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Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b TNK1
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b PLK4
Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b MAPK7
Selectivity interaction (Kinase panel (ATP-site competition binding assay)) EUB0000122b DCLK2
Affinity Biochemical interaction (ATP-binding displacement assay) EUB0000122b MAPK7
Binding affinity to recombinant human N-terminal hexaHis-tagged BRDT expressed in Escherichia coli BL21 (DE3) cells by qPCR assay
Assay data:7 Active, 7 Activity ≤ 1 µM, 7 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by ITC analysis
Assay data:8 Active, 8 Activity ≤ 1 µM, 8 Tested
Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by qPCR assay
Binding affinity to recombinant human N-terminal hexaHis-tagged BRD4 expressed in Escherichia coli BL21 (DE3) cells by MST assay
In vitro Erk5 from US Patent US9266890: "Pyrimido-diazepinone kinase scaffold compounds and methods of treating disorders"
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Biochemical Assay from Article 10.1016/j.chembiol.2011.05.010: "High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors."
Assay data:6 Active, 6 Activity ≤ 1 µM, 6 Tested
Primary qHTS assay for inhibitors of human arachidonate 12S-lipoxygenase (ALOX12): Round 2
Assay data:6069 Active, 5332 Activity ≤ 1 µM, 575118 Tested
Inhibition of recombinant human GST-tagged LRRK2 catalytic domain (970 to 2527 residues) expressed in baculovirus expression system using LRRKtide as substrate measured after 1 hr by Alexa fluor-647 ADP tracer-based ADAPTA assay
Assay data:35 Active, 30 Activity ≤ 1 µM, 36 Tested
Inhibition of recombinant human N-terminal His6-tagged DCLK1 (G351 to H689 residues) expressed in Escherichia coli BL21 DE3 using 5-FAM-KKLRRTLSVA-COOH as substrate measured after 2 hrs by mobility shift assay
Assay data:31 Active, 1 Activity ≤ 1 nM, 33 Activity ≤ 1 µM, 38 Tested
Inhibition of ERK5 in human HeLa cells incubated for 15 mins prior to ATP addition by KiNativ profiling method
Inhibition of His-tagged MAP2K5 activated N-terminal GST-tagged recombinant human ERK5 (1 to 398 residues) expressed in Escherichia coli using biotin-Ahx-PPGDYSTTPGGTLFSTTPGGTRI peptide as substrate preincubated for 15 mins followed by substrate addition and measured after 60 mins in presence of ATP by TR-FRET assay
Assay data:31 Active, 20 Activity ≤ 1 µM, 41 Tested
Cmax in rat at 2 mg/kg, po
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed Citation
Cmax in rat at 1 mg/kg, iv
Inhibition of EGF-induced BMK1 autophosphorylation in human HeLa cells by SDS-PAGE analysis
Assay data:18 Active, 15 Activity ≤ 1 µM, 19 Tested
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