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Assay Detail

CHEMBL4376727

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

Binding
Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histone deacetylase 3 (CHEMBL1829)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Class I/IIb-Selective HDAC Inhibitor Exhibits Oral Bioavailability and Therapeutic Efficacy in Acute Myeloid Leukemia.
Shouksmith AE, Gawel JM, Nawar N, Sina D, Raouf YS, Bukhari S, He L, Johns AE, Manaswiyoungkul P, Olaoye OO, Cabral AD, Sedighi A, de Araujo ED, Gunning PT.
ACS Med Chem Lett (2020) 11 : 56 -64
PubMed 31938464 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.62 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 8.18
CHEMBL4563224 1 6.88
CHEMBL4452620 1 6.73
CHEMBL4565392 1 6.67
CHEMBL4437895 1 6.67
CHEMBL4565296 1 6.56
CHEMBL4560533 1 6.43
CHEMBL4559559 1 6.43
CHEMBL4576056 1 6.31
CHEMBL4472310 1 6.30
CHEMBL4520400 1 6.18
CHEMBL4464527 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 6.57 nM 8.18
CHEMBL4563224 IC50 = 132.0 nM 6.88
CHEMBL4452620 IC50 = 187.0 nM 6.73
CHEMBL4565392 IC50 = 213.0 nM 6.67
CHEMBL4437895 IC50 = 213.0 nM 6.67
CHEMBL4565296 IC50 = 276.0 nM 6.56
CHEMBL4560533 IC50 = 372.0 nM 6.43
CHEMBL4559559 IC50 = 374.0 nM 6.43
CHEMBL4576056 IC50 = 492.0 nM 6.31
CHEMBL4472310 IC50 = 503.0 nM 6.30
CHEMBL4520400 IC50 = 654.0 nM 6.18
CHEMBL4464527 IC50 = 708.0 nM 6.15