YKL-5-124 is a novel potent, selective, and covalent CDK7 inhibitor (IC50=53.5 nM), inhibits CDK7/CycH/MAT1 enzymatic activity with IC50 of 9.7 nM.

OSW-1 is a natural anti-enterovirus and anti-cancer compound that targets oxysterol-binding protein (OSBP) with Ki of 26 and 54 nM for OSBP and ORP4L, respectively.

Bigelovin, a sesquiterpene lactone isolated from Inula helianthus-aquatica, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.

Quillaic acid(Quillaja sapogenin) is the major aglycone of the widely studied saponins of the Chilean indigenous tree Quillaja saponaria Mol; can elicit dose-dependent antinociceptive effects in two murine thermal models.

GDC-0077 is an orally available PI3K inhibitor with potential antineoplastic activity. GDC-0077 is extracted from patent WO 2017001645 A1, formula I.

Natural inducer of apoptosis via Akt/NF-κB signaling suppression

Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 µM and 22.8 µM for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects.

R-7128(Mericitabine) is a selective nucleoside analog inhibitor of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, with activity across all HCV genotypes.

A novel human RBC Cl-conductance blocker (IC50=210 nM) and HERG channel activitor (EC50=79.4 uM, HERG1 channel activation).

WM-3835 is a potent and high-specific HBO1 (KAT7 or MYST2) inhibitor and binds directly to the acetyl-CoA binding site of HBO1 33. WM-3835 activates apoptosis while inhibits osteosarcoma (OS) cell proliferation, migration and invasion. WM-3835 has antitumor activity and potently inhibits pOS-1 xenograft growth in mice.

Centrinone is a selective and reversible inhibitor of polo-like kinase 4 (Plk4), a serine-threonine protein kinase that initiates centriole/centrosome assembly.

KU 0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases.

A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1 respectively.

CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities.

Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts.

Fostamatinib (R788) is a prodrug of the active metabolite R406, which is a potent, ATP-competitive inhibitor of Syk kinase with Ki/IC50 of 30/41 nM.

HG-7-92-01 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 292 nM, displays intermediate selectivity profiles (selectivity score=0.18) against 353 kinases..

Rhodamine 123 is a chemical compound and a dye.

PF-3644022 is a potent and selective, freely reversible, ATP-competitive inhibitor of MAPKAP2 (MK2) with Ki of 3 nM.

Adefovir Dipivoxil(Preveon, Hepsera) works by blocking reverse transcriptase, an enzyme that is crucial for the hepatitis B virus (HBV) to reproduce in the body.

PD-161570 is a selective FGFR inhibitor (IC50 values are 40, 262 and 3700 nM for FGFR, PDGFR and EGFR respectively). PD 161570 had about 5- and 100-fold greater selectivity toward the FGF-1 receptor (IC50 = 40 nM) compared with the PDGFbeta receptor (IC50 = 262 nM) or EGF receptor (IC50 = 3.7 microM) tyrosine kinases, respectively. In addition, PD 161570 suppressed constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture. The results demonstrate a novel synthetic inhibitor with nanomolar potency and specificity towards the FGF-1 receptor tyrosine kinase.

An oxazolidinone antibiotic that possesses potent antimicrobial activity in vitro and in vivo..

JHU37152 is a Designer Receptors Exclusively Activated by Designer Drug (DREADD) agonist with Ki of 1.8 nM and 8.7 nM for human muscarinic acetylcholine M3 receptors (hM3Dq) and hM4Di in vitro, respectively. And EC50 values are 5 nM and 0.5 nM for hM3Dq and hM4Di in fluorescent and BRET-based assays in HEK-293 cells, respectively.,hM4Di [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM3Dq [1](Cell-free assay) hM4Di [1](Cell-free assay) 0.5 nM(EC50) 1.8 nM(Ki) 5 nM(EC50) 8.7 nM(Ki),JHU37152 is a potent DREADD agonist with high potency and efficacy in fluorescent and BRET-based assays in HEK-293 cells, whereas no responses are observed in untransfected HEK-293 cells.[1],JHU37152 exhibits high in vivo DREADD potency. JHU37152 exhibits selective [3H]clozapine displacement from DREADDs in brain tissue from WT and D1-DREADD mice.[1]

AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.

PD166285 (PD 0166285) is a broad-spectrum receptor tyrosine kinase (RTK) inhibitor that inhibits PDGFR-β, EGFR, and FGFR1 and c-Src with IC50 of 7-85 nM.

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.

Tadalafil is a potent and selective inhibitor of Phosphodiesterase-5 (PDE5) This compound prevents the breakdown of phosphodiesterases, many of which are used as secondary messengers. By preventing the breakdown of these messenger molecules, tadalafil can

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).

FTI 277 HCl is the methyl ester of FTI 277, which is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I.