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Assay Detail

CHEMBL5043233

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

Binding
Binding affinity to wild-type human full length BMX (M1 to H675 residues) expressed in bacterial expression system by Kinomescan method
1
Total Activities
1
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

Target

Cytoplasmic tyrosine-protein kinase BMX (CHEMBL3834)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Hopkins BT, Bame E, Bajrami B, Black C, Bohnert T, Boiselle C, Burdette D, Burns JC, Delva L, Donaldson D, Grater R, Gu C, Hoemberger M, Johnson J, Kapadnis S, King K, Lulla M, Ma B, Marx I, Magee T, Meissner R, Metrick CM, Mingueneau M, Murugan P, Otipoby KL, Polack E, Poreci U, Prince R, Roach AM, Rowbottom C, Santoro JC, Schroeder P, Tang H, Tien E, Zhang F, Lyssikatos J.
J Med Chem (2022) 65 : 1206 -1224
PubMed 34734694 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 7.06 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5083772 BIIB-091 2.0 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5083772 BIIB-091 Kd = 88.0 nM 7.06