Assay Detail

CHEMBL5043231

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Binding

Binding affinity to wild-type human full length BTK (M1 to S659 residues) expressed in mammalian expression system by Kinomescan method

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
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
Kd	4	9.24	10.15

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5083772	BIIB-091	2.0	1	10.15
CHEMBL4066176	—	—	1	9.62
CHEMBL4650323	TOLEBRUTINIB	3.0	1	8.85
CHEMBL4072833	EVOBRUTINIB	3.0	1	8.34

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5083772	BIIB-091	Kd	=	0.07	nM	10.15
CHEMBL4066176	—	Kd	=	0.24	nM	9.62
CHEMBL4650323	TOLEBRUTINIB	Kd	=	1.4	nM	8.85
CHEMBL4072833	EVOBRUTINIB	Kd	=	4.6	nM	8.34