Novel metabotropic glutamate receptor 5 positive allosteric modulator

Novel selective inhibitor of collagen prolyl 4-hydroxylase, neither causing general toxicity nor disrupting iron homeostasis

SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

Novel type II α2/α4 Subtype-Selective Positive Allosteric Modulator (PAM) of Nicotinic Acetylcholine Receptors Acting From the C-tail of an α Subunit.Reference:1) A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Rec

Novel Activator of Satellite Cell Proliferation and Enhance Repair of Damaged Muscle

A potent c-Src inhibitor

Potent, selective and reversible inhibitor of human and canine stomach-derived acetylcholinesterase (AChE)

Novel proteasome inhibitor, inducing human myeloid tumor-selective apoptosis

Cytokine release inhibitor, inhibiting production of IL-1ß, IL-8, IL-6, IL-10 and TNFalpha

An inducer for Cell Apoptosis Through JNK and ERK1/2 Signaling Pathways in Colon Cancer Cells

Bioavailable metabolite of the prodrug GW5638 as an antiestrogen thought to promote degradation of Er?

Selective group I mGlu receptor agonist

Novel potent inhibitor of the lysophospholipase autotaxin

Potent inhibitor of SUV420H1 (IC50 = 25 nM) and SUV420H2 (IC50 = 144 nM), a closely related pair of proteins which catalyze the di- and tri-methylation of H4K20

The first potent biased small molecule agonist at the apelin receptor, increasing cardiac contractility in vivo

Novel class of noncompetitive NR2C/D subunit-selective N-methyl-D-aspartate(NMDA) receptor antagonist

Novel Inhibitor of the Disordered Protein, p27(Kip1)

A novel potent, selective and cell permeable inhibitor of BET bromodomain

Irreversible inhibitor of amiloride-sensitive Na channels; derivative of amiloride

Negative control for GSK'963 (AOB9775). Novel highly potent and selective RIP1 inhibitor

Strong neuroleptic agent, showing no cataleptic effect and antagonism against apomorphine

Potent inhibitor of LpxC and lipid A biosynthesis

A potent, irreversible, type II inhibitor against FGFR (IC50 = 2.6, 2.6, 5.6, 9.2 nM, respectively, against FGFR1-4) whose 4-acrylamidebenzyl moiety covalently modifies FGFR P-loop cysteine in its DFG-out conformation with good target selectivity based on

Novel potent and selective reversible KDM1A inhibitor and Lysine-specific demethylase 1 (LSD1)-specific inhibitor

Novel modulator of the UNC119-Cargo Interaction, potently and selectively inhibiting the binding of a myristoylated peptide representing the N-terminus of Src kinase to UNC119A

Potent and selective antagonist of the 5-HT1A receptor

Long acting potent steroidal progestin

Novel inhibitor of the cytosolic enzyme N-glycanase 1 (NGLY1, the human PNGase), inactivating the transcription factor Nrf1 and potentiating proteasome inhibitor cytotoxicity

Novel CXCR4 antagonist

Selective estrogen receptor modulator (SERM), inhibiting mammalian PLD (PLD1 and PLD2)

A picolinic acid derivative isolated from various Fusarium species.

The only known preferential antagonist for P2Y(AC) receptor; this is the platelet ADP receptor that is coupled to adenyl cyclase and is also referred to as the P2Y ADP receptor.

Novel subtilisin kexin isozyme-1/site-1 (SKI-1/S1P) protease inhibitor

Yoda1 analogue, antagonizing Yoda1-evoked activation of Piezo1 and aortic relaxation.

Used experimentally as a beta blocker and clinically as a strong vasodilator with the noted side effects of reduced systolic, diastolic and mean arterial pressure.

NMDA antagonist acting at the polyamine site; Neuroprotective agent; α-Adrenergic central and peripheral vasodilator; α2 adrenergic receptor ligand

Prodrug of Fenclonine as a selective and irreversible inhibitor of tryptophan hydroxylase

Novel highly potent, selective, and irreversible GSTP1 inhibitor

Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.

Antagonist of the actions of ethanol, attenuating the ethanol-induced reduction in cerebellar cyclic guanosine monophosphate (cGMP) content, but significantly elevating cGMP levels when given alone

Suicide substrate for serine proteases, irreversibly inactivating human leukocyte (HL) elastase, porcine pancreatic (PP) elastase, and chymotrypsin

Dopamine antagonist; Antipsychotic agent

Neutral retinoic acid receptor (RAR) α-selective antagonist

CID 2745687 is a competitive, reversible antagonist of the orphan receptor GPR35.