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Assay Detail

CHEMBL4276012

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

Binding
Inhibition of human IKKepsilon (1 to 655 residues) expressed in Baculovirus infected SF9 insect cells using myelin basic protein as substrate in presence of [gamma-33P]-ATP by radiometric kinase assay
ChEMBL ↗
54
Total Activities
32
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

Target

Inhibitor of nuclear factor kappa-B kinase subunit epsilon (CHEMBL3529) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological activity of substituted 2-amino-5-oxo-5H-chromeno[2,3-b]pyridine-3-carboxylic acid derivatives as inhibitors of the inflammatory kinases TBK1 and IKKε for the treatment of obesity.
Beyett TS, Gan X, Reilly SM, Gomez AV, Chang L, Tesmer JJG, Saltiel AR, Showalter HD.
Bioorg Med Chem (2018) 26 : 5443 -5461
PubMed 30270002 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.58 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291966 — — 2 6.68
CHEMBL4288542 — — 2 6.51
CHEMBL4281345 — — 2 6.24
CHEMBL4284757 — — 2 6.00
CHEMBL4277887 — — 1 5.92
CHEMBL4293403 — — 2 5.92
CHEMBL4277614 — — 2 5.89
CHEMBL4281788 — — 2 5.82
CHEMBL4279379 — — 2 5.80
CHEMBL4292344 — — 2 5.77
CHEMBL4289613 — — 2 5.72
CHEMBL4279336 — — 2 5.70
CHEMBL4278727 — — 1 5.68
CHEMBL4287847 — — 2 5.51
CHEMBL4290720 — — 1 5.51
CHEMBL4285588 — — 1 5.50
CHEMBL4295050 — — 2 5.47
CHEMBL4285560 — — 2 5.33
CHEMBL4290544 — — 2 5.31
CHEMBL1096 AMLEXANOX 4.0 2 5.29
CHEMBL4281733 — — 1 5.28
CHEMBL4277195 — — 2 5.28
CHEMBL4276661 — — 1 5.27
CHEMBL4284443 — — 2 5.27
CHEMBL4288939 — — 2 5.22
CHEMBL4280074 — — 1 5.20
CHEMBL4281039 — — 2 5.14
CHEMBL4278101 — — 1 4.97
CHEMBL4290024 — — 1 4.96
CHEMBL4282790 — — 1 4.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291966 — IC50 = 210.0 nM 6.68
CHEMBL4291966 — IC50 = 208.93 nM 6.68
CHEMBL4288542 — IC50 = 310.0 nM 6.51
CHEMBL4288542 — IC50 = 309.03 nM 6.51
CHEMBL4281345 — IC50 = 575.44 nM 6.24
CHEMBL4281345 — IC50 = 580.0 nM 6.24
CHEMBL4284757 — IC50 = 1000.0 nM 6.00
CHEMBL4284757 — IC50 = 1000.0 nM 6.00
CHEMBL4293403 — IC50 = 1202.26 nM 5.92
CHEMBL4277887 — IC50 = 1200.0 nM 5.92
CHEMBL4293403 — IC50 = 1200.0 nM 5.92
CHEMBL4277614 — IC50 = 1300.0 nM 5.89
CHEMBL4277614 — IC50 = 1288.25 nM 5.89
CHEMBL4281788 — IC50 = 1513.56 nM 5.82
CHEMBL4281788 — IC50 = 1500.0 nM 5.82
CHEMBL4279379 — IC50 = 1600.0 nM 5.80
CHEMBL4279379 — IC50 = 1584.89 nM 5.80
CHEMBL4292344 — IC50 = 1698.24 nM 5.77
CHEMBL4292344 — IC50 = 1700.0 nM 5.77
CHEMBL4289613 — IC50 = 1905.46 nM 5.72
CHEMBL4289613 — IC50 = 1900.0 nM 5.72
CHEMBL4279336 — IC50 = 1995.26 nM 5.70
CHEMBL4279336 — IC50 = 2000.0 nM 5.70
CHEMBL4278727 — IC50 = 2100.0 nM 5.68
CHEMBL4287847 — IC50 = 3100.0 nM 5.51
CHEMBL4287847 — IC50 = 3090.3 nM 5.51
CHEMBL4290720 — IC50 = 3100.0 nM 5.51
CHEMBL4285588 — IC50 = 3200.0 nM 5.50
CHEMBL4295050 — IC50 = 3388.44 nM 5.47
CHEMBL4295050 — IC50 = 3400.0 nM 5.47
CHEMBL4285560 — IC50 = 4700.0 nM 5.33
CHEMBL4285560 — IC50 = 4677.35 nM 5.33
CHEMBL4290544 — IC50 = 4897.79 nM 5.31
CHEMBL4290544 — IC50 = 4900.0 nM 5.31
CHEMBL1096 AMLEXANOX IC50 = 5128.61 nM 5.29
CHEMBL1096 AMLEXANOX IC50 = 5100.0 nM 5.29
CHEMBL4281733 — IC50 = 5200.0 nM 5.28
CHEMBL4277195 — IC50 = 5248.07 nM 5.28
CHEMBL4277195 — IC50 = 5300.0 nM 5.28
CHEMBL4284443 — IC50 = 5370.32 nM 5.27
CHEMBL4284443 — IC50 = 5400.0 nM 5.27
CHEMBL4276661 — IC50 = 5400.0 nM 5.27
CHEMBL4288939 — IC50 = 6025.6 nM 5.22
CHEMBL4288939 — IC50 = 6000.0 nM 5.22
CHEMBL4280074 — IC50 = 6300.0 nM 5.20
CHEMBL4281039 — IC50 = 7244.36 nM 5.14
CHEMBL4281039 — IC50 = 7200.0 nM 5.14
CHEMBL4278101 — IC50 = 10600.0 nM 4.97
CHEMBL4290024 — IC50 = 11000.0 nM 4.96
CHEMBL4282790 — IC50 = 11000.0 nM 4.96