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Assay Detail

CHEMBL3865679

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

Binding
Inhibition of GST-tagged recombinant human LRRK2 (970 to 2527 residues) expressed in baculovirus
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

Carboxamide Spleen Tyrosine Kinase (Syk) Inhibitors: Leveraging Ground State Interactions To Accelerate Optimization.
Ellis JM, Altman MD, Cash B, Haidle AM, Kubiak RL, Maddess ML, Yan Y, Northrup AB.
ACS Med Chem Lett (2016) 7 : 1151 -1155
PubMed 27994755 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.30 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3414584 1 7.52
CHEMBL3415610 1 7.48
CHEMBL3943181 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3414584 IC50 = 30.0 nM 7.52
CHEMBL3415610 IC50 = 33.0 nM 7.48
CHEMBL3943181 IC50 = 130.0 nM 6.89