Gracillin is a kind of steroidal saponin isolated from the root bark of wild yam Dioscorea nipponica with antitumor agent.

GRGDSP (TFA) is an integrin inhibitor.

GRL-0617 is a potent, noncovalent SARS-CoV papain-like protease (PLpro) inhibitor with IC50 of 0.6 uM, Ki of 0.49 uM.

GS 462808 is a potent Late INa current inhibitor with IC50 of 1.33 uM.

GS-1 is a close structural analog of GS-5806 that acts an RSV fusion inhibitor.

GS-493 is a novel potent, selective SHP2 inhibitor with IC50 of 71±15 nM in enzyme assay.

GS-626510 (GS-6510, GS 6510, GS 626510) is a novel BET family bromodomains inhibitor with Kd of 0.5-2.8 nM for BRD2/3/4, and BRDT.

GS-9451 (Vedroprevir) is a potent HCV NS3/4A protease inhibitor with Ki of 0.41 nM, inhibits HCV GT-1b NS3/4A with IC50 of 3.2 nM in enzymatic assays.

GS-9695 is a potent, non-catalytic site HIV integrase inhibitor with wild type EC50 of 1.2 nM..

GS-9822 is a novel, potent NCINI with a higher barrier to resistance relative to early prototype NCINIs, including GS-9695.

GSA-10 is a novel small-molecule positive modulator of Smoothened with EC50 of 1.2 uM in the differentiation assay.

GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.

GSK1292263 is a novel GPR119 receptor agonist used for the treatment of type 2 diabetes.

GSK1904529A is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM, respectively.

GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms.

GSK2292767 is a potent and selective PI3Kδ inhibitor.

GSK2330672 is a highly potent, nonabsorbable ASBT(apical sodium-dependent bile acid transporter) inhibitor (hASBT IC50=42 ± 3 nM) .

GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM, with no activity at other close related AGC-kinases.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

GSK2814338, also known as Lp-PLA2 -IN-1, is a Lp-PLA2 inhibitor

GSK2983559 active metabolite is an active metabolite of GSK2983559. GSK2983559 active metabolite is a receptor interacting protein-2 (RIP2) kinase inhibitor extracted from patent WO/2014043446 A1, compound example 1.

GSK3039294 is a Serum amyloid P component inhibitor.

GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.

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

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

GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM.

GSK-F1 is a potent inhibitor of PI4KA.

GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM for human JMJD3 in vitro).

GSM-1 (GSM1) is a γ-secretase modulator that directly targets the transmembrane domain (TMD) 1 of presenilin 1, shows potent Aβ42-lowering effect (IC50=0.348 uM) in a cell-based assay.

GSM-2 is a second-generation γ-secretase modulator (GSM) that only decreases Aβ42 (IC50=65.2 nM), while inversely increasing Aβ38 and having no effect on β-CTF and Aβ40 levels.

GSTO1 inhibitor C1-27 is a potent, selective, covalent glutathione S-transferase omega 1 (GSTO1) inhibitor with IC50 of 31 nM.

GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.

GTC-365 (NSC 177365) is a small drug-like pharmacological chaperone that induces cancer cell death by restoring tertiary DNA structures in mutant human telomerase reverse transcriptase (hTERT) promoters.

GTC-365 (NSC 177365) is a small drug-like pharmacological chaperone that induces cancer cell death by restoring tertiary DNA structures in mutant human telomerase reverse transcriptase (hTERT) promoters.

Guanabenz (WY 8678) is an α2 adrenergic receptor agonist that is used as an antihypertensive agent, also has been proposed to exert protective effects against misfolding by interfering with eIF2α-P dephosphorylation through selective disruption of a PP1-P

Guanfacine Hydrochloride is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.

Guanidinosuccinic acid is a nitrogenous metabolite isolated in excess from serum and urine.

GUT-70 is a tricyclic coumarin derived from Calophyllum brasiliense, markedly reduces cell proliferation, viability through G1 cell cycle arrest and increases apoptosis.

GV-58 is a potent, selective N-Type and P/Q-type Ca2+ Channel agonist with EC50 of 7.2 and 8.8 uM, shows no acitivity for L-type calcium channels (EC50>100 uM).

