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Assay Detail

CHEMBL1806177

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

Binding
Inhibition of Hsp90alpha in human SKBR3 cells assessed as up-regulation of HSP70 protein by Western blot analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-BR-3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

N-aryl-benzimidazolones as novel small molecule HSP90 inhibitors.
Bruncko M, Tahir SK, Song X, Chen J, Ding H, Huth JR, Jin S, Judge RA, Madar DJ, Park CH, Park CM, Petros AM, Tse C, Rosenberg SH, Elmore SW.
Bioorg Med Chem Lett (2010) 20 : 7503 -7506
PubMed 21106457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.91 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109480 TANESPIMYCIN 3.0 1 7.22
CHEMBL1801578 1 7.22
CHEMBL365617 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109480 TANESPIMYCIN EC50 = 60.0 nM 7.22
CHEMBL1801578 EC50 = 60.0 nM 7.22
CHEMBL365617 EC50 = 500.0 nM 6.30