Assay Detail

CHEMBL3293395

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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) ↗

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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
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

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

Johnson TW, Richardson PF, Bailey S, Brooun A, Burke BJ, Collins MR, Cui JJ, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Huang Q, Kania RS, Kath JC, Lam H, Lam JL, Le PT, Lingardo L, Liu W, McTigue M, Palmer CL, Sach NW, Smeal T, Smith GL, Stewart AE, Timofeevski S, Zhu H, Zhu J, Zou HY, Edwards MP.
J Med Chem (2014) 57 : 4720 -4744
PubMed 24819116 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.24	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3286830	LORLATINIB	4.0	1	9.70
CHEMBL601719	CRIZOTINIB	4.0	1	6.78

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3286830	LORLATINIB	IC50	=	0.2	nM	9.70
CHEMBL601719	CRIZOTINIB	IC50	=	165.0	nM	6.78