EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM.

EPZ020411 is a potent and selective inhibitor of PRMT6 with IC50 of 10 nM, has ＞10 fold selectivity for PRMT6 over PRMT1 and PRMT8.

Erianin, often used as an antipyretic and analgesic agent, could inhibit IDO-induced tumor angiogenesis.

ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively.

Erlotinib (OSI-744; NSC 718781; R1415) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

Esonarimod (KE-298) is a new antirheumatic drug.

ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).

ETH 157（Sodium ionophore II）is a neutral ionophore for liquid-membrane electrodes of high selectivity for Na+.

Etofenamate is a non-steroidal anti-inflammatory drug used for the treatment joint and muscular pain.

ETP-46321 is a potent and orally bioavailable PI3K α/δ inhibitor with IC50 of 2.3/14.2 nM for p110α/p110β; exhibits potency on mutated p110α(IC50=1.77-2.33 nM, p110a E542K; E545K; H1047R).

ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively).

BI-0115 is a selective small molecule inhibitor of LOX-1 that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain. The structure of LOX-1 bound to BI-0115 shows that inter-ligand interactions at the receptor interfaces are key to the formation of the receptor tetramer thereby blocking oxLDL binding.

Org-41841 is an agonist for the luteinizing hormone/chorionic gonadotropin receptor (LHCGR) and partial agonist for TSHR.

AS2717638 is an oral active lysophosphatidic acid receptor 5 (LPA5) antagonist in rodents. AS2717638 also significantly improves PGE2-, PGF2α-, and AMPA-induced allodynia.

Aplaviroc, also known as AK-602; GW-873140; GW873140A; ONO-4128, is a CCR5 entry inhibitor for the potential treatment of HIV infection. Aplaviroc (GW873140) binds specifically to human cellular CC chemokine receptor 5 (CCR5) and demonstrates potent anti-human immunodeficiency virus activity in vitro in the subnanomolar range. In vitro studies show that aplaviroc selectively inhibits the binding of a particular monoclonal antibody, 45531, to CCR5.

SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD SAR439859 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells

Piperidolate is a tertiary amine antimuscarinic. It is similar to atropine. It is mainly used in the smooth muscle spasm of the gastrointestinal tract and inhibits intestinal cramp induced by acetylcholine in rats and dogs.

LY-3475070 is a potent and selective CD73 Inhibitor with IC50 of 28 nM. LY3475070 Alone or in Combination With Pembrolizumab is now under trials for patients with Advanced Cancer.

ZAP-180013 is a Zap70 inhibitor, which inhibits interaction with ITAMs (immunoreceptor tyrosine-based activation motifs).

MK2 Inhibitor III is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis.

NK-252 is a Nrf2 activator. It acts by interacting with the Nrf2-binding site of Keap1 and downregulates the expression of fibrogenic genes.

Evacetrapib (LY2484595) is a potent and selective inhibitor of CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure.

Evatanepag (CP-533536) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.

Rhosin (G04) is a potent, specific RhoA subfamily Rho GTPases inhibitor that specifically binds to RhoA to inhibit GEF reaction of RhoA with Kd of 0.4 uM, does not interact with Cdc42 or Rac1, nor the LARG.

F1063-0967 is a Dual-specificity phosphatase 26 (DUSP26) inhibitor with an IC50 of 11.62 μM.

Fantofarone is a calcium channel blocker.

Fascaplysin is a potent, selective ATP-competitive CDK4 inhibitor (IC50 = 350 nM).

FG-2216 is a potent HIF-prolyl hydroxylase inhibitor with IC50 of 3.9 uM for PDH2 enzyme; orally bioavailable and induced significant and reversible Epo induction in vivo.

FH1 (BRD-K4477) is a small molecule, which promotes differentiation of iPS-derived hepatocytes.