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Assay Detail

CHEMBL4378244

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

Binding
Inhibition of ALK G1202R (unknown origin)
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

Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK).
Kong X, Pan P, Sun H, Xia H, Wang X, Li Y, Hou T.
J Med Chem (2019) 62 : 10927 -10954
PubMed 31419130 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.21 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4298138 REPOTRECTINIB 4.0 1 8.90
CHEMBL3735401 1 8.70
CHEMBL1738797 ALECTINIB 4.0 1 8.68
CHEMBL3747406 1 7.68
CHEMBL4436406 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4298138 REPOTRECTINIB IC50 = 1.26 nM 8.90
CHEMBL3735401 IC50 = 2.0 nM 8.70
CHEMBL1738797 ALECTINIB IC50 = 2.07 nM 8.68
CHEMBL3747406 IC50 = 21.0 nM 7.68
CHEMBL4436406 IC50 = 77.0 nM 7.11