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Assay Detail

CHEMBL3796125

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

Binding
Inhibition of HDAC4 in human Jurkat E6-1 cells using Lys-TFA as substrate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Jurkat
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 4 (CHEMBL3524)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.
Luckhurst CA, Breccia P, Stott AJ, Aziz O, Birch HL, Bürli RW, Hughes SJ, Jarvis RE, Lamers M, Leonard PM, Matthews KL, McAllister G, Pollack S, Saville-Stones E, Wishart G, Yates D, Dominguez C.
ACS Med Chem Lett (2016) 7 : 34 -39
PubMed 26819662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.50 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3793439 1 6.92
CHEMBL3793392 1 6.92
CHEMBL3792545 1 6.89
CHEMBL3794485 1 6.82
CHEMBL3110021 1 6.64
CHEMBL3794140 1 6.64
CHEMBL3793932 1 6.55
CHEMBL3110015 1 6.48
CHEMBL3794544 1 6.37
CHEMBL3793034 1 6.29
CHEMBL3793739 1 6.26
CHEMBL3794334 1 6.17
CHEMBL3793569 1 6.14
CHEMBL3793455 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3793439 IC50 = 120.0 nM 6.92
CHEMBL3793392 IC50 = 120.0 nM 6.92
CHEMBL3792545 IC50 = 130.0 nM 6.89
CHEMBL3794485 IC50 = 150.0 nM 6.82
CHEMBL3110021 IC50 = 230.0 nM 6.64
CHEMBL3794140 IC50 = 230.0 nM 6.64
CHEMBL3793932 IC50 = 280.0 nM 6.55
CHEMBL3110015 IC50 = 330.0 nM 6.48
CHEMBL3794544 IC50 = 430.0 nM 6.37
CHEMBL3793034 IC50 = 510.0 nM 6.29
CHEMBL3793739 IC50 = 550.0 nM 6.26
CHEMBL3794334 IC50 = 680.0 nM 6.17
CHEMBL3793569 IC50 = 730.0 nM 6.14
CHEMBL3793455 IC50 = 1150.0 nM 5.94