BPR1R024 is an orally active and selective CSF1R inhibitor with IC50 of 0.53 nM. BPR1R024 specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth.

BMS-963272 is a potent, selective MGAT2 inhibitor with IC50 of 7.1 nM/18 nM (hMGAT2/mMGAT2) and shows excellent efficacy, safety, and tolerability profile.

JNJ-67569762 is a tetrahydropyridine-based BACE1 inhibitor targeting the S3 pocket with IC50 of 2.7 nM and shows 71-fold selectivity over BACE2.

GSK-3685032(GSK 3685032) is a first-in-class, potent, non-nucleoside, reversible, selective inhibitor of DNMT1 with IC50 of 0.036 μM. GSK3685032 induces robust loss of DNA methylation, transcriptional activation and cancer cell growth inhibition in vitro.

FRM-024 is a potent CNS-penetrant gamma secretase modulator for familial Alzheimer’s disease.

AS-1763 is an orally available, potent, and selective BTK inhibitor and shows excellent potency against both wild/C481S mutant BTKs with IC50 of 0.85 nM/0.99 nM.

PZ703b is highly potent in killing BCL-XL dependent, BCL-2 dependent, and BCL-XL/BCL-2 dual-dependent cells in an E3 ligase (VHL)-dependent fashion.

UNC7145 is a negative control for UNC6934 (GLXC-22088).

(+)-JNJ-A07 is a highly potent, orally active pan-serotype dengue virus inhibitor targeting the NS3-NS4B interaction. (+)-JNJ-A07 exerts nanomolar to picomolar activity against a panel of 21 clinical isolates. (+)-JNJ-A07 has a favourable pharmacokinetic profile that results in outstanding efficacy against dengue virus infection in mouse infection models.

MK-8262 is an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor with an IC50 of 53 nM and a log D of 5.3. MK-8262, a bistrifluoromethyl analogue, has the potential for coronary heart disease (CHD) correlated high-density lipoprotein (HDL) and low-density lipoprotein (LDL) research.

BAY 1251152 (VIP152 ) is the first potent, selective, orally available PTEFb/CDK9 inhibitor with biochemical IC50 of 9 nM and MOLM13 cell IC50 of 29 nM, displays> 50-fold selectivity against other CDKs.

EEDi-5273 is an exceptionally potent and orally efficacious embryonic ectoderm development (EED) inhibitor with IC50 of 0.2 nM and inhibits the KARPAS422 cell growth with IC50 of 1.2 nM. EEDi-5273 demonstrates an excellent PK and ADME profile, and its oral administration leads to complete and persistent tumor regression in the KARPAS422 xenograft model with no signs of toxicity.

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.

IACS-9779 is a Potent IDO1 Inhibitor Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme. IACS-9779 with a predicted human efficacious once daily dose below 1 mg/kg to sustain >90% inhibition of IDO1 displayed an acceptable safety margin in rodent toxicology and dog cardiovascular studies to support advancement into preclinical safety evaluation for human development.

VPC-70063 is a Myc-Max inhibitor. VPC-70067 is a close analog of the previously identified Myc inhibitor 10058-F4. VPC-70063, of a chemically different scaffold, was the best performer in a panel of in vitro assays, and the forerunner for future hit-to-lead optimization efforts.

A synthetic curcuminoid that selectively inhibits STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs.

MMPP is a novel potent inhibitor of pro-inflammatory responses by inhibiting in vitro STAT3 activation and its downstream signalling in murine macrophages and human synoviocytes from patients with RA.

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.