FLX-475 is a novel CCR4 antagonist for the treatment of cancer.

Fluoxazolevir (NCGC00351982) is a potent, small molecule entry inhibitor of HCV with EC50 of 18.8 nM.Fluoxazolevir inhibits fusion of HCV with hepatic cells by binding HCV envelope protein 1 (E1) to prevent fusion.Fluoxazolevir was generally effective against all chimeric HCV-RLuc genotypes including 1a, 1b, 2b, 3a, 4a, 5a, 6a and 7a, was most effective against HCV 2a and 2b, followed by 3a and 6a, all within sub-μM EC50 values, with little to no cytotoxicity (CC50>20 uM).Fluoxazolevir was highly synergistic with other anti-HCV drugs (interferon-α, ribavirin, daclatasvir, sofosbuvir and simeprevir (NS3/4A protease inhibitor)).Fluoxazolevir suppresses HCV infection in humanized chimeric mice, and is active against multidrug-resistant HCV.Fluoxazolevir also broadly blocked human coronavirus entry into various cell types, inhibit SARS-CoV S- and SARS-CoV-2 S-mediated infection MA104 cells with EC50 of 6.49 and 3.86 uM, respectively.

FL-18 (p97 inhibitor FL-18) is is the first small-molecule covalent inhibitor of VCP/p97 AAA ATPase with IC50 of 59.3 nM, capable of covalent engagement of p97 with proteome-wide selectivity.FL-18 showed better inhibition potency than NMS-873, a well-known p97 inhibitor.FL-18 covalently modified C522 residue in p97 and showed potent enzymatic inhibition.FL-18 showed potent inhibition towards U87MG glioma cancer cells (IC50=31 nM).FL-18 inhibited the p97 activity and induced aggregation of ubiquitinated proteins in U87MG cells.

Firazorexton is a potent, selective, experimental orexin 2 receptor (OX2R) agonist.

FIM1033 (FIM-1033) is a potent small-molecule inhibitor of FimH with HAI EC90 of 8 nM, with antibiotica activities, significantly attenuated bacterial loads in pyelonephritis in treated mice.

Filovirus inhibitor compd-A is a small molecule filovirus entry inhibitor targeting the endosomal receptor NPC1 binding site, shows potent inhibitory activity against both Ebola and Marburg viruses with IC50 of 0.86 uM against pseudotyped Marburg virus entry.

FGFR4-IN-2 is a potent, selective, covalent FGFR4 inhibitor with cellualr IC50 of 8.8 nM, 100-fold selectivity over FGFR2.FGFR4-IN-2 potently and selectively inhibit FGFR4 signaling through covalent modification of Cys552.FGFR4-IN-2 induces tumor regression in preclinical models of orthotopic and sorafenib-resistant HCC.

FG944 (FG-944) is a potent selective LpxC inhibitor with MIC50 of 0.5 ug/mL against K.pneumoniae, synergizes with rifampin in carbapenem resistant K. pneumoniae and E. coli.

FFA2R agonist 58 is a potent, allosteric FFAR2 (GPR43) agonist/modulator.FFA2R agonist 58 functions as a positive/priming modulator in these cells by turning the natural FFA2R agonist acetate into a potent activator of the neutrophil NADPH-oxidase.FFA2R agonist 58 lowers the concentration of acetate required to induce a transient rise in the concentration of intracellular Ca2+ in neutrophils, has no direct effect on the neutrophil NADPH-oxidase activity but affects the response induced by acetate.FFA2R agonist 58 significantly reduced the amount of internalized influenza A virus (IAV) in treated A549 cells.

FF-10101 (FF10101) is a potent, selective, and irreversible FLT3 inhibitor with IC50 of 0.14 nM (FLT3 Wt), covalent binds to the C695 residue of FLT3.FF-10101 potently inhibited the phosphorylation of FLT3-ITD than that of FLT3-ITD-C695S (IC50 values 2.4 nM and 79 nM, respectively).FF-10101 potently and selectively inhibits the growth of mutant FLT3-expressing leukemia cells in vitro (MV4-11 c ell, IC50=0.83 nM), potently inhibits kinase activities of wild-type FLT3 and FLT3-D835Y with IC50 values of 0.20 nM and 0.16 nM, respectively.FF-10101 demonstrated high kinase selectivity to wild-type FLT3 with >30-fold margins against the other kinases except for FMS and KIT with IC50 values of 0.94 nM and 2.0 nM, respectively.FF-10101 showed growth inhibitory effects on all tested types of FLT3-TKD mutation- and FLT3-ITD with D835Y, Y842C, Y842H, or F691L mutation-expressing 32D cells with GI50 values from 0.43 nM to 6.1 nM.FF-10101 (2, 5, and 10 mg/kg) demonstrated anti-leukemic effects in in vivo models, FF-10101 more potently inhibited the growth of tumors with FLT3-ITD-D835Y and FLT3-ITD-F691L than quizartinib.

