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Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000154b PRKCQ
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of PKCtheta (unknown origin) at 1 uM in presence of ATP at Km concentration by mobility shift assay relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of PKCtheta (unknown origin) by Z'LYTE screening method relative to control
Assay data:2 Tested
Inhibition of full length human PKCtheta using 5-FAM-RFARKGSLRQKNV-OH peptide substrate incubated for 30 mins by IMAP kinase assay
Assay data:2 Active, 1 Activity ≤ 1 nM, 1 Activity ≤ 1 µM, 2 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of PKCtheta (unknown origin) at 50 nM by Z'LYTE screening method relative to control
Assay data:14 Tested
Inhibition of PKC (unknown origin)
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of PRKCQ (unknown origin) at 0.5 uM relative to control
PRKCQ DiscoveRx kinase panel
SummaryRelated BioAssays by Target
PKCtheta (h) Kinase panel
Inhibition of PKCtheta (unknown origin) at 1 uM
Inhibition of wild type partial length human PRKCQ (L350 to S706 residues) expressed in bacterial expression system by KdELECT assay
Assay data:2 Active, 2 Tested
Inhibition of Kinase Activity from US Patent US10870651: "Inhibitors of cyclin-dependent kinase 7 (CDK7)"
Assay data:33 Active, 40 Activity ≤ 1 µM, 40 Tested
In Vitro Inhibition Activity Assay from US Patent US9452998: "Protein kinase C inhibitors and methods of their use"
Assay data:116 Active, 81 Activity ≤ 1 nM, 116 Activity ≤ 1 µM, 116 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
HMT Assay from Article 10.1038/nchembio.2304: "An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED."
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
PKC IMAP Kinase Assay from Article 10.1016/j.bmc.2009.10.020: "5-Vinyl-3-pyridinecarbonitrile inhibitors of PKCtheta: optimization of enzymatic and functional activity."
Assay data:50 Active, 1 Activity ≤ 1 nM, 50 Activity ≤ 1 µM, 50 Tested
Protein Kinase Assays from Article 10.1021/jm901108b: "Discovery of 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione (AEB071), a potent and selective inhibitor of protein kinase C isotypes."
Assay data:19 Active, 2 Activity ≤ 1 nM, 14 Activity ≤ 1 µM, 33 Tested
GSK-3beta Kinase Inhibition Assay from Article 10.1016/j.bmc.2009.01.019: "Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta."
Assay data:29 Active, 29 Activity ≤ 1 µM, 30 Tested
PKC theta IMAP Kinase Assay from Article 10.1016/j.bmcl.2009.03.053: "Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles."
Assay data:14 Active, 11 Activity ≤ 1 µM, 14 Tested
PKC theta IMAP Kinase Assay from Article 10.1021/jm800214a: "Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors."
Assay data:16 Active, 6 Activity ≤ 1 µM, 18 Tested
Kinase Inhibition Assay from Article 10.1016/S0960-894X(97)00445-9: "DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS"
Assay data:25 Active, 15 Activity ≤ 1 µM, 28 Tested
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