Assay Detail

CHEMBL5043294

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Binding

Inhibition of BTK in anti-IgM stimulated human PBMC cells assessed as reduction in PLCgamma2 phosphorylation

ChEMBL ↗

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Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

Open DB target context

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Tyrosine-protein kinase BTK (CHEMBL5251) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase BTK

CHEMBL5251

Anchored from Assay target.

Protein identity Tyrosine-protein kinase BTK

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	PBMC
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

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
IC50	1	8.27	8.27

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5083772	BIIB-091	2.0	1	8.27

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5083772	BIIB-091	IC50	=	5.4	nM	8.27