Novel profluorescent RAMOSUS3 (RMS3) probe with strigolactone-like bioactivity

Potent and selective 5-HT2 serotonin receptor agonist

Inhibitor of ADP-induced platelet aggregation; anti-thrombotic

Novel potassium channel opener

Novel angiogenesis inhibitor, regulating endothelial cell fate and angiogenesis

Novel probe for mycobacterial and fungal carbonic anhydrase

Catecholamine-depleting agent, actively against the 3 major monoamines in the CNS

Novel potent anti-malarial agent against multiple resistant strains of P. falciparum in vitro and show no cytotoxicity to mammalian cells

Folate-PEG2-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Folate-PEG3-amine is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

A potent and selective Adenosine receptor A2A agonist

Seletalisib (UCB5857) is potent and selective PI3Kδ inhibitor with an IC50 of 12 nM.

A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor.

LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.

JMV 2959 (AEZS-123) is a potent ghrelin receptor (GHS-R1A) antaognist with binding IC50 of 32 nM.

Nutlin-3a is arbitrarily referred to as enantiomer a because it appears as the first peak from chiral purification of racemic nutlin-3 and its absolute stereocenter assignment is not known.

IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma.

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2.

PF-03758309 is an orally bioavailable small-molecule inhibitor of p21-activated kinase 4 (PAK4) with potential antineoplastic activity.

CWHM-12 a novel small molecule inhibitor of αV integrins with IC50s of 1.8/0.8/1.5/0.2 nM for αvβ1/αvβ3/αvβ8; less potency on αvβ5(IC50=61 nM) and on inhibition on αIIbβ3/α2β1/α10β1.

Fmk is an irreversible ribosomal S6 kinase inhibitor 1/2 inhibitor.

A-366 is a potent and selective G9a/GLP histone lysine methyltransferase inhibitor (IC50 = 3.3 nM).

Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.

CFI-400945 is a potent, highly selective PLK4 inhibitor with Ki of 0.26 nM and IC50 of 2.8 nM, does not significantly inhibits PLK1/2/3 at 50 uM; causes dysregulated centriole duplication, mitotic defects, and cell death in multiple cancer cell lines (A549 GI50=5 nM, OVCAR-3 GI50=18 nM); significantly inhibits human cancer xenografts; causes polyploidy, growth inhibition, and apoptotic death of murine and human lung cancer cells, despite expression of mutated KRAS or p53, produces supernumerary centrosomes and mitotic defects in lung cancer cells.

Birinapant (TL32711) is a SMAC mimetic antagonist, mostly to cIAP1 with Kd of <1 nM, less potent to XIAP.

GDC-0973 is a potent, highly selective inhibitor of mitogen-activated protein kinase kinase, also known as MEK, a serine/threonine kinase that is a component of the RAS/RAF/MEK/ERK pathway.

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with mean EC50 of 0.43 nM against a panel of 75 RSV A and B clinical isolates.

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

Deltarasin is a novel and small molecule inhibitor which can inhibit the KRAS-PDEδ interaction(Kd= 41 nM. binding to PDEδ) and impairs oncogenic KRAS signalling.

EPZ-005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases.