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Assay Detail

CHEMBL1103009

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

Binding
Inhibition of HSP90-mediated client protein HER2 degradation
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Heat shock protein 90: inhibitors in clinical trials.
Biamonte MA, Van de Water R, Arndt JW, Scannevin RH, Perret D, Lee WC.
J Med Chem (2010) 53 : 3 -17
PubMed 20055425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.15 8.15
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109480 TANESPIMYCIN 3.0 1 8.15
CHEMBL339231 1 8.15
CHEMBL560895 SNX-2112 -1.0 1 8.15
CHEMBL252164 LUMINESPIB 2.0 1 8.15
CHEMBL467399 BIIB021 2.0 1 8.15
CHEMBL1082229 1 -
CHEMBL381115 1 -
CHEMBL365159 1 -
CHEMBL377371 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109480 TANESPIMYCIN IC50 = 7.0 nM 8.15
CHEMBL339231 IC50 = 7.0 nM 8.15
CHEMBL560895 SNX-2112 IC50 = 7.0 nM 8.15
CHEMBL252164 LUMINESPIB IC50 = 7.0 nM 8.15
CHEMBL467399 BIIB021 IC50 = 7.0 nM 8.15
CHEMBL1082229 Activity = 40.0 uM -
CHEMBL381115 Activity = 30.0 nM -
CHEMBL365159 Activity = 30.0 nM -
CHEMBL377371 Activity = 30.0 nM -