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Assay Detail

CHEMBL5552299

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

Binding
Binding affinity to human N-terminal his tagged Hsp90alpha (1 to 241 residues) expressed in Escherichia coli (DE3) strain assessed as dissociation constant by ITC method
7
Total Activities
7
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

Comprehensive analysis of resorcinyl-imidazole Hsp90 inhibitor design.
Gedgaudas M, Kaziukonytė P, Kairys V, Mickevičiūtė A, Zubrienė A, Brukštus A, Matulis D, Kazlauskas E.
Eur J Med Chem (2024) 273 : 116505 -116505
PubMed 38788300 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 7 6.51 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5569309 1 8.70
CHEMBL5574581 1 8.10
CHEMBL5562891 1 6.05
CHEMBL5567226 1 5.85
CHEMBL5570148 1 5.85
CHEMBL5562627 1 5.52
CHEMBL5566352 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5569309 Kd = 2.0 nM 8.70
CHEMBL5574581 Kd = 8.0 nM 8.10
CHEMBL5562891 Kd = 900.0 nM 6.05
CHEMBL5567226 Kd = 1400.0 nM 5.85
CHEMBL5570148 Kd = 1400.0 nM 5.85
CHEMBL5562627 Kd = 3000.0 nM 5.52
CHEMBL5566352 Kd = 3300.0 nM 5.48