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

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

VTP-43742 (VTP43742) is a highly potent, selective, oral RORγt inverse agonist for the treatment of autoimmune disorders, including multiple sclerosis and psoriasis..

VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.

VX-702 is a highly selective inhibitor of p38 MAPKα with IC50 of 4-20 nM.

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

VX-809 is a CFTR modulator with EC50 of 0.1 μM.

WAY-362450 (XL335; Turofexorate isopropyl) is a highly potent, selective, and orally active farnesoid X receptor (FXR) agonist with an EC50 of 4 nM.WAY-362450 is useful for dyslipidemia.

Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist.

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.

XL647 is a novel spectrum-selective kinase inhibitor for EGFR, ErbB2, KDR, Flt-4 and EphB4 with IC50 of 0.3 nM, 16 nM, 1.5 nM, 8.7 nM and 1.4 nM, respectively.

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

Zafirlukast(Accolate)

Zanamivir is an influenza viral neuraminidase inhibitor with IC50 values of 0.95 nM and 2.7 nM for influenza A and B, respectively.

Zatebradine hydrochloride is a bradycardic agent that creates use-dependent inhibition of hyperpolarization-activated current (If) in sinoatrial node cells (EC50 = 480 nM) and Purkinje fibres.

Zatebradine(UL-FS49) is a potent HCN channels antagonist, which decreased the heartbeat in a reversible manner; 92% inhibition of the hHCN1-mediated current at 10 uM.

Zaurategrast(CDP-323) is an oral α4-integrin inhibitor.

Zibotentan (ZD4054) is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

Ziprasidone HCl

ZLN024 Hcl is a novel AMPK allosteric activator; activated α1β1γ1 and α2β1γ1 by around 2–2.5 fold with an EC50 of about 1–2 uM. IC50 value: 1-2 uM (EC50) [1] Target: AMPK activator ZLN024 activated AMPK in L6 myotubes and stimulated glucose uptake and

ZM-447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively.

Zoliflodacin (ETX0914;AZD0914) is a novel spiropyrimidinetrione bacterial DNA gyrase/topoisomerase inhibitor.

ZSTK474 is a potent pan-class I PI3K inhibitor with IC50 of 37 nM.

Mosapride citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

Theliatinib (HMPL-309) is a novel small molecule, EGFR tyrosine kinase inhibitor with potential antineoplastic and anti-angiogenesis activities.

Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ～1 nM.

Aviptadil (INN) is an analog of vasoactive intestinal polypeptide (VIP) for the treatment of erectile dysfunction,showed potent activity against COVID-19(SARS-COV-2).

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM.

AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.

Go6976 is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.

GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity.

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

FOY 251 is a metabolite of Camostat and a pollen protease inhibitor for prevention and control of allergy.

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

Deforolimus(AP23573; MK-8669; Ridaforolimus) is a selective mTOR inhibitor with IC50 of 0.2 nM; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. IC50 value: 0.2 nM [1] Target: mTOR in vitro: Treatment of HT

Tacalcitol is a synthetic vitamin D3 analog. This compound has been shown to regulate calcium levels and induce nerve growth factor production in epidermal keratinocytes. Additionally, Tacalcitol has been noted to promotes normal bone development by regul

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)

Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.

MK-0752 is a moderately potent γ-secretase inhibitor, which reduces Aβ40 production with IC50 of 5 nM. Phase 1/2.

Q203 is a promising new clinical candidate for the treatment of tuberculosis.

Selpercatinib is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 163, has an IC50 of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M) , and RET (G810R), respectively. Antineoplastic activity.

TAS-116 is a highly selective inhibitor of heat shock protein 90α and β, demonstrates potent antitumor activity and minimal ocular toxicity in preclinical models.

Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of  0.62 nM, which used in the treatment of adults with essential hypertension.

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.

BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).

Camostat mesylate is a synthetic, orally bioavailable is a serine protease inhibitor. Used for the treatment of chronic pancreatitis. It attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity.

ZLN005 is a novel transcriptional regulator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).

RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.

SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 uM.

Selonsertib（GS-4997）is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

Ceralifimod is selective, high potent agonist for sphingosine 1-phosphate receptors 1 and 5, with EC50s of 27.3, 334 pM for human S1P receptor 1 and 5, respectively.

BAF312 is a potent and selective agonist of S1P with EC50 value of 0.39nM for S1P1 receptors and 0.98nM for S1P5 receptors, respectively

GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM.

CP-945598 HCl is a potent and selective cannabinoid type 1 receptor antagonist with Ki of 0.7 nM.

Remdesivir is a novel RNA-dependent RNA Polymerase,(RdRp) inhibitor. The purity of remdesivir>99.8%,signal impurity<0.05%.

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).

