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Inhibitory Activity on mTOR Kinase from US Patent US11731973: "Substituted pyrazolo[3,4-d]pyrimidines as mTOR inhibitors"
Assay data:31 Active, 11 Activity ≤ 1 nM, 31 Activity ≤ 1 µM, 31 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Lipophilicity, chromatographic hydrophobicity index of compound at 0.5 mM at pH 6.5 by UPLC-UV analysis
Assay data:19 Tested
SummaryPubMed Citation
Kinetic aqueous solubility of compound in phosphate buffer at pH 7.4 at 100 uM at 20 degree C shaken for 24 hrs by HPLC analysis
Assay data:14 Active, 6 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Inhibition of PI3Kalpha (unknown origin) using PIP2 as substrate measured after 30 mins by TR-FRET assay
Assay data:12 Active, 8 Activity ≤ 1 µM, 19 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of mTORC2 in human A431 cells assessed as AKT phosphorylation at S473 residue incubated for 3 hrs by HTRF assay
Assay data:15 Active, 15 Activity ≤ 1 µM, 19 Tested
Inhibition of mTORC1 in human A431 cells assessed as S6RP phosphorylation incubated for 3 hrs by HTRF assay
Assay data:15 Active, 1 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 19 Tested
Inhibition of human recombinant GST-tagged mTOR catalytic domain (1360 to 2549 residues) expressed in baculovirus expression system using GFP-4E-BP1 peptide as substrate incubated for 1 hr by LanthaScreen assay
Assay data:19 Active, 1 Activity ≤ 1 nM, 15 Activity ≤ 1 µM, 19 Tested
Hepatic intrinsic clearance in human Hepatocytes assessed per at 1 uM measured upto 90 mins by LC-MS/MS analysis
Assay data:17 Tested
Metabolic stability in human liver microsomes assessed as parent compound remaining at 1 uM measured at 15 mins in presence of phase 1 metabolism cofactors by LC-MS/MS analysis
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