GSK620 is a potent and orally active pan-BD2 with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620

Giredestrant (GDC-9545), a non-steroidal estrogen receptor (ER) ligand, is an orally active and selective ER antagonist. Giredestrant potently competes with Estradiol for binding and induces a conformational change within the ER ligand binding domain. Gir

GSK963 is a chiral, highly potent and selective inhibitor of RIP1 kinase, with an IC50 of 29 nM. GSK963 is a selective and potent inhibitor of necroptosis in murine and human cells in vitro.

IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and

GSK481 is a Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitor (RIP1 inhibitor). The recent discovery of the role of receptor interacting protein 1 (RIP1) kinase in tumor necrosis factor (TNF)-mediated inflammation has led to

GSK2983559 free acid (compound 3) is a potent, specific and oral bioavailable receptor interacting protein 2 (RIP2) kinase inhibitor. GSK2983559 free acid has excellent activity in blocking many proinflammatory cytokine responses in vivo and in human infl

GC376 is a novel, first-in-class, small molecule protease inhibitor with a favorable therapeutic index demonstrated in preclinical studies. A common feature of viruses in the picornavirus-like supercluster (including coronaviruses) is a 3C or 3C-like prot

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2)

GLPG0187 is a small molecule integrin receptor antagonist (IRA) with potential antineoplastic activity.

GDC-0810 (ARN-810, Brilanestrant) is a non-steroidal, orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM (ER-α degradation), binds to ERα and ERβ with with Ki of 3.8 and 3.7 nM, respectively.

Ifenprodil tartrate is a NMDA receptor antagonist, specifically targets GluN1 and GluN2B subunits, also inhibits GIRK channels, and interacts with alpha1 adrenergic, serotonin, and sigma receptors..

Inhibitor of plasminogen activator inhibitor-1 (PAI-1)

INF39 is an irreversible and noncytotoxic NLRP3 inhibitor.

Indirubin is a potent cyclin-dependent kinases and GSK-3β inhibitor with IC50 of about 5 μM and 0.6 μM.

Indiplon is a novel sedative-hypnotic recently approved for the treatment of insomnia.

INCB28060 is a novel orally active inhibitor (IC50=0.13 nM) of c-MET kinase.

INCB024360 is a potent IDO1 inhibitor(IC50=10 nM) with desirable pharmaceutical properties, which is poised to start clinical trials in cancer patients.

Inarigivir(SB-9000) is a novel dinucleotide, evaluated in transgenic mice expressing hepatitis B virus (HBV), significantly reduced liver HBV DNA。

Imiquimod is an immune response modifier that acts as a toll-like receptor 7 agonist and is commonly used topically to treat warts on the skin of the genital and anal areas.

Imidafenacin(KRP-197; ONO-8025) is a potent and selective inhibitor of M3 receptors with Kb of 0.317 nM; less potent for M2 receptors(IC50=4.13 nM).

IMD-0354 is a synthetic selective NF-kB inhibitor.

IM176OUT05 is a novel, and safe small molecule that improves the acquisition and maintenance of stem cell pluripotency, inhibits electron transport chain (ETC) in the A549 lung carcinoma cell line with IC50 of 3.2 uM.

Ilaprazole (IY-81149) is a proton pump inhibitor; inhibits H+/K+-ATPase with an IC50 of 6.0 μM.

IKKε-IN-1 is a potent IKKε inhibitor; inhibit the in-situ ΙKΚ ε-mediated phosphorylation of IRF3 with an IC50 value of less than about 100 nM.

IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.

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

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.

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.

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.

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).