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Assay Detail

CHEMBL4359677

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

Binding
Inhibition of recombinant human full length HSP90 alpha expressed in Escherichia coli cells after 1 hr by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Heat shock protein HSP 90-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of HSP90 Inhibitor-SN38 Conjugates for Targeted Drug Accumulation.
Zhu S, Shen Q, Gao Y, Wang L, Fang Y, Chen Y, Lu W.
J Med Chem (2020) 63 : 5421 -5441
PubMed 32352777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.74 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252164 LUMINESPIB 2.0 1 7.92
CHEMBL1195136 SNX 5422 2.0 1 7.42
CHEMBL4436271 1 7.16
CHEMBL4460245 1 7.14
CHEMBL4446403 1 6.79
CHEMBL4534534 1 5.90
CHEMBL4574129 1 5.82
CHEMBL4457759 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252164 LUMINESPIB IC50 = 12.0 nM 7.92
CHEMBL1195136 SNX 5422 IC50 = 38.0 nM 7.42
CHEMBL4436271 IC50 = 70.0 nM 7.16
CHEMBL4460245 IC50 = 72.0 nM 7.14
CHEMBL4446403 IC50 = 164.0 nM 6.79
CHEMBL4534534 IC50 = 1258.0 nM 5.90
CHEMBL4574129 IC50 = 1506.0 nM 5.82
CHEMBL4457759 IC50 = 1702.0 nM 5.77