Assay Detail

CHEMBL5502974

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Binding

Inhibition of human full-length wild type BTK (M1 to S659 residues) expressed in mammalian expression system

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 BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis.

Himmelbauer MK, Bajrami B, Basile R, Capacci A, Chen T, Choi CK, Gilfillan R, Gonzalez-Lopez de Turiso F, Gu C, Hoemberger M, Johnson DS, Jones JH, Kadakia E, Kirkland M, Lin EY, Liu Y, Ma B, Magee T, Mantena S, Marx IE, Metrick CM, Mingueneau M, Murugan P, Muste CA, Nadella P, Nevalainen M, Parker Harp CR, Pattaropong V, Pietrasiewicz A, Prince RJ, Purgett TJ, Santoro JC, Schulz J, Sciabola S, Tang H, Vandeveer HG, Wang T, Yousaf Z, Helal CJ, Hopkins BT.
J Med Chem (2024) 67 : 8122 -8140
PubMed 38712838 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	5	9.02	9.51

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL5557589	—	—	1	9.51
CHEMBL5558638	—	—	1	9.22
CHEMBL5532458	—	—	1	9.20
CHEMBL4650323	TOLEBRUTINIB	3.0	1	8.85
CHEMBL4072833	EVOBRUTINIB	3.0	1	8.34

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL5557589	—	Kd	=	0.31	nM	9.51
CHEMBL5558638	—	Kd	=	0.6	nM	9.22
CHEMBL5532458	—	Kd	=	0.63	nM	9.20
CHEMBL4650323	TOLEBRUTINIB	Kd	=	1.4	nM	8.85
CHEMBL4072833	EVOBRUTINIB	Kd	=	4.6	nM	8.34