Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

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

T863 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor

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.

PF-06928215 (PF06928215) is a high affinity Cyclic GMP-AMP synthase (cGAS) inhibitor with Kd of 200 nM, IC50 of 4.9 uM.

RBN013209 is a potent CD38 inhibitor and is useful in the treatment of cancer.

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

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

E3L-4133, also known as E3 ligase Ligand 5, is an E3 ligase Ligand that can be used in PROTAC (proteolysis targeting chimera) technology to engage an E3 ubiquitin ligase. PROTAC is a two-headed molecule capable of removing specific unwanted proteins. E3L-4133 has CAS#1264754-13-3. The last 4 digits was used for name.

G10 (STING Agonist 1) is a novel human-specific STING agonist.

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

TH5487 (TH-5487, TH 5487) is a potent, selective, active-site inhibitor of 8-oxoguanine DNA glycosylase 1 (OGG1) with IC50 of 342 nM, prevents OGG1 from binding to its DNA substrate.

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

Endovion (NS 3728, SCO-101) is an potent anion channel inhibitor that blocks the Volume Regulated Anion Channels (VRAC).

NS 11021 is an activator of large-conductance Ca2+-activated potassium channels (BKCa, KCa1.1).

RS-1 is a stimulator of the human homologous recombination protein RAD51,enhances homology-directed repair ~2 to 5-fold and increases CRISPR-mediated knock-in efficiencies in vitro and in vivo.

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.

Bindarit exhibits selective inhibition against monocyte chemotactic proteins MCP-1/CCL2, MCP-3/CCL7 and MCP-2/CCL8.

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

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).

UCB9608 is a Potent, Orally Bioavailable PI4KIIIβ Inhibitor.

CEP33779(< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5(pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells.

AS 602801(Bentamapimod) is a novel, orally active inhibitor of JNK.

Rhonin is a first small-molecule ligand of the RHO GDP-dissociation inhibitor 1 (RHOGDI1), binds to RHOGDI (Ki=2.2 uM), is an inhibitor of Hh-induced osteogenesis.Rhonin interferes with its function by disrupting the interaction between RHOGDI and RHO GTPases.Rhonin alters the subcellular localization of RHO GTPases.Rhonin inhibited RHOGDI1-mediated extraction of RAC1 from liposomes, Rhonin increased the levels of GTP-bound RHO GTPases, did not alter the total levels of the three RHO GTPasesRhonin an inhibitor of Hh-induced osteogenesis, but does not efficiently target canonical Hh signaling and SMO, directly targets RHOGDI, impairs RHOGDI function.

KAL-21404358 (KAL21404358) is a small-molecule, allosteric inhibitor of K-Ras(G12D), binds to K-Ras(G12D) P110 site with KD of 88 uM in MST assay; KAL-21404358 disrupts the K-RasG12D-B-Raf interaction using a NanoBiT split luciferase assay, and to impair the Raf-MEK-ERK and the PI3K-AKT signaling pathways. KAL-21404358 exhibited specificity for K-RasG12D over K-RasWT, H-RasWT, Rap1a, R-Ras and R-Ras2.

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.