Assay Detail

CHEMBL5705010

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Binding

Inhibition of human ALK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assay

ChEMBL ↗

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Target

ALK tyrosine kinase receptor (CHEMBL4247) ↗

Open DB target context

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Primary target ALK tyrosine kinase receptor

CHEMBL4247

Anchored from Assay target.

Protein identity ALK tyrosine kinase receptor

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

ALK tyrosine kinase receptor (CHEMBL4247) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.

Zhang S, Anjum R, Squillace R, Nadworny S, Zhou T, Keats J, Ning Y, Wardwell SD, Miller D, Song Y, Eichinger L, Moran L, Huang WS, Liu S, Zou D, Wang Y, Mohemmad Q, Jang HG, Ye E, Narasimhan N, Wang F, Miret J, Zhu X, Clackson T, Dalgarno D, Shakespeare WC, Rivera VM.
Clin Cancer Res (2016) 22 : 5527 -5538
PubMed 27780853 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.22	9.22

Assay Parameters

Parameter	Type	Value	Units	Text
EFO_ID	EFO_ID	-	—	EFO:0003060
EFO_TERM	EFO_TERM	-	—	non-small cell lung carcinoma

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3545311	BRIGATINIB	4.0	1	9.22

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3545311	BRIGATINIB	IC50	=	0.6	nM	9.22