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Assay Detail

CHEMBL4139705

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

Binding
Inhibition of KAT3B catalytic domain (1284 to 1673 residues) (unknown origin) using SGRGKGGKGLGKGGAKRHRK-NH2 as substrate after 5 mins in presence of Ac-CoA by fluorescence assay
20
Total Activities
20
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 p300 (CHEMBL3784)
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 20 5.11 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4159902 1 5.96
CHEMBL576321 1 5.85
CHEMBL4166834 1 5.58
CHEMBL4172065 1 5.52
CHEMBL4160049 1 5.43
CHEMBL4170165 1 4.28
CHEMBL4170179 1 4.22
CHEMBL4175261 1 4.02
CHEMBL1232567 1 -
CHEMBL4174622 1 -
CHEMBL4166714 1 -
CHEMBL2312200 1 -
CHEMBL4172714 1 -
CHEMBL4168293 1 -
CHEMBL4172575 1 -
CHEMBL4168302 1 -
CHEMBL4161954 1 -
CHEMBL4163878 1 -
CHEMBL1142 4-AMINOPHENOL 1 -
CHEMBL4168076 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4159902 IC50 = 1100.0 nM 5.96
CHEMBL576321 IC50 = 1400.0 nM 5.85
CHEMBL4166834 IC50 = 2600.0 nM 5.58
CHEMBL4172065 IC50 = 3000.0 nM 5.52
CHEMBL4160049 IC50 = 3700.0 nM 5.43
CHEMBL4170165 IC50 = 52000.0 nM 4.28
CHEMBL4170179 IC50 = 60000.0 nM 4.22
CHEMBL4175261 IC50 = 95000.0 nM 4.02
CHEMBL1232567 IC50 - -
CHEMBL4174622 IC50 - -
CHEMBL4166714 IC50 - -
CHEMBL2312200 IC50 = 106000.0 nM -
CHEMBL4172714 IC50 - -
CHEMBL4168293 IC50 - -
CHEMBL4172575 IC50 - -
CHEMBL4168302 IC50 - -
CHEMBL4161954 IC50 - -
CHEMBL4163878 IC50 = 250000.0 nM -
CHEMBL1142 4-AMINOPHENOL IC50 > 500000.0 nM -
CHEMBL4168076 IC50 - -