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Assay Detail

CHEMBL962086

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

Binding
Inhibition of human recombinant ARK5
6
Total Activities
6
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

NUAK family SNF1-like kinase 1 (CHEMBL5784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as vascular endothelial growth factor receptor (VEGF-R) inhibitors.
Peifer C, Selig R, Kinkel K, Ott D, Totzke F, Schächtele C, Heidenreich R, Röcken M, Schollmeyer D, Laufer S.
J Med Chem (2008) 51 : 3814 -3824
PubMed 18529047 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.17 5.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521201 1 5.75
CHEMBL452812 1 5.70
CHEMBL507056 1 5.44
CHEMBL509435 1 5.31
CHEMBL453593 1 4.47
CHEMBL201511 MALEIMIDE 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521201 IC50 = 1800.0 nM 5.75
CHEMBL452812 IC50 = 2000.0 nM 5.70
CHEMBL507056 IC50 = 3600.0 nM 5.44
CHEMBL509435 IC50 = 4900.0 nM 5.31
CHEMBL453593 IC50 = 34000.0 nM 4.47
CHEMBL201511 MALEIMIDE IC50 = 43000.0 nM 4.37