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Assay Detail

CHEMBL3626893

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

Binding
Inhibition of recombinant human CBP using biotinylated histone H3 (1 to 21 amino acid residues) as substrate preincubated for 10 mins followed by acetyl-CoA addition measured after 10 mins by time resolved fluorescence assay
9
Total Activities
9
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

CREB-binding protein (CHEMBL5747)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs)
Furdas SD, Hoffmann I, Robaa D, Herquel B, Malinka W, Swiatek P, Akhtar A, Sippl W, Jung M
Medchemcomm (2014) 5 : 1856 -1862
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.70 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1370704 1 6.36
CHEMBL1795619 1 5.90
CHEMBL1795801 1 5.84
CHEMBL2419973 1 5.78
CHEMBL1795618 1 5.71
CHEMBL106011 1 5.60
CHEMBL1795624 1 5.54
CHEMBL318367 1 5.28
CHEMBL3621671 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1370704 IC50 = 440.0 nM 6.36
CHEMBL1795619 IC50 = 1270.0 nM 5.90
CHEMBL1795801 IC50 = 1440.0 nM 5.84
CHEMBL2419973 IC50 = 1670.0 nM 5.78
CHEMBL1795618 IC50 = 1950.0 nM 5.71
CHEMBL106011 IC50 = 2490.0 nM 5.60
CHEMBL1795624 IC50 = 2850.0 nM 5.54
CHEMBL318367 IC50 = 5280.0 nM 5.28
CHEMBL3621671 IC50 = 5370.0 nM 5.27