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Assay Detail

CHEMBL2073527

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

Binding
Inhibition of IKKbeta in mouse CIA model splenocytes assessed as inhibition of TNFalpha production after 72 hrs by ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Discovery of potent and selective rhodanine type IKKβ inhibitors by hit-to-lead strategy.
Song H, Lee YS, Roh EJ, Seo JH, Oh KS, Lee BH, Han H, Shin KJ.
Bioorg Med Chem Lett (2012) 22 : 5668 -5674
PubMed 22858099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.13 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360077 1 5.75
CHEMBL2070413 1 5.70
CHEMBL2070414 1 5.40
CHEMBL2070416 1 5.30
CHEMBL2070412 1 5.30
CHEMBL2070423 1 5.16
CHEMBL2070426 1 5.16
CHEMBL2070433 1 5.10
CHEMBL2070424 1 5.10
CHEMBL2070432 1 5.00
CHEMBL2070411 1 4.92
CHEMBL2070430 1 4.89
CHEMBL2070418 1 4.52
CHEMBL2070419 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360077 IC50 = 1800.0 nM 5.75
CHEMBL2070413 IC50 = 2000.0 nM 5.70
CHEMBL2070414 IC50 = 4000.0 nM 5.40
CHEMBL2070416 IC50 = 5000.0 nM 5.30
CHEMBL2070412 IC50 = 5000.0 nM 5.30
CHEMBL2070423 IC50 = 7000.0 nM 5.16
CHEMBL2070426 IC50 = 7000.0 nM 5.16
CHEMBL2070433 IC50 = 8000.0 nM 5.10
CHEMBL2070424 IC50 = 8000.0 nM 5.10
CHEMBL2070432 IC50 = 10000.0 nM 5.00
CHEMBL2070411 IC50 = 12000.0 nM 4.92
CHEMBL2070430 IC50 = 13000.0 nM 4.89
CHEMBL2070418 IC50 = 30000.0 nM 4.52
CHEMBL2070419 IC50 = 30000.0 nM 4.52