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Assay Detail

CHEMBL3385960

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Binding
Inhibition of YAP/ GST-TEAD1 (unknown origin) interaction by surface plasmon resonance assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Transcriptional coactivator YAP1/Transcriptional enhancer factor TEF-1 (CHEMBL3430909)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.
Zhang Z, Lin Z, Zhou Z, Shen HC, Yan SF, Mayweg AV, Xu Z, Qin N, Wong JC, Zhang Z, Rong Y, Fry DC, Hu T.
ACS Med Chem Lett (2014) 5 : 993 -998
PubMed 25221655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.98 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3335461 1 7.60
CHEMBL3335458 1 7.39
CHEMBL3335453 1 7.38
CHEMBL3335463 1 7.12
CHEMBL3335452 1 6.82
CHEMBL3335456 1 6.51
CHEMBL3335457 1 6.47
CHEMBL3335459 1 6.46
CHEMBL3335454 1 6.43
CHEMBL3335460 1 6.42
CHEMBL3335462 1 6.28
CHEMBL3335455 1 6.21
CHEMBL3335450 1 5.82
CHEMBL3335451 1 5.77
CHEMBL3335447 1 5.16
CHEMBL3335437 1 4.60
CHEMBL3335391 1 4.43
CHEMBL3335444 1 4.37
CHEMBL3335388 1 4.31
CHEMBL3335446 1 4.07
CHEMBL3335445 1 -
CHEMBL3335448 1 -
CHEMBL3335449 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3335461 IC50 = 25.0 nM 7.60
CHEMBL3335458 IC50 = 41.0 nM 7.39
CHEMBL3335453 IC50 = 42.0 nM 7.38
CHEMBL3335463 IC50 = 75.0 nM 7.12
CHEMBL3335452 IC50 = 150.0 nM 6.82
CHEMBL3335456 IC50 = 310.0 nM 6.51
CHEMBL3335457 IC50 = 340.0 nM 6.47
CHEMBL3335459 IC50 = 350.0 nM 6.46
CHEMBL3335454 IC50 = 370.0 nM 6.43
CHEMBL3335460 IC50 = 380.0 nM 6.42
CHEMBL3335462 IC50 = 530.0 nM 6.28
CHEMBL3335455 IC50 = 620.0 nM 6.21
CHEMBL3335450 IC50 = 1500.0 nM 5.82
CHEMBL3335451 IC50 = 1700.0 nM 5.77
CHEMBL3335447 IC50 = 6900.0 nM 5.16
CHEMBL3335437 IC50 = 25000.0 nM 4.60
CHEMBL3335391 IC50 = 37000.0 nM 4.43
CHEMBL3335444 IC50 = 43000.0 nM 4.37
CHEMBL3335388 IC50 = 49000.0 nM 4.31
CHEMBL3335446 IC50 = 85000.0 nM 4.07
CHEMBL3335445 IC50 > 100000.0 nM -
CHEMBL3335448 IC50 > 100000.0 nM -
CHEMBL3335449 IC50 > 100000.0 nM -