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Assay Detail

CHEMBL1798511

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

Binding
Inhibition of histone acetylase activity of human recombinant PCAF expressed in Escherichia coli using biotinylated oligopeptide sequences from histone H4 (2-24) substrate by In-vitro time-resolved fluorescence immunosorbent acetyltransferase assay
35
Total Activities
35
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 acetyltransferase KAT2B (CHEMBL5500)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological testing of novel pyridoisothiazolones as histone acetyltransferase inhibitors.
Furdas SD, Shekfeh S, Bissinger EM, Wagner JM, Schlimme S, Valkov V, Hendzel M, Jung M, Sippl W.
Bioorg Med Chem (2011) 19 : 3678 -3689
PubMed 21353783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 5.34 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106011 1 6.14
CHEMBL1795605 1 6.07
CHEMBL1795609 1 5.74
CHEMBL1795611 1 5.57
CHEMBL99137 1 5.52
CHEMBL1795606 1 4.80
CHEMBL1795624 1 4.59
CHEMBL1795799 1 4.29
CHEMBL1732009 1 -
CHEMBL1795610 1 -
CHEMBL1795802 1 -
CHEMBL1795619 1 -
CHEMBL1795618 1 -
CHEMBL98663 1 -
CHEMBL1795617 1 -
CHEMBL102387 1 -
CHEMBL1795615 1 -
CHEMBL1795613 1 -
CHEMBL1795612 1 -
CHEMBL1795801 1 -
CHEMBL1795800 1 -
CHEMBL1795798 1 -
CHEMBL1795796 1 -
CHEMBL1795795 1 -
CHEMBL1795625 1 -
CHEMBL1795623 1 -
CHEMBL1795622 1 -
CHEMBL1795621 1 -
CHEMBL1370704 1 -
CHEMBL1795620 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106011 IC50 = 720.0 nM 6.14
CHEMBL1795605 IC50 = 860.0 nM 6.07
CHEMBL1795609 IC50 = 1830.0 nM 5.74
CHEMBL1795611 IC50 = 2720.0 nM 5.57
CHEMBL99137 IC50 = 2990.0 nM 5.52
CHEMBL1795606 IC50 = 15800.0 nM 4.80
CHEMBL1795624 IC50 = 25500.0 nM 4.59
CHEMBL1795799 IC50 = 51300.0 nM 4.29
CHEMBL1795618 IC50 - -
CHEMBL1795604 IC50 - -
CHEMBL98663 IC50 - -
CHEMBL1795617 IC50 - -
CHEMBL102387 IC50 - -
CHEMBL1795615 IC50 - -
CHEMBL1795613 IC50 - -
CHEMBL1795612 IC50 - -
CHEMBL1795610 IC50 - -
CHEMBL95284 IC50 - -
CHEMBL1795608 IC50 - -
CHEMBL1795607 IC50 - -
CHEMBL101422 IC50 - -
CHEMBL1795619 IC50 - -
CHEMBL1795802 IC50 - -
CHEMBL1732009 IC50 - -
CHEMBL1795801 IC50 - -
CHEMBL1795800 IC50 - -
CHEMBL1795798 IC50 - -
CHEMBL1795796 IC50 - -
CHEMBL1795795 IC50 - -
CHEMBL1795625 IC50 - -
CHEMBL1795623 IC50 - -
CHEMBL1795622 IC50 - -
CHEMBL1795621 IC50 - -
CHEMBL1370704 IC50 - -
CHEMBL1795620 IC50 - -