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Assay Detail

CHEMBL3632095

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Binding
Inhibition of TAK1 (unknown origin)
15
Total Activities
15
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

Mitogen-activated protein kinase kinase kinase 7 (CHEMBL5776)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Isolation, semisynthesis, covalent docking and transforming growth factor beta-activated kinase 1 (TAK1)-inhibitory activities of (5Z)-7-oxozeaenol analogues.
Fakhouri L, El-Elimat T, Hurst DP, Reggio PH, Pearce CJ, Oberlies NH, Croatt MP.
Bioorg Med Chem (2015) 23 : 6993 -6999
PubMed 26481152 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.23 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1077979 1 7.96
CHEMBL471474 HYPOTHEMYCIN 1 7.48
CHEMBL3629241 1 7.11
CHEMBL3629242 1 6.44
CHEMBL3629243 1 6.42
CHEMBL3629244 1 6.00
CHEMBL1801950 1 5.89
CHEMBL1801951 1 5.58
CHEMBL3629245 1 5.58
CHEMBL3629246 1 5.05
CHEMBL1099228 ZEAENOL 1 5.00
CHEMBL3628303 1 -
CHEMBL3629248 1 -
CHEMBL3334712 1 -
CHEMBL3629247 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1077979 IC50 = 11.0 nM 7.96
CHEMBL471474 HYPOTHEMYCIN IC50 = 33.0 nM 7.48
CHEMBL3629241 IC50 = 77.0 nM 7.11
CHEMBL3629242 IC50 = 360.0 nM 6.44
CHEMBL3629243 IC50 = 380.0 nM 6.42
CHEMBL3629244 IC50 = 990.0 nM 6.00
CHEMBL1801950 IC50 = 1300.0 nM 5.89
CHEMBL1801951 IC50 = 2600.0 nM 5.58
CHEMBL3629245 IC50 = 2600.0 nM 5.58
CHEMBL3629246 IC50 = 8900.0 nM 5.05
CHEMBL1099228 ZEAENOL IC50 = 10000.0 nM 5.00
CHEMBL3628303 IC50 > 30000.0 nM -
CHEMBL3629248 IC50 > 30000.0 nM -
CHEMBL3334712 IC50 > 30000.0 nM -
CHEMBL3629247 IC50 > 30000.0 nM -