ABL127 (ML174) is a potent, selective, covalent inhibitor of protein methylesterase 1 (PME-1) with IC50 of 10 nM.

Rupintrivir (AG-7088, AG7088) is a potent, irreversible inhibitor of human rhinovirus 3C protease, inhibits the replication of all HRV serotypes with EC50 of 23 nM and EC90 of 82 nM.

KN-92 is an inactive derivative of KN-93. KN-93 is a selective inhibitor of Ca2+/calmodulin-dependent kinase II (CaMKII), competitively blocking CaM binding to the kinase (Ki = 370 nM).

KPT-6566 is a covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action.

KYP-2047 is a very potent, selective inhibitor of Prolyl oligopeptidase (POP), also known as prolyl endopeptidase (PEP or PE). Ki = .023nM (porcine).

L-189 is a DNA ligase I, III and IV inhibitor (IC50 values are 5, 9 and 5 μM respectively) that blocks DNA binding (Ki = 5 μM for DNA ligase I).

L67 is a novel, competitive human DNA ligase inhibitor, inhibits DNA ligases I and III with IC50 of 10 μM and 10 μM.

A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay.

CAN-508 is a potent, selective CDK9 inhibitor with IC50 of 0.35 uM (CDK9/cyclin T1), displays >35 fold selectivity over CDK1/2/4/7 (IC50=13.5-70 uM).

CK 666 (CK 0944666) is a small molecule Arp2/3 complex inhibitor with IC50 of 4 uM, inhibits actin polymerization with either BtArp2/3 complex (IC50=17 uM) or SpArp2/3 complex (IC50=5 uM).

NKH 477 hydrochloride (Colforsin dapropate) is a water-soluble analog of Forskolin and a potent activator of adenylyl cyclase, shows some selectivity for cardiac (type V) adenylyl cyclase.

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.

L-778123 hydrochloride is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.

Laquinimod (ABR-215062) is a potent immunomodulator.

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.

Leonurine hydrochloride is an alkaloid isolated from Herba leonuri, with anti-oxidative and anti-inflammatory.

Lesinurad sodium (RDEA594 sodium) is an once-daily inhibitor of URAT1; URAT1 is a transporter in the kidney that regulates uric acid excretion from the body.