ME-3277 is a potent GPIIb/IIIa antagonist. ME-3277 reduces cerebral infarction without enhancing intracranial hemorrhage in photothrombotic occlusion of rabbit middle cerebral artery (MCA). ME-3277 can be used for the acute cerebral infarction research.

LY377604 hydrochloride is a human β3-adrenergic receptor agonist with an EC50 of 2.4 nM and also a β1- and β2-adrenergic receptor antagonist.

Hakin-1 is a E3 Ubiquitin-Ligase Hakai inhibitor. Hakin-1 blocks Hakai-mediated global ubiquitination and specific ubiquitination of E-cadherin and inhibits epithelial-mesenchymal transition (EMT) progression. Hakan-1 inhibits tumor progression and cancer metastasis. Hakin-1 can be used for the study of carcinoma such as colorectal cancer.

UNC10415667 is a NSD2 degrader, with a DC50 values of 460 nM. UNC10415667 can be used for the study of cancers driven by NSD2 overexpression or dysregulation, such as multiple myeloma, acute lymphocytic leukemia, and prostate cancer.

LY334370 fumarate is the fumarate of LY334370). LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.

IHCH-7179 is a 5-HT receptor modulator. IHCH-7179 can antagonize 5-HT2A receptor and activate 5-HT1A receptor. IHCH-7179 can be used for the research of neurological disease.

PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.

ML189 is an HSP90 inhibitor. ML189 can be used in the research of infectious diseases such as candidiasis.

NCX-530 is an Indomethacin molecule chemically conjugated with a NO moiety. NCX-530 can release NO. NCX-530 can inhibit cancer cells proliferation and induce apoptosis. NCX-530 can be used for the researches of cancer and inflammation.

ZA18 is a selective TRPM2 channel inhibitor, with an IC50 value of 6.2 μM. ZA18 can effectively suppress intracellular Ca2+ overload triggered by TRPM2 channel activation. ZA18 significantly reduce the mortality of SH-SY5Y cells induced by H2O2. ZA18 can be used for the study of ischemia-reperfusion injury, inflammation, or other neurodegenerative diseases.

UR-1505 is a nuclear factor of activated T cells (NF-AT) inhibitor. UR-1505 can suppress CD3/CD28 induced T cell proliferation, increase p27KIP levels, and induce G1/S cell cycle arrest. UR-1505 can also inhibit the production of IL-5 and IFN-γ in activated T cells. UR-1505 has immunomodulatory properties and can be used in the study of atopic dermatitis.

SCYX-6759 is an orally active, blood-brain barrier permeable anti-T. brucei agent. SCYX-6759 inhibits cytochrome P450 (IC50s: 30.3, 30.6, 47.4 μM for 2D6, 2C9, 2C19, respectively.) SCYX-6759 exhibits potent activity against T. b. brucei 427, T. b. rhodesiense STIB900, and T. b. gambiense STIB930, with IC50s of 0.07, 0.038 and 0.030 μg/mL, respectively.

KMS99220 is an orally active Nrf2 inhibitory protein Keap-1 activator. KMS99220 promotes Nrf2 nuclear translocation, up-regulates the gene expression of antioxidant enzymes (such as heme oxygenase-1, etc.) and proteasome subunits, alleviates oxidative stress and protein aggregation damage. KMS99220 can be used in the research of Parkinson’s disease (PD).

Z169667518 is a ligand of IL-6. Z169667518 can inhibit IL-6-induced STAT3 reporter activity with an IC50 of 2.7 µM. Z169667518 can be used in the research of IL-6-related diseases.

NRX-204647 is a potent activator of retinoic acid nuclear (RARγ) with higher specificity than that to RARα and RARβ. NRX-204647 can be studied in anti-cancer research.

ZC9 is a novel androgen receptor (AR) degrader. ZC9 directly binds to AR and inhibits Dihydrotestosterone-induced nuclear translocation of AR. ZC9 promotes AR degradation via the ubiquitin-proteasome system and suppresses AR transcriptional activity. ZC9 significantly decreases the mRNA levels of other AR downstream genes, including PSA, TMPRSS2, and PMEPA1. ZC9 promotes Apoptosis. ZC9 exhibits anticancer activity against prostate cancer.

CDD-1154 is an aminopyrimidine analog. CDD-1154 is a BRDT-BD2 inhibitor (IC50: 139 nM). CDD-1154 is used in male contraceptive research.

CDD-1498 (Compound 12) is a potent inhibitor of BRDT-BD2. CDD-1498 has an IC50 of 978 nM against BRDT-BD2. CDD-1498 can be studied in research on nonhormonal contraceptive agent.

CDD-1128 (Compound 11) is a potent inhibitor of BRDT-BD2. CDD-1128 has an IC50 of 521 nM against BRDT-BD2. CDD-1128 can be studied in research on nonhormonal contraceptive agent.

CDD-1147 is a BRDT-BD2 inhibitor with an IC50 of 94 nM. CDD-1147 can be used in the research of non-hormonal contraceptives for men.

CDD-1349 (Compound 15) is a BRDT-BD2/BRD4-BD2 selective inhibitor. CDD-1349is an analog with sixfold selectivity for BRDT-BD2 versus BRD4-BD2. CDD-1349 has an IC50 of 22 nM against BRDT. CDD-1349 can be studied in research on nonhormonal contraceptive agent.

INI3069 is a selective human stimulator of interferon gene (STING) agonist. INI3069 is promising for research of cancers.

CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC50 of 17 nM for MEK1.

NGI-235 is a selective OST-A inhibitor that inhibits NF-κB inflammatory signaling by blocking TLR4 glycosylation.

Pyridostatin (RR82) trihydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin trihydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin trihydrochloride targets the proto-oncogene Src. Pyridostatin trihydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.

C791-0064 is a RAD52 inhibitor. C791-0064 specifically binds to RAD52 and disrupts its single-strand annealing activity. C791-0064 specifically inhibits the proliferation of cancer cells with BRCA2 deficiency, inducing DNA damage and apoptosis (apoptosis). C791-0064 can be used for the study of BRCA mutation-related cancers (such as breast cancer and ovarian cancer).

FR-181074 is a selective and orally active PDE V inhibitor. FR-181074 can specifically block PDE V to inhibit the degradation of cyclic guanosine monophosphate (cGMP) in order to relax smooth muscle. FR-181074 can be used for the research of cardiovascular disease and endocrinology, such as hypertension and erectile dysfunction.

CTS-21166 is a blood-brain barrier-permeable and orally active BACE1 inhibitor. CTS-21166 reduces brain Aβ levels. CTS-21166 can be used in the research of Alzheimer's disease.

MP1202 is a dual-functional agonist of MOR and KOR with EC50s of 0.32 and 0.13  μM for mMOR-1 and mKOR-1, respectively. MP1202 has functional selectivity with reduction of β-arrestin1/2 recruitment but significant activation of G-protein and Gα-subtype at hMOR and hKOR. MP1202 has potent antinociceptive effects without typical opioid side effects, but it shows conditioned place preference and aversion behaviors in subtype-selective opioid KO mice model, promising for analgesia research.

ABT-255 free base is an orally active anti-bacterial agent. ABT-255 free base exhibits potent in vitro potency (MIC = 0.016-0.031 μg/mL) against drug-susceptible and Rifampin- or Ethambutol-resistant Mycobacterium tuberculosis. ABT-255 free base shows efficacy against S. aureus, S. pneumoniae and E. coli and reduces viable counts of drug-resistant Mycobacterium tuberculosis in CF-1 mice. ABT-255 free base can be used for the study of pulmonary tuberculosis.