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Assay Detail

CHEMBL1763403

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

Binding
Competitive inhibition of recombinant TAK1-TAB1 assessed as [33P]gamma-ATP incorporation into substrate histone H1 peptide by filter plate assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

TAK1/TAB1 (CHEMBL3038499)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Oxindole derivatives as inhibitors of TAK1 kinase.
Lockman JW, Reeder MD, Robinson R, Ormonde PA, Cimbora DM, Williams BL, Willardsen JA.
Bioorg Med Chem Lett (2011) 21 : 1724 -1727
PubMed 21316225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 6.17 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1077979 1 8.10
CHEMBL1761718 1 8.05
CHEMBL1761588 1 7.68
CHEMBL1761586 1 7.38
CHEMBL1761585 1 7.34
CHEMBL1761587 1 7.00
CHEMBL1761749 1 6.25
CHEMBL1761742 1 6.20
CHEMBL1761747 1 5.77
CHEMBL1761719 1 5.52
CHEMBL1761750 1 5.39
CHEMBL1761739 1 5.24
CHEMBL1761737 1 5.09
CHEMBL1761738 1 4.60
CHEMBL1761740 1 4.60
CHEMBL1761736 1 4.52
CHEMBL1761743 1 -
CHEMBL1761744 1 -
CHEMBL1761746 1 -
CHEMBL1761735 1 -
CHEMBL1761730 1 -
CHEMBL1761729 1 -
CHEMBL190880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1077979 IC50 = 8.0 nM 8.10
CHEMBL1761718 IC50 = 8.9 nM 8.05
CHEMBL1761588 IC50 = 21.0 nM 7.68
CHEMBL1761586 IC50 = 42.0 nM 7.38
CHEMBL1761585 IC50 = 46.0 nM 7.34
CHEMBL1761587 IC50 = 99.0 nM 7.00
CHEMBL1761749 IC50 = 560.0 nM 6.25
CHEMBL1761742 IC50 = 630.0 nM 6.20
CHEMBL1761747 IC50 = 1700.0 nM 5.77
CHEMBL1761719 IC50 = 3000.0 nM 5.52
CHEMBL1761750 IC50 = 4100.0 nM 5.39
CHEMBL1761739 IC50 = 5800.0 nM 5.24
CHEMBL1761737 IC50 = 8200.0 nM 5.09
CHEMBL1761738 IC50 = 25000.0 nM 4.60
CHEMBL1761740 IC50 = 25000.0 nM 4.60
CHEMBL1761736 IC50 = 30000.0 nM 4.52
CHEMBL1761743 IC50 > 5000.0 nM -
CHEMBL1761744 IC50 > 5000.0 nM -
CHEMBL1761746 IC50 > 5000.0 nM -
CHEMBL1761735 IC50 > 50000.0 nM -
CHEMBL1761730 IC50 > 5000.0 nM -
CHEMBL1761729 IC50 > 5000.0 nM -
CHEMBL190880 IC50 > 5000.0 nM -