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Assay Detail

CHEMBL2013354

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Ikkepsilon using 5FAM-AKELDQGSLCTpSFVGTLQ-NH2 as substrate by microfluidic mobility shift assay
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Discovery of azabenzimidazole derivatives as potent, selective inhibitors of TBK1/IKKε kinases.
Wang T, Block MA, Cowen S, Davies AM, Devereaux E, Gingipalli L, Johannes J, Larsen NA, Su Q, Tucker JA, Whitston D, Wu J, Zhang HJ, Zinda M, Chuaqui C.
Bioorg Med Chem Lett (2012) 22 : 2063 -2069
PubMed 22305584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 6.70 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2011940 1 8.40
CHEMBL2011932 1 8.30
CHEMBL2011942 1 8.05
CHEMBL2011941 1 7.77
CHEMBL2011934 1 7.70
CHEMBL2011933 1 7.68
CHEMBL2011935 1 7.34
CHEMBL2011943 1 7.34
CHEMBL2011930 1 7.22
CHEMBL2011936 1 7.12
CHEMBL2011929 1 7.08
CHEMBL2011910 1 7.03
CHEMBL2011944 1 6.99
CHEMBL2011931 1 6.94
CHEMBL2011912 1 6.92
CHEMBL2011945 1 6.91
CHEMBL2011927 1 6.76
CHEMBL2010815 1 6.69
CHEMBL2011926 1 6.58
CHEMBL2011938 1 6.56
CHEMBL2011911 1 6.37
CHEMBL2011920 1 6.29
CHEMBL2011899 1 6.28
CHEMBL2011939 1 6.27
CHEMBL2011928 1 6.26
CHEMBL2011907 1 6.23
CHEMBL2011919 1 6.20
CHEMBL2011895 1 6.15
CHEMBL2011922 1 5.61
CHEMBL2011900 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2011940 IC50 = 4.0 nM 8.40
CHEMBL2011932 IC50 = 5.0 nM 8.30
CHEMBL2011942 IC50 = 9.0 nM 8.05
CHEMBL2011941 IC50 = 17.0 nM 7.77
CHEMBL2011934 IC50 = 20.0 nM 7.70
CHEMBL2011933 IC50 = 21.0 nM 7.68
CHEMBL2011935 IC50 = 46.0 nM 7.34
CHEMBL2011943 IC50 = 46.0 nM 7.34
CHEMBL2011930 IC50 = 60.0 nM 7.22
CHEMBL2011936 IC50 = 76.0 nM 7.12
CHEMBL2011929 IC50 = 84.0 nM 7.08
CHEMBL2011910 IC50 = 93.0 nM 7.03
CHEMBL2011944 IC50 = 102.0 nM 6.99
CHEMBL2011931 IC50 = 115.0 nM 6.94
CHEMBL2011912 IC50 = 120.0 nM 6.92
CHEMBL2011945 IC50 = 122.0 nM 6.91
CHEMBL2011927 IC50 = 172.0 nM 6.76
CHEMBL2010815 IC50 = 204.0 nM 6.69
CHEMBL2011926 IC50 = 265.0 nM 6.58
CHEMBL2011938 IC50 = 278.0 nM 6.56
CHEMBL2011911 IC50 = 425.0 nM 6.37
CHEMBL2011920 IC50 = 510.0 nM 6.29
CHEMBL2011899 IC50 = 523.0 nM 6.28
CHEMBL2011939 IC50 = 541.0 nM 6.27
CHEMBL2011928 IC50 = 543.0 nM 6.26
CHEMBL2011907 IC50 = 590.0 nM 6.23
CHEMBL2011919 IC50 = 627.0 nM 6.20
CHEMBL2011895 IC50 = 707.0 nM 6.15
CHEMBL2011922 IC50 = 2460.0 nM 5.61
CHEMBL2011900 IC50 = 4320.0 nM 5.37
CHEMBL2011914 IC50 = 5960.0 nM 5.22
CHEMBL2011937 IC50 = 14900.0 nM 4.83
CHEMBL2011924 IC50 = 16100.0 nM 4.79
CHEMBL2011917 IC50 - -
CHEMBL2011916 IC50 - -
CHEMBL2011915 IC50 - -
CHEMBL2011913 IC50 - -
CHEMBL2011909 IC50 > 30000.0 nM -
CHEMBL2011908 IC50 - -
CHEMBL2011925 IC50 - -
CHEMBL2011905 IC50 - -
CHEMBL2011904 IC50 - -
CHEMBL2011903 IC50 - -
CHEMBL2011902 IC50 - -
CHEMBL2011901 IC50 - -
CHEMBL2011898 IC50 - -
CHEMBL2011897 IC50 - -
CHEMBL2011896 IC50 - -
CHEMBL2011906 IC50 - -
CHEMBL2011921 IC50 - -