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Assay Detail

CHEMBL5046600

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

Binding
Inhibition of recombinant human LRRK2 (970 to end residues) using RLGRDKYKTLRQIRQ as substrate incubated for 40 mins in presence of [gamma-33P-ATP] by radiometric scintillation assay
3
Total Activities
3
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

Publication

Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.
Drewry DH, Annor-Gyamfi JK, Wells CI, Pickett JE, Dederer V, Preuss F, Mathea S, Axtman AD.
J Med Chem (2022) 65 : 1313 -1328
PubMed 34333981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.19 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079601 1 7.72
CHEMBL5086901 1 7.05
CHEMBL4446892 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079601 IC50 = 19.0 nM 7.72
CHEMBL5086901 IC50 = 89.0 nM 7.05
CHEMBL4446892 IC50 = 159.0 nM 6.80