Assay Detail

CHEMBL3129270

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Binding

Inhibition of human EML4-fused ALK F1174L mutant expressed in mouse NIH-3T3 cells assessed as phospho-ALK level after 1 hr by sandwich ELISA

ChEMBL ↗

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Target

ALK tyrosine kinase receptor (CHEMBL4247) ↗

Open DB target context

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ALK tyrosine kinase receptor (CHEMBL4247) is the working anchor for this assay review. Loading the live Open DB target snapshot…

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
Cell Type	NIH3T3
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

ALK tyrosine kinase receptor (CHEMBL4247) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP.
J Med Chem (2014) 57 : 1170 -1187
PubMed 24432909 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.24	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3128069	—	—	1	9.70
CHEMBL601719	CRIZOTINIB	4.0	1	6.78

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3128069	—	IC50	=	0.2	nM	9.70
CHEMBL601719	CRIZOTINIB	IC50	=	165.0	nM	6.78