FE 205030 (FE205030) is a potent, selective peptidic CGRP antagonist with IC50 of 0.2 nM.FE 205030 displays>100,000 fold against hAM1R and >6363 fold against hAM2R tested in Human CGRP, AM1R and AM2R receptor cAMP assays.FE 205030 inhibited CGRP-induced vasodilation in isolated human mesenteric resistance arteries in an ex vivo isometric myograph study; effectively blocked CGRP-induced vasodilation with a pA2 of 9.3.FE 205030 is a first in class injectable fast acting selective and potent agent for the treatment of acute episodic migraine.

FD028 is a small-molecule HIV-1 inactivator by conjugating FD016 (gp120-CD4 binding inhibitor) with FD017 (HIV-1 fusion inhibitor), inactivates cell-free virions (IC50=0.7 uM) of by targeting both HIV-1 gp120 and gp41.FD028 is not significantly toxic and has broad-spectrum HIV-1 inhibitory and inactivation activity, including T20-resistant viruses and T2635-resistant viruses.

FC-8052 (FC8052) is a highly potent inhibitor of HIV-1 Nef-effector kinase, binds to recombinant Nef in vitro with Kd of 10 pM; FC-8052 inhibits Nef-dependent HIV-1 replication in PBMCs in the subnanomolar range.

FAPL-PI3Ki1 is a specific FAP-targeted PI3K inhibitor that selectively targets FAP-expressing human IPF lung fibroblasts and potently inhibits collagen synthesis.FAPL-PI3Ki1 significantly inhibited phosphorylation of Akt in IPF fibroblasts with IC50 of 200 nM, also inhibited phosphorylation of 4E-BP1.FAPL-PI3Ki1 induced suppression of TGFb1-stimulated collagen production and phosphorylation of Akt in IPF fibroblasts requires participation of FAP.FAPL-PI3Ki1 suppressed production of hydroxyproline (major building block of collagen), reduced collagen deposition, and increased mouse survival in a mouse model of IPF inhibited PI3K activation in fibrotic lungs.

F114 is a novel, first-in-class, dual aurora and lim kinase inhibitor with IC50 of 72 nM and 137 nM against Aurora-A and Limk1, respectively, F114 inhibits GBM proliferation and invasion.

F1021-0686 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=1.55 uM).F1021-0686 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F1021-0686 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 5.27 uM.

F0909-0360 is a novel small molecule inhibitor of c-Myc, causes the functional repression of c-Myc target gene, shows appreciable anticancer activity against c-Myc expressing cell lines (HT29, IC50=0.2 uM).F0909-0360 showed c-Myc dependent apoptotic cell death, efficiently inhibited the functionality of c-Myc, suppressed the expression of c-Myc target genes (CAD, ODC1, NOP58, and NOP56) both at the transcriptional and translational levels.F0909-0360 showed considerable in vitro efficacy against cancer stem cells (CSCs), inhibited sphere forming capacity of D341-CSCs with IC50 of 4.06 uM.

Exicorilant (CORT125281, CORT-125281) is a potent, selective glucocorticoid receptor (GR) antagonist, exhibits no cross-reactivity for the PR and AR receptors.

Evixapodlin is a highly potent, small molecule human PD-1/PD-L1 protein-protein interaction inhibitor with IC50 of 0.213 nM, exhibits potential anticancer and antiviral activities.

Etripamil (MSP-2017) is a novel intranasal non-dihydropyridine calcium channel blocker that has begun phase III clinical trials for the treatment of paroxysmal supraventricular tachycardias.

ER-001259851-000 is a potent, selective, orally active Axl inhibitor with IC50 of 5.2 nM in cell free assays, displays >35-fold selectivity against Mer (IC50=190 nM).ER-001259851-000 shows a promising pharmacokinetic profile in mice.

