LC28 is a novel inhibitor of STAT3 signaling, suppressing survival of cisplatin-resistant ovarian cancer cells.

SKLB-C2807 is an AR-DBD binder.

GSK743 is a Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitor.

GSK097 is a potent and selective Inhibitor of the second bromodomain (BD2) of the bromodomain and extra-terminal domain (BET) proteins. GSK097 displays 2000-fold selective for BD2 over BD1 (BRD4 data) with >1 mg/mL solubility in FaSSIF media.

M3258 (M 3258) is a potent, reversible, highly selective and orally acitve LMP7 inhibitor with ceullar IC50 of 4.1 nM.M3258 does not inhibit other constitutive proteasome and immunoproteasome subunits (IC50>2.5 uM).M3258 demonstrated strong antitumor efficacy in multiple myeloma xenograft models.M3258 treatment led to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells both in vitro and in vivo.M3258 showed superior antitumor efficacy in selected multiple myeloma and mantle cell lymphoma xenograft models compared with the approved nonselective proteasome inhibitors bortezomib and ixazomib.

JNJ-61803534 is a potent RORγt inverse agonist with IC50 of 9.6 nM, selectively inhibiting RORγt-driven transcription versus closely-related family members, RORα and RORβ.

SMU-C80 is a TLR2 agonist (EC50 = 31.02 ± 1.01 nM). SMU-C80, through TLR1/2, recruits the adaptor protein MyD88 and triggers the NF-κB pathway to release cytokines such as TNF-α and IL-1β from human, but not murine, cells. To the best of our knowledge, it is the first species-specific TLR1/2 agonist reported until now. Moreover, SMU-C80 increased the percentage of T, B, and NK cells ex vivo and activated the immune cells, which suppressed cancer cell growth in vitro.

GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits (IC50=0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC50: purified 26S=13 µM; enriched THP-1 extracts IC50=40µM). GSK3494245 exhibits attractive biological and biosafety properties.

GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment.

SR-1114 is a first-in-class ENL PROTAC.

HST5040 is a clinical candidate for the treatment of propionic acidemia (PA) and methylmalonic acidemia (MMA) with EC50 of 0.94 μM in P-CoA-lowering activity.

GNE-0749 is a potent and selective pan-RAF inhibitor with Ki of 0.061 nM and <0.08 nM for CRAF and BRAF, respectively. Combinated with cobimetinib, GNE-0749 demonstrates synergistic pharmacodynamic effects in the KRAS mutant HCT116 tumor-bearing mice.

BMS-986224 is a potent and selective apelin receptor (APJ) agonist with Ki of 0.074 nM, exhibiting similar receptor binding and signaling profile to (Pyr1) apelin-13.

BMS-986313 is a potent, selective, orally active RORγt inverse agonist with EC50 of 3.6 nM in GAL-4 reporter assay in Jurkat cell line, and 50 nM in IL-17 human whole blood assay.BMS-986313 demonstrated robust efficacy in preclinical models of psoriasis (the IMQ-induced skin lesion model and the IL-23-induced acanthosis model).

MI-09 is a SARS-CoV-2 Protease inhibitor (IC50 = 15.2 nM). In a transgenic mouse model of SARS-CoV-2 infection, oral or intraperitoneal treatment with MI-09 significantly reduced lung viral loads and lung lesions.

DS79932728 is a Potent, Orally Available G9a/GLP Inhibitor for Treating β‑Thalassemia and Sickle Cell Disease.

KGN-00429 is a novel selective bromodomain and extra-terminal domain (BET) protein family inhibitor (BETi ), inducing an ‘activated’ keratinocyte transcriptional profile with reversal of chronic wound biomarkers in human skin ex vivo. This product has no formal name. For the convenience of scientific communication, we named it by combining its InChi Key (3 letters from the first letter of each section) with the last 5 digit of its CAS#) according to MedKoo Chemical Nomenclature (https://www.medkoo.com/page/naming).

NVS-BET-1 is a BET bromodomain inhibitor that regulates keratinocyte plasticity.

PIPE-359 is a brain-penetrant and selective antagonist of the muscarinic acetylcholine receptor subtype 1.

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.

BI 730357 is a RORγ Antagonist for the treatment of autoimmune diseases.

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, >10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 μM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with an IC50 value of 3.2 nM.

CG416 is a tropomyosin receptor kinase (TRK) degrader that targets the intracellular kinase domain of TRK. CG416 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12 colorectal carcinoma cells and inhibited downstream PLCγ1 signaling at sub-nanomolar concentrations. CG416 also degraded human wild-type TRKA.

MLT-985 is a highly selective allosteric MALT1 inhibitor with an IC50 value of 3 nM.

MLT-231 is a potent, highly selective allosteric MALT1 with an IC50 of 9 nM. MLT-231 specifically prevents endogenous BCL10 cleavage with IC50 of 160 nM. MLT-231 shows antitumor activity in an ABC-DLBCL type xenograft model in mouse.

C5-RIBOTAC is a RIBOTAC degrader, targeting the SARS-CoV-2 RNA genome

PQR626 is an orally available, and brain-penetrant mTOR inhibitor extracted from patent WO2017198346A1, compound example 44, has an IC50 of 5 nM for mTOR. PQR626 can be used for the research of neurological disorder.

ORM‐11372 is a potent and highly selective NCX 1.1 inhibitor, inhibits human NCX 1.1 reverse and forward currents with IC50 of 5 and 6 nM respectively.ORM‐11372 weakly inhibits human cardiac sodium 1.5 (I Na) and hERG KV11.1 currents (I hERG) with IC50 of 23.2 and 10.0 uM.ORM‐11372 decreased both the outward and inward currents of hiPSC‐CMs with IC50 of 4.8 and 5.6 nM respectively, reduced the magnitude of outward I NCX (the reverse mode) in rat primary ventricular CMs with IC50 of 11.3 nM.ORM‐11372 concentration‐dependently inhibited the calcium efflux signa with an IC50 of 142 and 164 nM for experimental conditions increasing intracellular calcium and eliciting NCX forward mode activity, repectively.ORM‐11372 induced positive inotropic effects of 18 ± 6% and 35 ± 8% in anaesthetized rats with myocardial infarctions and in healthy rabbits respectively with no other haemodynamic effects.