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Assay Detail

CHEMBL3428036

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

Binding
Displacement of FITC-GM from recombinant Grp94 (unknown origin) after 24 hrs by fluorescence polarization assay
1
Total Activities
1
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

Endoplasmin (CHEMBL1075323)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship in a purine-scaffold compound series with selectivity for the endoplasmic reticulum Hsp90 paralog Grp94.
Patel HJ, Patel PD, Ochiana SO, Yan P, Sun W, Patel MR, Shah SK, Tramentozzi E, Brooks J, Bolaender A, Shrestha L, Stephani R, Finotti P, Leifer C, Li Z, Gewirth DT, Taldone T, Chiosis G.
J Med Chem (2015) 58 : 3922 -3943
PubMed 25901531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.94 5.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426787 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426787 IC50 = 1150.0 nM 5.94