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).

3-(2-Hydroxyethyl) thio withaferin A is a Withaferin A derivative. Withaferin A, a steroidal lactone, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.

11-O-Methylpseurotin A is a compound of mixed polyketide synthase–nonribosomal peptide synthetase (PKS/NRPS) origin. 11-O-Methylpseurotin A selectively inhibits a Hof1 deletion strain.

Aspulvinone O is a natural inhibitor of aspartate transaminase 1 (GOT1). GOT1 plays an important role in energy metabolism and Reactive Oxygen Species (ROS) balance. GOT1 may serve as an important target in PDAC. Aspulvinone O suppresses pancreatic ductal adenocarcinoma cells growth by interfering glutamine metabolism.

Choline oxidase catalyzes the oxidation of choline to glycine betaine via betaine aldehyde in glycine betaine biosynthesis and betaine acts as an osmolyte. Choline oxidase has potential in enzymatic betaine production.

Glucoarabin is a bioactive glucosinolate. In Hepa1c1c7 cells, hydrolyzed Glucoarabin (hGSL 9) upregulates the phase II detoxification enzyme quinone reductase (NQO1), with no effect on cytochrome P450 (CYP) 1A1 activity.

Anhydroophiobolin A is a potent inhibitor of photosynthesis with IC50s of 77 and 14 mM in the photosynthesis of chlorella and spinach, respectively. Anhydroophiobolin A is an analog of Ophiobolin A.

Agonodepside B is a compound isolated from a nonsporulating filamentous fungus, F7524.

(-)-(E)-Guggulsterone is the metabolite of Z-guggulsterone. Guggulsterone is an active constituent of guggulipid, an ayurvedic drug derived from Commiphora mukul. Guggulsterone has hypolipidaemic activity.

Muristerone A is a phytoecdysteroid analog of ecdysone and a potent agonist of ecdysteroid receptor with a Kd of 1 nM.

Mycestericin C is a compound isolated from the culture broth of Mycelia sterilia ATCC 20349. Mycestericin C suppresses the proliferation of lymphocytes in the mouse allogeneic mixed lymphocyte reaction.

Tajixanthone is the fungus metabolite from Aspergillus variecolor.

Hortein is a natural product from the fungus Hortaea werneckii associated with the sponge Aplysina aerophoba.