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Assay Detail

CHEMBL3128985

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

Binding
Displacement of GM-cy3B from Hsp90 in human SKBR3 cells after 24 hrs by fluorescence polarization assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-BR-3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Heat shock protein HSP 90-beta (CHEMBL4303)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heat shock protein 70 inhibitors. 1. 2,5'-thiodipyrimidine and 5-(phenylthio)pyrimidine acrylamides as irreversible binders to an allosteric site on heat shock protein 70.
Kang Y, Taldone T, Patel HJ, Patel PD, Rodina A, Gozman A, Maharaj R, Clement CC, Patel MR, Brodsky JL, Young JC, Chiosis G.
J Med Chem (2014) 57 : 1188 -1207
PubMed 24548207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.53 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112953 1 6.18
CHEMBL164 MYRICETIN 1 4.87
CHEMBL3128291 1 -
CHEMBL3128288 1 -
CHEMBL3128287 1 -
CHEMBL3128285 1 -
CHEMBL3128284 1 -
CHEMBL3128282 1 -
CHEMBL3128279 1 -
CHEMBL3128276 1 -
CHEMBL3128275 1 -
CHEMBL3128273 1 -
CHEMBL3128272 1 -
CHEMBL3128270 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112953 IC50 = 660.0 nM 6.18
CHEMBL164 MYRICETIN IC50 = 13500.0 nM 4.87
CHEMBL3128291 IC50 > 500000.0 nM -
CHEMBL3128288 IC50 > 500000.0 nM -
CHEMBL3128287 IC50 > 500000.0 nM -
CHEMBL3128285 IC50 > 500000.0 nM -
CHEMBL3128284 IC50 > 500000.0 nM -
CHEMBL3128282 IC50 > 500000.0 nM -
CHEMBL3128279 IC50 > 500000.0 nM -
CHEMBL3128276 IC50 > 500000.0 nM -
CHEMBL3128275 IC50 > 500000.0 nM -
CHEMBL3128273 IC50 > 500000.0 nM -
CHEMBL3128272 IC50 > 250000.0 nM -
CHEMBL3128270 IC50 > 500000.0 nM -