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Assay Detail

CHEMBL859807

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

Binding
Inhibitory activity against Hsp90 in human breast cancer MDA-MB-468 cell line
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-468
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90.
He H, Zatorska D, Kim J, Aguirre J, Llauger L, She Y, Wu N, Immormino RM, Gewirth DT, Chiosis G.
J Med Chem (2006) 49 : 381 -390
PubMed 16392823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 7.28 7.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200102 PU-H71 2.0 1 7.99
CHEMBL372962 1 7.96
CHEMBL377482 1 7.62
CHEMBL199283 1 7.52
CHEMBL200001 1 7.41
CHEMBL201683 1 7.29
CHEMBL383189 1 7.26
CHEMBL365159 1 7.11
CHEMBL199505 1 5.35
CHEMBL372791 1 -
CHEMBL202777 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200102 PU-H71 EC50 = 10.2 nM 7.99
CHEMBL372962 EC50 = 10.9 nM 7.96
CHEMBL377482 EC50 = 23.7 nM 7.62
CHEMBL199283 EC50 = 30.5 nM 7.52
CHEMBL200001 EC50 = 39.1 nM 7.41
CHEMBL201683 EC50 = 51.2 nM 7.29
CHEMBL383189 EC50 = 55.4 nM 7.26
CHEMBL365159 EC50 = 77.1 nM 7.11
CHEMBL199505 EC50 = 4500.0 nM 5.35
CHEMBL372791 EC50 > 15000.0 nM -
CHEMBL202777 EC50 > 15000.0 nM -