NLX-204 is a potent and selective ERK1/2 phosphorylation-preferring serotonin 5 HT1A receptor agonist with pKi = 10.19. NLX-204 displayed high selectivity in the SafetyScreen44 panel (including hERG channel), high solubility, metabolic stability, and Caco-2 penetration and did not block CYP3A4, CYP2D6 isoenzymes, or P-glycoprotein. Preliminary in vivo studies confirmed its promising pharmacokinetic profile. NLX-204 also robustly stimulated ERK1/2 phosphorylation in rat cortex and showed highly potent (MED = 0.16 mg/kg) and efficacious antidepressant-like activity, totally eliminating immobility in the rat Porsolt test.

ABBV-4083 is an analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity.

JNJ-64326067 is a potent and selective binder to aggregated tau with a favorable pharmacokinetic profile and no apparent off-target binding. This was confirmed in rat and monkey positron emission tomography studies using [18F]-JNJ-64326067.

BMS-986166 (BMS986166) is a potent, selective S1P receptor modulator for the treatment of ulcerative colitis..

AES-135 (AES135) is a novel HDAC inhibitor that biochemically inhibits HDACs 3, 6, 8 and 11 with IC50 values of 190-1100 nM.

EML741 is a histone lysine methyltransferase G9a/GLP inhibitor, with an IC50 of 23 nM, Kd of 1.13 μM for G9a. EML741 also inhibits DNMT1 (IC50, 3.1 μM), with no effect on DNMT3a or DNMT3b. EML741 exhibits low cell toxicity, and is membrane permeable and blood-brain barrier penetrated.

(S)-DO271 is an inactive control for the α/β-hydrolase domain-containing protein 12 (ABHD12) inhibitor DO264.

MIDD0301 is a potent, positive allosteric, α5β3γ2 selective, GABAA receptor (GABAAR) ligand with EC50 of 17 nM, shows no significant binding at the peripheral GABAAR at 10 uM.

CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM.

LAS190792 (AZD8999) is a potent muscarinic antagonist and β2-adrenoceptor agonist with pIC50 8.9, 8.8, 8.8, 9.2, 8.2, 7.5, 9.1, 5.6 for M1, M2, M3, M4, M5, β1, β2, β3, respectively. LAS190792 can be used as a bronchodilator.

Elenbecestat (E2609) is a novel potent, oral BACE1 inhibitor for treatment of Alzheimer's disease..

beta-secretase inhibitor.

T-448 (T448) is a specific inhibitor of LSD1 enzyme activity, enhances H3K4 methylation in primary cultured rat neurons but has little impact on LSD1-GFI1B complex in human TF-1a erythroblasts.

AZD 5991 (AZD5991) is a potent and selective macrocyclic inhibitor of Mcl-1 with sub-nanomolar affinity.

ASP7657 (ASP-7657) is a potent, selective, orally active prostaglandin EP4 receptor antagonist with Ki values of 6.02 nM and 2.21 nM for rat and human EP4 receptors, resepctively.

SGL5213 is a potent, oral active and low-absorbable sodium-dependent glucose cotransporter 1 (SGLT1) inhibitor, with IC50 values of 29 nM and 20 nM for hSGLT1 and hSGLT2, respectively. SGL5213 has potential to treat type 2 diabetes treatment.

VT-1598 is a potent, high-affinity, oral inhibitor of fungal sterol 14α-demethylase (CYP51B) with Kd of 13 nM.

CL27c is a cell-permeable, inhaled lipophilic ester prodrug of CL27e, which is a potent, selective pan-class I PI3K inhibitor, CL27c is inactive in PI3K enzymatic assay, once inside the cytoplasm, CL27c is metabolized by unspecific esterases into CL27e.

AKB-9778 is a potent, selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP) with IC50 of 17 pM.

Sephin1 is a selective inhibitor of stress-induced PPP1R15A and targets disease associated with accumulation of misfolded protein.

RMC-4630 is a potent and selective inhibitor of SHP2, a central node in the RAS signaling pathway.

TD-0212 (TD0212) is a potent, orally efficacious, dual AT1 antagonist/Neprilysin (NEP) inhibitor with pKi of 8.9 (AT1) and pIC50 of 9.2 (NEP).

PF-06305591 (PF06305591) is a potent, highly selective selective NaV1.8 blocker with IC50 of 15 nM, displays no significant activity against other sodium channel subtypes, K+ channels and Ca2+ channels.

E3330 is a potent and selective APE1(Ref-1) inhibitor, which suppressed NF-kappa B DNA-binding activity.

PC786 (PC-786) is a potent non-nucleoside RSV L-protein polymerase inhibitor with IC50 of 2.1 nM and 0.5 nM in cell-free enzyme assay and mini-genome assay in HEp-2 cells, respectively.

CG-806 (CG806, CG'806) is a novel potent, pan-FLT3/BTK multi-kinase inhibitor with impressive inhibition of leukemic cell proliferation with IC50 at sub-nanomolar or low nanomolar levels.

TBAJ-587 is a potent anti-tuberculosis agent. TBAJ-587 inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. BAJ-587 has more potent activity against M. tuberculosis and better efficacy in animal models of TB.