GX-936 (PF 05196233) is a potent Nav1.7 inhibitor that binds to the activated state of voltage-sensor domain IV (VSD4), exhibits robust inhibition of the 1KαPMTX-evoked N1742K response with IC50 of 40 nM.

GYKI 52466 dihydrochloride is a selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). Skeletal muscle relaxant and orally-active anticonvulsant.

GZ389988 (GZ-389988) is a novel potent, selective, locally delivered TrkA inhibitor for the treatment osteoarthritis.

GZD856 is a novel and orally bioavailable PDGFRα/β inhibitor with IC50s of 68.6 and 136.6 nM, respectively. Anti-lung cancer activities. Also a Bcr-AblT315I inhibitor with IC50s of 19.9 and 15.4 nM for Bcr-Abl and T315I mutant.

H3B-5942 is an orally available, selective estrogen receptor covalent antagonist (SERCA), demonstrates potent ERαantagonist activity in vitro and in vivo.

H3B8800 is an orally available splicing modulator that targets spliceosome SF3b complex containing either WT or mutant SF3B1 (binding IC50 of 0.3-2 nM),demonstrates dose-dependent inhibition of both canonical splicing and aberrant splicing induced by mutant SF3B1 in in vitro assays of biochemical splicing, induces lethality in spliceosome-mutant cancer cells.. H3B-8800 potently and preferentially kills spliceosome-mutant epithelial and hematologic tumor cells.

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.

H4R antagonist 1

HA14-1 is a nonpeptidic ligand of a Bcl-2 surface pocket with IC50 of~9 μM.

Halcinonide is a high potency corticosteroid used topically in the treatment of certain skin conditions.

Halofuginone is the competitively inhibitor of prolyl-tRNA synthetase with Ki of 18.3 nM.It could also down-regulate Smad3 and blocked TGF-β signaling at 10 ng/ml in mammal.

HAMI3379 (HAMI-3379) is a potent and selective antagonist of cysteinyl leukotriene 2 (CysLT(2)) receptor, inhibits LTD4- and LTC4-induced intracellular calcium mobilization withIC50 of 3.8 nM and 4.4 nM respectively.

HAP-12 is a small molecule HBV capsid assembly effector that inhibits HBV DNA replication with EC50 of 0.5 uM..

HAR-171 is a small molecule gp120-CD40 blocker that acts as a highly potent HIV entry inhibitor with IC50 of 0.43 uM against YTA48P virus with no significant cytotoxicity (CC50>120 uM)..

H-Arg-4MβNA is a substrate for cathepsin H, used for the detection of enzyme activity in gel electrophoresis.

HBT1 is a novel potent AMPA receptor potentiator with lower agonistic effect compared with LY451395 and OXP1..

HBV Capsid inhibitor 3711 (Compound 3711) is a nonnucleosidic HBV inhibitor, inhibits hepatitis B virus replication by inducing genome-free capsid formation.

HBX 19818 is a selective USP7 inhibitor with IC50 of 28.1 uM .

HBX 28258 is a potent, selective USP7 inhibitor with IC50 of 22.6 uM, exhibits high selectivity over other USP members, such as USP8, USP5, USP2, and USP20 (IC50 >200 uM), and no activity against UCH-L1, UCH-L3 and SENP1.

HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na+]i rise is slowed by HC-056456 (IC50~3 µM).

HC-070 is a potent, selective, orally active inhibitor of TRPC4 and TRPC5 channel with IC50 of 9.3 and 46 nM (calcium influx inhibition), respectively.

HDAC6 degrader 9c (dHDAC6 9c) is a bifunctional molecule (dHDAC6) that could selectively degrade HDAC6, by conjugating non-selective HDAC inhibitor to a thalidomide-type E3 ligase ligand.