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Assay Detail

CHEMBL4152830

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to wild-type human partial length ALK (I1088 to E1409 residues) expressed in mammalian expression system by KINOMEscan assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
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

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).
Zhang C, Han XR, Yang X, Jiang B, Liu J, Xiong Y, Jin J.
Eur J Med Chem (2018) 151 : 304 -314
PubMed 29627725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 5 7.68 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2403108 CERITINIB 4.0 1 8.89
CHEMBL4161454 1 7.72
CHEMBL4165519 1 7.43
CHEMBL4159122 1 7.27
CHEMBL4169769 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2403108 CERITINIB Kd = 1.3 nM 8.89
CHEMBL4161454 Kd = 19.0 nM 7.72
CHEMBL4165519 Kd = 37.0 nM 7.43
CHEMBL4159122 Kd = 54.0 nM 7.27
CHEMBL4169769 Kd = 78.0 nM 7.11