IWP-2 is an inhibitor of Wnt processing and secretion with IC50 of 27 nM, selective blockage of Porcn-mediated Wnt palmitoylation, does not affect Wnt/β-catenin in general and displays no effect against Wnt-stimulated cellular responses.

IWP L6 is a Porcn inhibitor with EC50 of 0.5 nM.

Ivacaftor (VX-770, Kalydeco) is a potentiator of CFTR targeting G551D-CFTR and F508del-CFTR with EC50 of 100 nM and 25 nM, respectively.

Ivabradine, a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent.

ITD-1 is a novel and highly selective TGFβ pathway inhibitor. ITD-1 molecule turns stem cells into heart cells.

Itacitinib is a potent and selective inhibitor of JAK1, with >20-fold selectivity for JAK1 over JAK2 and >100-fold over JAK3 and TYK2; Itacitinib is used in the research of myelofibrosis.

ISX-9 is a small molecule inducer of adult neural stem cell differentiation both in vitro and in vivo.

Istradefylline(KW6002) is a very potent, selective and orally active adenosine A2A receptor antagonist(Ki=2.2 nM) in experimental models of Parkinson's disease.

ISRIB (trans-isomer), the trans-isomer of ISRIB, is a potent and selective PERK inhibitor with IC50 of 5 nM.

Irinotecan(CPT-11) prevents DNA from unwinding by inhibition of topoisomerase 1.

Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.

Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.

IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.

IOX1 is a potent and broad-spectrum inhibitor of 2OG oxygenases, including the JmjC demethylases.

IOX 2 is a potent inhibitor of HIF-1α prolyl hydroxylase-2 (PHD2) (IC50 = 21 nM). IOX 2 displays over 100-fold selectivity for PHD2 over factor inhibiting HIF-1 (FIH-1) and histone demethylases.

Ionophore suitable for the assay of sodium activity in blood, plasma, serum. etc. with a solvent polymeric membrane electrode.

Interleukin-1 Receptor-Associated-Kinase-1/4 Inhibitor is a benzimidazole compound that acts as a cell-permeable, potent selective inhibitor of IL-1 kinases.

INT-747(Obeticholic acid; 6-ECDCA) is a potent and selective FXR agonist(EC50=99 nM) endowed with anticholestatic activity.

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.

Inhibitor of protease-activated receptor 1 (PAR1)-mediated platelet activation (IC50 = 0.26 μM for the inhibition of platelet P-selectin expression on human platelets). Thought to act allosterically. Also inhibits thrombin-induced platelet activation.

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.