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

Teglicar, in vitro and in animal models, reduces gluconeogenesis and improves glucose homeostasis, refreshing the interest in selective and reversible L-CPT1 inhibition as a potential antihyperglycemic approach.

NBD-556 is small molecule mimetic of CD4, NBD-556 recognizes the HIV-1 envelope protein gp120 and induces restructuring of gp120 analogous to CD4 binding.

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

AG-120 is a first-in-class, orally available, selective, potent inhibitor of the mutated IDH1 protein.

FLT3/AXL inhibitor

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

ABT-263 (Navitoclax) is a potent inhibitor of Bcl-xL, Bcl-2 and Bcl-w with Ki of ≤ 0.5 nM, ≤1 nM and ≤ 1 nM, respectively.

BMS-779788(XL652) is a novel small-molecule modulator of the Liver X Receptor (LXR), a nuclear hormone receptor implicated in a variety of cardiovascular and metabolic disorders.

BVT 14225 is a new selective 11b-HSD1 inhibitor, it belongs to a class of arylsulfonamidothiazoles with in vitro and in vivo antidiabetic effects

CC-115 is a dual inhibitor of DNA-dependent protein kinase (DNA-PK) and mammalian target of rapamycin (mTOR), with potential antineoplastic activity.

Cobicistat (GS-9350) is a potent and selective inhibitor of CYP3A with IC50 of 30-285 nM.

Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.

BMS-986205 is an optimized indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor, is well tolerated with potent pharmacodynamic activity, alone and in combination with nivolumab in advanced cancers in a phase 1/2a trial

Lemborexant (E-2006) is a dual antagonist of the orexin OX1 and OX2 receptors which is under development for treatment of insomnia.

LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.

Epalrestat is an orally active aldose reductase inhibitor that acts on diabetic neuropathy.

GSK 525762A is a potent small molecule inhibitors that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4).

Repotrectinib(TPX-005) is a multi-target macrocycle inhibitor of anaplastic lymphoma kinase (ALK), c-ros proto-oncogene 1 receptor tyrosine kinase (ROS1), and neurotrophic tyrosine kinase receptor (TRK)

Ispinesib (SB 715992) is a potent mitotic kinesin KSP (Eg5) inhibitor with a Ki and an IC50 of 0.6 and 4.1 nM, respectively.

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.

AZD7762 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM; equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck.

MK 0524 is a potent, selective DP1 receptor antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.

Idarubicin Hcl is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor.

Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM, and CDK7 with IC50 of 300 nM.