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Assay Detail

CHEMBL944009

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

Binding
Inhibition of human Hsp90-alpha by fluorescence polarization assay
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of benzisoxazoles as potent inhibitors of chaperone heat shock protein 90.
Gopalsamy A, Shi M, Golas J, Vogan E, Jacob J, Johnson M, Lee F, Nilakantan R, Petersen R, Svenson K, Chopra R, Tam MS, Wen Y, Ellingboe J, Arndt K, Boschelli F.
J Med Chem (2008) 51 : 373 -375
PubMed 18197612 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.78 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278315 GELDANAMYCIN 2.0 1 7.70
CHEMBL404630 1 7.52
CHEMBL254875 1 7.40
CHEMBL362307 1 7.22
CHEMBL361078 1 6.72
CHEMBL402712 1 6.10
CHEMBL360410 1 4.82
CHEMBL254876 1 -
CHEMBL254874 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278315 GELDANAMYCIN IC50 = 20.0 nM 7.70
CHEMBL404630 IC50 = 30.0 nM 7.52
CHEMBL254875 IC50 = 40.0 nM 7.40
CHEMBL362307 IC50 = 60.0 nM 7.22
CHEMBL361078 IC50 = 190.0 nM 6.72
CHEMBL402712 IC50 = 800.0 nM 6.10
CHEMBL360410 IC50 = 15200.0 nM 4.82
CHEMBL254876 IC50 > 20000.0 nM -
CHEMBL254874 IC50 > 20000.0 nM -