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Assay Detail

CHEMBL3132513

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Binding
Inhibition of IKK-epsilon (unknown origin) using 5FAM-AKELDQGSLCTpSFVGTLQ-NH2 as substrate by microfluidic mobility shift assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of 6-aryl-azabenzimidazoles that inhibit the TBK1/IKK-ε kinases.
Johannes JW, Chuaqui C, Cowen S, Devereaux E, Gingipalli L, Molina A, Wang T, Whitston D, Wu X, Zhang HJ, Zinda M.
Bioorg Med Chem Lett (2014) 24 : 1138 -1143
PubMed 24462666 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.26 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011933 1 7.68
CHEMBL3125721 1 7.38
CHEMBL2011936 1 7.12
CHEMBL3125741 1 6.94
CHEMBL3125722 1 6.80
CHEMBL3125732 1 6.69
CHEMBL3125727 1 6.56
CHEMBL3125730 1 6.48
CHEMBL3125739 1 6.40
CHEMBL3125731 1 6.38
CHEMBL3125723 1 6.35
CHEMBL373751 GSK-319347A 1 6.33
CHEMBL3125726 1 6.30
CHEMBL3125738 1 6.06
CHEMBL3125724 1 5.96
CHEMBL3125729 1 5.96
CHEMBL3125728 1 5.76
CHEMBL3125733 1 5.59
CHEMBL3125720 1 5.49
CHEMBL3125737 1 5.48
CHEMBL3125734 1 5.17
CHEMBL3125740 1 4.94
CHEMBL3125742 1 -
CHEMBL3125725 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011933 IC50 = 21.0 nM 7.68
CHEMBL3125721 IC50 = 42.0 nM 7.38
CHEMBL2011936 IC50 = 76.0 nM 7.12
CHEMBL3125741 IC50 = 114.0 nM 6.94
CHEMBL3125722 IC50 = 158.0 nM 6.80
CHEMBL3125732 IC50 = 205.0 nM 6.69
CHEMBL3125727 IC50 = 273.0 nM 6.56
CHEMBL3125730 IC50 = 330.0 nM 6.48
CHEMBL3125739 IC50 = 395.0 nM 6.40
CHEMBL3125731 IC50 = 412.0 nM 6.38
CHEMBL3125723 IC50 = 448.0 nM 6.35
CHEMBL373751 GSK-319347A IC50 = 469.0 nM 6.33
CHEMBL3125726 IC50 = 497.0 nM 6.30
CHEMBL3125738 IC50 = 867.0 nM 6.06
CHEMBL3125724 IC50 = 1100.0 nM 5.96
CHEMBL3125729 IC50 = 1090.0 nM 5.96
CHEMBL3125728 IC50 = 1750.0 nM 5.76
CHEMBL3125733 IC50 = 2560.0 nM 5.59
CHEMBL3125720 IC50 = 3230.0 nM 5.49
CHEMBL3125737 IC50 = 3300.0 nM 5.48
CHEMBL3125734 IC50 = 6750.0 nM 5.17
CHEMBL3125740 IC50 = 11600.0 nM 4.94
CHEMBL3125742 IC50 > 30000.0 nM -
CHEMBL3125725 IC50 > 30000.0 nM -