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Assay Detail

CHEMBL833584

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

Binding
Inhibition of recombinant human I-kappa-B-kinase beta (IKK beta)
32
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 Expert

Publication

Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 3: Orally active anti-inflammatory agents.
Murata T, Shimada M, Sakakibara S, Yoshino T, Masuda T, Shintani T, Sato H, Koriyama Y, Fukushima K, Nunami N, Yamauchi M, Fuchikami K, Komura H, Watanabe A, Ziegelbauer KB, Bacon KB, Lowinger TB.
Bioorg Med Chem Lett (2004) 14 : 4019 -4022
PubMed 15225718 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 7.27 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182407 1 8.52
CHEMBL183703 1 8.40
CHEMBL181495 1 8.30
CHEMBL181334 1 8.30
CHEMBL182749 1 8.22
CHEMBL368427 1 8.07
CHEMBL361233 1 8.05
CHEMBL361841 1 7.92
CHEMBL182173 1 7.85
CHEMBL181756 1 7.85
CHEMBL182358 1 7.82
CHEMBL360337 1 7.82
CHEMBL181434 1 7.82
CHEMBL361548 1 7.70
CHEMBL369306 1 7.62
CHEMBL360691 1 7.60
CHEMBL360077 1 7.60
CHEMBL425346 1 7.58
CHEMBL363706 1 7.47
CHEMBL185509 1 7.30
CHEMBL182282 1 7.22
CHEMBL180452 1 7.09
CHEMBL425883 1 6.96
CHEMBL183341 1 6.92
CHEMBL183187 1 6.57
CHEMBL181358 1 6.52
CHEMBL361171 1 6.25
CHEMBL182722 1 5.89
CHEMBL173050 1 5.82
CHEMBL433565 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182407 IC50 = 3.0 nM 8.52
CHEMBL183703 IC50 = 4.0 nM 8.40
CHEMBL181495 IC50 = 5.0 nM 8.30
CHEMBL181334 IC50 = 5.0 nM 8.30
CHEMBL182749 IC50 = 6.0 nM 8.22
CHEMBL368427 IC50 = 8.5 nM 8.07
CHEMBL361233 IC50 = 9.0 nM 8.05
CHEMBL361841 IC50 = 12.0 nM 7.92
CHEMBL182173 IC50 = 14.0 nM 7.85
CHEMBL181756 IC50 = 14.0 nM 7.85
CHEMBL182358 IC50 = 15.0 nM 7.82
CHEMBL360337 IC50 = 15.0 nM 7.82
CHEMBL181434 IC50 = 15.0 nM 7.82
CHEMBL361548 IC50 = 20.0 nM 7.70
CHEMBL369306 IC50 = 24.0 nM 7.62
CHEMBL360077 IC50 = 25.0 nM 7.60
CHEMBL360691 IC50 = 25.0 nM 7.60
CHEMBL425346 IC50 = 26.0 nM 7.58
CHEMBL363706 IC50 = 34.0 nM 7.47
CHEMBL185509 IC50 = 50.0 nM 7.30
CHEMBL182282 IC50 = 60.0 nM 7.22
CHEMBL180452 IC50 = 81.0 nM 7.09
CHEMBL425883 IC50 = 110.0 nM 6.96
CHEMBL183341 IC50 = 120.0 nM 6.92
CHEMBL183187 IC50 = 270.0 nM 6.57
CHEMBL181358 IC50 = 300.0 nM 6.52
CHEMBL361171 IC50 = 560.0 nM 6.25
CHEMBL182722 IC50 = 1300.0 nM 5.89
CHEMBL173050 IC50 = 1500.0 nM 5.82
CHEMBL433565 IC50 = 2400.0 nM 5.62
CHEMBL182417 IC50 = 7800.0 nM 5.11
CHEMBL183024 IC50 = 20000.0 nM 4.70