PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

PF-05175157 is a potent and selective inhibitor of both acetyl-CoA carboxylase isoform ACC1 located primarily in liver and adipose tissue and isoform ACC2 dominant in skeletal and heart muscle, with IC50 values of 27 nM and 33 nM, respectively.

AM-2394 is a potent and selective Glucokinase agonist (GKA), which catalyzes the phosphorylation of glucose to glucose-6-phosphate.

MGL-3196 is a potent and highly selective thyroid hormone receptor β agonist in clinical trials for the treatment of dyslipidemia.

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

Amcasertib(BBI503) is an orally administered investigational agent designed to inhibit cancer stem cell pathways, including Nanog, by targeting stemness kinases.

E-7050 is hepatocyte growth factor receptors (HGFR).

MK-3102 (MSD) is a novel DPP-4 Inhibitor, which improves glycaemic control with low risk of symptomatic hypoglycaemia.

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.

Apilimod(STA 5326) is a potent IL-12/IL-23 inhibitor, IL-12 production in cultures of IFN-r/LPS–stimulated human PBMCs is strongly inhibited by STA-5326 with an IC50 of 10 nM.

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

BMS-986195 is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK).

Lipoic acid is a selective, small molecule large-conductance Ca(2+)-activated K(+) channel (BKCa, KCa1.1, MaxiK) positive modulator with EC50 of 11 uM. Lipoic acid shows a favorable selectivity profile on Nav, Cav, SK, and IK channels. Lipoic acid causes distinct activation from a concentration of 0.3 and 10 µM Lipoic acid left-shifted the voltage activation curve by 60 mV. Lipoic acid reduces spontaneous phasic contractions in guinea pig urinary bladder strips at 1 uM, while having only a modest effect on contractions evoked by electrical field stimulation (EFS) and no effect on high K+-induced contractions.

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.

GBT-440(Voxelotor) is a novel small molecule hemoglobin modifier which increases hemoglobin oxygen affinity.

AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism.

Cinacalcet(AMG-073) is an orally active, second-generation calcimimetic compound; AMG 073 represents a new class of compounds for the treatment of hyperparathyroidism.

AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.

Bexagliflozin is a potent and selective SGLT2 inhibitor with IC50 value of 5.6 μM /2 nM in SGLT1 /SGLT2 respectively.

GYKI 52466 dihydrochloride is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant.

PD 123319 is a potent, selective AT2 angiotensin II receptor antagonist with IC50 of 34 nM.

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.