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Assay Detail

CHEMBL5130722

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

Binding
Protac activity at VHL/HDAC4 in human Jurkat E6.1 cells assessed as induction of HDAC4 degradation preincubated with elacridar for 1 hr followed by compound addition and measured after 24 hrs by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat E6.1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

von Hippel-Lindau disease tumor suppressor/Histone deacetylase 4 (CHEMBL4630746)
Type PROTEIN-PROTEIN INTERACTION
Organism Homo sapiens

Publication

Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.
Macabuag N, Esmieu W, Breccia P, Jarvis R, Blackaby W, Lazari O, Urbonas L, Eznarriaga M, Williams R, Strijbosch A, Van de Bospoort R, Matthews K, Clissold C, Ladduwahetty T, Vater H, Heaphy P, Stafford DG, Wang HJ, Mangette JE, McAllister G, Beaumont V, Vogt TF, Wilkinson HA, Doherty EM, Dominguez C.
J Med Chem (2022) 65 : 12445 -12459
PubMed 36098485 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.80 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208515 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208515 EC50 = 1.6 nM 8.80