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Assay Detail

CHEMBL4713207

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

Binding
Inhibition of FITC-GDA binding to human HSP90-alpha incubated for 2 hrs by fluorescence polarization assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The Development of Hsp90β-Selective Inhibitors to Overcome Detriments Associated with pan-Hsp90 Inhibition.
Mishra SJ,Liu W,Beebe K,Banerjee M,Kent CN,Munthali V,Koren J,Taylor JA,Neckers LM,Holzbeierlein J,Blagg BSJ
J Med Chem (2021) 64 : 1545 -1557
PubMed 33428418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.27 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3235353 1 8.30
CHEMBL560895 SNX-2112 -1.0 1 8.22
CHEMBL4756421 1 6.76
CHEMBL4474770 1 6.75
CHEMBL4740273 1 6.75
CHEMBL4763549 1 6.53
CHEMBL4791530 1 6.51
CHEMBL4763239 1 6.08
CHEMBL4796520 1 6.05
CHEMBL4740377 1 5.80
CHEMBL4796556 1 5.73
CHEMBL4786075 1 5.07
CHEMBL4756340 1 4.77
CHEMBL4787078 1 4.42
CHEMBL4761885 1 -
CHEMBL4789323 1 -
CHEMBL4791941 1 -
CHEMBL4762355 1 -
CHEMBL4739925 1 -
CHEMBL4781194 1 -
CHEMBL4744768 1 -
CHEMBL4761498 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3235353 IC50 = 5.0 nM 8.30
CHEMBL560895 SNX-2112 IC50 = 6.0 nM 8.22
CHEMBL4756421 IC50 = 173.0 nM 6.76
CHEMBL4474770 IC50 = 180.0 nM 6.75
CHEMBL4740273 IC50 = 180.0 nM 6.75
CHEMBL4763549 IC50 = 294.0 nM 6.53
CHEMBL4791530 IC50 = 306.0 nM 6.51
CHEMBL4763239 IC50 = 824.0 nM 6.08
CHEMBL4796520 IC50 = 886.0 nM 6.05
CHEMBL4740377 IC50 = 1600.0 nM 5.80
CHEMBL4796556 IC50 = 1880.0 nM 5.73
CHEMBL4786075 IC50 = 8520.0 nM 5.07
CHEMBL4756340 IC50 = 17083.0 nM 4.77
CHEMBL4787078 IC50 = 38000.0 nM 4.42
CHEMBL4761885 IC50 > 50000.0 nM -
CHEMBL4789323 IC50 > 50000.0 nM -
CHEMBL4791941 IC50 > 50000.0 nM -
CHEMBL4762355 IC50 > 50000.0 nM -
CHEMBL4739925 IC50 > 50000.0 nM -
CHEMBL4781194 IC50 > 50000.0 nM -
CHEMBL4744768 IC50 > 10000.0 nM -
CHEMBL4761498 IC50 > 50000.0 nM -