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Assay Detail

CHEMBL5157022

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

Binding
Inhibition of full length wild type LRRK2 (unknown origin) by LRRKtide Adapta assay
52
Total Activities
52
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

Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy.
Leśniak RK, Nichols RJ, Schonemann M, Zhao J, Gajera CR, Fitch WL, Lam G, Nguyen KC, Smith M, Montine TJ.
Eur J Med Chem (2022) 229 : 114080 -114080
PubMed 34992038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.23 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098877 MLi-2 1 9.00
CHEMBL5187271 1 8.30
CHEMBL5170359 1 8.15
CHEMBL5194735 1 8.10
CHEMBL5177346 1 8.10
CHEMBL5206337 1 8.00
CHEMBL5207998 1 7.96
CHEMBL5201248 1 7.85
CHEMBL5174552 1 7.75
CHEMBL5176421 1 7.72
CHEMBL5182067 1 7.70
CHEMBL5196967 1 7.68
CHEMBL5200822 1 7.66
CHEMBL5184816 1 7.66
CHEMBL5182980 1 7.64
CHEMBL5179734 1 7.62
CHEMBL5209350 1 7.60
CHEMBL5172598 1 7.58
CHEMBL5186450 1 7.58
CHEMBL5182227 1 7.52
CHEMBL5169393 1 7.47
CHEMBL5171585 1 7.46
CHEMBL5185049 1 7.42
CHEMBL5169734 1 7.42
CHEMBL5169946 1 7.40
CHEMBL5179942 1 7.40
CHEMBL5208819 1 7.38
CHEMBL5202237 1 7.37
CHEMBL5192191 1 7.25
CHEMBL5198050 1 7.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098877 MLi-2 IC50 = 1.0 nM 9.00
CHEMBL5187271 IC50 = 5.0 nM 8.30
CHEMBL5170359 IC50 = 7.0 nM 8.15
CHEMBL5194735 IC50 = 8.0 nM 8.10
CHEMBL5177346 IC50 = 8.0 nM 8.10
CHEMBL5206337 IC50 = 10.0 nM 8.00
CHEMBL5207998 IC50 = 11.0 nM 7.96
CHEMBL5201248 IC50 = 14.0 nM 7.85
CHEMBL5174552 IC50 = 18.0 nM 7.75
CHEMBL5176421 IC50 = 19.0 nM 7.72
CHEMBL5182067 IC50 = 20.0 nM 7.70
CHEMBL5196967 IC50 = 21.0 nM 7.68
CHEMBL5184816 IC50 = 22.0 nM 7.66
CHEMBL5200822 IC50 = 22.0 nM 7.66
CHEMBL5182980 IC50 = 23.0 nM 7.64
CHEMBL5179734 IC50 = 24.0 nM 7.62
CHEMBL5209350 IC50 = 25.0 nM 7.60
CHEMBL5172598 IC50 = 26.0 nM 7.58
CHEMBL5186450 IC50 = 26.0 nM 7.58
CHEMBL5182227 IC50 = 30.0 nM 7.52
CHEMBL5169393 IC50 = 34.0 nM 7.47
CHEMBL5171585 IC50 = 35.0 nM 7.46
CHEMBL5185049 IC50 = 38.0 nM 7.42
CHEMBL5169734 IC50 = 38.0 nM 7.42
CHEMBL5179942 IC50 = 40.0 nM 7.40
CHEMBL5169946 IC50 = 40.0 nM 7.40
CHEMBL5208819 IC50 = 42.0 nM 7.38
CHEMBL5202237 IC50 = 43.0 nM 7.37
CHEMBL5192191 IC50 = 56.0 nM 7.25
CHEMBL5198050 IC50 = 57.0 nM 7.24
CHEMBL5179131 IC50 = 61.0 nM 7.21
CHEMBL5207003 IC50 = 67.0 nM 7.17
CHEMBL5197876 IC50 = 69.0 nM 7.16
CHEMBL5188644 IC50 = 82.0 nM 7.09
CHEMBL5201629 IC50 = 115.0 nM 6.94
CHEMBL5200012 IC50 = 118.0 nM 6.93
CHEMBL5186274 IC50 = 132.0 nM 6.88
CHEMBL5194659 IC50 = 134.0 nM 6.87
CHEMBL5189165 IC50 = 154.0 nM 6.81
CHEMBL5206958 IC50 = 156.0 nM 6.81
CHEMBL5195812 IC50 = 163.0 nM 6.79
CHEMBL5198808 IC50 = 189.0 nM 6.72
CHEMBL5193770 IC50 = 218.0 nM 6.66
CHEMBL5173860 IC50 = 227.0 nM 6.64
CHEMBL5204222 IC50 = 276.0 nM 6.56
CHEMBL5194653 IC50 = 346.0 nM 6.46
CHEMBL5171090 IC50 = 527.0 nM 6.28
CHEMBL5206767 IC50 = 637.0 nM 6.20
CHEMBL5196195 IC50 = 646.0 nM 6.19
CHEMBL5189805 IC50 = 866.0 nM 6.06