Tat-NR2B9c (NA-1) is a neuroprotective agent.

VVD-214 (RO7589831) is a synthetic lethal allosteric inhibitor of WRN helicase. VD-214 covalently engages cysteine 727 of WRN in a nucleotide cooperative manner and inhibits ATP hydrolysis and helicase activity, resulting in widespread double-stranded DNA breaks, nuclear swelling, and cell death in MSI-high, but not microsatellite stable cells.

ABBV-303 is a novel c-Met targeted multispecific NK cell engager. ABBV-303 binding to NKG2D and CD16a results in redirection of both innate (NK cells) and adaptive (CD8+ T cells) immune cells to lyse c-Met expressing tumor cells.

A-1155463 is a highly potent and selective BCL-XL inhibitor.

LUNA18 is an 11-mer cyclic peptide inhibitor for the intracellular tough target RAS with Kd (KRAS/G12D) of 0.043 nM and cellular IC50 of 1.4 nM (AsPC-1). LUNA18 orally and dose-dependently exhibits potent anti-cancer activities in a mouse xenograft model. LUNA18 shows 21–47% oral bioavailability in animals such as mouse, rat, monkey, and dog and notably does not require special formulations.

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.

Melittin (MLT, Forapin, Forapine) is an activator of phospholipase A2 (PLA2) that stimulates the activity of the low molecular weight PLA2, while it does not the increase the activity of the high molecular weight enzyme.

Palmitoyl hexapeptide-12 is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient.

Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.

DBCO intermidate 3 is a Click Chemistry intermidate used for antibody-drug conjugates..

CMS121 is a substituted quinoline that has neuroprotective, anti-inflammatory, antioxidative, and renoprotective activities.