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

GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).

GSK-137647 is a potent and selective FFA4 (GPR120) agonist (pEC50 values are 6.3, 6.2 and 6.1 at the human, mouse and rat receptor, respectively). Exhibits ≥100-fold selectivity against a panel of 61 targets including FFA1, FFA2 and FFA3.

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.

GSK180736A is a G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.

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.

GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.

GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.

GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively.

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.

GSK2256098 is small molecule FAK kinase inhibitor.

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).

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.

GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.

GSK2606414 is an orally available, potent, and selective PERK inhibitor with an IC50 of 0.4 nM.

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.

GSK2643943A is a potent USP20 inhibitor with IC50 = 160 nM.

GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC50 of 0.9 nM. It is highly selective for PERK with IC50 values >100 nM against a panel of 300 kinases.

GSK269962A(GSK269962) is a potent ROCK inhibitor (IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively); displays greater than 30-fold selectivity for ROCK against a panel of serine/threonine kinases.

GSK2801 is a very potent inhibitor of the BAZ2 family of bromodomain containing proteins.

GSK-2807 (GSK 2807, GSK2807) is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki of 14 nM.

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

GSK2838232 is a novel human immune virus (HIV) maturation inhibitor being developed for the treatment of chronic HIV infection.

GSK2879552 is an orally available, irreversible, inhibitor of lysine specific demethylase 1 (LSD1), with potential antineoplastic activity.

GSK-2881078 is an orally active and nonsteroidal selective androgen receptor modulator (SARM) which act as partial AR agonists in androgenic tissues while mainly as complete AR agonists in synthetic metabolic tissues,induces AR-mediated transcriptional activation in PC3(AR)2 cells (EC50 = 3.99 nM) and the effect can be inhibited by the non-steroidal AR antagonist Bicalutamide. GSK-2881078 can be used in research of muscle weakness and cachexia associated with both chronic and acute illness.

GSK-2894631A,GSK 2894631A，GSK2894631A

GSK2981278 is a highly potent and selective inverse agonist of retinoic acid receptor-related orphan receptor gamma (ROR gamma).

GSK2982772 is a potent and ATP competitive RIP1 inhibitor with an IC50 of 16 nM.

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.

GSK3117391 (CHR5154) is a HDAC inhibitor.

GSK3145095 is an orally available, small-molecule inhibitor of RIPK1, with potential antineoplastic and immunomodulatory activities.

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.

GSK3326595(EPZ015938) is the first-in-class protein arginine methyltransferase-5 (PRMT5) inhibitor.

GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases.

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

GSK3787 is as a potent and selective antagonist of PPARδ with pIC50 of 6.6.

GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

GSK467 is a potent and selective inhibitor of KDM5 (also known as JARID1). GSK467 exploits unique binding modes.

GSK484 is a reversible inhibitor of PAD4 (IC50 = 50 nM) that binds to the low-calcium form of the enzyme.

GSK503 is a specific EZH2 methyltransferase inhibitor.

GSK547 (RIP1i, GSK 547) is a highly selective and potent inhibitor of RIP1 kinase that robustly targets RIP1 in vivo.

GSK583 is a Highly Potent and Selective Inhibitor of RIP2 Kinase (RIP2K bing IC50=5 nM; rat in vivo PD IC50 = 50 nM).

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

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

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

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

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

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.

GSK9311 is a potent and highly selective inhibitor of the BRPF bromodomain (BRPDF1 pIC50 = 6.0; BRPDF2 pIC50 = 4.3).

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).

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

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

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

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

Guanoclor is a sympatholytic drug. It is known to bind to non-adrenergic sites in pig kidney membranes.

GW 4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.

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.

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 7647 is a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ.

GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

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.

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

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]

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

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

GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes.

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

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.

GW806742X is a novel VEGFR inhibitor.

GW843682X is a cell-permeable thiophene-benzimidazole compound and reversible PLK inhibitor

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

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

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

GX-674 is a potent, selective Nav1.7 inhibitor with IC50 of 0.1 nM.

GYY 4137 is a Water-soluble, slow-releasing hydrogen sulfide donor.

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.

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.

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.

H-151(H151) is a novel STING (stimulator of interferon genes) antagonist.

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

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.

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

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

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

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

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

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

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).

hClpP activator D9 is a potent and species-selective activator of human ClpP (hClpP, human Caseinolytic protease P) by mimicking the natural chaperone ClpX..

HDAC inhibitor IV is a cell-permeable pimeloylanilide compound that acts as a FXN- (frataxin gene) specific HDAC (histone deacetylase) inhibitor.