ENMD-1068 is a novel selective PAR2 antagonist without inhibitory activity against thrombin-mediated PAR3 and PAR4 signaling; blocks TNFα production in synovial explants from patients with arthritis, and inhibits mast cell tryptase-induced recruitment of eosinophils into the pleural cavity of mice, dose dependently attenuates joint inflammation.

ENL YEATS Domain inhibitor 7 is a selective, small molecule inhibitor of ENL YEATS Domain with IC50 of 0.62 uM in inhibiting the ENL-acetyl-H3 interaction.ENL YEATS Domain inhibitor 7 displayed strong selectivity toward the ENL YEATS domain over all other human YEATS domains.ENL YEATS Domain inhibitor 7 exhibited on-target inhibition of ENL in cultured cells and a synergistic effect with the bromodomain and extraterminal domain inhibitor JQ1 in killing leukemia cells.

Enerisant hydrochloride (TS091 hydrochloride) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

Enerisant (S091,TS-091) is a potent, selective histamine H3 receptor antagonist/inverse agonist with IC50 of 2.89 and 14.5 nM against hH3R and rH3R, respectively.Enerisant inhibited R-α-methylhistamine–stimulated [35S]GTPγS binding to human histamine H3 receptor and rat histamine H3 receptor with IC50 values of 1.06 and 10.05 nM, respectively, inhibited basal [35S]GTPγS binding to human histamine H3 receptor with an EC50 value of 0.357 nM.Enerisant displays negligible effects on binding to human histamine H1, H2, and H4 receptor subtypes, as well as negligible affinities for 66 other receptors, transporters, and ion channels at 1-10 uM.Oral administration of enerisant hydrochloride attenuated the dipsogenia response on R-α-methylhistamine–induced dipsogenia in rats, the intraperitoneal administration of enerisant hydrochloride increased the total extracellular acetylcholine levels in the mPFC.Enerisant hydrochloride significantly decreased slow-wave deep sleep at doses of 1-10 mg/kg (P < 0.01-0.05). Enerisant hydrochloride (1, 3 and 10 mg/kg, p.o.) did not affect the accumulated locomotor activity time at up to 7 hours after administration.

Endosidin 9 (ES9) is a novel mitochondrial uncoupler, and a potent inhibitor of clathrin-mediated endocytosis (CME) in different systems, strongly reduces FM4-64 uptake in Arabidopsis root cells with IC50 of 5 uM.Endosidin 9 (ES9) inhibits CME dynamics and organelle movement in the cytoplasm.Endosidin9 (ES9) inhibits clathrin-mediated endocytosis largely through cytoplasmic acidification.

EN523 (EN-523) is a small molecule covalent ligand EN523 that targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1, OTUB1 recruiter component of DUBTAC NJH-2-057.Deubiquitinase-targeting chimeras (DUBTACs), heterobifunctional small molecules consisting of a deubiquitinase recruiter linked to a protein-targeting ligand, to stabilize the levels of specific proteins degraded in a ubiquitin-dependent manner.

EMU-116 (EMU-000116) is a potent, selective CXCR4 antagonist with IC50 29.6 nM in Ca2+ flux assay.

EMI66 (EMI-66) is a small molecule that attenuates RTK expression and signalling and alters the electrophoretic mobility of Coatomer Protein Complex Beta 2 (COPB2, binding Kd=1.51 uM) in lung cancer cells.EMI66 affects the subcellular localization of EGFR and COPB2, altering the endoplasmic reticulum (ER) stress response pathway, resulting in growth inhibition of mutant EGFR lung cancer cells and organoids.EMI66 inhibited total EGFR and MET levels, activation, and downstream signalling at lower concentrations than EMI1, also binds to recombinant COPB2 protein with an increased affinity compared to EMI1.EMI66 exerts an anti-proliferative effect (EC50=3-5 uM) on primary lung cancer organoid models, including XDO-137 (EGFR ex19del), PDXO-4000 (EGFR ex19del) and XDO-344 (wild-type EGFR).

EC-11716 (EC/11716) is a novel mycobacterium tuberculosis gyrase inhibitor with potent anti-tubercular activity (MIC 0.38 uM, M. tuberculosis H37Rv).EC/11716 is active against M. abscessus subspecies and clinical isolates, maintains comparable activity against a panel of clinical isolates covering the M. abscessus complex.EC/11716 is effective against M. abscessus biofilms (MIC 0.78 uM), with better bactericidal activity against biofilms than moxifloxacin.EC/11716 is active against M. abscessus in vivo.