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Cyt387 Inhibitor 6 years 26 weeks ago

Cyt387, also called Momelotinib, under the IUPAC name N-(cyanomethyl)-4-(2-((4-(4-morpholinyl)phenyl)amino)-4-pyrimidinyl)benzamide, is an ATP competitive inhibitor of JAK1 (IC50 = 11 nM) and JAK2 (IC50 = 18 nM) with potential antineoplastic activity, which may result result in the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells.

Mk-2206 inhibitor 6 years 22 weeks ago

MK2206 is a Akt inhibitor, is also an orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor MK2206 binds to and inhibits the activity of Akt in a non-ATP competitive manner

Loratadine Inhibitor 6 years 8 weeks ago

Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Reference Reading
1.Effects of Prednisolone on the Pharmacokinetics of Loratadine after Oral and Intravenous Administration of Loratadine in Rats
2.Physicochemical characterization and dissolution enhancement of loratadine by solid dispersion technique

Quizartinib inhibitor 6 years 26 weeks ago

Quizartinib is an orally available small molecule with potential antineoplastic activity. Class III receptor tyrosine kinase inhibitor AC220 selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFRs), resulting in inhibition of ligand-independent leukemic cell proliferation and apoptosis.

Simvastatin Inhibitor 6 years 1 day ago

Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM .
TargetsHMG-CoA Reductase (HMGCR)
Reference Reading
1. Input of selected human pharmaceutical metabolites into the Norwegian aquatic environment
Although we did not detect any ATV metabolites in surface water, interestingly we did detect the presence of the main and active metabolite of the statin prodrug simvastatin (SV); simvastatin hydroxy carboxylic acid (SVA) in four of the surface water and sediments collected from Oslofjord.The surface water samples collected contained SVA at concentrations > LODand up to 66 ng L-1, whilst two sediment samples contained low ng g-1 (dw) concentrations of SVA also. No effluent concentrations of SVA were determined; however, we have previously reported the occurrence of SV at low ng L-1 in VEAS WwTW effluent suggesting from these preliminary data that effluent concentrations of SVA would indeed be higher.

WAY-252623 Inhibitor 6 years 26 weeks ago

WAY-252623 (LXR-623) is a highly selective and orally bioavailable synthetic modulator of LXR, which can reduces total serum cholesterol and LDL cholesterol and inhibits lesion growth in models of atherosclerosis. IC50 values= 24 and 179 nM (for LXRβ and LXRα, respectively)

Linaclotide inhibitor 6 years 30 weeks ago

Linaclotide is an peptide agonist of guanylate cyclase 2C that is undergoing clinical trials for use in treating abdominal pain in patients with irritable bowel syndrome (IBS) accompanied by constipation. The drug also has promising outlooks for the treatment of gastroparesis, ulcerative colitis, chronic intestinal pseudo-obstruction (CIPO), and inertia coli as well.