PKC-theta inhibitor is a selective PKC-θinhibitor, with an IC50 of 12 nM.

PIK-75 is a selective cell-permeable inhibitor of PI 3-kinase p110α (IC50 values are 5.8, 76 nM and 1.3 μM at PI 3-kinase p110α, PI 3-kinase p110γ and PI 3-kinase p110β respectively). Inhibits production of PIP2 and PIP3 in adipocytes, phosphorylation of

ICA 110381 (Compound 16) is a KCNQ2/Q3 potassium channel opener for the treatment of epilepsy. ICA 110381 is a KCNQ2/Q3 agonist (EC50=0.38 μM) as well as KCNQ1 antagonist (IC50=15 μM).

GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein.

Fluorofenidone is an inhibitor of nicotinamide adeninedinucleotide phosphate oxidase via PI3K/Akt pathway in the pathogenesis of renal interstitial fibrosis.

FGH10019 is a novel sterol regulatory element-binding protein (SREBP) inhibitor with IC50 of 1 μM.

Etosalamide, also known as Ethosalamide, is an antipyretic and analgesics agent.

DMNQ is a redox cycling agent that generates both superoxide and hydrogen peroxide intracellularly in a concentration dependent manner. DMNQ increases ROS generation.

ARN 272 is a fAAH-like anandamide transporter (FLAT) inhibitor (IC50 = 1.8 μM); cytosolic variant of FAAH-1 that binds anandamide.

Adenosine Amine Congener is shown to be an aqueous-soluble Adenosine A1-R agonist.

A 438079 is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

A specific blocker of the time dependent delayed rectifier potassium current, devoid of any β-adrenoceptor blocking activity. Exhibits proarrhythmic and prohypertensive activity in vivo.

1-BCP is a centrally active drug that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.

2-HBA, a synthetic analog of curcumin, is an indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway.

GSK3179106 (GSK-3179106, GSK 3179106) is a potent, selective, first-in-class and gut-restricted with IC50 of 0.4 and 11 nM in the biochemical assay and cellular assay respectively.

GSK 5959 is a potent, cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM).

GSK163090 is a potent, selective, and orally active 5-HT1A/B/D receptor antagonist with pKi of  9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3, respectively.

GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

GSK1940029 is a stearoyl CoA desaturase 1 inhibitor.

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC50 of 2 nM and 40 nM for rTRPV4 and hTRPV4.

GSK2200150A is an antimycobacterial agent against Mycobacterium tuberculosis and Mycobacterium bovis BCG.

GSK2838232 is a novel human immune virus (HIV) maturation inhibitor being developed for the treatment of chronic HIV infection.

GSK-2894631A,GSK 2894631A，GSK2894631A

GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain

GSK9311 is a potent and highly selective inhibitor of the BRPF bromodomain (BRPDF1 pIC50 = 6.0; BRPDF2 pIC50 = 4.3).

Arginase inhibitor 1 is a potent inhibitor of human arginases I and II with IC50s of 223 and 509 nM, respectively.

(S,R,S)-AHPC-PEG3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.