PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively. Anti-hyperalgesic effect.

A selective TRPM8 channel blocker with pEC50 of 6.91 in Ca(2+) influx assay, with no activity for TRPV4 (pEC50<4.6).

A potent, selective, non-pseudosubstrate inhibitor of O(6) -alkylguanine DNA methyltransferase (MGMT) with low-nanomolar potency.

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.

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.

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.