GW 1100 is a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells stimulated by GW 9508 (an agonist of both GPR40 and GPR120, another GPCR activated by long chain fatty acids) or linoleic acid with a pIC50 value equal to 5.99.

GW 275175X is a derivative of BDCRB that displays anti-HCMV activity by inhibition of viral DNA maturation.

GW 841819X is an analogue of (+)-JQ1 and a novel inhibitor of BET bromodomain that displays activity in vivo against NUT-midline carcinoma, multiple myeloma, mixed-lineage leukemia, and acute myeloid leukemia..

GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse, respectively.

GW274150 is a novel arginine-competitive, NADPH-dependent iNOS inhibitor that has been identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration.Target: iNOSin vivo: GW274150 demonstrates a narrow neuroprotective therapeutic window against the toxic actions of 6-OHDA. GW274150 administration leads to a dose-dependent decrease in the number of iNOS-positive cells in the SNc of the 6-OHDA-lesioned animals. The iNOS inhibitor GW274150 fails to produce long-term neuroprotection after its withdrawal in the 6-OHDA-lesioned rat. [1]

GW311616A is a potent, intracellular human neutrophil elastase (HNE, α-1-proteinase) inhibitor.

GW406108X (GW-406108X, GW108X) is specific inhibitor of Kif15 (Kinesin-12) with IC50 of 0.82 uM in ATPase assays.

GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity.

GW-766994 (GW766994) is a potent, selective, orally available CCR3 antagonist with pKi of 7.86 for inhibiting eotaxin-induced eosinophil chemotaxis in vitro assays.

GW-766994 (GW766994) is a potent, selective, orally available CCR3 antagonist with pKi of 7.86 for inhibiting eotaxin-induced eosinophil chemotaxis in vitro assays.

GW-8510 (GW8510) is a potent, selective inhibitor of CDK2 with IC50 of 10 nM.

GWJ-A-23 (GWJ-23, GWJ23) is a potent, selective autotaxin inhibitor with Ki of 18 nM, an analog of the known ATX inhibitor S32826 and has improved aqueous solubility compared with the parent compound.

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.

HDAC6-AR-IN-10 is a potent dual HDAC6/AR inhibitor with IC50 of 35.6 nM/<30 nM, shows weak inhibition on HDAC1/2/3 (IC50>1 uM).

HDAC8-IN-20a is a potent, selective HDAC8 inhibitor with IC50 of 27 nM.

HEC72702 is a novel potent, orally active inhibitor of HBV capsid assembly, inhibits HBV-DNA levels in HepG.2.2.15 cells with IC50 of 39 nM.

HEC-73543 is a novel potent, selective, orally bioavailable FLT3 inhibitor for the treatment of refractory acute myeloid leukemia (AML).

Hedgehog-IN-7d is a potent, cell-permeable Hedgehog (Hh) pathway inhibitor that inhibits Gli transcription activity with an IC50 value of 70 nM..

Helenalin (NSC 85236) is a sesquiterpene lactone that covalently targets Cys38 on p65 transcription factor in the canonical NF-κB signaling pathway.

Hemicholinium-3 (HC-3) is a competitive, small molecule inhibitor of choline kinase (ChoK) with ex vivo IC50 of 500 uM, also bolcks the sodium and chloride-dependent transport system and affects choline acetyltransferase.

Hemin, a physiological erythroid maturation stimulator, is able to induce the expression of critical autophagic genes (Map1a1b (LC3), Beclin-1 gen, Atg5) in an erythroleukemia cell type.

Hemoglobin modulator TD-1 (TD-1) is a novel allosteric effector of hemoglobin that increases hemoglobin oxygen affinity and reduces SS erythrocyte sickling.

Heparin Lithium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII).

Heptamethine cyanine dye-1 is a near-infrared cyanine dye for fluorescence imaging in biological systems.

HER2-IN-2 is a potent, selective HER2 inhibitor, only shows potent inhibition for EGFR and Abl in a panel of kinases.

HER2-IN-3 is a type I HER2 inhibitor that has a similar profile to HER2-IN-2.

Herboxidiene (GEX1A, TAN-1609) is a polyketide molecule first isolated from the fermentation broth of Streptomyces chromofuscus, shows in vitro antitumor activity by targeting the SF3B protein in the splicesosome.

