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Assay Detail

CHEMBL3366599

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

Binding
Inhibition of mouse HDAC6 using fluorescent substrate Ac-KGLGK(Ac)-MCA after 30 mins by fluorescence plate reader in presence of 0.1 mM dithiothreitol
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 6 (CHEMBL2878)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design and synthesis of CHAP31, trapoxin B and HC-toxin based bicyclic tetrapeptides disulfide as potent histone deacetylase inhibitors.
Hoque MA, Islam MN, Islam MS, Kato T, Nishino N, Ito A, Yoshida M.
Bioorg Med Chem (2014) 22 : 3850 -3855
PubMed 24997578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.52 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL343448 ROMIDEPSIN 4.0 1 9.20
CHEMBL3310510 1 7.08
CHEMBL3310509 1 6.50
CHEMBL3310511 1 6.23
CHEMBL3310506 1 5.89
CHEMBL3310508 1 5.63
CHEMBL3310507 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL343448 ROMIDEPSIN IC50 = 0.625 nM 9.20
CHEMBL3310510 IC50 = 83.0 nM 7.08
CHEMBL3310509 IC50 = 320.0 nM 6.50
CHEMBL3310511 IC50 = 590.0 nM 6.23
CHEMBL3310506 IC50 = 1301.0 nM 5.89
CHEMBL3310508 IC50 = 2319.0 nM 5.63
CHEMBL3310507 IC50 = 7300.0 nM 5.14