Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4383832

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

Binding
Inhibition of human DAPK1 (1 to 363 residues) using KKLNRTLSFAEPG as substrate after 120 mins in presence of 10 uM [gamma-33P]-ATP by filtration method
12
Total Activities
12
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

Death-associated protein kinase 1 (CHEMBL2558)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First-in-class DAPK1/CSF1R dual inhibitors: Discovery of 3,5-dimethoxy-N-(4-(4-methoxyphenoxy)-2-((6-morpholinopyridin-3-yl)amino)pyrimidin-5-yl)benzamide as a potential anti-tauopathies agent.
Farag AK, Hassan AHE, Jeong H, Kwon Y, Choi JG, Oh MS, Park KD, Kim YK, Roh EJ.
Eur J Med Chem (2019) 162 : 161 -175
PubMed 30445265 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.42 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4461911 1 5.90
CHEMBL4467582 1 5.58
CHEMBL4461940 1 5.57
CHEMBL4464585 1 5.56
CHEMBL4521651 1 5.37
CHEMBL4568513 1 5.13
CHEMBL4459764 1 4.84
CHEMBL4585766 1 -
CHEMBL4522113 1 -
CHEMBL4434760 1 -
CHEMBL4443393 1 -
CHEMBL4587860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4461911 IC50 = 1250.0 nM 5.90
CHEMBL4467582 IC50 = 2610.0 nM 5.58
CHEMBL4461940 IC50 = 2690.0 nM 5.57
CHEMBL4464585 IC50 = 2770.0 nM 5.56
CHEMBL4521651 IC50 = 4290.0 nM 5.37
CHEMBL4568513 IC50 = 7440.0 nM 5.13
CHEMBL4459764 IC50 = 14300.0 nM 4.84
CHEMBL4585766 IC50 - -
CHEMBL4522113 IC50 - -
CHEMBL4434760 IC50 - -
CHEMBL4443393 IC50 - -
CHEMBL4587860 IC50 - -