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Assay Detail

CHEMBL4059436

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

ADMET
Binding affinity to human N-terminal 6His-tagged HSP90alpha (1 to 236 residues) expressed in Escherichia coli BL21star/Rosetta2 (DE3) at 298 K by ITC assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Structure Based Design of a Grp94-Selective Inhibitor: Exploiting a Key Residue in Grp94 To Optimize Paralog-Selective Binding.
Que NLS, Crowley VM, Duerfeldt AS, Zhao J, Kent CN, Blagg BSJ, Gewirth DT.
J Med Chem (2018) 61 : 2793 -2805
PubMed 29528635 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.36 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075556 1 6.50
CHEMBL3426787 1 6.21
CHEMBL4098757 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075556 Kd = 320.0 nM 6.50
CHEMBL3426787 Kd = 620.0 nM 6.21
CHEMBL4098757 Kd - -