ESI-05 is a potent EAPC2-specific antagonist that inhibits cAMP-mediated EPAC2 GEF activity with apparent IC50 of 0.43 uM.

JNJ-47965567 is a potent, selective, centrally permeable P2X7 receptor antagonist with pKi of 7.9 and 8.7 for human and rat P2X7, respectively.

MJN110 (MJN-110) is a potent, selective, and orally active MAGL inhibitor with IC50 of 2.1 nM (2-AG hydrolysis).

KT-109 is a potent, selective inhibitor of DAGLβ with IC50 of 42 nM, displays about 60-fold selectivity over DAGLα.

Apicidin (OSI 2040) is a fungal metabolite that exhibits potent, broad spectrum antiprotozoal activity in vitro, potently inhibits HDAC with IC50 of 0.7 nM in an enzyme activity assay.

A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.

Dotinurad is a novel compound that exhibits a remarkable uric acid excretion-promoting action.

UPCDC30245 is an allosteric inhibitor of AAA ATPase p97 with IC50 of 27 nM, binds at the junction between the D1 and D2 domains of p97..

A selective GPR68 positive allosteric modulator (pEC50=6.83) with minimal PAM activity at the related proton-sensing GPCRs GPR4 and GPR65.

KY-05009 (KY05009) is a potent, ATP-competitive inhibitor of Traf2- and Nck-interacting kinase (TNIK) with Ki of 100 nM.

BMS-986122 is a potent positive allosteric modulator of μ-opioid receptor, significantly increases the inhibition of forskolin-stimulated adenylyl cyclase activity produced by an EC10 (30 pM) concentration of endomorphin-I in CHO-μ cells..

LE135 is a retinoid acid receptor antagonist, produces pain through direct activation of TRP channels.

Atpenin A5, an antifungal antibiotic, is an ubiquinone-binding site inhibitor of succinate dehydrogenase. Atpenin A5 has cardioprotective effects against simulated ischemia-reperfusion injury in cardiomyocytes.

Sumanirole maleate(PNU 95666E; U95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM.

Coumestrol, a phytoestrogen present in soybean products, exhibits activities against cancers, neurological disorders, and autoimmune diseases. It suppresses proliferation of ES2 cells with an IC50 of 50 μM.

Fluoxetine HCl is an antidepressant of the selective serotonin reuptake inhibitor (SSRI) class.

MST312 is a telomerase inhibitor (IC50 = 0.67 μM in a TRAP assay).

TPMPA is a GABAA-ρ1 (ρ1 GABAC) receptor antagonist that is 8-fold selective for GABAA-ρ1 over GABAA-ρ2 (ρ2 GABAC) receptors expressed in X.

Hygromycin B is a protein translocation inhibitor that suppresses protein and RNA synthesis of bacteria. and viruses by inducing misreadings during translation.

LY320135 is a selective cannabinoid (CB) receptor 1 antagonist (Kis = 224 and >10,000 nM for CB1 and CB2, respectively, in vitro).

SKA-121 is a positive-gating modulator of intermediate-conductance calcium-activated potassium channels (IKCa1/KCa3.1) with an EC50 value of 109 nM using whole-cell patch-clamp electrophysiology with calcium in the internal solution.

A potent, selective KDM5 sub-family(JARID1) inhibitor with biochemical IC50 of 71/19/69/69 nM for KDM5A/B/C/D, respectively.

PK 11195 is a ligand of translocator protein. It targets Leishmania chemotherapy (IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively).

A potent, ATP-competetive CDKs inhibitor with IC50 of 7, 7, 7, 3 uM for Cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, and Cdk/p35 kinase.

Iperoxo is a superagonist of the muscarinic acetylcholine receptors and an OxotremorineM analog.

BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM). BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively

Fosmidomycin sodium salt is a phosphonic acid antibiotic and a antimalarial drug, which is active against both Gram-negative and Gram-positive bacteria.

AC-55649 is a potent, highly isoform-selective agonist of human RARβ2 receptor, with a pEC50 of 6.9.

Pinacidil monohydrate, an antihypertensive drug, is a potassium channel activator.

Dodecanoylcarnitine is present in fatty acid oxidation disorders such as long-chain acyl CoA dehydrogenase deficiency, carnitine palmitoyltransferase I/II deficiency, and is also associated with celiac disease.