TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM.

A cell-permeable benzochromene that selectively impairs the viability and growth of IGF2-overexpressing hepatocellular carcinoma cells, binds to MFP-2, stimulates the expression of IGFBP-1 and SOCS-3 through activation of STAT6.

A potent, selective, brain penetrant PDE10A inhibitor with Ki of 4 nM.

A potent blocker of voltage-gated potassium channels Kv7 (KCNQ) that enhances ACh release from rat hippocampal slices in vitro with EC50 of 0.7 uM.

Firategrast is an orally bioavailable alpha4 beta1/alpha4 beta7 integrin antagonist designed to reduce trafficking of lymphocytes into the central nervous system (CNS).

CH7057288 (CH-7057288) is a novel potent and selective pan-TRK inhibitor with IC50 of 1.1/7.8/5.1 nM for TRKA/TRKB/TRKC, respectively.

AZD1390 is a first-in-class orally available and CNS penetrant ATM inhibitor with an IC50 of 0.78 nM in cells and >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases

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

Bradanicline (TC-5619) is an experimental pharmaceutical drugthat acts as a partial agonist at the α7 subtype of the neural nicotinic acetylcholine receptors.

Nelivaptan is a non-peptide vasopressin receptor antagonist that is selective for the V1B subtype.

CM-4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor, with IC50s of 119 nM, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

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;

MG624 is a potent and selective neuronal α7 nAChR antagonist with a Ki of 106 nM.

N2-OH-PhIP is a PhIP metabolite.

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]

GSK-J1 is a potent and selective inhibitor of the H3K27 histone demethylases JMJD3 and UTX (IC50 = 60 nM for human JMJD3 in vitro).

Selective urotensin-II (UT) receptor antagonist (Ki values are 61, 17, 30, 65 and 56 nM at human, monkey, cat, rat and mouse receptors respectively). Inhibits U-II-induced intracellular Ca2+ mobilization (IC50 = 180 nM) and antagonizes the contractile act

BOC-D-FMK is a cell-permeable, irreversible, broad spectrum caspase inhibitor, inhibits apoptosis stimulated by TNF-α with IC50 of 39 uM.

IMTPPE (SID3712502) is a novel small molecule capable of inhibiting androgen receptor (AR) transcriptional activity (IC50=1 uM) and protein level in C4-2 prostate cancer cells.

RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely.

CCR2 antagonist 3 is a chemokine receptor 2 (CCR2) antagonist.

BDP8900 (BDP-8900) is a highly potent and selective Myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with IC50 of 43 nM (MRCKβ), >100-fold selectivity over related ROCK1 or ROCK2.

BDP9066 (BDP-9066) is a highly potent and selective Myotonic dystrophy-related Cdc42-binding kinase MRCK inhibitor with IC50 of 43 nM, >100-fold selectivity over related ROCK1 or ROCK2.

VT-1161 is a potent, highly-selective, and oral fungal CYP51 inhibitor with Kd of ≤ 39 nM.

W-7 isomer hydrochloride is an isomer of W-7 hydrochloride. W-7 hydrochloride is a selective calmodulin antagonist.

CCB02 (CCB 02) is a specific small molecule inhibitor of CPAP-tubulin interaction with IC50 of 0.689 uM in AlphaScreen assay, selectively binds at the CPAP binding site of tubulin.

WEHI-539 is a highly potent and selective BCL-XL inhibitor. The prosurvival BCL-2 family protein BCL-X(L) is often overexpressed in solid tumors and renders malignant tumor cells resistant to anticancer therapeutics. WEHI-539 has high affinity (subnanomolar) and selectivity for BCL-X(L) and potently kills cells by selectively antagonizing its prosurvival activity. WEHI-539 will be an invaluable tool for distinguishing the roles of BCL-X(L) from those of its prosurvival relatives, both in normal cells and notably in malignant tumor cells, many of which may prove to rely upon BCL-X(L) for their sustained.

MMAF-Ome belongs to ADC, and inhibits several tumor cell lines with IC50s of 0.056 nM, 0.166 nM, 0.183 nM, and 0.449 nM for MDAMB435/5T4, MDAMB361DYT2, MDAMB468, and Raji (5T4-) cell lines, respectively.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation[1].

Eltrombopag olamine is a new, orally active thrombopoietin-receptor (c-mpl) agonist that stimulates thrombopoiesis.