A novel potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 of 2.3 nM and 0.7 nM for human KMO and Pf-KMO, respectively.

A novel potent IRE1α-selective kinase inhibitor that inhibits both the kinase and RNase activities of IRE1α with IC50 of 20 nM and 200 nM, respectively; binds to pIRE1α and inhibits XBP 1 splicing; only weakly inhibits Ron (IC50= 4.4 uM) and FGFR1 V561M (IC50=17 uM) in a panel of 284 kinases.

A highly potent, selective HCV NS5B polymerase inhibitor for treatment of HCV infection.

A drug-linker conjugate for antibody-drug conjugate by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide SuO-Val-Cit-PAB.

A derivative of BAM-7 that acts as a nove potent, direct activator of Bax with EC50 of 700 nM; inhibits GBM cell proliferation, arrests the cell cycle, and induces apoptosis through the induction of mitochondrial membrane permeabilization; also blocks proliferation and self-renewal of GSCs and induces their apoptosis; sensitizes both GBM cells and GSCs to the alkylating agent Temozolomide.

A cell-permeable small molecule inhibitor of Fumarase (fumarate hydratase), an enzyme of the tricarboxylic acid cycle (TCA cycle); elicits a nutrient-dependent cytotoxicity in a number of cancer cell lines, and displays increased growth-inhibitory activity toward SW620 cell line grown in the absence of glucose (mean IC50=2.2 uM).

90 (CBR-490) is a potent and selective antiwolbachial activity compound (Anti-Wolbachia wMel In vitro HCI cell-based assay IC50=33 nM, IC90=283 nM).CBR490 demonstrates potent antiwolbachial activity was confirmed in L. sigmodontis, Brugia malayi, and Onchocerca ochengi in vivo preclinical models of filarial disease.CBR490 demonbstrated in vitro selectivity against Loa loa (a safety concern in endemic areas).

8-BOA is a selective and potent mechanism-based inactivator of breast cancer-associated CYP4Z1.8-BOA exhibited favourable inhibitory activity in vitro, thus meriting in vivo characterization.

3JC48-3 is a potent, cellularly active and stable c-Myc inhibitor, inhibits c-Myc-max dimerization with IC50 of 34 uM, 5 times more potent than 10074-G5, exhibits an approximate twofold selectivity for c-Myc-Max heterodimers over Max-Max homodimers.3JC48-3 inhibited the proliferation of c-Myc-over-expressing HL60 and Daudi cells with single-digit micromolar IC50 values by causing growth arrest at the G0 /G1 phase.3JC48-3 inhibited c-Myc-Max dimerization in cells validated by CoIP.3JC48-3 decreased prostate cancer cells' growth and viability in a dose-dependent fashion in vitro, upregulated PrKD1 expression and phosphorylation of known PrKD1 substrates: the threonine 120 (Thr-120) residue in beta-catenin and the serine 216 (Ser-216) in Cell Division Cycle 25 (CDC25C).3JC48-3 (1 g/kg, i.p.) decreased the rate of tumor growth in mice with patient-derived prostate cancer xenografts (PDX), without dose-limiting toxicity.

3-Deazauridine (DAU, NSC 126849) is a nucleoside analog that competitively inhibits cytidine triphosphate synthetase (CTP).3-Deazauridine inhibits the growth of L1210 leukemia cells when used at a concentration of 6 µM and dose-dependently reduces mortality in a mouse model of leukemia.3-Deazauridine selectively suppresses cell viability in a MYC-dependent manner in ARPE-19 cells.3-Deazauridine causes selective replication stress in MYC-overexpressing cells, which originates from MYC-driven rRNA synthesis.3-Deazauridine combined with ATR inhibitor BAY-1895344 induces synthetic lethality to MYC-overexpressing cells, and suppresses tumor growth in 3D assays and in vivo.

2S-alkyne is an irreversible and clickable inhibitor of Streptococcal pyrogenic exotoxin B (SpeB) with IC50 of 1.4 uM; 2S-alkyne showed irreversible enzyme inhibition in biochemical assays and labeled endogenous SpeB in cultured S. pyogenes supernatants. 2S-alkyne decreased S. pyogenes survival in the presence of human neutrophils and supports the role of SpeB-mediated proteolysis as a mechanism to limit complement-mediated host defense.

