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 hydrochloride 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.

(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.

(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for BET-Targeted PROTAC.

E3 ligase Ligand 17 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 17 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

Thalidomide-PEG2-C2-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.

Thalidomide-NH-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Thalidomide-O-amido-C8-NH2 (Cereblon Ligand-Linker Conjugates 2), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.

9-(2-Deoxy-2-fluoroarabinofuranosyl)guanine|2'-FANA-G

ACH-000143 is a novel potent melatonin receptor agonist with EC50 of 0.06 nM/0.32 nM against MT1/MT2. ACH-000143 leads to a reduction in body weight gain similar to dapagliflozin with superior results on hepatic steatosis and triglyceride levels in high-fat diet rats.

ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).

Colchicine is a potent therapeutic tool against COVID-19. Colchicine is a tricyclic alkaloid that is extracted from the plant Colchicum autumnale. Colchicine acts as a potent inhibitor of tubulin polymerization.

Cinobufagin, a kind of Chinese materia medica with antitumor effect, is widely used in clinical practice, especially in anti-liver cancer. IC50 value: Target: In vitro: Cinobufagin inhibited proliferation of cancer cells at doses of 0.1, 1, or 10 μM after 2–4 days of culture. Cytotoxicity of cinobufagin on the DU145 and LNCaP cells was dose-dependent. Cinobufagin increased [Ca2+]i and apoptosis in cancer cells after a 24-hr culture as well as caspase 3 activities in DU145 and PC3 cells and caspase 9 activities in LNCaP cells [1]. Cinobufagin suppresses cell proliferation and causees apoptosis in prostate cancer cells via a sequence of apoptotic modulators, including Bax, cytochrome c and caspases [2].

UCB-9260, an orally active compound, inhibits TNF signalling by stabilising an asymmetric form of the trimer. UCB-9260 is selective for TNF over other superfamily members, and binds TNF with a similar Kd of 13 nM.

EDP-305 is a novel and potent farnesoid X receptor (FXR) agonist, with no/minimal cross-reactivity to TGR5 or other nuclear receptors.

(S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs.

PF00835231(SARS-CoV-2 inhibitor 5h) is areversible-covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 4.2 µM. Compound 5h blocks the infectivity and cytopathicity of the virus with high potency and without any detectable cytotoxicity even at 200 µM.PF-00835231 is a potent inhibitor of CoV-2 3CLpro with IC50 of 4 nM and shows suitable pharmaceutical properties to warrant further development as an intravenous treatment for COVID-19.

GRL-1720 is an irreversible, covalent inhibitor of SARS-CoV-2 main protease (Mpro) with EC50 of 15 µM.

Compound 5i is a novel and brain-penetrant O-GlcNAcase inhibitor with IC50 of 46 nM.