HDBA, a derivative of a Streptomyces griseolavendus butyl acetate extract, is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase with an IC50 value of 0.012 µM.

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

Hederacoside C is a principal bioactive pharmaceutical ingredient of Hedera helix leaf that can treat respiratory disorders, because of its expectorant, bronchodilator, antibacterial, and bronchospasmolytic effects.

Hederagenin a triterpenoid saponin, is used to study the properties of triterpenoid saponins as biopesticides that prevent fungal growth, bacterial growth, and viral plant diseases.

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

Hesperadin inhibits Aurora B and T. brucei Aurora kinase-1 (TbAUK1) with IC50 of 250 nM and 40 nM, respectively.

Hexadimethrine bromide is a cationic polymer discovered to enhance retroviral transduction.

HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.

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..

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.

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

HhAntag is a GLI1-Mediated transcription inhibitor.

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.

Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.

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.

Darunavir(TMC114) is an HIV protease inhibitor,showed potent activity against COVID-19(SARS-COV-2) .

HIV-1 attachment inhibitor,a prodrug of the small-molecule inhibitor BMS-626529

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-0350 is a selective Epac2 inhibitor (IC50 = 0.3 μM). Displays no effect on Epac1. Blocks stimulation of the Epac2-FL FRET sensor in HEK293 cells.

HLCL-61 is a first-in-class small-molecule inhibitor of PRMT5 for treatment of acute myeloid leukemia.

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

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

HM-61713 (BI-1482694) is an orally available small molecule, mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity.

HMN-154 is a novel benzenesulfonamide anticancer compound; inhibits KB and colon38 cells with IC50 values of 0.0026 and 0.003 μg/mL, respectively.

HMN-176 is a stilbene derivative which inhibits mitosis without significant effect on tubulin polymerization.

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

HOE-140 (Icatibant) is a potent and selective bradykinin B2 receptor antagonist (pA2 = 9.04). Also inhibits aminopeptidase N (Ki = 9.1 μM).

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

Homoharringtonine(HHT) is a cytotoxic alkaloid from the evergreen tree.

Honokiol(NSC-293100), a hydroxylated biphenyl compound isolated from the Chinese herb Magnolia officinalis, has been reported to have anticancer activities in a variety of cancer cell lines.

HPGDS inhibitor 1 is a novel and selective Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value of 0.7 nM.

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).

HPOB is a novel selective inhibitor of HDAC6 catalytic activity in vivo and in vitro.

HS-10 is a novel Hsp90 inhibitor increases the Tm of Hsp90 by 10.5°C.

HS-10296 is an orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant form T790M, with potential antineoplastic activity.

HS-1371 is a novel kinase inhibitor of RIP3-mediated necroptosis.

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

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

Hs-27 is a Novel Hsp90 Inhibitor, Exhibits Diagnostic and Therapeutic Potential in Triple Negative Breast Cancer.

HS-38 is a potent and selective DAPK1 and DAPK3 (ZIPK) inhibitor with IC50 of 200 nM for DAPK1 and Kd of 280 nM for ZIPK, also inhibits Pim3 (IC50=200 nM), and displays no activity against Src or Abl, little activity against EGFR;

HS94 (DAPK3 inhibitor HS94) is a selective DAPK3 inhibitor with Ki of 126 nM, >20-fold selectivity over Pim kinases..

HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1).

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

HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.

HT-2157 (SNAP 37889) is a selective, high-affinity, competitive antagonists of galanin-3 receptor (Gal3).

HTH-01-015 is a selective inhibitor of NUAK1 kinase with an IC50 value of 100 nM.

HTHQ, which is a hydroquinone monoalkyl ether, is a potent anti-oxidative agent, even at low dose levels.

HUHS015 is a prostate cancer antigen (PCA)-1/AlkB homologue 3 (ALKBH3) inhibitor.

hVEGF-IN-1 represses human VEGF-A translation and shows antitumor activity.

Hycanthone, the most potent mutagen in a series of nine thiaxanthenones, is a potent inducer of nuclear immunoreactivity to antinucleoside antibodies in HeLa cells.

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.

Hydroxyfasudil Hcl(HA1100 Hcl), metabolite of Fasudil, is a potent Rho-kinase inhibitor and vasodilator.

Hydroxy-Fasudil is a metabolite of Fasudil, acting as a potent Rho-kinase inhibitor and vasodilator.

Hydroxyhexamide is a pharmacologically active metabolite of Acetohexamide, used as a hypoglycemic agents.

