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Assay Detail

CHEMBL1020372

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

Binding
Binding affinity to Hsp90 by fluorescence polarization assay
9
Total Activities
9
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Heat shock protein HSP 90-beta (CHEMBL4303)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and development of heat shock protein 90 inhibitors.
Taldone T, Sun W, Chiosis G.
Bioorg Med Chem (2009) 17 : 2225 -2235
PubMed 19017562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.98 7.70
EC50 1 7.66 7.66
Ki 1 5.40 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278315 GELDANAMYCIN 2.0 1 7.70
CHEMBL200001 1 7.66
CHEMBL365617 1 7.60
CHEMBL252124 1 7.55
CHEMBL404630 1 7.52
CHEMBL251974 1 6.22
CHEMBL371915 1 6.16
CHEMBL208239 1 6.13
CHEMBL514440 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278315 GELDANAMYCIN IC50 = 20.0 nM 7.70
CHEMBL200001 EC50 = 22.0 nM 7.66
CHEMBL365617 IC50 = 25.0 nM 7.60
CHEMBL252124 IC50 = 28.0 nM 7.55
CHEMBL404630 IC50 = 30.0 nM 7.52
CHEMBL251974 IC50 = 600.0 nM 6.22
CHEMBL371915 IC50 = 700.0 nM 6.16
CHEMBL208239 IC50 = 740.0 nM 6.13
CHEMBL514440 Ki = 4000.0 nM 5.40