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Assay Detail

CHEMBL1020360

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

Binding
Inhibition of Hsp90
13
Total Activities
12
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 6.70 7.70
EC50 4 6.54 7.80
ED50 2 7.08 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200102 PU-H71 2.0 1 7.80
CHEMBL414883 RADICICOL 2 7.70
CHEMBL365159 1 7.52
CHEMBL526127 POCHONIN D 1 7.10
CHEMBL491499 ZEARALANONE 1 7.05
CHEMBL512064 POCHONIN A 1 7.05
CHEMBL468439 CYCLOPROPARADICICOL 1 6.80
CHEMBL200469 1 6.59
CHEMBL200255 1 6.34
CHEMBL109480 TANESPIMYCIN 3.0 1 6.00
CHEMBL456678 1 5.05
CHEMBL113690 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200102 PU-H71 EC50 = 16.0 nM 7.80
CHEMBL414883 RADICICOL IC50 = 20.0 nM 7.70
CHEMBL365159 EC50 = 30.0 nM 7.52
CHEMBL414883 RADICICOL ED50 = 45.0 nM 7.35
CHEMBL526127 POCHONIN D IC50 = 80.0 nM 7.10
CHEMBL491499 ZEARALANONE IC50 = 90.0 nM 7.05
CHEMBL512064 POCHONIN A IC50 = 90.0 nM 7.05
CHEMBL468439 CYCLOPROPARADICICOL ED50 = 160.0 nM 6.80
CHEMBL200469 IC50 = 258.0 nM 6.59
CHEMBL200255 IC50 = 461.0 nM 6.34
CHEMBL109480 TANESPIMYCIN EC50 = 1000.0 nM 6.00
CHEMBL456678 IC50 = 9000.0 nM 5.05
CHEMBL113690 EC50 = 15000.0 nM 4.82