SRI 6409-94 is an orally active Ro 13-6298 analogue that is teratogenic. SRI 6409-94 serves as a molecular tool to study the effect of the three-dimensional configuration of retinol on teratogenic activity.

UNC1021 is a selective L3MBTL3 inhibitor with an IC50 of 0.048 μM.

Oct4 inducer-1 (compound OAC-3) is a potent Oct4 activator. Oct4 inducer-1 activates Oct4 and Nanog promoters and enhances induced pluripotent stem cells (iPSC) formation. Oct4 inducer-1 facilitates the reprogramming of cells by enhancing efficiency and shortening the reprogramming time.

Tucidinostat (Chidamide, HBI-8000, CS055) is a novel histone deacetylase (HDAC) inhibitor with IC50 of 95/160/67/733/78/432 nM for HDAC1/2/3/8/10/11, respectively; shows no activity against Class IIa HDAC4/4/7/9 and HDAC6; demonstrates significant and broad spectrum in vitro and in vivo antitumor activity, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells.

SW203668 is a potent, tumor-specific inhibitor of stearoyl CoA desaturase (SCD) with better bioavailability than SW208108.

Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.

Capmatinib, also known as INCB28060 and INC280, is an orally bioavailable inhibitor of the proto-oncogene c-Met with potential antineoplastic activity. c-Met inhibitor INC280 selectively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing constitutively activated c-Met protein. Capmatinib was approved in 2020.

Tepotinib (EMD1214063, MSC2156119) is a potent, specific and ATP-competitive inhibitor of MET (HGFR) with IC50 of 23 nM for MET WT autophosphorylation and 2.2-42.6 nM for M1268T, Y1248H, H1112Y, L1213V, H1112L, V1110I, V1206L, and V1238I MET-mutated varia

DSF-102 (DSF102) is a small molecule EGFR inhibitor that interacts with the extracellular domain (ECD) of EGFR, inhibits the interaction with the EGF instead of blocking the intracellular kinase activity, shows inhibition of EGFR dimerization with IC50 of

Sotorasib racemate (Compound A) is an orally active racemate of Sotorasib, a covalent inhibitor of KRAS G12C mutant which induces adaptive feedback activation of MAPK pathway. Sotorasib racemate also exerts inhibitor activity against KRAS G12C induced cancer and can be applied to cancer research.

AMG-510 is a specific covalent inhibitor of K-RAS(G12C) with potential antineoplastic activity.

HRO761 is a potent, selective, allosteric WRN inhibitor with IC50 of 100 nM (ATPase assay) and GI50 of 40 nM (SW48 cells), respectively. HRO761 binds at the interface of the D1 and D2 helicase domains, locking WRN in an inactive conformation.

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

Auranofin, also known as Ridaura and SKF-39162, is an oral chrysotherapeutic agent for the treatment of rheumatoid arthritis. Auranofin's exact mechanism of action is unknown, but it is believed to act via immunological mechanisms and alteration of lysosomal enzyme activity. Auranofin's efficacy is slightly less than that of injected gold salts, but it is better tolerated, and side effects which occur are potentially less serious.

GLPG3970 (compound 88) is a first-in-class SIK2/SIK3 inhibitor. GLPG3970 can be used for the research of inflammation and autoimmune disease.

TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).

ACT-1016-0707 is a potent, selective, and orally active lysophosphatidic acid receptor subtype 1 receptor (LPA1 receptor, LPAR1) antagonist with IC50 of 3.1 nM, highly selective over LPAR2 or LPAR3.

Nivasorexant is a potent orexin receptor antagonist.

IL-17A inhibitor 1 (example 24) is a IL-17A inhibitor, with IC50 values of <9.45 nM and 9.3 nM in alphalisa assay and HT-29 cells.

TM38837 is a peripheral selective cannabinoid receptor type 1 (CB1) receptor antagonist. TM38837 shows limited penetrance to the brain in order to minimize or prevent CNS adverse reactions, and preserves potential antiobesity effects. TM38837 reduces propensity for psychiatric side effects.

ET-JQ1-OH is an allele-specific BET inhibitor.

BI 1265162 is a potent ENaC inhibitor, inhibits Na+ transport with IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in cell line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.

AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.

CS27109 is a potent, selective thyroid hormone receptor-β (THR-β) agonist with AC50 value of 1.98 uM, 12.6-fold selectivity over THR-α.

Astrophloxine is a fluorescent imaging probe capable of targeting antiparallel dimers. Astrophloxine can be used to detect aggregated Aβ in brain tissue and cerebrospinal fluid samples of Alzheimer's disease (AD) mice.

GGTI 2417 is the methyl ester prodrug of GGTI-2418, a highly potent, competitive, and selective inhibitor of GGTase I.

GGTI-2147 is a non-thiol peptidomimetic that inhibits GGTase I and blocks geranyl-geranylation of Rap1A (IC50=0.5 uM).

PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R).

Rezafungin (Biafungin) is a next-generation, broad-spectrum, and long-lasting echinocandin. Rezafungin shows potent antifungal activity against Candida spp., Aspergillus spp., and Pneumocystis spp..

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.