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Assay Detail

CHEMBL4266256

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Binding
Inhibition of ALK (unknown origin)
3
Total Activities
3
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

First macrocyclic 3rd-generation ALK inhibitor for treatment of ALK/ROS1 cancer: Clinical and designing strategy update of lorlatinib.
Basit S, Ashraf Z, Lee K, Latif M.
Eur J Med Chem (2017) 134 : 348 -356
PubMed 28431340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 9.14 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3286830 LORLATINIB 4.0 1 9.15
CHEMBL601719 CRIZOTINIB 4.0 1 9.13
CHEMBL4286522 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3286830 LORLATINIB Ki = 0.7 nM 9.15
CHEMBL601719 CRIZOTINIB Ki = 0.74 nM 9.13
CHEMBL4286522 Ki < 0.2 nM -