GDC-1971 showed outstanding potency in biochemical and cell models, and it had a predicted human PK profile that suggested it would achieve target engagement at reasonable doses. GDC-1971 showed an IC50 below the limit of detection of the assay (≪0.001 μM), while that IC50 shifted to 0.17 μM in the same biochemical assay with the constitutively active E76K SHP2 mutant.

diABZI STING agonist-1 is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM for human and mouse, respectively.

TUG-891 is a potent and selective agonist of GPR120 with pEC50 values of 7.36 and 7.77 for human and mouse GPR120, respectively.

GW 4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.

BS-181 is a highly selective CDK7 inhibitor with IC50 of 21 nM. ; >40-fold selective for CDK7 than CDK1, 2, 4, 5, 6, or 9.

MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. generation of catalytically active enzyme.

CP-640186 is an isozyme-nonselective acetyl-CoA carboxylase inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively.

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.