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Assay Detail

CHEMBL4158858

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

Binding
Inhibition of FITC-geldanamycin binding to HSP90alpha (unknown origin) incubated for 5 hrs by fluorescence polarization assay
4
Total Activities
4
Compounds Tested
2
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

Discovery of a Potent Grp94 Selective Inhibitor with Anti-Inflammatory Efficacy in a Mouse Model of Ulcerative Colitis.
Jiang F, Guo AP, Xu JC, You QD, Xu XL.
J Med Chem (2018) 61 : 9513 -9533
PubMed 30351001 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 2 6.14 6.21
IC50 2 4.41 4.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426787 1 6.21
CHEMBL3426786 1 6.06
CHEMBL4159086 1 4.41
CHEMBL4168274 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426787 Kd = 620.0 nM 6.21
CHEMBL3426786 Kd = 870.0 nM 6.06
CHEMBL4159086 IC50 = 39200.0 nM 4.41
CHEMBL4168274 IC50 > 100000.0 nM -