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Assay Detail

CHEMBL5131019

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

Binding
Inhibition of human myc-His6-tagged zDHHC20 expressed in HEK293T cells using 5-FAM-GTQGCMGLPCVVM-COOH as substrate preincubated for 1 hr followed by substrate addition and measured at 1 min interval for 2 hrs in presence of palmitoyl-CoA by fluorescence polarization assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Palmitoyltransferase ZDHHC20 (CHEMBL5169156)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Charting the Chemical Space of Acrylamide-Based Inhibitors of zDHHC20.
Azizi SA, Delalande C, Lan T, Qiu T, Dickinson BC.
ACS Med Chem Lett (2022) 13 : 1648 -1654
PubMed 36262404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.37 5.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201039 1 5.87
CHEMBL5186346 1 5.71
CHEMBL5199102 1 5.54
CHEMBL5205503 1 5.46
CHEMBL5191244 1 5.46
CHEMBL118417 1 5.26
CHEMBL5181387 1 5.01
CHEMBL5171728 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201039 IC50 = 1350.0 nM 5.87
CHEMBL5186346 IC50 = 1970.0 nM 5.71
CHEMBL5199102 IC50 = 2870.0 nM 5.54
CHEMBL5205503 IC50 = 3450.0 nM 5.46
CHEMBL5191244 IC50 = 3430.0 nM 5.46
CHEMBL118417 IC50 = 5550.0 nM 5.26
CHEMBL5181387 IC50 = 9730.0 nM 5.01
CHEMBL5171728 IC50 = 21400.0 nM 4.67