MT-7716 (also known as W-212393) is a novel, potent and selective non-peptide nociceptin receptor (NOP) agonist with the potential to be used for treatment of alcohol abuse and relapse prevention. The effects of MT-7716 (0.3 and 1 mg/kg; PO) on alcohol self-administration were determined 2 weeks following dependence induction, when baseline self-administration was restored. Effects […]

PI-828 is a novel and potent PI3K (phosphatidylinositol 3-kinase) inhibitor.

Ajulemic acid (also known as lenabasum) is a cannabinoid CB2 receptor agonist with the potential for treatment of skin-predominant dermatomyositis. Ajulemic acid is a synthetic cannabinoid derivative of the non-psychoactive THC metabolite 11-nor-9-carboxy-THC that shows useful analgesic and anti-inflammatory effects without causing a subjective ‘high’. It is being developed for the treatment of neuropathic pain […]

BI-8622 is a novel, potent and specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARF-BP1, MULE) associates with both MYC and the MYC-associated protein MIZ1.

JNJ-61432059 is a novel, potent, oral bioactive and selective negative modulator of AMPAR (α-amino-3-hydroxy-5-methylisoxazole-4-propionate receptors) associated with trans-membrane AMPAR regulatory protein (TARP) γ-8, with a pIC50 of 9.7 for GluA1/γ-8. It exhibits time- and dose-dependent AMPAR/γ-8 receptor occupancy in mouse hippocampus, resulting in robust seizure protection in corneal kindling and pentylenetetrazole (PTZ) anticonvulsant models.

PROTAC BET Degrader-3 is a novel and potent BET degrader based on PROTAC technology.

MRS-2179 (MRS2179) is a novel, potent and competitive P2Y1 receptor antagonist with anti-thrombotic/anti-platelet effects. It inhibits PY1 with a Kb of 100 nM and without appreciable activity at P2Y2, P2Y4, or P2Y6 at concentrations up to 30 µM, or at P2Y12 and P2Y13. It inhibits ADP-induced platelet shape change and aggregation (pA2 = 6.55) in […]

ACY-1083 is a novel, potent, selective and brain-penetrant HDAC6 inhibitor with an IC50 of 3 nM. ACY-1083 shows 260-fold selectivity towards HDAC6 vs other HDACs. HDAC6 inhibition by ACY-1083 prevented cisplatin-induced mechanical allodynia, and also completely reversed already existing cisplatin-induced mechanical allodynia, spontaneous pain, and numbness. These findings were confirmed using the established HDAC6 inhibitor […]

K-Ras G12C-IN-1 is a novel, potent and irreversible/covalent inhibitor of K-Ras protein with G12C mutation. The compound inhibits KRAS G12C which is a well-validated driver mutation present in approximately 14% of NSCLC adenocarcinoma patients and 5% of CRC patients. Patients with KRAS mutation-positives cancers generally have a poor prognosis and resistant to standard therapies.

PD-176252 is a novel and potent non-peptide antagonist of gastrin-releasing peptide receptor (GRP-R, BB2) and neuromedin B receptor (NMB-R, BB1)with Ki values of 0.17 and 1.0 nM for BB1 and BB2 respectively. It inhibits proliferation of rat C6 glioma cells (IC50 = 2 μM) and inhibits NCI-H1299 xenograft proliferation in nude mice (IC50 = 5 […]