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Assay Detail

CHEMBL4124129

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

Binding
Inhibition of FITC-geldanamycin binding to recombinant human HSP90alpha expressed in Escherichia coli by fluorescence anisotropy method
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New TRAP1 and Hsp90 chaperone inhibitors with cationic components: Preliminary studies on mitochondrial targeting.
Rondanin R, Lettini G, Oliva P, Baruchello R, Costantini C, Trapella C, Simoni D, Bernardi T, Sisinni L, Pietrafesa M, Ponterini G, Costi MP, Vignudelli T, Luciani R, Matassa DS, Esposito F, Landriscina M.
Bioorg Med Chem Lett (2018) 28 : 2289 -2293
PubMed 29807796 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 8.82 8.82
IC50 1 7.68 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4126250 2 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4126250 Kd = 1.5 nM 8.82
CHEMBL4126250 IC50 = 21.0 nM 7.68