BGG463 can inhibit c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants with a 50% inhibitory concentration (IC50) of 0.25 μM, 0.09 μM and 0.590 μM, respectively.

BIX 02565 is a novel ribosomal S6 kinase 2 (RSK2) inhibitor with an IC50 of 1.1 nM.

CFI-400437 is potent against PLK4 (IC50 = 0.6 nM) and selective against other members of the PLK family (>10 uM).

Mubritinib is a potent inhibitor of the human epidermal growth factor receptor 2 (HER2) tyrosine kinase.

SD169 is an orally available, ATP-competitive, isoenzyme-selective Mitogen-Activated Protein Kinase (MAPK) inhibitor.

RET-IN-1 is a RET kinase inhibitor extracted from patent WO2018071447A1, Compound Example 552, has IC50s of 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively .

A potent PIKfyve inhibitor that inhibits autophagy by impairing lysosomal maturation, potently and reversibly inhibits autophagosome-lysosome fusion by activating RAB5A.

COG 133 is a fragment of Apolipoprotein E (APOE) peptide. COG 133 competes with the ApoE holoprotein for binding the LDL receptor, with potent anti-inflammatory and neuroprotective effects. COG 133 is also a nAChR antagonist with an IC50 of 445 nM[1][2].Substantially reduces the symptoms of experimental autoimmune encephalomyelitis, a model of human multiple sclerosis, and suppresses inflammation, demyelination and infiltration of cells into the spinal cord. Also acts as a non-competitive antagonist at α7 nicotinic acetylcholine receptors (IC50 = 445 nM).

A potent inhibitor of hTGase (Tissue transglutaminase) with IC50 of 0.8 uM.

TY-52156 is a potent and selective inhibitor of S1P3 receptor (Ki=110 nM).

HLM006474 is a pan-E2F inhibitor. It inhibits DNA binding to E2F1, E2F2, and E2F4 in A375 melanoma cells when used at a concentration of 40 μM.

Astemizole is a histamine H1-receptor antagonist. Astemizole competitively binds to histamine H1-receptor sites in the gastrointestinal tract, uterus, blood vessels, and bronchial muscle. This suppresses the formation of edema and pruritus caused by histamine. Astemizole is structurally similar to terfenadine and haloperidol; it has anticholinergic and antipruritic effects.

Lersivirine (UK-453061) is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) under development for the treatment of HIV-1 infection.

BI 167107 is a highly potent agonist of the β2 adrenergic receptor (β2AR) and β1AR (IC50=3.2 nM) and shows some activity as α1A antagonist (IC50 = 32 nM).

AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β.

OSU-T315 (ILK-IN-1) is a potent and specific integrin-linked kinase (ILK) inhibitor which inhibits PDK2 function in the AKT pathway activation

K-7174 dihydrochloride is a selctive small molecule inhibitor of the transcription factor GATA-binding protein 2 (GATA2).

MsbA inhibitor 1 is a novel small molecule lipopolysaccharide biogenesis inhibitor, inhibits MsbA, an ATP-dependent flippase that translocates LPS across the inner membrane; causes mislocalization of LPS to the cell interior, inhibits Δ5 strain with MIC o

SLMP53-1 is a novel reactivator of wild-type and mutant p53, shows a p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells.

TRIF agonist AV-C is a novel TRIF pathway agonist that activates innate and interferon-associated responses, strongly inhibits replication of ZIKV, CHIKV, and DENV (IC90~5 uM).

A potent, specific, competitive inhibitor of choline kinase-α (Chok-α) by targeting the choline binding site; significantly increases LC3II expression in MCF-7 and MCF-7/TAM cells, increases the size and number of autophagosome, causes MCF-7 and MCF-7/TAM

PF 04878691 (PF 4878691, S 32865, 852A, 3M 001) is a selective TLR7 agonist that potently induces IFN-α and IFN-regulated proteins from human PBMC.

BK-1361(BK1361, cyclo-RLsKDK) is a cyclic peptide with RLsKDK (s=D-serine) that functions as a potent, selective inhibitor of ADAM8 with IC50 of 120 nM.

GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.

LLY-283 (LLY283) is a potent, selective inhibitor of arginine methyltransferase 5 (PRMT5) with IC50 of 22 nM.

S-99 inhibits LPS-induced TNFa release assay in vivo

RO495 is a very potent TYK2 inhibitor with a IC50 of 1.5nM on TYK2 as tested in cell-based pharmacological assays

NIBR-17 is a pan class I PI3K inhibitor with IC50 values of 1, 9.2, 9 and 20 nM respectively for PI3Kapha - delta.

GDC046 is a potent lead analog with good kinase selectivity, physicochemical properties, and pharmacokinetic profile.

The compound (Akt-I-1) inhibits only Akt1 (IC50 4.6 μM) and does not inhibit AKT2, or AKT3.