HET0016 (HET-0016) is a potent, selective inhibitor of CYP4A, potently inhibits the formation of 20-HETE with IC50 of 8.9 nM in human renal microsomes.

Hetrombopag is a potent, selective, orally-active Thrombopoietin (TPO) receptor agonist.

Hexacosanoic acid is a long-chain fatty acid related to various diseases such as adrenoleukodystrophy (ALD), adrenomyeloneuropathy (AMN) and atherosclerosis.

Hexamethylquercetagetin is a polymethoxylated flavone in peels of citrus cultivars.

Hexaminolevulinate hydrochloride is a fluorescent agent, has approved for cystoscopic detection of papillary bladder cancer.

Hexokinase 2 modulator Comp-1 is a potent, selective small molecule modulator of Hexokinase 2 (HK2) interaction with the mitochondria, selectively dissociates HK2 from VDAC1 in vitro with IC50 of 92 nM.

HG-12-6 is a small-molecule inhibitor that bind preferentially to unphosphorylated IRAK4 with IC50 of 165.1 nM, displays 15-fold selectivity over phosphorylated IRAK4 (IC50=2876 nM).

HG6-64-1 is a potent dual TAK1 and MAP4K2 ((germinal center kinase, GCK)) inhibitor with IC50 of 41 nM and 98 nM, respectively.

HG-7-27-01 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 224 nM, displays intermediate selectivity profiles (selectivity score=0.16) against 442 kinases..

HG-7-92-01 is a potent, selective c-Fes protein-tyrosine kinase inhibitor with IC50 of 292 nM, displays intermediate selectivity profiles (selectivity score=0.18) against 353 kinases..

H-Gly-Arg-pNA is a colorimetric substrate for thrombin.

HIF2α-IN-2 is a potent, selective, allosteric inhibitor of HIF-2α PAS-B domain with Kd of 81 nM, shows high selectivity and does not affect HIF-1 function.

Highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.

H-Ile-Pro-Pro-OH, a milk-derived peptide, inhibits angiotensin-converting enzyme (ACE) with an IC50 of 5 μM. Antihypertensive tripeptides.

Hinokitiol (4-Isopropyltropolone.

Hippuristanol is a potent, steroid inhibitor of eukaryotic initiation factor 4A (eIF4A), results in cell cycle arrest at G1 phase, and induces caspases activation and apoptosis.

HIV-1 inhibitor 18A is a novel broad HIV-1 inhibitor that blocks envelope glycoprotein transitions critical for entry, specifically inhibits the entry of a wide range of HIV-1 isolates with mean IC50 of 6.4 uM.

HIV-1 integrase inhibitor ((Z)-4-(3-(azidomethyl)phenyl)-2-hydroxy-4-oxobut-2-enoic acid) is uesful for anti-HIV.

HIV-1 Integrase Inhibitor 7 is an allosteric HIV-1 integrase inhibitor that inhibits the LEDGF/p75-integrase interaction with IC50 of 0.58 uM, antiviral activity EC50 of 0.76 uM..

HIV-1 integrase inhibitor, in the treatment of human immunodeficiency virus (HIV) infection.

HJC0197 is a potent Epac1 (exchange protein directly activated by cAMP 1) and Epac2 (IC50=5.9 μM for Epac2) antagonist. HJC0197 selectively blocks cAMP-induced Epac activation. HJC0197 inhibits Epac1-mediated Rap1-GDP exchange activity at 25 μM in the presence of equal concentration of cAMP.

HJC 0726 is a potent Exchange proteins directly activated by cAMP (EPAC) inhibitor, inhibits cAMP-mediated EPAC2 GEF activity with IC50 of 1.0 uM.

HJC0152 is a signal transducer and activator of transcription 3 (STAT3) inhibitor with remarkably improved aqueous solubility.

HJC-0338 is a potent and specific EPAC2 antagonist with IC50 of 0.4 uM for competing with 8-NBD-cAMP in binding EPAC2.

HKI 357 is an irreversible dual inhibitor of the EGF receptor tyrosine kinases EGFR and HER2 (IC50s = 34 and 33 nM, respectively).

