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Assay Detail

CHEMBL2445178

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

Binding
Inhibition of Hsp90 in human BT474 cells assessed as degradation of Her2 protein level by immunocytochemistry assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BT-474
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Heat shock protein HSP90 (CHEMBL2095165)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of NMS-E973 as novel, selective and potent inhibitor of heat shock protein 90 (Hsp90).
Brasca MG, Mantegani S, Amboldi N, Bindi S, Caronni D, Casale E, Ceccarelli W, Colombo N, De Ponti A, Donati D, Ermoli A, Fachin G, Felder ER, Ferguson RD, Fiorelli C, Guanci M, Isacchi A, Pesenti E, Polucci P, Riceputi L, Sola F, Visco C, Zuccotto F, Fogliatto G.
Bioorg Med Chem (2013) 21 : 7047 -7063
PubMed 24100158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.15 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2443025 1 7.70
CHEMBL2443024 1 7.60
CHEMBL2443026 1 7.55
CHEMBL2443136 1 7.50
CHEMBL2443138 1 7.48
CHEMBL2443139 1 7.19
CHEMBL2443047 1 7.15
CHEMBL2443131 1 7.15
CHEMBL2443034 1 7.07
CHEMBL2443135 1 7.06
CHEMBL2443137 1 7.03
CHEMBL2443020 1 6.97
CHEMBL2443044 1 6.96
CHEMBL2443029 1 6.94
CHEMBL2443133 1 6.89
CHEMBL2443132 1 6.68
CHEMBL2443048 1 6.56
CHEMBL3215941 1 -
CHEMBL2443033 1 -
CHEMBL2443022 1 -
CHEMBL2443035 1 -
CHEMBL2443036 1 -
CHEMBL2443037 1 -
CHEMBL2443038 1 -
CHEMBL2443039 1 -
CHEMBL2443040 1 -
CHEMBL2443041 1 -
CHEMBL2443042 1 -
CHEMBL2443043 1 -
CHEMBL2443021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2443025 IC50 = 20.0 nM 7.70
CHEMBL2443024 IC50 = 25.0 nM 7.60
CHEMBL2443026 IC50 = 28.0 nM 7.55
CHEMBL2443136 IC50 = 32.0 nM 7.50
CHEMBL2443138 IC50 = 33.0 nM 7.48
CHEMBL2443139 IC50 = 65.0 nM 7.19
CHEMBL2443047 IC50 = 71.0 nM 7.15
CHEMBL2443131 IC50 = 71.0 nM 7.15
CHEMBL2443034 IC50 = 86.0 nM 7.07
CHEMBL2443135 IC50 = 88.0 nM 7.06
CHEMBL2443137 IC50 = 94.0 nM 7.03
CHEMBL2443020 IC50 = 107.0 nM 6.97
CHEMBL2443044 IC50 = 110.0 nM 6.96
CHEMBL2443029 IC50 = 114.0 nM 6.94
CHEMBL2443133 IC50 = 130.0 nM 6.89
CHEMBL2443132 IC50 = 210.0 nM 6.68
CHEMBL2443048 IC50 = 277.0 nM 6.56
CHEMBL3215941 IC50 - -
CHEMBL2443033 IC50 - -
CHEMBL2443022 IC50 - -
CHEMBL2443035 IC50 - -
CHEMBL2443036 IC50 - -
CHEMBL2443037 IC50 - -
CHEMBL2443038 IC50 - -
CHEMBL2443039 IC50 - -
CHEMBL2443040 IC50 - -
CHEMBL2443041 IC50 - -
CHEMBL2443042 IC50 - -
CHEMBL2443043 IC50 - -
CHEMBL2443021 IC50 - -
CHEMBL2443045 IC50 - -
CHEMBL2443046 IC50 - -
CHEMBL2443134 IC50 - -