ACC2 inhibitor 2e is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 1.9 nM and 1950 nM for ACC2 and ACC1, respectively.ACC2 inhibitor 2e exhibited good PK profile and in vivo antidiabetic efficacy in C57BL/6 mice.

AA6216 (AA 6216) is novel potent, selective PDE4 inhibitor with IC50 of 0.63 nM.AA6216 showed stronger inhibitory effects against PDE4 than other PDE family members. AA6216 potently inhibits cytokine production (TNF-α,IL-12p40, IL-4, and IL-13, IC50s=2.2-7.9 nM) by PBMCs stimulated with PHA.AA6216 inhibited the production of TGF-β1 by a human monocytic cell line THP-1, AA6216 dose-dependently reduced the production of TNF-α by alveolar macrophages from patients with IPF.AA6216 demonstrated anti-fibrotic potency on mouse model of bleomycin-induced lung fibrosis.

A-908292 is a highly potent and selective acetyl-CoA carboxylase 2 (ACC2) inhibitor with IC50 of 38 nM (hACC2), no activity against ACC1 (IC50>30 uM).

A potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively; displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins; increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM; attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion.

A potent, selective PDE4 inhibitor with pIC50 of 11.5, 11.3, 11.4, and 11.9 for PDE4B, A, C, and D, respectively; displays >380,000-fold selectivity over PDE1/23/5/6/7; inhibits TNFα production by lLPS-stimulated human peripheral blood monocytes with IC50 of 0.01 nM; inhibites LPS-induced pulmonary neutrophilia with ED50 of 1.1 ug/kg (aqueous suspension) and 2.9 ug/kg (dry powder formulation) in rats.

A novel potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 of 4.5 nM.

A novel potent kynurenine-3-monooxygenase (KMO) inhibitor with IC50 of 2.3 nM and 0.7 nM for human KMO and Pf-KMO, respectively.

A cell-permeable small molecule inhibitor of Fumarase (fumarate hydratase), an enzyme of the tricarboxylic acid cycle (TCA cycle); elicits a nutrient-dependent cytotoxicity in a number of cancer cell lines, and displays increased growth-inhibitory activity toward SW620 cell line grown in the absence of glucose (mean IC50=2.2 uM).

8-BOA is a selective and potent mechanism-based inactivator of breast cancer-associated CYP4Z1.8-BOA exhibited favourable inhibitory activity in vitro, thus meriting in vivo characterization.

NSC45586 free base (NCS 45586, NCI45586) is a potent, specific PHLPP2 inhibitor with IC50 of 4 uM, targets the PHLPP2 PP2C domain, suppresses MYC and triggers cell death.

WX-UK1 (UKI-1) is a small synthetic serine protease uPA (urokinase-type plasminogen activator) inhibitor that blocks tumor cell invasion, metastasis and primary tumor growth.

GLPG1972 (Aldumastat, S201086) is a potent and selective small-molecule inhibitor of ADAMTS5 with IC50 of 19 and <23 nM against human and rat ADAMTS5, respectively.

GSK 2793660(GSK2793660) is a potent, selective, irreversible and orally bioavailable cathepsin C inhibitor, but not the activity of downstream neutrophil serine proteases, for the treatment of cystic fibrosis, non-cystic fibrosis bronchiectasis, ANCA-associated vasculitis and bronchiectasis..

GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).

SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo.

(S)-ABBV-CLS-484 is a potent PTPN1 or PTPN2 inhibitor.

SHP2 inhibitor is an effective SHP2 allosteric inhibitors (IC50≤50 nM), blocking the activation of SHP2 by targeting the auto-inhibited conformation of SHP2 (WO2019183367A1, compound 118).

Rubratoxin A is a natural mycotoxin and competitive inhibitor of protein phosphatase 2A (PP2A) with an IC50 of 170 nM. Rubratoxin A causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.

Trichomide A is a potent activator of SHP2. Trichomide A is a natural cyclodepsipeptide. Trichomide A displays immunosuppressive activity against activated T lymphocyte–mediated immune responses in Con A-activated T cells. Trichomide A have the potential for the research of immune-related skin diseases.

Geodin, a fungal metabolite, shows antibacterial activity. Geodin also is an inhibitor of plasminogen activator inhibitor- 1 (PAI-1).

Monoacylglycerol lipase inhibitor 1 is a potent monoacylglycerol lipase inhibitor (compound 13).

LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM.

Ellipyrone B, an antihyperglycemic γ-pyrone enclosed macrocyclic polyketide, shows inhibition potential against dipeptidyl peptidase-4 (IC50=0.48 mM).

Ellipyrone A, a γ-pyrone enclosed macrocyclic poyketide, shows inhibition potential against dipeptidyl peptidase-4 (IC50=0.35 mM). Ellipyrone A also has anti-carbolytic property against α-glucosidase (IC50=0.74 mM) and α-amylase (IC50=0.59 mM).

DHODH-IN-19 is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-19 inhibits tumor growth. DHODH-IN-19 has the potential for the research of cancer and inflammation disease (extracted from patent WO2021238881A1, compound 1).

DHODH-IN-20 (Compound 133) is a potent inhibitor of DHODH. DHODH is present in the inner membrane of human mitochondria and is an iron-containing flavin-dependent enzyme. DHODH-IN-20 inhibits tumor growth. DHODH-IN-20 has the potential for the research of acute myelogenous leukemia.

CYP121A1-IN-1 is a potent CYP121A1 inhibitor with favorable activity against Mycobacterium tuberculosis (H37Rv MIC90∼6.25 μM, ∼2.2 μg/mL). CYP121A1-IN-1 can markedly reduce the production of mycocyclosin via inhibiting the CYP121A1 mediated turnover of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin.

Cholesterol 24-hydroxylase-IN-1 (compound 17) is a potent, orally active, and highly selective cholesterol 24-hydroxylase (CH24H or CYP46A1) inhibitor (IC50=8.5 nM). Cholesterol 24-hydroxylase-IN-1 can cross blood-brain barrier.

BACE1-IN-7-18F can be developed as a PET tracer for in vivo imaging of BACE1. The unlabeled BACE1-IN-7 is a potent BACE1 inhibitor (IC50=13.2 nM).

hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD).