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Assay Detail

CHEMBL4670810

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

Binding
Binding affinity to nonacylated N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells assessed as inhibition of protein-FAM-YAP (50 to 100 residues) interaction preincubated for 10 mins followed by FAM YAP addition and measured after 1 hr by fluorescence assay
2
Total Activities
2
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-3 (CHEMBL4295828)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Covalent Inhibitors Targeting the Transcriptional Enhanced Associate Domain Central Pocket.
Karatas H,Akbarzadeh M,Adihou H,Hahne G,Pobbati AV,Yihui Ng E,Guéret SM,Sievers S,Pahl A,Metz M,Zinken S,Dötsch L,Nowak C,Thavam S,Friese A,Kang C,Hong W,Waldmann H
J Med Chem (2020) 63 : 11972 -11989
PubMed 32907324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.09 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242708 1 7.16
CHEMBL4786804 1 5.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242708 IC50 = 70.0 nM 7.16
CHEMBL4786804 IC50 = 9500.0 nM 5.02