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Assay Detail

CHEMBL3106552

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Binding
Binding affinity to human N-terminal polyHis-tagged HSP90alpha (D9 to E236) closed loop conformation expressed in insect sf9 cells after 3 hrs by fluorescence polarization assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Heat shock protein HSP 90-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Correlation between chemotype-dependent binding conformations of HSP90α/β and isoform selectivity-Implications for the structure-based design of HSP90α/β selective inhibitors for treating neurodegenerative diseases.
Ernst JT, Liu M, Zuccola H, Neubert T, Beaumont K, Turnbull A, Kallel A, Vought B, Stamos D.
Bioorg Med Chem Lett (2014) 24 : 204 -208
PubMed 24332488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.70 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252164 LUMINESPIB 2.0 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252164 LUMINESPIB Ki = 2.0 nM 8.70