Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.

HhAntag is a GLI1-Mediated transcription inhibitor.

HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively.

HDM201 is an orally bioavailable human double minute 2 homolog (HDM2) inhibitor with potential antineoplastic activity.

HC-067047 is a potent and selective TRPV4 antagonist with IC50 values of 48 ± 6 nM, 133 ± 25 nM, and 17 ± 3 nM, respectively in human, rat, and mouse. Also inhibits the endogenous TRPV4-mediated response to 4α-PDH (IC50 = 22 nM).

HC-030031 is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively.

HBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM).

HAMNO is a novel protein interaction inhibitor of replication protein A (RPA).

HA15 displayed anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors.

HA130 is a selective ATX (autotaxin) inhibitor with IC50 of 28 nM.

H3B-6527 is an orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity.

H 89 2HCl is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II.

GZD824 is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

GW9662 is a selective PPAR antagonist, inhibiting PPARγ, PPARα and PPARδ with IC50 of 3.3 nM, 32 nM and 2 μM, respectively.

GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32.

GW806742X is a novel VEGFR inhibitor.

GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, also inhibits TGF-β type II receptor and activin type II receptor activities, but does not inhibit BMP type II receptor.

GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.

GW2580 is a selective inhibitor of human c-FMS with IC50 of 30 nM.

GW 627368X is a selective prostanoid EP4 receptor competitive antagonist with additional affinity at TP receptors (pKi values are 7.0 and 6.8 in competition radioligand bioassays).

GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM); displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fms.

GTS 21 dihydrochloride is a partial agonist of α7 nicotinic acetylcholine receptors (nAChRs); also a weak α4β2 and 5-HT3 antagonist at micromolar concentrations.

GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1).

GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183.

GSK-872 is a potent and selective RIPK3 (receptor-interacting protein kinase-3) inhibitor.

GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.

GSK-8573 is the inactive control of GSK-2801.

GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively.

GSK6853 is a potent, soluble, cell active, and highly selective inhibitor of the BRPF1 bromodomain