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Assay Detail

CHEMBL5373316

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

Binding
Inhibition of HDAC6 in human BEAS-2B cells assessed as deacetylation of acetylated alpha-tubulin level incubated for 24 hrs by Western blot analysis
20
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BEAS-2B
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL1865)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective and Bioavailable HDAC6 2-(Difluoromethyl)-1,3,4-oxadiazole Substrate Inhibitors and Modeling of Their Bioactivation Mechanism.
Ripa L, Sandmark J, Hughes G, Shamovsky I, Gunnarsson A, Johansson J, Llinas A, Collins M, Jung B, Novén A, Pemberton N, Mogemark M, Xiong Y, Li Q, Tångefjord S, Ek M, Åstrand A.
J Med Chem (2023) 66 : 14188 -14207
PubMed 37797307 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.37 7.70
IC50 2 7.35 8.00
pEC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5435916 1 8.00
CHEMBL4440341 1 7.70
CHEMBL5410192 1 7.20
CHEMBL3935992 1 7.10
CHEMBL5438547 1 6.70
CHEMBL5429808 1 6.60
CHEMBL5408305 1 6.50
CHEMBL5425061 1 6.50
CHEMBL5408594 1 6.50
CHEMBL5440081 1 6.40
CHEMBL5425437 1 6.30
CHEMBL5421243 1 6.20
CHEMBL5440297 1 6.20
CHEMBL5429654 1 6.00
CHEMBL5403250 1 5.90
CHEMBL5434758 1 5.80
CHEMBL5417383 1 5.50
CHEMBL5411782 1 5.50
CHEMBL5429543 1 -
CHEMBL5403435 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5435916 IC50 = 10.0 nM 8.00
CHEMBL4440341 EC50 = 19.95 nM 7.70
CHEMBL5410192 EC50 = 63.1 nM 7.20
CHEMBL3935992 EC50 = 79.43 nM 7.10
CHEMBL5438547 IC50 = 199.53 nM 6.70
CHEMBL5429808 EC50 = 251.19 nM 6.60
CHEMBL5408305 EC50 = 316.23 nM 6.50
CHEMBL5425061 EC50 = 316.23 nM 6.50
CHEMBL5408594 EC50 = 316.23 nM 6.50
CHEMBL5440081 EC50 = 398.11 nM 6.40
CHEMBL5425437 EC50 = 501.19 nM 6.30
CHEMBL5421243 EC50 = 630.96 nM 6.20
CHEMBL5440297 EC50 = 630.96 nM 6.20
CHEMBL5429654 EC50 = 1000.0 nM 6.00
CHEMBL5403250 EC50 = 1258.93 nM 5.90
CHEMBL5434758 EC50 = 1584.89 nM 5.80
CHEMBL5417383 EC50 = 3162.28 nM 5.50
CHEMBL5411782 EC50 = 3162.28 nM 5.50
CHEMBL5429543 pEC50 - -
CHEMBL5403435 EC50 > 10000.0 nM -