nM; less potent for A1(Ki=69 nM).

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

VL285 is a potent VHL ligand, degrading HaloTag7 fusion proteins.

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.

Voltage-independent, selective CFTR chloride channel blocker (Ki = 300 nM) that alters channel gating.

VO-Ohpic is a potent inhibitor of PTEN (phosphatase and tensin homolog) with IC50 of 35 nM.

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

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.

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

Voruciclib is a protein kinase inhibitor specific for the cyclin-dependent kinase 4 (CDK4) with potential antineoplastic activity.

Voxilaprevir (GS-9857) is a potent HCV NS3/4A protease inhibitor that is used in combination with sofosbuvir and velpatasvir for treatment of HCV infection.

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

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

VPC 14449 is a potent and selective androgen receptor DNA-binding domain (AR-DBD) inhibitor with IC50 of 0.34 uM, without affecting AR protein expression.

VPC-18005 (VPC18005) is a novel small molecule ERG (ETS-related gene) antagonist that inhibits ERG-induced transcription and interacts directly with the ERG-ETS domain, disrupts the ERG binding to DNA (Kd=250 uM).

VPC-80051 (VPC80051) is the first small molecule inhibitor of hnRNP A1 splicing activity, targets RNA-binding domain (RBD) of hnRNP A1.

VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.

VPS34-IN1 is a potent and highly selective Vps34 inhibitor with IC50 of 25 nM invitro,which does not significantly inhibit the isoforms of class I as well as class II PI3Ks.

VR-23 is a Quinoline-Sulfonyl Hybrid Proteasome Inhibitor That Selectively Kills Cancer via Cyclin E–Mediated Centrosome Amplification

VS-5584 (SB2343) is a potent and selective dual PI3K/mTOR inhibitor for mTOR, PI3Kα/β/δ/γ with IC50 of 3.4 nM and 2.6-21 nM, respectively.

VT-1161 is a potent, highly-selective, and oral fungal CYP51 inhibitor with Kd of ≤ 39 nM.

VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM.

VTI-1002 is a potent and specific inhibitor of human (K i = 4.4 ± 2.0 nM) and murine (IC 50 = 179 ± 18 nM) GzmB, with minimal activity (IC 50 > 300 nM) against Cathepsin-G, neutrophil elastase and caspases (−3, −4, −5, −7, −8 and −9). In addition to its high specificity for GzmB, VTI-1002 is retained in murine skin for up to 24 hours and exhibits minimal toxicity in vivo with no observed adverse effects after 30 consecutive days of systemic administration in mice [31]. VTI-1002-mediated GzmB inhibition was first reported to augment type I collagen fibrillogenesis and improve tensile strength in a murine diabetic burn model, notably by preventing decorin cleavage and dermal fibrillar collagen network disorganization.

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

VTX-27 is a selective protein kinase C θ (PKC θ) inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ.

VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.

VU 0365114 is a mAChR M5 positive allosteric modulator, with an EC50 of 2.7 μM.

VU0134992 (VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays; displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV; VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 in Tl+ flux assays; causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment; VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.

VU0152100 is a potent and selective allosteric potentiator of M4 mAChR with an EC50 of 380 ± 93 nM.

VU0155041 is a Potent, positive allosteric modulator/allosteric agonist at mGlu4 receptors (EC50 = 798 and 693 nM at human and rat mGlu4 receptors respectively).

VU0155094 is a potent, selective pan-Group III mGlu positive allosteric modulator with IC50 of 3.43/1.5/0.93 uM for mGlu8/7/4, respectively.

VU0357017 hydrochloride is a highly selective M1 agonists that appear to act at an allosteric site to activate the receptor (EC50 = 477 ± 172 nM; pEC50 = 6.37 ± 0.15).

VU0357121 is a novel allosteric modulator of mGlu5 with EC50 of 33 nM.