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Assay Detail

CHEMBL4139708

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

Binding
Inhibition of N-terminal His6-tagged KAT8 catalytic domain (125 to 458 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA and TCEP by fluorescence assay
1
Total Activities
1
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 KAT8 (CHEMBL1932912)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The relevance of Ki calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor.
Wapenaar H, van den Bosch T, Leus NGJ, van der Wouden PE, Eleftheriadis N, Hermans J, Hailu GS, Rotili D, Mai A, Dömling A, Bischoff R, Haisma HJ, Dekker FJ.
Eur J Med Chem (2017) 136 : 480 -486
PubMed 28527406 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.75 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576321 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576321 IC50 = 1800.0 nM 5.75