Furin inhibitor I is a selective, irreversible, and cell-permeable competitive inhibitor of proprotein convertases, including furin/SPC1 (Ki = ~1 nM), SPC2/PC2 (Ki = 0.36 nM), SPC3/PC1/PC3 (Ki = 2.0 nM), SPC4/PACE4 (Ki = 3.6 nM), SPC6/PC5/PC6, and SPC7/LP

DX600 is a potent and selective peptide inhibitor of angiotensin-converting enzyme 2 (ACE2; Kis = 2.8, 200, and 1,200 nM for recombinant, human, and murine ACE2, respectively).

Inhibitor of furin (Ki values are 0.106, 0.58 and 13.2 μM for furin, PACE4 and PC1 respectively).

SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits

A Arbidol analog which showed affinity against both H3 (1150-fold) and H1 (98-fold) hemagglutinin subtypes than Arbidol.

Molnupiravir, also known as EIDD-2801 and MK-4482, is an orally bioavailable form of a highly potent ribonucleoside analog that inhibits the replication of multiple RNA viruses including SARS-CoV-2, the causative agent of COVID-19. EIDD-2801 has been show

Carolacton is a novel MTHFD1 inhibitor,an antibacterial compound,also showed potent activity against COVID-19(SARS-COV-2).

SBP1(spike-binding peptide 1) is a first-in-class peptide binder to the SARS-CoV-2 spike protein. SBP1 specifically binds SARS-CoV-2-RBD with low nanomolar affinity. SBP1 to the RBD was determined to be 47 nM with the average Kon = 4.69*104M-1S-1 and Koff

Biotin modification of SBP1.SBP1(spike-binding peptide 1) is a first-in-class peptide binder to the SARS-CoV-2 spike protein. SBP1 specifically binds SARS-CoV-2-RBD with low nanomolar affinity. SBP1 to the RBD was determined to be 47 nM with the average Kon = 4.69*104M-1S-1 and Koff=2.2*10-3.The interaction between SBP1 and the RBD of SARS-CoV-2 spike protein was validated by bio-layer interferometry. The KD, derived from protein association and dissociation kinetics, was found to be 47 nM after averaging the fitting values at different protein concentrations. The amino acid sequence of SBP1 is entirely derived from human ACE2 and should be recognized as endogenous by the human immune system. This feature could be highly beneficial in later stages of pre-clinical development.

GRP-60367 is a first-in-class direct-acting RABV inhibitor with EC50 from 2 to 52 nM (different host cell lines) that blocks RABV G protein-mediated viral entry.

WP-1122(WP 1122) is a candidate drug to treat SARS-COV-2(COVID-19) .2-DG completely prevented SARS-CoV–2 replication in Caco–2 cells. Glycolysis is a process by which cells convert glucose into energy and infected (host) cells are induced by viruses to dramatically increase their dependence on glycolysis. WP1122 is a prodrug of 2-DG whereby chemical elements are added to 2-DG to improve its delivery in vivo.

S enantiomer of Hydroxychloroquine. Hydroxychloroquine is a potent drug for the COVID-19 trement.

R enantiomer of Hydroxychloroquine. Hydroxychloroquine is a potent drug for the COVID-19 trement.

AT-511, the free base form of AT-527, against several coronaviruses, including SARS-CoV-2, the causative agent of COVID-19. In normal human airway epithelial (HAE) cell preparations, the average concentration of AT-511 required to inhibit replication of S

AT-527(Bemnifosbuvir hemisulfate), a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. AT-527 is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC90=0.47 μM). Bemnifosbuvir hemisulfate has pangenotypic antiviral activity[1][2][3].Bemnifosbuvir hemisulfate has pan-genotypic antiviral activities that inhibits HCV genotype 1a (HCV GT1a), HCV GT1b, HCV GT2a, HCV GT3a, HCV GT4a, and HCV GT5a replication with EC50 values of 12.8 nM, 12.5 nM, 9.2 nM, 10.3 nM, 14.7 nM, and 28.5 nM, respectively[1]. In normal human airway epithelial cells, the concentration of Bemnifosbuvir hemisulfate required to inhibit replication of SARS-CoV-2 by EC90 is 0.47 μM, very similar to its EC90 against HCoV-229E, HCoV-OC43 and SARS-CoV in Huh-7 cells[2].When given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg or 300 mg/kg), Bemnifosbuvir hemisulfate preferentially delivers high levels of AT-9010 in the liver in vivo[1].

FOY 251 is a metabolite of Camostat and a pollen protease inhibitor for prevention and control of allergy.

Sisunatovir (RV521), an orally available inhibitor of the RSV fusion (RSV-F) protein, exhibits potent efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses, with IC50s of 1.4 nM and 1.0 nM, respectively.

Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clinical isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclinical species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers experimentally infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization.

GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM.

PF00835231(SARS-CoV-2 inhibitor 5h) is areversible-covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 4.2 µM. Compound 5h blocks the infectivity and cytopathicity of the virus with high potency and without any detectable cytotoxicity even at 200 µM.PF-00835231 is a potent inhibitor of CoV-2 3CLpro with IC50 of 4 nM and shows suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.