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Assay Detail

CHEMBL3379280

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

Binding
Inhibition of HSP90 in rabbit reticulocyte lysate after 90 mins by luciferase renaturation assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Heat shock protein HSP 90 (CHEMBL1667702)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Potential C-terminal-domain inhibitors of heat shock protein 90 derived from a C-terminal peptide helix.
Gavenonis J, Jonas NE, Kritzer JA.
Bioorg Med Chem (2014) 22 : 3989 -3993
PubMed 24984936 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.82 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL278315 GELDANAMYCIN 2.0 1 6.55
CHEMBL3360777 1 5.39
CHEMBL3360776 1 5.07
CHEMBL3360770 1 4.84
CHEMBL389471 COUMERMYCIN A1 1 4.55
CHEMBL3360775 1 4.50
CHEMBL3360773 1 4.43
CHEMBL3360769 1 4.42
CHEMBL3360774 1 4.42
CHEMBL3360767 1 4.03
CHEMBL36506 NOVOBIOCIN 4.0 1 -
CHEMBL3360762 1 -
CHEMBL3360771 1 -
CHEMBL3360772 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL278315 GELDANAMYCIN IC50 = 282.0 nM 6.55
CHEMBL3360777 IC50 = 4110.0 nM 5.39
CHEMBL3360776 IC50 = 8430.0 nM 5.07
CHEMBL3360770 IC50 = 14400.0 nM 4.84
CHEMBL389471 COUMERMYCIN A1 IC50 = 28100.0 nM 4.55
CHEMBL3360775 IC50 = 32000.0 nM 4.50
CHEMBL3360773 IC50 = 37000.0 nM 4.43
CHEMBL3360769 IC50 = 37900.0 nM 4.42
CHEMBL3360774 IC50 = 38000.0 nM 4.42
CHEMBL3360767 IC50 = 94500.0 nM 4.03
CHEMBL36506 NOVOBIOCIN IC50 = 414000.0 nM -
CHEMBL3360762 IC50 = 233000.0 nM -
CHEMBL3360771 IC50 = 168000.0 nM -
CHEMBL3360772 IC50 = 137000.0 nM -