JAK1-IN-31 is a potent and selective JAK1 inhibitor with Ki of 1.9 nM, less potent for JAK3 (Ki=280 nM) and Tyk2 (Ki=12 nM) and no inhibition on hERG and CYP3A4 (IC50>10 uM).

J-113397 is a potent, selective nociceptin/orphanin FQ receptor (NOP receptor/ORL1) antagonist with IC50 of 2.3 nM.

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM.

Ivacaftor (VX-770, VX770) is a potent, orally bioavailable CFTR potentiator, increases G551D- and F508del CFTR-mediated Cl- secretion with EC50 of 100 nM.

ITZ-1 is a client-selective Hsp90 inhibitor that efficiently induces heat shock factor 1 (HSF1) activation, selectively inhibits IL-1β-induced MMP-13 production (IC50=0.51 uM) via inhibition of ERK activation.

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels.

ITI-214 is a potent, selective, orally active phosphodiesterase 1 (PDE1) inhibitor with Ki of 58 pM, displays >1,000-fold selectivity over PDE4A/4D and other PDE isoforms.

IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

Istaroxime(PST2744) is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

Istaroxime(PST2744) is a positive inotropic agent that mediates its action through inhibition of sodium/potassium adenosine triphosphatase (Na+/K+ ATPase).

iST2-1 is a first-in-class, in vivo active ST2 (suppression of tumorigenicity 2) inhibitor with IC50 of 56.14 and 54.62 uM in AlphaLISA and the HEK-Blue IL-33 assay, respectively.

Isothiafludine (NZ-4) is a novel HBV capsid assembly inhibitor that inhibits HBV replication through blocking pregenomic RNA encapsidation, suppresses HBV replication in HepG2.2.15 cells with IC50 of 1.33 uM.

Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.

Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13, 0.432 μM for α-glucosidase and AGE, respectively.

Isoquercitrin is an effective antioxidant and an eosinophilic inflammation suppressor.

Isonicotinic acid is a metabolite of isoniazid. It is an isomer of nicotinic acid.

Isomigrastatin (iso-Migrastatin) is an analogue of migrastatin that shows potent antiproliferative effect on tumor cell lines and selectively inhibits translation.

Isomangiferin is the major tetracyclic oxindole alkaloid components of Uncaira species, inhibits NMDA receptor with IC50 of 43.2 uM, also blocks calcium channel.

Isoginkgetin (Iso-ginkgetin.

Isocryptotanshinone is a potent signal transducer and activator of transcription 3 (STAT3) and protein tyrosine phosphatase 1B PTP1B inhibitor, with an IC50 of 56.1 μM for PTP1B.

Isocarboxazid is a non-selective and irreversible inhibitor of monoamine oxidase, with an IC50 of 4.8 μM for rat brain monoamine oxidase in vitro.

Isoastragaloside IV is a triterpene oligoglycoside isolated from Astragali Radix.

ISO-92 is a potent inhibitor of macrophage migration inhibitory factor (MIF) tautomerase activity with IC50 of 0.55 uM..

ISO-66 is a novel, highly stable, small-molecule MIF inhibitor that inhibits MIF tautomerase activity with IC50 of 1.4 uM.

Isavuconazonium is a water-soluble prodrug form of the azole antifungal isavuconazole (ISA).

Isavuconazole(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557, exhibits MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata.

Isatoribine is a selective agonist of TLR7

Isatin is an endogenous MAO inhibitor.

ISA27 is a novel small molecule that blocks p53-MDM2 interaction and induces apoptosis both in vitro and in vivo.

ISA-2011B is a PIP5Kα inhibitor with promising anticancer effects .