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Assay Detail

CHEMBL904867

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

Binding
Binding affinity to HSP90 in human NDF cell lysates assessed as inhibition of biotinylated-geldanamycin binding
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type NDF
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 5.85 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557165 1 6.40
CHEMBL229943 1 6.10
CHEMBL109480 TANESPIMYCIN 3.0 1 6.00
CHEMBL389164 1 6.00
CHEMBL112953 1 4.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557165 IC50 = 400.0 nM 6.40
CHEMBL229943 IC50 = 800.0 nM 6.10
CHEMBL109480 TANESPIMYCIN IC50 = 1000.0 nM 6.00
CHEMBL389164 IC50 = 1000.0 nM 6.00
CHEMBL112953 IC50 = 18000.0 nM 4.75