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Assay Detail

CHEMBL4059435

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

Binding
Binding affinity to dog N-terminal GST-tagged GRP94 N41 deletion mutant (69 to 337 residues) expressed in Escherichia coli BL21star (DE3) at 298 K by ITC assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 6.44 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414883 RADICICOL 1 8.32
CHEMBL4075556 1 6.19
CHEMBL3426787 1 5.86
CHEMBL4098757 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414883 RADICICOL Kd = 4.8 nM 8.32
CHEMBL4075556 Kd = 650.0 nM 6.19
CHEMBL3426787 Kd = 1380.0 nM 5.86
CHEMBL4098757 Kd = 4000.0 nM 5.40