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Assay Detail

CHEMBL1006964

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

Binding
Inhibition of GST-fused recombinant HAT p300 expressed in Escherichia coli by filter assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).
Gorsuch S, Bavetsias V, Rowlands MG, Aherne GW, Workman P, Jarman M, McDonald E.
Bioorg Med Chem (2009) 17 : 467 -474
PubMed 19101154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.91 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL499919 1 5.52
CHEMBL491092 1 5.00
CHEMBL487498 1 4.84
CHEMBL99594 1 4.64
CHEMBL489494 1 4.55
CHEMBL443951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL499919 IC50 = 3000.0 nM 5.52
CHEMBL491092 IC50 = 9900.0 nM 5.00
CHEMBL487498 IC50 = 14400.0 nM 4.84
CHEMBL99594 IC50 = 23000.0 nM 4.64
CHEMBL489494 IC50 = 28000.0 nM 4.55
CHEMBL443951 IC50 - -