GCPII-IN-1 TFA is a glutamate carboxypeptidase II (GCPII, or PSMA) inhibitor scaffold with a Ki of 44.3 nM.

Sterculic acid is a stearoyl-CoA desaturase-1 (SCD1) inhibitor. Sterculic acid specifically inhibits the delta-9 desaturase (Δ9D) activity with an IC50 value of 0.9 μM.

NSC74429 is a CNS-active, small molecule PHLPP inhibitor with IC50 of <5 uM, shows neuroprotective activity in primary rat cortical neurons in STS assay.

GSK-484 is a potent, highly selective and reversible protein arginine deiminase PAD4 inhibitor with IC50 of 80 nM in FP binding assay (0.2 mM Ca), 50 nM in PAD4 NH3 release inhibition assay.

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.

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.

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

ZED3197 (ZED-3197) is a novel peptidomimetic direct-acting, potent and selective inhibitor of human FXIIIa, inhibits human plasma derived FXIII‐A2B2 and the recombinant cellular form (FXIII‐A2) with IC50 of 10 and 14 nM, respectively.ZED3197 strongly blocks FXIII‐A2 from mouse, rat, rabbit, dog, and cynomolgus monkey (IC50 8-30 nM), is a significantly weaker inhibitor of FXIII‐A2 from pig (IC50=220 nM).ZED3197 displays 20‐fold to 3000‐fold selectivity against human transglutaminases TG1, TG2, TG3, and TG7.ZED3197 prolonged clot formation, reduced clot firmness, and facilitated clot lysis in whole human blood without affecting the clotting time, indicating minimal impact on hemostasis.ZED3197 effectively decreased the weight of clots and facilitated flow restoration without prolongation of the bleeding time in vivo.

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM.

(+)-Narwedine. Galantamine(Narwedin) is a competitive and reversible cholinesterase(AChE) inhibitor.

CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.

GKT136901 is a potent, selective and orally active inhibitor of NADPH oxidase (NOX1/4), with Kis of 160 and 165 nM, respectively. GKT136901 also is a selective and direct scavenger of peroxynitrite. GKT136901 can be used for the research of diabetic nephropathy, stroke, and neurodegeneration. GKT136901 also has anti-inflammatory activity.

Prinomastat (AG3340) is a potent, selective MMP inhibitor with pM affinities for inhibiting gelatinases (MMP-2 and -9, Ki=50-150 pM), MMP-14 and MMP-13; demonstrates broad antitumor activity in a number of tumor models, inhibits glioma invasion or growth of the human malignant glioma cell line U87; also suppresses tumor growth in a malignant glioma tumor model.

Atabecestat (JNJ-54861911, JNJ54861911) is a novel potent, oral beta-secretase (BACE) inhibitor for treatment of Alzheimer's Disease.

NAMPT activator (NAT) is a potent, small molecule activator of nicotinamide phosphoribosyltransferase (NAMPT) with ITC KD of 500 nM.

MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.

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

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.

Prostaglandin D2 (PGD2) is one of the major PGs actively produced in the brain of various mammals. Prostaglandin D2 is one of the most potent endogenous sleep promoting substances. PGD2 plays a protective role by suppressing inflammation.

TDI-11861 is second-generation soluble Adenylyl Cyclase (sAC, ADCY10) inhibitor with slow dissociation rates. TDI-11861 inhibits sAC cellular with an IC50 value of 5.5 nM.

Dnp-PLG-Cys(Me)-HA-DArg-NH2 is a peptide substrate for matrix metalloproteinase-1 (MMP-1).It has an improved kcat/Km ratio compared with the MMP-1 flurogenic substrate Dnp-PLGLWA-DArg-NH2.

MMP-3 inhibitor is a peptide inhibitor of matrix metalloproteinase-3 (MMP-3) with a Ki value of 95 nM.

Ribavirin carboxylic acid (TR-COOH) is a metabolite of ribavirin, ribavirin has strong antiviral activity.

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

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

(2E)-OBAA is a potent phospholipase A2 (PLA2) inhibitor, with an IC50 of 70 nM. (2E)-OBAA induces apoptosis of HUVEC cells. (2E)-OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei, with an IC50 of 0.4 μM.

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