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Assay Detail

CHEMBL5369243

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

Binding
Displacement of biotinylated lipid pocket probes from His-tagged TEAD2 (unknown origin) preincubated for 4 hrs followed by lipid pocket probe addition and measured after 60 mins by TR-FRET assay
6
Total Activities
6
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

Transcriptional enhancer factor TEF-4 (CHEMBL4523301)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Compounds as TEAD Inhibitors for Treating Cancer.
Sabnis RW.
ACS Med Chem Lett (2023) 14 : 1152 -1153
PubMed 37736181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.38 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419829 1 8.52
CHEMBL5401444 1 8.52
CHEMBL5422959 1 8.40
CHEMBL5400400 1 8.40
CHEMBL5416415 1 8.22
CHEMBL5415215 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419829 IC50 = 3.0 nM 8.52
CHEMBL5401444 IC50 = 3.0 nM 8.52
CHEMBL5422959 IC50 = 4.0 nM 8.40
CHEMBL5400400 IC50 = 4.0 nM 8.40
CHEMBL5416415 IC50 = 6.0 nM 8.22
CHEMBL5415215 IC50 = 6.0 nM 8.22