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Assay Detail

CHEMBL5317664

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

Binding
Inhibition of BRD4-BD1 (unknown origin) by fluorescence polarization assay
12
Total Activities
12
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

Bromodomain-containing protein 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Physachenolide C is a Potent, Selective BET Inhibitor.
Zerio CJ, Sivinski J, Wijeratne EMK, Xu YM, Ngo DT, Ambrose AJ, Villa-Celis L, Ghadirian N, Clarkson MW, Zhang DD, Horton NC, Gunatilaka AAL, Fromme R, Chapman E.
J Med Chem (2023) 66 : 913 -933
PubMed 36577036 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.64 7.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3605564 1 7.71
CHEMBL3605566 1 7.51
CHEMBL4074906 1 7.32
CHEMBL4082632 1 7.22
CHEMBL5412959 1 6.55
CHEMBL1097107 WITHANOLIDE E 1 6.25
CHEMBL3605560 1 6.04
CHEMBL4075419 1 5.71
CHEMBL5401408 1 5.41
CHEMBL517080 WITHAFERIN A 1.0 1 -
CHEMBL5416439 1 -
CHEMBL5438438 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3605564 IC50 = 19.3 nM 7.71
CHEMBL3605566 IC50 = 31.2 nM 7.51
CHEMBL4074906 IC50 = 47.6 nM 7.32
CHEMBL4082632 IC50 = 60.0 nM 7.22
CHEMBL5412959 IC50 = 281.0 nM 6.55
CHEMBL1097107 WITHANOLIDE E IC50 = 556.2 nM 6.25
CHEMBL3605560 IC50 = 909.0 nM 6.04
CHEMBL4075419 IC50 = 1934.0 nM 5.71
CHEMBL5401408 IC50 = 3875.0 nM 5.41
CHEMBL517080 WITHAFERIN A IC50 > 20000.0 nM -
CHEMBL5416439 IC50 > 20000.0 nM -
CHEMBL5438438 IC50 > 20000.0 nM -