Hypocrellin B is an apoptosis inducer. The hypocrellins are pigments isolated from the fungi Hypocrella bambusae and Shiraia bambusicola. They are used as photosensitizers for photodynamic therapy of cancer.

Hypoxia-inducible factor prolyl hydroxylase inhibitor

HZ-1157 is a novel potent inhibitor of HCV NS3/4A protease; Potent Dengue virus inhibitor

I-191 is a novel potent, selective protease-activated receptor 2 (PAR2) antagonist with pIC50 of 7.2 in cell-based assays.

IACS-010759 (IACS010759) is a small molecule inhibitor of mitochondrial oxidative phosphorylation (OXPHOS), targets complex I of the mitochondrial electron transport chain.

Iberdomide (CC-220) is a cereblon modulator in clinical development for systemic lupus erythematosis. Iberdomide exhibits an IC50 of 60 nM in TR-FRET cereblon binding assay.

Iberin, a sulfoxide analogue of sulforaphane, is a naturally occurring member of isothiocyanate family. It inhibits cell survival with an IC50 of 2.3 μM in HL60 cell.

I-BET151 (GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM, respectively.

Ibiglustat (Genz-682452,SAR402671), is a potent and selective Glucosylceramide synthase inhibitor and ceramide glucosyltransferase inhibitor.

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).

IBMX(NSC165960; SC2964) is a competitive nonselective PDEs inhibitor with IC50 of 2-50 uM but does not inhibit PDE8 or PDE9; nonselective adenosine receptor antagonist.

I-BRD9 is a potent and selective BRD9 inhibitor (pIC50 = 7.3). Exhibits >70-fold selectivity for BRD9 over a panel of 34 other bromodomains and >700-fold selectivity over the BET family.

Ibudilast(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor which has been marketed for treating asthma,ibudilast (MN-166) is tested to treat acute respiratory distress syndrome (ARDS) associated with Covid-19.

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue.

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).

IC261 is a novel inhibitor of CK1, triggers the mitotic checkpoint control. The IC50 of IC261 for CK1 was 16 μM and for Cdk5 is 4.5 mM.

IC-87114 was the first isoform-selective PI3K inhibitor. p110δ(IC50 = 0.13 μM) vs. p110α(IC50 = 200 μM), p110β(IC50 = 16 μM) and p110γ(IC50 = 61 μM).

ICA 069673 is a potassium channel opener with selective action for KCNQ2 and KCNQ3 (EC50=0.69 μM). No meeasurable activity was displayed over a variety of cardiac ion channels.

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.

ICA-121431 is a potent, selective inhibitor of the human Nav1.3 and Nav1.1 voltage gated sodium channels (IC50 = 19 nM) with little or no activity against human Nav1.5 or Nav1.7 channels.

Icariside I is a metabolite of Icarlin, which could regulate bone remodeling and is recognized as an effective agent for the treatment of osteoporosis.

Icaritin shows potent anti-leukemia activity on chronic myeloid leukemia in vitro and in vivo by regulating MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings.

I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively).

ICEC0942 is a selective CDK7 inhibitor, with IC50s of 41 nM and 578 nM for CDK7/CycH/MAT1 and CDK2/cycE1, respectively.

ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding pro

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.

Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel.

Icotinib 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 14 is a novel potent inhibitor of β-catenin-responsive transcription (CRT) (IC50 = 40.3 nM in assays of Wnt pathway activity).

iCRT3 is an inhibitor of both Wnt and β-catenin-responsive transcription.

Idarubicin Free Base is an orally administered anthracycline antineoplastic. The compound has shown activity against BREAST NEOPLASMS; LYMPHOMA; and LEUKEMIA.

Idarubicin Hcl is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor.

IDE-1 induces definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 125 nM).

IDE-2 is a cell-permeable inducer of definitive endoderm formation in mouse and human embryonic stem cells (ESCs) (EC50 = 223 nM for induction of Sox17 expression in ESCs).

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

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

IDH889 is a potent and selective inhibitors of IDH1. IDH899 shows IDH (R132H) IC50 = 20 nM; Cell 2-HG IC50 = 14 nM.

IDO-IN-1 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50 of 59 nM, shows activity in Hela cell (IC50=12 nM).

IDO-IN-2 is an IDO inhibitor extracted from patent WO/2015031295 A1, compound example 1, has IC50 values of 0.068 μM in HeLa cell and 0.16 μM in HEK293 cell.

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

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

IITZ-01 is a novel potent lysosomotropic autophagy inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo.

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.