Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Gir

BMS-986122 is a potent positive allosteric modulator of μ-opioid receptor, significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by an EC10 (30 pM) concentration of endomorphin-I in CHO-μ cells..

Pramlintide is a polypeptide analogue of human amylin. Pramlintide, an antidiabetic agent, is antineoplastic in colorectal cancer.

BLU-808 is a potent and highly selective GSPT1 molecular gel degrader, with a DC50 of 154 nM. GSPT1 degrader-15 has almost no effect on the expression of other proteins. GSPT1 degrader-15 exhibits significant anti-proliferative activity against leukemia cells and lymphoma cells. GSPT1 degrader-15 can be used in leukemia and lymphoma research.

NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, has high affinity for humanized rat SUCNR1 with a Ki value of 17.4 nM.

WX-340 is a highly specific and selective, peptidic cyclic competitive inhibitor of urokinase-type plasminogen activator (uPA) with Ki of 12 and 170 nM for human and mouse uPA, respectively, inhibit 10 Units of human uPA with IC50 of 90 nM.

Influenza virus-IN-10 is a dual-target antiviral agents for influenza that targets both PAC (KD = 8.9 μM) and NP (KD = 52.5 μM) simultaneously. Influenza virus-IN-10 exhibits an EC50 values of 1.64 μM) against influenza A virus (H1N1, A/WSN/33) and broad-spectrum activity against other influenza strains, including influenza B virus and multiple subtypes of influenza A.

(±)-U-50488 ((±)-trans-(1R,2R)-U-50488) is a selective kappa opioid receptor agonist. (±)-U-50488 can improve symptoms related to status epilepticus, but has no significant effect on spontaneous seizure episodes. (±)-U-50488 can be used for research of epilepsy.

Dorzolamide is a carbonic anhydrase inhibitor. It is an anti-glaucoma agent, and acts by decreasing the production of aqueous humour. It is administered as a topical ophthalmic in the form of a 2% solution.

IM176OUT05 is a novel, and safe small molecule that improves the acquisition and maintenance of stem cell pluripotency, inhibits electron transport chain (ETC) in the A549 lung carcinoma cell line with IC50 of 3.2 uM.

MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6.

WX-02-23 is a small-molecule probe that stereoselectively and site-specifically binds to C258 of FOXA1 and C1111 of SF3B1. WX-02-23 remodels FOXA1's chromatin binding and pioneer activity in a DNA-dependent manner, disrupts spliceosome assembly, and enhances the thermal stability of SF3B1. WX-02-23 inhibits tumor cell proliferation and induces apoptosis. WX-02-23 can be used for research on cancers such as prostate cancer.

AM4113 is a cannabinoid receptor 1 (CB1)-selective antagonist.

PKI-402 is a potent dual pan-PI3K/mTOR inhibitor targeting PI3Kα/β/γ/δ and mTOR with IC50 of 2 nM/7 nM/16 nM/14 nM and 3 nM, respectively; also potent to PI3Kα mutants E545K and H1047R.

PROTAC c-Met Degrader-4 (compound D15) is a potent orally active PROTAC c-MET degrader. PROTAC c-Met Degrader-4 demonstrates excellent intracellular degradation potency with a DC50 < 0.5 nM. PROTAC c-Met Degrader-4 induces cell cycle arrest and apoptosis, inhibits cell invasion and migration, thereby suppressing cell proliferation. PROTAC c-Met Degrader-4 inhibits the growth of Hs746T xenograft tumors in nude mice. PROTAC c-Met Degrader-4 can be used for cancer research, such as non-small cell lung cancer and gastric cancer.

4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.

CGP-77675 is a potent and selective Src family kinase (SFK) inhibitor. CGP-77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively). The dual inhibition of Src and GSK-3 signaling by CGP 77675 and CHIR 99021 was found to maintain mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression as efficiently as the dual inhibition of MAPK and GSK-3 by PD 0325901 and CHIR 99021.

Aureusidin is an aurone with high antioxidant and lipoxygenase inhibitory activity. Aureusidin also shows anti-inflammatory effects.

K252c is a staurosporine analog and inhibitor of PKC and PKA. It inhibits proliferation of human cytomegalovirus and induces apoptosis in cancer cells.

Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.

LSN3172176 is a novel potent, selectiive M1 mAChR partial agonist (EC50 2.4-7.0nM, Emax 43%-73%), shows binding selectivity for M1 mAChRs (Kd=1.5 nM); LSN3172176 is a potential PET tracer for assessment of M1 mAChR target engagement in the clinic and to further elucidate the function of M1 mAChRs in health and disease.

CCT 365623 (CCT365623) hydrochloride is a potent, orally active small molecule inhibitor of lysyl oxidase (LOX) with IC50 of 0.89 uM.

VU6007477 is a novel potent, selective, CNS penetrant M1 positive allosteric modulator (PAM) with EC50 of 230 nM, 93% ACh max with minimal M1 agonist activity.

Gene-selective LXR modulator that mediates potent transcriptional activation of ABCA1 gene expression while exhibiting minimal effects on SREBP-1c

ML-191 is a potent, selective GPR55 antagonist with 160 nM potency for GPR55 and >100-fold selectivity against GPR35, CB1 and CB2.

CM-TPMF is a K(Ca)2 channel modulator with selective activation and inhibition of K(Ca)2.1 subtypes. CM-TPMF can act on K(Ca)2.1 channels as an activator or inhibitor, and its activity is affected by the stereochemical structure.

Selective antagonist of NMDA receptors NR2B subunits

PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).

SAFit2 is a selective inhibitor of the ?FK506-binding protein 51 (FKBP51).

Novel highly potent, selective, and irreversible GSTP1 inhibitor