1-ECBC is a small molecule inhibiting C. albicans filamentation, 1-ABC targets DYRK1-family kinase Yak1, the sole DYRK-family member expressed in C. albicans.1-ECBC blocked C. albicans biofilm formation in several co-culture models and a rat catheter infection model.

13PCSK9i is a highly potent PCSK9-LDLR disruptor peptide with EC50 of 2 nM, SPR Kd of 6.1 nM and 21 nM for hPCSK9 and mPCSK9.13PCSK9i reduces plasma cholesterol levels and increases hepatic LDLR density in a dose-dependent manner.13PCSK9i functions by a unique, allosteric mechanism and is the smallest molecule identified to date with in vivo PCSK9-LDLR disruptor function.

(R,S′)-MNF is a bi-functional GPR55 inhibitor and biased β2 adrenergic agonist, inhibits proliferation of PDAC cell lines (IC50=0.11 uM, PANC-1 cells). (R,S′)-MNF is a biased β2-AR agonist that selectively signals through Gαs and does not recruit β-arrestin-2. (R,S′)-MNF attenuates pro-oncogenic signaling and cellular proliferation in PANC-1 cells. (R,S′)-MNF (1 uM) significantly decreased ERK phosphorylation stimulated by the GPR55 ligand O-1602, (R,S′)-MNF is an effective inhibitor of GPR55 internalization and signaling. (R,S′)-MNF (20-40 mg/Kg) reduces PANC-1 tumor growth in a mouse xenograft model.

(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.(R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.(R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.(R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.

(R)-LMI (H2N-R-Leu-Met-Ile-COOH) is a tripeptide analogue of corticotropin-releasing factor (CRF) and CRF antagonist targeting the N-domain of CRF1 receptor; (R)-LMI inhibits CRF-stimulated cAMP accumulation with IC50 of 1.7 uM. (R)-LMI inhibits the production of interleukins by adipocytes and the proliferation rate of RAW 264.7 cells.

(–)-IHCH7041 is a potent, selective partial agonist at DRD2/3 and 5-HT1AR, EC50 of 1.38 nM in Gαi1–γ9 dissociation and 2.75 nM in β-arrestin2 recruitment assays, with negligible 5-HT2AR binding (>100-fold selectivity).(–)-IHCH7041 exhibits negligible affinities for a large number of tested GPCRs, ion channels and transporters (Ki>500 nM), good affinities for DRD2 and DRD3 (Ki=14.42 nM), and moderate binding to 5-HT1A (Ki=60.62 nM).(–)-IHCH7041 behaves as a partial agonist in both G-protein signaling and β-arrestin recruitment activities at DRD2, DRD3 and 5-HT1AR.(–)-IHCH7041 displayed potent antipsychotic activity and has antidepressant properties and reverses cognitive impairmentin mice.

GSK598809 (GSK-598809) is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

GSK598809 hydrochloride is a potent, selective, CNS penetrant and orally bioavailable dopamine D3 receptor antagonist with pKi of 8.9.

NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death.

MyoMed-205 is a small moelcule that inhibits MuRF1 (TRIM63) activity and MuRF1/MuRF2 expression.

Flonoltinib maleate is a potent, highly selective, dual JAK2/FLT3 inhibitor with IC50 of 0.8, 1.4, and 15 nM for JAK2, JAK2V617F, and FLT3, respectively.

DS12881479 (DS 12881479) is a novel potent, selective inhibitor of MAPK-interacting kinase 1 (Mnk1) with IC50 of 21 nM, stabilizes the autoinhibited state of Mnk1.

SRI-37264 (SRI 37264) is a small molecule inhibitor of HIV-1 Nef-mediated activation of the myeloid Src-family kinase Hck, blocks HIV-1 replication in macrophages and disrupts MHC-I downregulation.

MEDS433 is a potent DHODH inhibitor with IC50 of 1.2 nM (hDHODH), inhibits in vitro replication of HSV-1 and HSV-2 in the nanomolar range.

WX-UK1 (UKI-1) is a small synthetic serine protease uPA (urokinase-type plasminogen activator) inhibitor that blocks tumor cell invasion, metastasis and primary tumor growth.

GSK3004774 (GSK-3004774) is a potent, nonabsorbable, gastrointestinally-restricted agonist agonist of calcium-sensing receptor (CaSR) with pEC50 of 7.3.

GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.

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..