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

CHEMBL4010143

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

Functional
In vivo inhibition of LRRK2 Ser935 phosphorylation in mouse brain assessed as unbound plasma concentration causing reduction in ratio of phosphorylated Ser935 to total LRRK2 protein at 1 to 100 mg/kg, po administered 1 hr post treatment by Western blot analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 1 — Organism
Curated By Autocuration

Target

Mus musculus (CHEMBL375)
Type ORGANISM
Organism Mus musculus

Publication

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW.
J Med Chem (2017) 60 : 2983 -2992
PubMed 28245354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.96 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098877 MLi-2 1 8.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098877 MLi-2 IC50 = 1.1 nM 8.96