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Assay Detail

CHEMBL5372006

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

Binding
Binding affinity to recombinant human HSP90alpha assessed as dissociation constant by isothermal titration calorimetry assay
4
Total Activities
4
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

Modifications of geldanamycin via CuAAC altering affinity to chaperone protein Hsp90 and cytotoxicity.
Skrzypczak N, Buczkowski A, Bohusz W, Nowak E, Tokarska K, Leśniewska A, Alzebari AM, Ruszkowski P, Gdaniec M, Bartl F, Przybylski P.
Eur J Med Chem (2023) 256 : 115450 -115450
PubMed 37210951 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 5.33 5.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5407855 1 5.41
CHEMBL278315 GELDANAMYCIN 2.0 1 5.33
CHEMBL5422446 1 5.31
CHEMBL5438336 1 5.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5407855 Kd = 3860.0 nM 5.41
CHEMBL278315 GELDANAMYCIN Kd = 4670.0 nM 5.33
CHEMBL5422446 Kd = 4930.0 nM 5.31
CHEMBL5438336 Kd = 5530.0 nM 5.26