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In Vitro Enzymatic Inhibitory Activity Assay from US Patent US20240132489: "AROMATIC HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION, AND USE THEREOF"
Assay data:55 Active, 55 Activity ≤ 1 µM, 55 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of recombinant full length human C-terminal His6-tagged CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 cells using 5-FAM-ACSYSPTSPSYSPTSPSYSPTSPSKK as substrate at 10 uM incubated for 60 mins in presence of ATP relative to control
Assay data:1 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of recombinant full length human C-terminal His6-tagged CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 cells using 5-FAM-ACSYSPTSPSYSPTSPSYSPTSPSKK as substrate incubated for 60 mins in presence of ATP
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Inhibition of CDK7/Cyclin H/MNAT1 (unknown origin) using 5-FAM-YSPTSPSYSPTSPSYSPTSPSKKK as substrate in presence of ATP by spectroscopic analysis
CDK7/CyclinH/MAT1 Enzyme Reaction System from US Patent US20230303564: "PYRIMIDINE RING COMPOUND"
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by DepositorRelated BioAssays by Target
Enzyme Activity Test from US Patent US20230295130: "COMPOUND USEFUL AS CDK7 KINASE INHIBITOR AND USE THEREOF"
Assay data:164 Active, 170 Activity ≤ 1 µM, 170 Tested
CDK2/Cyclin E1 Full Length Mobility Shift Assay from US Patent US11718603: "CDK2 inhibitors"
Assay data:570 Active, 350 Activity ≤ 1 nM, 570 Activity ≤ 1 µM, 570 Tested
Kinase Assay from US Patent US11542261: "Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors"
Assay data:8 Active, 7 Activity ≤ 1 nM, 8 Activity ≤ 1 µM, 8 Tested
HotSpot Assay from US Patent US11542261: "Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors"
Assay data:30 Active, 6 Activity ≤ 1 nM, 30 Activity ≤ 1 µM, 30 Tested
In Vitro Kinase assay (CDK7) and IC 50 determination from WIPO Patent WO2023001061: "CDK7 SELECTIVE INHIBITORS AS ANTICANCER AGENTS"
Assay data:25 Active, 25 Activity ≤ 1 µM, 25 Tested
Inhibition of CDK7/cyclin H/MAT1 (unknown origin)
Assay data:1 Active, 1 Activity ≤ 1 µM, 3 Tested
Inhibition of CDK7/cyclin H/MNAT1 (unknown origin) at 1 uM in presence of ATP by Z'-LYTE assay relative to control
Assay data:2 Tested
Inhibition of CDK7/Cyclin H (unknown origin) incubated for 20 mins followed by [33P]gamma-ATP addition and measured after 2 hrs by radiometric HotSpot Kinase assay
Inhibition of CDK7/cyclin H (unknown origin) preincubated for 10 mins followed by ATP and substrate addition and measured after 60 mins by HTRF analysis
Inhibition of CDK7/Cyclin H (unknown origin)
Assay data:5 Active, 1 Activity ≤ 1 nM, 5 Activity ≤ 1 µM, 5 Tested
Induction of HyT-mediated degradation of cyclin H in human 22Rv1 cells at 0.38 to 6 uM incubated for 24 hrs by immunoblot analysis
Inhibition of CDK7/Cyclin H/MAT1 (unknown origin) in leukemia cells
Assay data:2 Active, 2 Activity ≤ 1 µM, 2 Tested
Inhibition of recombinant full length human CDK7/C-terminal His-tagged Cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus in Sf21 insect cells using peptide substrate incubated for 30 mins in presence of [32P]gamma-ATP by scintillation counter method
Assay data:1 Active, 1 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Inhibition of CDK7/cyclin H/MAT1 (unknown origin) in presence of ATP by time resolved-FRET assay
Assay data:3 Active, 4 Tested
Inhibition of CDK7/cyclin-H/MNAT1 (unknown origin) at 1 uM
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