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.

SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively. SGL5213 has potential to treat type 2 diabetes treatment.

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

CL27c is a cell-permeable, inhaled lipophilic ester prodrug of CL27e, which is a potent, selective pan-class I PI3K inhibitor, CL27c is inactive in PI3K enzymatic assay, once inside the cytoplasm, CL27c is metabolized by unspecific esterases into CL27e.

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.

Sephin1 is a selective inhibitor of stress-induced PPP1R15A and targets disease associated with accumulation of misfolded protein.

RMC-4630 is a potent and selective inhibitor of SHP2, a central node in the RAS signaling pathway.

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).

PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels.

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.

CG-806 (CG806, CG'806) is a novel potent, pan-FLT3/BTK multi-kinase inhibitor with impressive inhibition of leukemic cell proliferation with IC50 at sub-nanomolar or low nanomolar levels.

TBAJ-587 is a potent anti-tuberculosis agent. TBAJ-587 inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. BAJ-587 has more potent activity against M. tuberculosis and better efficacy in animal models of TB.

PF-4211 is a potent D1 receptor agonist.

PF-06256142 (PF06256142) is a potent and selective orthosteric agonist of the D1 receptor with EC50 (cAMP) of 33 nM, shows exquisitely selectivity over D2.

VU0652835 is a metabotropic glutamate receptor subtype 5 (mGlu5) negative allosteric modulator with an IC50 of 81 nM.

VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration.

NVR 3-778 (NVR3-778, NVR 3778) is a small molecule inhibitor of HBV replication that targets the viral core protein, a first-in-class capsid assembly modulator.

MDL-800 is a first-in-class cellularly active SIRT6 allosteric activator.

Osimertinib analogue (C-005) is a potent EGFR inhibitor, which is 2-5 fold more selective than Osimertinib between above EGFR mutants and wild-type EGFR(A431) cells.

YLT-11 is a novel and specific PLK4 inhibitor with IC50 of 22 nM and Kd of 5.2 nM.

LRRK2 inhibitor 18(Compound 18) is a potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 4.1 nM.

S18-000003 (S18-000003) is a potent, selective, orally bioavailable RORγt inhibitor with IC50 of 29 nM (hRORγt, GAL4), shows no significant activity against RORα, RORβ and LXRα/β(IC50>10 uM).

TP0438836 is a potent, low-absorbable sodium-dependent glucose cotransporter (SGLT) inhibitor with IC50 of 28 nM/7 nM for hSGLT1 and hSGLT2, respectively.

AM-0466 is a potent and selective NaV1.7 Inhibitor (Nav 1.7 IC50 = 21 nM; Nav 1.5 IC50 =>30.0 uM. PXR = 22% @10 uM; CYP 2C9 IC50 = 4.6 uM; CYP3A4 TDI IC50 =>50.0 uM.).

GSK2646264 (GSK-2646264) is a potent, selective Spleen Tyrosine Kinase (Syk) inhibitor with pIC50 of 7.1, >300-fold selectivity over Autota B; inhibits anti-IgM induced Erk1/2 phosphorylation in Ramos B cells with pIC50 of 6.7.

DK419 (DK-419) a potent, orally acitve inhibitor of Wnt/β-catenin signaling with IC50 of 0.19 uM in Wnt3A-stimulated TOPFlash assays.