Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).

LCH 7749944 (GNF-PF-2356) is a novel and potent PAK4 with IC50 of 14.93 uM, shows weak activity against other PAK family members.

DHODH-IN-11 (Compound 14b) is a Leflunomide derivative and a weak dihydroorotate dehydrogenase (DHODH) inhibitor with a pKa of 5.03[1].

SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).

CDPPB is a potent, selective, brain penetrant positive allosteric modulator of mGlu5 receptor with EC50 of 10 nM and 20 nM for human and rat mGluR5, respectively.

LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.

Tianeptine is a selective facilitator of 5-HT uptake in vitro and in vivo.

Blasticidin S hydrochloride is a nucleoside antibiotic isolated from Streptomyces griseochromogenes. Blasticidin S is a potent inhibitor of protein synthesis in both prokaryotic and eukaryotic cells.

AAK1-IN-1(BMS-986176) is a chemical probe for AAK1 and BIKE that potently targets the ATP-binding site (AAK1 Ki = 9.1 nM; BIKE Ki = 17 nM). Regarding kinase selectivity, only three kinases were observed to bind SGC-AAK1-1 within 30-fold of the KD of AAK1 in a KINOMEscan assay (DiscoverX) at 1 μM followed by KD determinations: RIOK1 (KD = 72 nM), RIOK3 (KD = 290 nM), and PIP5K1C (KD = 260 nM). In a live cell NanoBRET assay (Promega) SGC-AAK1-1 has potency for ectopically expressed full-length AAK1- and BIKE-Nluc fusion proteins (AAK1 IC50 = 230 nM; BIKE IC50 = 1.5 μM).

ADX-102 (Reproxalap, NS-2) is a novel small molecule immunomodulator that covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal, which have been shown to mediate inflammatory pain; DX-102 is a promising agent for the treatment of dry eye disease.

OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.

MDI-2268 (MDI2268) is a small-molecule, in vivo-active inhibitor of plasminogen activator inhibitor type-1 (PAI-1), demonstrates excellent pharmacokinetics, potent activity against vitronectin-bound PAI-1 in vivo, and efficacy in murine model of venous thrombosis.

SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..

UT-155 is a selective androgen receptor (AR) antagonist, with a Ki of 267 nM for AR-RBD.

AZD-7986(Brensocatib) is a highly potent, reversible, and selective DPP1 inhibitor with enzyme and cell pIC50 of 8.4.

5-Lipoxygenases (15-LO) inhibitor 1 is a heterocyclic pyrimidobenzothiazine compound that inhibits 15-LO with an IC50 value of 18 µM.

CBS-1117 is a novel fusion inhibitor with EC50 ∼3 μM against group 1 HA.

Tafluprost(AFP-168) is an anti-glaucoma prostaglandin (PG) analog.A number of 17-phenyl trinor PGF2α derivatives have been approved for the treatment of glaucoma.1,2,3,4 Of these, the ones wherein the 13,14-double bond has been hydrogenated retain relatively good potency.

Difluprednate(Durezol) is a corticosteroid, approved difluprednate for the treatment of post-operative ocular inflammation and pain.

STING agonist 4 is an amidobenzimidazole (ABZI)-based compound that functions as a STING agonist with Kd of 1.6 nM (binding of endogenous full-length STING, THP-1 cell lysates); caused dose-dependent phosphorylation of IRF3 and STING that was inhibited by the TBK1 inhibitor BX795, induced dose-dependent secretion of IFN-β with EC50 of 3.1 uM in PBMCs (18-fold more potent than cGAMP); promotes production of IFN-γ-induced protein 10 (IP-10), IL-6 and TNFα by a mechanism that is dependent on STING-mediated activation of TBK1; unlike cGAMP and DMXAA, compound 2 efficiently activates STING function while maintaining an open STING confirmation.

Butoconazole is an imidazole antifungal used in gynecology. It is administered as a vaginal cream.

CLP290 (CLP-290) is an orally acirtve small molecule K+-Cl- cotransporter isotype 2 (KCC2) activator, the carbamate prodrug of CLP257; In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in SDH neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior.

BIBF0775 is an inhibitor of the transforming growth factor β receptor I (TGFβRI). X-ray structure analysis showed that BIBF0775 soaked into the kinase domain of TGFβRI.

QBS(CU-242) or 2-Amino-N-quinolin-8-yl-benzenesulfonamide, is an Inhibitor of cell cycle at G2 phase; apoptosis inducer. NUN82647 has CAS#16082-64-7, and inchi key: NIOOKXAMJQVDGB-UHFFFAOYSA-N. According to Hodoodo Chemical Nomenclature, It is named: NUN-82647.

AS601245 is an orally active, selective, ATP competitive JNK (c-Jun NH2-terminal protein kinase) inhibitor with IC50s of 150, 220, and 70 nM for three JNK human isoforms (hJNK1, hJNK2, and hJNK3), respectively. AS601245 exhibits 10- to 20-fold selectivity over c-src, CDK2, and c-Raf and more than 50- to 100-fold selectivity over a range of Ser/Thr- and Tyr-protein kinases. Neuroprotective properties.

PNU-112455A is an ATP-competitive CDK2/5 inhibitor with Ki of 2 uM and 2 uM for cdk2·GST-cyclin E and cdk5·GST-p25 respectively, shows no activity against c-c-Met, IGR-1R, and ERK2..

SB-334867 is a selective orexin-1 (OX1) receptor antagonist.

L-765,314 is a drug which acts as a potent and selective antagonist for the Alpha-1 adrenergic receptor subtype α1B. It has mainly been used to investigate the role of α1B receptors in the regulation of blood pressure.

MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice.

Brassinazole is an inhibitor of brassinosteroid biosynthesis that has been developed in order to probe the myriad functions of brassinosteroids.