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Assay Detail

CHEMBL4358535

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Binding
Inhibition of human ERG by Qpatch clamp method
2
Total Activities
2
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 LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G, Gutmann S, Scheufler C, Hinniger A, Zimmerlin A, Funhoff EG, Pulz R, Cenni B.
J Med Chem (2020) 63 : 5102 -5118
PubMed 32083858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.70 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4483575 REMIBRUTINIB 3.0 1 5.85
CHEMBL4468719 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4483575 REMIBRUTINIB IC50 = 1400.0 nM 5.85
CHEMBL4468719 IC50 = 2900.0 nM 5.54