CAS NO. |
Products Name |
2230496-80-5 |
ZL0420 |
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ZL0420 is a potent and selective bromodomain-containing protein 4 (BRD4) inhibitor with IC50 values of 27 nM against BRD4 BD1 and 32 nM against BRD4 BD2. |
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2158197-70-5 |
HS1371 |
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HS-1371 is a potent and ATP-competitive receptor-interacting protein kinase 3 (RIP3) inhibitor with an IC50 of 20.8 nM |
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1346528-50-4 |
JNJ42165279 |
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JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively. IC50 value: 70 ± 8 nM (for hFAAH), 313 ± 28 nM (for rFAAH ) Target:FAAH JNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. [1] in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats. |
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2086772-26-9 |
JNJ64619178 |
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JNJ-64619178 is a selective, orally active and pseudo-irreversible PRMT5 inhibitor with an IC50 of 0.14 nM. JNJ-64619178 has potent activity In lung cancer |
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1202402-40-1 |
CPI444 |
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CPI-444 is a potent, oral and selective A2A receptor (A2AR) antagonist, which induces antitumor responses. |
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2009273-67-8 |
GNE-6640 |
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GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP43 and Ub-MDM2, respectively. |
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1307245-86-8 |
LY-2940094 |
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LY-2940094 is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY-2940094 reduces ethanol self-administration in animal models |
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1375466-18-4 |
ACY775 |
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ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM. |
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