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Assay Detail

CHEMBL904868

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Binding
Selectivity for HSP90 in MCF7 cells over HSP90 in NDF cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
Kasibhatla SR, Hong K, Biamonte MA, Busch DJ, Karjian PL, Sensintaffar JL, Kamal A, Lough RE, Brekken J, Lundgren K, Grecko R, Timony GA, Ran Y, Mansfield R, Fritz LC, Ulm E, Burrows FJ, Boehm MF.
J Med Chem (2007) 50 : 2767 -2778
PubMed 17488003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.72 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112953 1 5.16
CHEMBL557165 1 4.70
CHEMBL109480 TANESPIMYCIN 3.0 1 4.30
CHEMBL389164 1 -
CHEMBL229943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112953 IC50 = 7000.0 nM 5.16
CHEMBL557165 IC50 = 20000.0 nM 4.70
CHEMBL109480 TANESPIMYCIN IC50 = 50000.0 nM 4.30
CHEMBL389164 IC50 = 333000.0 nM -
CHEMBL229943 IC50 = 400000.0 nM -