(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABA

(+)-JQ1 PA is a Click-activated (alkyne) version of the BET bromodomain inhibitor (+)-JQ1.

(+)-JQ1 carboxylic acid is the carboxylic acid form of (+)-JQ1 for derivative synthesis.

(+)-Bicuculline is a competitive antagonist of GABAA receptors with IC50 of 2 μM, also blocks Ca(2+)-activated potassium channels.

(-)-MK 801 Maleate is the enantiomer of (+)-MK-801; (+)-MK-801 is a highly potent and selective non-competitive NMDA glutamate receptor antagonist .

(-)-Eburnamonine is a vasodilator that also acts as a cerebral metabolic stimulant.

(-)-CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 13.5 uM.

(-)-BAY-1251152 is an enanthiomer of BAY-1251152 with rotation (-). BAY-1251152 is a potent and highly selective PTEF/CDK9 inhibitor.

(-) BI97D6 (BI112D1) is a potent, pan-active inhibitor of Bcl-2 family proteins with IC50 of 76, 31, 25, and 122 nM for Bcl-xL, Bcl-2, Mcl-1, and Bfl-1, respectively.

INU-101 (INU101) is a highly potent, selective, orally acitve 11β-HSD1 inhibitor with IC50 of 26.2 nM, 37 nM and 0.6 nM for mice, rats, and human 11β-HSD1, respectively.

ASP3662 is a potent, selective, CNS-penetrable and orally active inhibitor of 11β-HSD1 with Ki of 5.3, 2.6 and 23 nM for human, mouse and rat 11β-HSD1, does not inhibit human 11β-HSD2 at 30 uM.

GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes.

NSD1 inhibitor BT5 is a covalent, small molecule inhibitor of NSD1 histone methyltransferase with IC50 of 1.4 uM, shows no covalent binding to NSD2.

IM-250 is a potent HSV-1 helicase primase inhibitor, inhibits HSV-1 replication with IC50 of 20 nM (clinical isolate of HSV-1).IM-250 dispalys similar IC50 values (20-30 nM) against ACV-resistant HSV-1 clinical isolates 2 and 3 and ACV-resistant HSV-2 clinical isolates 7 and 8.IM-250 exhibits a broad therapeutic window against HSV-1 in vitro with pronounced higher SI values as obtained for acyclovir (ACV).IM-250 shows in vivo efficacy and attenuates viral burden in HSV-1 infection mouse model.

Enclomiphene is a non-steroidal estrogen receptor antagonist that promotes gonadotropin-dependent testosterone secretion by the testes.

BLU-285 is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

SLLK, Control Peptide for TSP1 Inhibitor (TFA) is a control peptide for LSKL, which is a Thrombospondin (TSP-1) inhibitor.

Dinoprost (Prostaglandin F2α, PGF2α) is a naturally occurring prostaglandin used to induce labor and as an abortifacient, causes contraction of vascular, bronchial, intestinal, and myometrial smooth muscle, and also exhibits potent luteolytic activity..

Ulevostinag (MK-1454) is a STING agonist.

CFI-402257(luvixasertib) is a potent and selective Mps1/TTK kinase inhibitor with Ki of 0.1 nM and cellular Mps1 EC50 of 6.5 nM.

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with IC50 of 47 and 16 nM, respectively.TH9619 displays high potency and cancer selectivity in AML models. induce thymine-less DNA damage and apoptosis, causes uracil misincorporation into DNA, sensitize cancer cells to ATR-signaling blockade.TH9619 impairs cancer progression in vivo.TH9619 displays high selectivity toward binding and stabilizing MTHFD2 over other common folate metabolism targets such as DHFR, thymidylate synthase (TYMS), serine hydroxymethyltransferase (SHMT) 1 and SHMT2.

Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery.

POMHEX, a racemic mixture and a cell-permeable pivaloyloxymethyl (POM) prodrug of HEX, is a potent, ENO2-specific of enolase. POMHEX exhibits low-nanomolar potency against ENO1-deleted cells in vitro and is capable of eradicating ENO1-deleted xenografted tumours in vivo. POMHEX is a potent glycolysis.

VRK-IN-1 is a potent and selective inhibitor of vaccinia-related kinases 1 (VRK1), with an IC50 of 150 nM. VRK1 is human Ser/Thr protein kinases associated with increased cell division and neurological disorders.

YC-001 is a novel pharmacological chaperone of rod photoreceptor opsin, rescues the transport of multiple rod opsin mutants in mammalian cells.

T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 µM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).

GAT1508 (GAT-1508) is a potent, specific activator for brain-expressed GIRK1/2 channels (EC50=75 nM), specifically activates the brain GIRK1/2 over the cardiac GIRK1/4; GAT1508 is an allosteric modulator of channel–phosphatidylinositol 4,5-bisphosphate interactions. GAT1508 effectively extinguished conditioned fear in rodents and lacked cardiac and behavioral side effects, suggesting its potential for use in pharmacotherapy for post-traumatic stress disorder.

Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer.

Rv1625c agonist V-59 (V-59) is a specific small molecule agonist of the Mtb adenylyl cyclase Rv1625c, inhibits Mtb growth in macrophages (EC50=0.3 uM) in an Rv1625c-dependent mechanism.V-59 inhibits Mtb growth in cholesterol media (EC50 0.70 uM), but not in media containing the two-carbon fatty acid acetate, or in standard rich growth media.V-59 stimulates Rv1625c to produce cAMP, which is necessary for V-59 to inhibit Mtb growth.Chemically activating Rv1625c via V-59 preferentially inhibits cholesterol utilization in WT Mtb, rather than equally inhibiting all lipid utilization by the bacterium.

AEP07 (AEP 07) is a selective small molecule inhibitor of PARP4 (vPARP) inhibitor with IC50 of 0.8 uM, >12-fold selective over other PARP family members.