Assay Report Card

Basic Information

ID: ALA3887107

Type: Binding

Description: Inhibition Assay: 11 data point. Cdc7 kinase assays were carried out in 25 mM HEPES, pH 7.5, 1 mM DTT, 10 mM MgCl2, 100 μM Na3VO4, and 0.075 mg/ml Triton X-100 using 12 ng baculovirus-expressed Cdc7/Dbf4 and 2 μM Jerini peptide substrate A-A11 (biotin-C6linker-TPSDSLIYDDGLS) (SEQ ID NO:5). Reactions were initiated with λ-[33P]-ATP (1 μM, 20 mCi/μmol) and quenched after 1 hour with 5 volumes of stop buffer (50 mM EDTA, 2 M NaCl). The reactions were incubated for 30 minutes on streptavidin-coated plates, washed, and quantified using a TopCount scintillation plate reader (Packard). IC50 values are determined via non-linear regression fitting of the data. Ki values are generated assuming ATP-competitive (equilibrium) inhibition and using the experimentally determined apparent ATP Km of Cdc7 (0.7 μM).

Organism: Homo sapiens

Activity Charts

Compound Summary

Parent Molecular WeightALogPPolar Surface Area
290.332.452.45
293.313.013.01
432.494.184.18
409.504.184.18
351.414.544.54
366.434.124.12
383.434.984.98
351.414.544.54
379.475.155.15
384.424.264.26
304.362.762.76
394.444.124.12
380.464.434.43
412.434.264.26
330.403.333.33
372.464.184.18
505.005.205.20
454.976.016.01
372.484.184.18
346.392.572.57
333.352.662.66
362.392.452.45
388.483.363.36
403.493.153.15
398.454.624.62
470.545.795.79
361.413.013.01
405.474.354.35
358.433.993.99
414.905.145.14
382.452.632.63
346.444.084.08
515.586.196.19
261.292.812.81
370.422.852.85
403.492.612.61
452.425.285.28
401.472.952.95
451.533.963.96
358.413.003.00
357.444.604.60
416.444.764.76
422.513.513.51
344.423.693.69
430.471.241.24
386.504.574.57
375.443.163.16
483.965.625.62
386.504.864.86
380.464.044.04
429.533.733.73
454.976.016.01
373.462.622.62
355.413.273.27
452.495.145.14
505.005.205.20
538.616.166.16
372.484.504.50
344.214.184.18
468.955.655.65
377.424.054.05
463.554.834.83
275.322.872.87
360.422.712.71
470.564.554.55
410.484.494.49
380.454.484.48
506.595.345.34