A partial/full agonist of dopamine receptor with Ki of 3.9/2.2/0.5/5.1 nM for D2S/D2L/D3/D4, respeectively.

Hispidin, a PKC inhibitor and a phenolic compound from Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties.

Alpinumisoflavone (compound 2) is a flavonoid derivative isolated from the stem bark of Erythrina lysistemon Hutch.

Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.

Wighteone is a compound isolated from the aerial parts of Genista ephedroides.

Osajin is the major bioactive isoflavone present in the fruit of Maclura pomifera with antitumor, antioxidant and anti-inflammatory activities.

Hispolon, a polyphenol, can be isolated from Phellinus linteus. Hispolon possesses anticancer, antidiabetic, antioxidant, antiviral, hepatoprotective, anti-diabetic, and anti-inflammatory activities.

Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM)[1][2][3]. Bexarotene can be used for the research of cutaneous T-cell lymphoma.

C53 (PC-C53-N, Z1861995405) is a novel small molecule enhancer of the CUL3/LZTR1 E3 ligase KRAS complex.

Z86 (Z6466689386) is a novel small molecule enhancer of the CUL3/LZTR1 E3 ligase KRAS complex.

A novel small molecule that inhibits GATA4/NKX2-5 transcriptional synergy with IC50 of 3 uM, with no activity on the protein kinases involved in the regulation of GATA4 phosphorylation.

Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.

PD-166793 is a cell-permeable biphenylsulfonylvaline compound that acts as a potent inhibitor against MMP-2, -3, and -13 (IC50 = 47, 12, and 8 nM, respectively) and a weaker inhibitor against AMP deaminase (20% inhibition at 0.1 μM), MMP-1, -7, -9, and -14 (IC50 = 6.1, 7.2, 7.9, and 0.24 μM, respectively). Shown to offer therapeutic benefits in vivo in various animal models of heart failure and diabetes.

TC KHNS 11 is a potent and selective PI 3-kinase δ inhibitor that is orally bioavailable.

Novel Integrin very late antigen-4 (VLA-4; α4β1) antagonist, blocking the activation of inflammatory cells.

FK-888 is a selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. FK-888 inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo.

ML354 (VU0099704) is a novel potent and selective PAR4 antagonist with IC50 of 140 nM, displays 71-fold selectivity versus PAR-1.

Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

CDK9 inhibitor HH1 is a novel potent, highly selective CDK9 inhibitor..

CHDI-390576 (CHDI390576) is a potent, cell permeable and CNS penetrant class IIa HDAC inhibitor with IC50 of 54/60/31/50 nM for HDAC4/5/7/9, respectively.

Floctafenine, also known as R-4318 and Idarac, is a cyclooxygenase inhibitor that inhibits prostaglandin synthesis.

Novel TRPM8 channel blocker

CCT129202 is a potent, selective, ATP-competitive pan-Aurora kinase inhibitor with IC50 of 42, 198 and 227 nM for Aurora A, Aurora B and Aurora C, respectively.

YTHDC1 inhibitor 40 is a potent, selective m6A reader YTHDC1 inhibitor with ITC Kd of 49 nM, HTRF IC50 of 0.35 uM. Compound 40 shows antiproliferative activity against the acute myeloid leukemia (AML) cell lines THP-1, MOLM-13, and NOMO-1.YTHDC1 inhibitor 40 exhibits antiproliferative activity against THP-1 (GI50 = 3.2 μM), MOLM-13 (5.6 μM) and NOMO-1 (8.2 μM), respectively. YTHDC1 inhibitor 40 displays IC50 values of 89, 60, and 83 μM against YTHDF1, YTHDF2, and YTHDF3, respectively, indicating a 200-fold selectivity.YTHDC1 inhibitor 40 does not display significant inhibition of a panel of 58 protein kinases.YTHDC1 inhibitor 40 (2.5-10 uM) induces apoptosis in THP-1 cell line after 24 h treatment.YTHDC1 inhibitor 40 is a tool compound for studying the role of YTHDC1 in AML.

NS-018 maleate (NS018, Ilginatinib) is a potent and highly selective JAK2 inhibitor (IC50=0.72 nM).