BRL-50481 is a novel and selective inhibitor of phosphodiesterase (PDE) 7 with a Ki value, derived from secondary (Dixon) plots, of 180±10 nM, being at least 200-fold selective for hrPDE7A1 over all other PDEs.

Eprobemide is a non-competitive reversible inhibitor of monoamine oxidase A.

JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.

VU 0238429 is positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5), with an EC50 of 1.16 μM.

A potent, orally-active MEK1/2 inhibitor with IC50 of 10-100 nM.

A potent glutaminyl cyclase (QC) inhibitor with Ki of 60 nM.

A novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM.

A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM.

QStatin is a novel, potent, and selective Vibrio quorum sensing (QS) inhibitor, shows pan-QS inhibitor activity in diverse Vibrio species.

HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of~9 μM.

BTZO-1 is a cardioprotective agent and Macrophage migration inhibitory factor (MIF) activator, binds to MIF with Kd of 68.6 nM, regulates ARE-mediated gene expression.

A potent and selective inhibitor of PDGFR with IC50 of about 0.4 uM both in vitro and in cells.

Cavosonstat is a potent, orally bioavailable inhibitor of S-nitrosoglutathione reductase (GSNOR) and CFTR modulator.

Mca-PL is a fluorogenic peptide that has been used as a building block in the synthesis of Mca-PLGL-Dpa-AR-NH2, a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) and MMP-7.

Tegobuvir (GS-9190; GS 333126) is a non-nucleoside nonstructural protein (NS)5B polymerase inhibitor.

4E2RCat is an inhibitor of eIF4E-eIF4G interaction with an IC50 of 13.5 μM.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

A potent, functionally selective TSH receptor (TSHR) positive allosteric modulator with EC50 of 11.6 uM (β-Arr 1 translocation).

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.

Vatalanib (PTK787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 1/2.

ARA-290 (Cibinetide) is a non-erythropoietic erythropoietin (EPO) derivative.

SC-236 (SC58236) is a potent, selective, orally active inhibitor of COX-2 with IC50 of 10 nM.

AA26-9 is a potent and broad spectrum serine hydrolase inhibitor.

AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

Conivaptan(YM 087) is a non-peptide inhibitor of antidiuretic hormone (vasopressin receptor antagonist) with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. Silodosin causes practically no orthostatic hypotension (in contrast to other α1 blockers). Since Silodosin is a highly selective inhibitor of the α1A adrenergic receptor, it ca

A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist.

Filastatin is a long-lasting inhibitor of Candida albicans filamentation. Filastatin inhibits adhesion by multiple pathogenic Candida species with an IC50 of ~3 μM in the GFP-based adhesion assay. Filastatin inhibits fungal adhesion to polystyrene and human cells, the yeast-to-hyphal morphological transition, induction of the hyphal-specific HWP1 promoter. Filastatin has potent antifungal effect.

A cytotoxic agent used in antibody-drug conjugates

TAK-981 is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities[1].