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Assay Detail

CHEMBL4670815

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

Binding
Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay
31
Total Activities
31
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 31 5.82 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4787565 1 7.00
CHEMBL4757369 1 6.70
CHEMBL242708 1 6.70
CHEMBL4745831 1 6.70
CHEMBL4745853 1 6.70
CHEMBL4757924 1 6.70
CHEMBL4776143 1 6.70
CHEMBL1701986 1 6.52
CHEMBL4789889 1 6.52
CHEMBL4797833 1 6.52
CHEMBL4744235 1 6.52
CHEMBL4783341 1 6.52
CHEMBL4750726 1 6.52
CHEMBL4800702 1 6.40
CHEMBL4750624 1 6.40
CHEMBL4757939 1 6.30
CHEMBL4784286 1 6.05
CHEMBL4797545 1 5.96
CHEMBL4778316 1 5.82
CHEMBL4751604 1 5.25
CHEMBL63323 NIFLUMIC ACID 2.0 1 5.23
CHEMBL4781890 1 5.19
CHEMBL4759333 1 4.87
CHEMBL4763473 1 4.85
CHEMBL4747774 1 4.83
CHEMBL4759934 1 4.80
CHEMBL4764516 1 4.65
CHEMBL4751406 1 4.44
CHEMBL4760394 1 4.42
CHEMBL4786804 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4787565 IC50 = 100.0 nM 7.00
CHEMBL4757369 IC50 = 200.0 nM 6.70
CHEMBL242708 IC50 = 200.0 nM 6.70
CHEMBL4745831 IC50 = 200.0 nM 6.70
CHEMBL4745853 IC50 = 200.0 nM 6.70
CHEMBL4757924 IC50 = 200.0 nM 6.70
CHEMBL4776143 IC50 = 200.0 nM 6.70
CHEMBL1701986 IC50 = 300.0 nM 6.52
CHEMBL4789889 IC50 = 300.0 nM 6.52
CHEMBL4797833 IC50 = 300.0 nM 6.52
CHEMBL4744235 IC50 = 300.0 nM 6.52
CHEMBL4783341 IC50 = 300.0 nM 6.52
CHEMBL4750726 IC50 = 300.0 nM 6.52
CHEMBL4800702 IC50 = 400.0 nM 6.40
CHEMBL4750624 IC50 = 400.0 nM 6.40
CHEMBL4757939 IC50 = 500.0 nM 6.30
CHEMBL4784286 IC50 = 900.0 nM 6.05
CHEMBL4797545 IC50 = 1100.0 nM 5.96
CHEMBL4778316 IC50 = 1500.0 nM 5.82
CHEMBL4751604 IC50 = 5600.0 nM 5.25
CHEMBL63323 NIFLUMIC ACID IC50 = 5900.0 nM 5.23
CHEMBL4781890 IC50 = 6400.0 nM 5.19
CHEMBL4759333 IC50 = 13400.0 nM 4.87
CHEMBL4763473 IC50 = 14100.0 nM 4.85
CHEMBL4747774 IC50 = 14700.0 nM 4.83
CHEMBL4759934 IC50 = 16000.0 nM 4.80
CHEMBL4764516 IC50 = 22600.0 nM 4.65
CHEMBL4751406 IC50 = 36400.0 nM 4.44
CHEMBL4760394 IC50 = 38100.0 nM 4.42
CHEMBL4786804 IC50 = 41600.0 nM 4.38
CHEMBL4798108 IC50 = 49900.0 nM 4.30