HL001 (HL 001) is a potent cyclophilin A (CypA) inhibitor with IC50 of 31.6 nM, induces NSCLC cell cycle arrest and apoptosis via restoring p53 expression.

HlyU inhibitor CM14 (1025E12) is a specifc, small-molecule inhibitor of transcriptional regulator HlyU activity with EC50 of 30.97 uM, inhibits HlyU from binding to target DNA by covalently modifying Cys30.

HM30181 is a potent and selective inhibitor of P-glycoprotein.

HM30181 mesylate is a competitive and potent P-glycoprotein inhibitor.

HMN-214(IVX214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM.

HMPC is a novel bacteriostatic agent that shows bacteriostatic activity against S. aureus (MIC=4 μg/ml) and rescues Caenorhabditis elegans from S. aureus infection.

HMS-101 (HMS101) is a potent, selective mutant IDH1 inhibitor, the IC50 is significantly lower in mouse bone marrow cells transduced with IDH1mut compared with IDH1wt (1 uM vs 12 uM, respectively).

Hoechst 33342 3Hcl(HOE 33342 3Hcl) is an AT-specific DNA minor groove ligand used fluorochrome for visualizing cellular DNA.

Hoechst stains are part of a family of blue fluorescent dyes used to stain DNA.

HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=2.8 uM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the N

HOIPIN-8 (HOIP inhibitor-8) is a potent chemical inhibitor of linear ubiquitin chain assembly complex (LUBAC, IC50=11 nM), specifically generates Met1-linked linear ubiquitin chains through the ubiquitin ligase activity in HOIP, and activates the NF-kB pa

Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinfammatory and antioxidant properties.

Hosenkoside A is a baccharane glycoside isolated from the seeds of impatiens balsamina.

Hosenkoside B is a baccharane glycoside isolated from the seeds of impatiens balsamina.

Hosenkoside F is a baccharane glycoside isolated from the seeds of impatiens balsamina.

Hosenkoside K is a baccharane glycoside isolated from the seeds of impatiens balsamina.

Hosenkoside M is a baccharane glycoside isolated from the seeds of impatiens balsamina.

hPGDS-IN-1 is a potent, selective hPGDS inhibitor with IC50 of 12 nM in FP or EIA assays..

HPI-1 is a Hedgehog (Hh) pathway inhibitor that suppresses signaling through Shh (IC50=1.5 uM) without significantly affecting Wnt signaling (IC50>30 uM).

HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.

HS148 (DAPK3 inhibitor HS148) is a selective DAPK3 inhibitor with Ki of 119 nM, >10-fold selectivity over Pim kinases..

HS-152 (HS152) is a specific small-molecule inhibitor of SMAD ubiquitin regulatory factor 1 (SMURF1), not only potently inhibits SMURF1-mediated RHOB degradation with IC50 of 3.2 uM, but also strongly blocks SMURF1-mediated RHOA and SMAD1 degradation (IC5

HS-173 is a potent PI3Kα inhibitor with IC50 of 0.8 nM.

HS220 (HS-220) is a Plasmodium-selective takinib analog that targets atypical P. falciparum protein kinase 9 (PfPK9, Kd=4.1 uM) but does not inhibit HsTAK1, decreases K63-linked ubiquitination in P. falciparum; inhibits P. berghei parasite load in HuH7 ce

HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3), shows micromolar potency toward Pim-1 and Pim-2 (Ki=1.5 and 17 uM).

HS-72 is an allosteric, selective, cell-permeable inhibitor of inducible Hsp70 (Hsp70i or Hsp72), shows selectivity for Hsp70i over the closely related Hsc70 as well as the broader purinome.

HSD1169 is a potent, dual FLT3/TOPK inhibitor with activity against FLT3-ITD secondary mutations (D835 or F691, Kd=1-5 nM), potently inhibits acute myeloid leukemia cell lines (IC50=5 nM).

HSD992 is a potent, selective CDK2/3 inhibitor with moderate CDK9 inhibition with IC50 of 18 nM, 57 nM and 49 nM for CDK3/cyclin E, CDK2/cyclin A1 and CDK2/cyclin E, respecively.

