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Assay Detail

CHEMBL4685115

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

Binding
Inhibition of HSP90a (unknown origin)
11
Total Activities
11
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

Isoindoline scaffold-based dual inhibitors of HDAC6 and HSP90 suppressing the growth of lung cancer in vitro and in vivo.
Ojha R,Nepali K,Chen CH,Chuang KH,Wu TY,Lin TE,Hsu KC,Chao MW,Lai MJ,Lin MH,Huang HL,Chang CD,Pan SL,Chen MC,Liou JP
Eur J Med Chem (2020) 190 : 112086 -112086
PubMed 32058238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.05 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4798549 1 7.36
CHEMBL4790559 1 7.36
CHEMBL4789155 1 7.33
CHEMBL4782478 1 7.18
CHEMBL467399 BIIB021 2.0 1 7.18
CHEMBL4747757 1 6.99
CHEMBL4741850 1 6.96
CHEMBL4749731 1 6.91
CHEMBL4740842 1 6.87
CHEMBL4790152 1 6.38
CHEMBL98 VORINOSTAT 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4798549 IC50 = 43.9 nM 7.36
CHEMBL4790559 IC50 = 43.9 nM 7.36
CHEMBL4789155 IC50 = 46.8 nM 7.33
CHEMBL4782478 IC50 = 66.0 nM 7.18
CHEMBL467399 BIIB021 IC50 = 65.7 nM 7.18
CHEMBL4747757 IC50 = 103.5 nM 6.99
CHEMBL4741850 IC50 = 108.7 nM 6.96
CHEMBL4749731 IC50 = 123.1 nM 6.91
CHEMBL4740842 IC50 = 135.6 nM 6.87
CHEMBL4790152 IC50 = 422.0 nM 6.38
CHEMBL98 VORINOSTAT IC50 > 1000.0 nM -