VUF11207 fumarate is a potent CXCR7 (ACKR3) agonist with EC50 of 1.6 nM, inducse recruitment of β-arrestin2 and subsequent internalization of CXCR7 in cells.

GSK 2793660(GSK2793660) is a potent, selective, irreversible and orally bioavailable cathepsin C inhibitor, but not the activity of downstream neutrophil serine proteases, for the treatment of cystic fibrosis, non-cystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis..

PRN473 (Atuzabrutinib, SAR 444727, PRN-473) is a potent, selective, covalent reversible BTK inhibitor.

GDC-0339 (GDC0339) is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).

GSK 2833503A (GSK2833503A, GSK503A) is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 4 nM/5 nM, respectively.

GSK-2485852 (GSK2485852, GSK5852) is a highly potent, selective HCV NS5B polymerase inhibitor with IC50 of 3.0 and 1.6 nM for HCV genotypes 1a and 1b in replicon assay, respectively.

Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.

ABC 294640 (ABC294640, Opaganib) is a is a selective, competitive and orally bioavailable sphingosine kinase-2 (SphK-2) inhibitor with IC50 of 60 uM, Ki of 9.8 uM.

GSK-2324 (GSK2324) is a potent, selective, full FXR agonist with EC50 of 120 nM in FRET assay.

A cathepsin cleavable ADC peptide linker.

THZ-1 hydrochloride is a potent, selective, covalent CDK7 inhibitor with IC50 of 3.2 nM.

PEAQX (NVP-AAM077) is a potent, selective, NR2A-preferring NMDA receptor antagonist with IC50 of 270 nM (NR1A/2A), >100-fold selectivity over NR1A/2B receptor (IC50=29,600 nM).

NSC194598 is a specific small molecule inhibitor that inhibits p53 sequence-specific DNA binding in vitro (IC50=180 nM) and in vivo.

USP7i-1 is a potent, selective USP7 inhibitor..

HS-276 is a potent, highly selective and orally bioavailable TAK1 inhibitor with Ki of 2.5 nM.

2GBI (2-guanidinobenzimidazole) is a guanidine derivative that inhibits voltage-gated proton channel Hv1 by binding to the VSD from its intracellular side..

SAR340835 (SAR 340835, SAR296968 prodrug) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, a water-soluble prodrug of SAR296968.

SAR296968 (SAR 296968) is a potent, selective Na+/Ca2+ exchanger (NCX) inhibitor, potently inhibits hNCX1/2/3 with IC50 of 74/23/129 nM, respectively.SAR296968 showed the same range of inhibitory potency on NCX1 orthologs from dog, guinea pig, pig, rabbit, and rat (IC50=20-200 nM).SAR296968 inhibited both the forward and reverse mode of the NCX current in a concentration-dependent manner with similarly high potency in voltage-clamp studies in guinea pig cardiomyocytes.SAR296968 displays little to no effect against 5-HT2B, benzodiazepine peripheral receptor, norepinephrine uptake, dopamine uptake, AR and PR.SAR296968 exhibited antiarrhythmic properties in animal models of arrhythmias related to early or late afterdepolarizations, significantly increased left ventricular contractility in anesthetized pigs.

Neurounina-1 is a small molecule Na+/Ca2+ exchanger (NCX) activator, stimulates NCX1 and NCX2 activities with EC50 of 1.1-2.7 nM, does not affect NCX3 activity.Neurounina-1 (10 nM) reduced cell death of primary cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation, also reduced γ-aminobutyric acid (GABA) release, enhanced GABA(A) currents, and inhibited both glutamate release and N-methyl-d-aspartate receptors in vitro.Neurounina-1 effectively protects against stroke damage in vivo.

ARN22089 (ARN 22089) is a specific small molecule inhibitor of putative CDC42 family effector interaction, binds to CDC42 and has broad anti-cancer activity and inhibits MAPK and S6 signaling.ARN22089 could inhibit CDC42-PAK interactions with EC50 of 0.1 uM, and inhibit RHOJ/PAK interactions with approximate EC50 of 1-5 uM.ARN22089 has a single-digit micromolar IC50 activity against sensitive cell lines (WM3248, SKMel3, A375, and SW480), has IC50 of < 10 uM for 55/100 cell lines in a panel of 100 cancer cell lines with various different mutations, including several cell lines with neuroblastoma RAS (NRAS) mutations.ARN22089 inhibits MAPK and S6 phosphorylation and influences NFkB signaling in vitro.ARN22089 specifically inhibits tumor angiogenesis in 3D vascularized microtumors, shows drug-like properties and inhibits tumor growth in vivo.ARN22089 selectively binds and inhibits CDC42 effector interactions.ARN22089 binds better to the purified CDC42 compared with other known CDC42 inhibitors (ZCL278, ML141, R-ketoralac, and Casin).CDC42 family GTPases (RHOJ, RHOQ, CDC42) are linked to multiple human cancers and modulate cell-cycle progression, tumor cell migration/invasion, and tumor angiogenesis.

3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.

11-O-Methylpseurotin A is a compound of mixed polyketide synthase–nonribosomal peptide synthetase (PKS/NRPS) origin. 11-O-Methylpseurotin A selectively inhibits a Hof1 deletion strain.

Aspulvinone O is a natural inhibitor of aspartate transaminase 1 (GOT1). GOT1 plays an important role in energy metabolism and Reactive Oxygen Species (ROS) balance. GOT1 may serve as an important target in PDAC. Aspulvinone O suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism.

Choline oxidase catalyzes the oxidation of choline to glycine betaine via betaine aldehyde in glycine betaine biosynthesis and betaine acts as an osmolyte. Choline oxidase has potential in enzymatic betaine production.

Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity.

Anhydroophiobolin A is a potent inhibitor of photosynthesis with IC50s of 77 and 14 mM in the photosynthesis of chlorella and spinach, respectively. Anhydroophiobolin A is an analog of Ophiobolin A.

Agonodepside B is a compound isolated from a nonsporulating filamentous fungus, F7524.

(-)-(E)-Guggulsterone is the metabolite of Z-guggulsterone. Guggulsterone is an active constituent of guggulipid, an ayurvedic drug derived from Commiphora mukul. Guggulsterone has hypolipidaemic activity.

Muristerone A is a phytoecdysteroid analog of ecdysone and a potent agonist of ecdysteroid receptor with a Kd of 1 nM.