Assay Detail

CHEMBL5710916

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Binding

Inhibition of recombinant BLK (unknown origin) preincubated for 1 hr in presence of ATP by Z-Lyte assay

ChEMBL ↗

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Target

Tyrosine-protein kinase Blk (CHEMBL2250) ↗

Open DB target context

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Tyrosine-protein kinase Blk (CHEMBL2250) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Tyrosine-protein kinase Blk

CHEMBL2250

Anchored from Assay target.

Protein identity Tyrosine-protein kinase Blk

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 Blk (CHEMBL2250) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.

Byrd JC, Harrington B, O'Brien S, Jones JA, Schuh A, Devereux S, Chaves J, Wierda WG, Awan FT, Brown JR, Hillmen P, Stephens DM, Ghia P, Barrientos JC, Pagel JM, Woyach J, Johnson D, Huang J, Wang X, Kaptein A, Lannutti BJ, Covey T, Fardis M, McGreivy J, Hamdy A, Rothbaum W, Izumi R, Diacovo TG, Johnson AJ, Furman RR.
N Engl J Med (2016) 374 : 323 -332
PubMed 26641137 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	10.00	10.00

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	10.00
CHEMBL3707348	ACALABRUTINIB	4.0	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1873475	IBRUTINIB	IC50	=	0.1	nM	10.00
CHEMBL3707348	ACALABRUTINIB	IC50	>	1000.0	nM	-