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Assay Detail

CHEMBL984452

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

Binding
Inhibition of Hsp90 in human SKBR3 cells assessed as interaction with Cy3b-conjugated geldanamycin by FP assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SK-BR-3
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.
Ganesh T, Thepchatri P, Li L, Du Y, Fu H, Snyder JP, Sun A.
Bioorg Med Chem Lett (2008) 18 : 4982 -4987
PubMed 18762423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.18 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL515000 1 6.26
CHEMBL371915 1 6.16
CHEMBL478665 1 5.89
CHEMBL476157 1 5.77
CHEMBL478879 1 5.75
CHEMBL478664 1 5.60
CHEMBL476359 1 5.36
CHEMBL444355 1 5.35
CHEMBL477824 1 5.03
CHEMBL477825 1 5.02
CHEMBL476368 1 4.84
CHEMBL476574 1 4.71
CHEMBL478890 1 4.71
CHEMBL514704 1 4.60
CHEMBL490783 1 4.58
CHEMBL489767 1 4.57
CHEMBL478891 1 4.55
CHEMBL476369 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL515000 IC50 = 550.0 nM 6.26
CHEMBL371915 IC50 = 700.0 nM 6.16
CHEMBL478665 IC50 = 1300.0 nM 5.89
CHEMBL476157 IC50 = 1700.0 nM 5.77
CHEMBL478879 IC50 = 1800.0 nM 5.75
CHEMBL478664 IC50 = 2500.0 nM 5.60
CHEMBL476359 IC50 = 4400.0 nM 5.36
CHEMBL444355 IC50 = 4500.0 nM 5.35
CHEMBL477824 IC50 = 9400.0 nM 5.03
CHEMBL477825 IC50 = 9500.0 nM 5.02
CHEMBL476368 IC50 = 14500.0 nM 4.84
CHEMBL476574 IC50 = 19400.0 nM 4.71
CHEMBL478890 IC50 = 19600.0 nM 4.71
CHEMBL514704 IC50 = 25000.0 nM 4.60
CHEMBL490783 IC50 = 26000.0 nM 4.58
CHEMBL489767 IC50 = 27000.0 nM 4.57
CHEMBL478891 IC50 = 28000.0 nM 4.55
CHEMBL476369 IC50 = 31300.0 nM 4.50