Alobresib is a novel BET bromodomain inhibitor with antineoplastic activity..

ML417 is a Highly Selective D3 Dopamine Receptor Agonist. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors. Screening of ML417 against multiple G protein-coupled receptors revealed exceptional global selectivity. Molecular modeling suggests that ML417 interacts with the D3R in a unique manner, possibly explaining its remarkable selectivity. ML417 was also found to protect against neurodegeneration of dopaminergic neurons derived from iPSCs.

NE 10790, a poor farnesyl pyrophosphate synthase inhibitor, is a phosphonocarboxylate analogue of the potent bisphosphonate risedronate and is a weak antiresorptive agent.

AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.

JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities.

STING agonist-3, compound 3, is a selective and non-nucleotide small-molecule STING agonist, which has durable anti-tumor effect and tremendous potential to improve treatment of cancer.

diABZI STING agonist-1 (trihydrochloride) is a selective stimulator of interferon genes (STING) receptor agonist.

MYCMI-6 (NSC354961) is a selective, high affinity inhibitor of MYC-MAX interaction, blocks MYC-driven transcription and binds selectively to the MYC bHLHZip domain with Kd of 1.6 uM in SPR assay.

BL-918 is a small molecule activator of ULK1 with EC50 of 24 nM (243% kinase activity at 100 nM), induces autophagy via the ULK complex in SH-SY5Y cells.

1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.

MYCi361, also known as NUCC-0196361, is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 suppresses tumor growth and enhances anti-PD1 immunotherapy.

A potent, selective 5-HT2A receptor antagonist with Ki of 0.36 nM, > 80-fold selectivity for 5-HT2A over other serotonergic receptors.

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).