HSK0935 is a potent, highly selective and orally available SGLT2 inhibitor with an IC50 of 1.3 nM. Antihyperglycemic activities.

hSMG-1 inhibitor 11e is a potent, selective hSMG-1 kinase inhibitor with IC50 of <0.05 nM, >900-fold selectivity over mTOR, and no significant activity against CDK1/2..

hSMG-1 inhibitor 11j is a potent, selective hSMG-1 kinase inhibitor with IC5 0of 0.11 nM, 455-fold selectivity over mTOR and no activity against CDK1/2.

HSP27 inhibitor J2 is a small molecule functional inhibitor of Hsp27, induces significant abnormal HSP27 dimer formation in cancer cells.

HSP70 modulator 115-7c is an artificial co-chaperone, enhancer of Hsp70, stimulats the ATPase and protein-folding activities of a prokaryotic Hsp70 (DnaK) and partially compensated for a Hsp40 loss-of-function mutation in yeast.

HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM.

HT-0712 (IPL-455903) is a novel potent, selective PDE4 inhibitor with IC50 of 0.15 uM for PDE4D3, without effect on PDE1B, PDE3A, and PDE10A.

hTG2 inhibitor VA4(VA4) is a novel potent, irreversible inhibitor of human tissue transglutaminase (hTG2) with Ki of 12.9 uM, allosterically abolishs its GTP binding ability with a high degree of selectivity and efficiency.

HTH-01-091 is a potent and selective, cell-permeable, ATP-competitive MELK inhibitor with biochemical IC50 of 10.5 nM.

HTS01037 is a highly potent ligand of adipocyte fatty acid binding protein (A-FABP/aP2) with Ki of 0.67 uM.

Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).

H-Val-Pro-Pro-OH (TFA), a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.

H-Val-Pro-Pro-OH, a milk-derived proline peptides derivative, is an inhibitor of Angiotensin I converting enzyme (ACE), with an IC50 of 9 μM.

HX600 (HX-600) is a synthetic agonist of RXR-Nurr1 heterodimer complex, also selectively activate NGFI-B/RXR heterodimers.

Hydrazinocurcumin is a synthetic curcumin derivative that inhibits the proliferation of bovine aortic endothelial cells (BAECs) with IC50 of 520 nM without cytotoxicity, inhibits STAT3 phosphorylation and downregulates an array of STAT3 downstream targets.

Hydroquinidine is an antiarrhythmic agent.

Hydroxyprogesterone Caproate is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.

Hydroxyzine is a histamine H1 receptor antagonist (Ki = 1.9 nM).

Hypericin is a photosensitive antiviral with anticancer and antidepressant agent derived from Hypericum perforatum. It can inhibit tyrosine kinases with IC50 of 7.5 μM.

HZ05 is a potent DHODH inhibitor with IC50 of 32 nM, accumulates cancer cells in S-phase, increases p53 synthesis, and synergizes with an inhibitor of p53 degradation (Nutlin-3a) to reduce tumor growth in vivo..

HZ-166 (HZ166) is a GABAA receptor subtype-selective benzodiazepine site ligand with preferential activity at α2- and α3-GABA(A) receptors.

IAA-94 is an indanyloxyacetic acid blocker of epithelial chloride channels.

IACS-10759 is a potent inhibitor of complex I of oxidative phosphorylation (OXPHOS).

IACS-4759 potent, selective aminopyrimidine MTH1 (MutT homolog 1) inhibitor with IC50 of 0.2 nM.

IACS-4759 potent, selective aminopyrimidine MTH1 (MutT homolog 1) inhibitor with IC50 of 0.6 nM.

IACS-7e is a potent TRIM24 bromodomain inhibitor with IC50 of 217.8 nM (TRIM24 ligand displacement)..

IACS-9571 is a potent, selective dual TRIM24-BRPF1 bromodomain inhibitor with Kd of 31 and 14 nM, respectively.

IAXO-102 is a novel selective TLR4 antagonist, negatively regulates non-hematopoietic TLR4 signalling and inhibits experimental AAA development.

IBET151-VHL-PROTAC is a novel PROTAC..

Ibiglustat (succinate) is a selective inhibitor of glucosylceramide synthase.

IB-MECA is a potent and selective A3 adenosine receptor agonist (Ki values are 1.1, 54 and 56 nM for A3, A1 and A2A receptors respectively).

