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Assay Detail

CHEMBL867908

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

Binding
Inhibition of BODIPY-AG binding to dog Grp94
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Canis lupus familiaris
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endoplasmin (CHEMBL4748)
Type SINGLE PROTEIN
Organism Canis lupus familiaris

Publication

Design, synthesis, and biological evaluation of hydroquinone derivatives of 17-amino-17-demethoxygeldanamycin as potent, water-soluble inhibitors of Hsp90.
Ge J, Normant E, Porter JR, Ali JA, Dembski MS, Gao Y, Georges AT, Grenier L, Pak RH, Patterson J, Sydor JR, Tibbitts TT, Tong JK, Adams J, Palombella VJ.
J Med Chem (2006) 49 : 4606 -4615
PubMed 16854066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 6.56 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL339231 1 7.32
CHEMBL209356 1 7.32
CHEMBL383824 ALVESPIMYCIN 2.0 1 7.19
CHEMBL211296 1 7.14
CHEMBL377559 RETASPIMYCIN HYDROCHLORIDE 3.0 1 6.92
CHEMBL109480 TANESPIMYCIN 3.0 1 6.91
CHEMBL211295 1 6.88
CHEMBL14249 ADENOSINE TRIPHOSPHATE 2.0 1 4.72
CHEMBL14830 ADENOSINE DIPHOSPHATE 0.5 1 4.68
CHEMBL377782 1 -
CHEMBL378936 1 -
CHEMBL378935 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL339231 EC50 = 48.0 nM 7.32
CHEMBL209356 EC50 = 48.0 nM 7.32
CHEMBL383824 ALVESPIMYCIN EC50 = 65.0 nM 7.19
CHEMBL211296 EC50 = 72.0 nM 7.14
CHEMBL377559 RETASPIMYCIN HYDROCHLORIDE EC50 = 119.0 nM 6.92
CHEMBL109480 TANESPIMYCIN EC50 = 124.0 nM 6.91
CHEMBL211295 EC50 = 131.0 nM 6.88
CHEMBL14249 ADENOSINE TRIPHOSPHATE EC50 = 19000.0 nM 4.72
CHEMBL14830 ADENOSINE DIPHOSPHATE EC50 = 21000.0 nM 4.68
CHEMBL377782 EC50 > 10000.0 nM -
CHEMBL378936 EC50 - -
CHEMBL378935 EC50 - -