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Assay Detail

CHEMBL5040136

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

Binding
Inhibition of LRRK2-WT-pSER935 in C57BL/6 mouse brain at 10 to 150 mg/kg and measured after 1 hrs by western blotting
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design and Synthesis of Pyrrolo[2,3-<i>d</i>]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate.
Williamson DS, Smith GP, Mikkelsen GK, Jensen T, Acheson-Dossang P, Badolo L, Bedford ST, Chell V, Chen IJ, Dokurno P, Hentzer M, Newland S, Ray SC, Shaw T, Surgenor AE, Terry L, Wang Y, Christensen KV.
J Med Chem (2021) 64 : 10312 -10332
PubMed 34184879 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.72 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5087055 1 7.80
CHEMBL5092087 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5087055 IC50 = 16.0 nM 7.80
CHEMBL5092087 IC50 = 23.0 nM 7.64