IBR2 is a novel small molecule RAD51 inhibitor that specifically binds to RAD51 and disrupts the BRC repeats of BRCA2/RAD51 interaction with IC50 of 0.11 uM.

IBS003031 (IBS-003031) is a novel chemical Yes-associated protein 1 (YAP1) activator, up-regulates H2B-mCherry expression at 1 and 3 uM in mCherry signal based reporter assays.

Ibufenac is an analog of the NSAID ibuprofen that inhibits COX-1 and -2 activity with IC50 values of 17.4 and 13.1 µM, respectively.

Ibulocydine is the prodrug of CDK inhibitor BMK-Y101, inhibits CDK7 and CDK9 with IC50 of 530 nM and 85 nM in kinase assays, respectively.

IC 86621 is a potent DNA-PK inhibitor with IC50 of 135 nM, also inhibits p110β (IC50=135 nM), less potent for p110α/γ/δ (IC50=880-1,400 nM).

IC 87361 is a potent and selective DNA-PK inhibitor with IC50 of 34 nM, shows >50-fold selectivity over p110β.

IC-9564 (AIDS033640) is a betulinic acid derivative and potent HIV entry inhibitor that blocks HIV-1 envelope-mediated membrane fusion with IC90 of 0.22 uM for NL4-3 strain.

ICA-1(ICA-1T)is a potent, specific inhibitor of Protein Kinase C-iota (PKC-ι) with IC50 of 0.1 uM, does not inhibit PKC-ζ, the closely related atypical PKC family member.

ICA135 (ICA-135, ICA 135) is a broad-spectrum inhibitor against human enteroviruses that inhibits Coxsackievirus A10 (CV-A10) replication in RD cells with IC50 of 1.446 uM.

ICI-118,551 is a selective beta-2 (β2) adrenergic receptor antagonist.ICI binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor.

Icotinib(BPI-2009) is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).

iCRT-5 is a selective, cell-permeable β-catenin responsive transcription (CRT) inhibitor with IC50 of 18 nM.

ICSN3250 (ICSN-3250) hydrochloride is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors.

ICSN3250 (ICSN-3250) is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors.

IDD388 is a potent aldose reductase (ALR2 or AKR1B1) inhibitor with IC50 of 0.4 uM, shows weak inhibition for AKR1B10 (IC50=4.4 uM)..

IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.

IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively. Anticancer activity.

IDRA-21 is a positive allosteric modulator of the AMPA receptor (AMPAR).

IDX-17119 is a potent, non-nucleoside, HCV NS5B RdRp inhibitor with IC50 of 0.4 nM in replicon luciferase assay.

IDX-375 is a novel potent, non-nucleoside, allosteric HCV NS5B RdRp inhibitor with IC50 of 15 nM and 5 nM for 1a-H77 HCV NS5B polymerase and 1b-J4 HCV NS5B polymerase, respectively.

IEM 1754 2HBr is a selective AMPA/kainate receptor blockers for GluR1 and GluR3 with IC50 of 6 μM.

IFNAR-IN-1 is a nonpeptidic, small molecule inhibitor of IFN-α and IFNAR interaction, specifically inhibits MVA-induced IFN-α responses by BM-pDCs with IC50 of 2-8 uM..

iGOT1-01 is a small molecule inhibitor of aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1 (GOT1)) with IC50 of 11.3 uM.

IGS-1.76 is a small molecule inhibitor of human NCS-1/Ric8a interaction with affinity of 1.25 uM (hNCS-1).

Iguratimod is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, analgesic and antipyretic activity.

IHVR-19029 is a novel antiviral compound that acts as ER α-glucosidase inhibitor, synergistically inhibits the replication of Yellow fever and Ebola viruses in cultured cells combined with favipiravir (T-705).

IIIC3 (Gallocyanine.

IIIM-290 is a potent, orally active cyclin-dependent kinase (CDK) inhiitor with IC50 of 1.9 and 16 nM for Cdk-9/T1 and Cdk-2/A, respectively.

GDC0214 is a potent, selective inhalable and lung-restricted inhibitor of JAK1 with IC50 of 8.52 nM, displays 6.3/704/28 fold selectivity over JAK2/JAK3/TYK2.