Assay Detail

CHEMBL5685066

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

Binding

Inhibition of human BTK by ATP-Competition Binding Assay

ChEMBL ↗

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Target

Tyrosine-protein kinase BTK (CHEMBL5251) ↗

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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

The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia.

Herman SEM, Montraveta A, Niemann CU, Mora-Jensen H, Gulrajani M, Krantz F, Mantel R, Smith LL, McClanahan F, Harrington BK, Colomer D, Covey T, Byrd JC, Izumi R, Kaptein A, Ulrich R, Johnson AJ, Lannutti BJ, Wiestner A, Woyach JA.
Clin Cancer Res (2017) 23 : 2831 -2841
PubMed 27903679 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.56	8.82

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0000095
EFO_TERM	EFO_TERM	-	—	chronic lymphocytic leukemia

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1873475	IBRUTINIB	4.0	1	8.82
CHEMBL3707348	ACALABRUTINIB	4.0	1	8.29

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1873475	IBRUTINIB	IC50	=	1.5	nM	8.82
CHEMBL3707348	ACALABRUTINIB	IC50	=	5.1	nM	8.29