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Assay Detail

CHEMBL2020396

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

Binding
Inhibition of human recombinant HDAC6 using RHKKAc peptide as substrate incubated for 5 to mins prior to substrate addition measured after 2 hrs
24
Total Activities
24
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

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

Publication

Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells.
Kalin JH, Butler KV, Akimova T, Hancock WW, Kozikowski AP.
J Med Chem (2012) 55 : 639 -651
PubMed 22165909 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.51 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018447 1 9.34
CHEMBL2018446 1 9.23
CHEMBL2018301 1 9.15
CHEMBL2018448 1 9.10
CHEMBL2018452 1 9.06
CHEMBL2018442 1 9.01
CHEMBL2018300 1 8.99
CHEMBL2018451 1 8.85
CHEMBL2018443 1 8.84
CHEMBL2018303 1 8.65
CHEMBL2018450 1 8.60
CHEMBL2018444 1 8.53
CHEMBL2018305 1 8.52
CHEMBL2018445 1 8.52
CHEMBL2018299 1 8.51
CHEMBL2018449 1 8.39
CHEMBL2018296 1 8.31
CHEMBL2018304 1 8.18
CHEMBL2018441 1 8.05
CHEMBL2018295 1 7.94
CHEMBL2018302 TUBASTATIN A 1 7.82
CHEMBL2018298 1 7.65
CHEMBL2018294 1 7.46
CHEMBL2018297 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018447 IC50 = 0.459 nM 9.34
CHEMBL2018446 IC50 = 0.582 nM 9.23
CHEMBL2018301 IC50 = 0.704 nM 9.15
CHEMBL2018448 IC50 = 0.799 nM 9.10
CHEMBL2018452 IC50 = 0.872 nM 9.06
CHEMBL2018442 IC50 = 0.972 nM 9.01
CHEMBL2018300 IC50 = 1.02 nM 8.99
CHEMBL2018451 IC50 = 1.4 nM 8.85
CHEMBL2018443 IC50 = 1.44 nM 8.84
CHEMBL2018303 IC50 = 2.25 nM 8.65
CHEMBL2018450 IC50 = 2.49 nM 8.60
CHEMBL2018444 IC50 = 2.96 nM 8.53
CHEMBL2018305 IC50 = 2.99 nM 8.52
CHEMBL2018445 IC50 = 3.05 nM 8.52
CHEMBL2018299 IC50 = 3.06 nM 8.51
CHEMBL2018449 IC50 = 4.06 nM 8.39
CHEMBL2018296 IC50 = 4.9 nM 8.31
CHEMBL2018304 IC50 = 6.56 nM 8.18
CHEMBL2018441 IC50 = 8.96 nM 8.05
CHEMBL2018295 IC50 = 11.5 nM 7.94
CHEMBL2018302 TUBASTATIN A IC50 = 15.0 nM 7.82
CHEMBL2018298 IC50 = 22.5 nM 7.65
CHEMBL2018294 IC50 = 34.7 nM 7.46
CHEMBL2018297 IC50 = 38.4 nM 7.42