Assay Detail

CHEMBL2406347

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Binding

Inhibition of ALK (unknown origin) after 60 mins

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
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

ALK tyrosine kinase receptor (CHEMBL4247) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY.
J Med Chem (2013) 56 : 5675 -5690
PubMed 23742252 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	9.70	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2403108	CERITINIB	4.0	1	9.70

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2403108	CERITINIB	IC50	=	0.2	nM	9.70