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Assay Detail

CHEMBL2067582

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

Binding
Inhibition of ALK tyrosine phosphorylation in human Karpas-299 cells after 2 hrs in presence of mouse plasma
14
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Plasma
Cell Type KARPAS-299
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

ALK tyrosine kinase receptor (CHEMBL4247)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Haltiwanger RC, Wells-Knecht K, Ott GR, Ghose AK, Ator MA, Ruggeri B, Dorsey BD.
J Med Chem (2012) 55 : 4580 -4593
PubMed 22564207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.23 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064722 2 7.70
CHEMBL2064666 1 7.70
CHEMBL2064663 1 7.52
CHEMBL1642258 1 7.52
CHEMBL2064667 2 7.40
CHEMBL2064664 2 7.40
CHEMBL2042829 1 7.35
CHEMBL2064662 1 7.19
CHEMBL2064665 1 6.92
CHEMBL2064723 2 6.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064722 IC50 = 20.0 nM 7.70
CHEMBL2064666 IC50 = 20.0 nM 7.70
CHEMBL2064663 IC50 = 30.0 nM 7.52
CHEMBL1642258 IC50 = 30.0 nM 7.52
CHEMBL2064667 IC50 = 40.0 nM 7.40
CHEMBL2064664 IC50 = 40.0 nM 7.40
CHEMBL2042829 IC50 = 45.0 nM 7.35
CHEMBL2064664 IC50 = 65.0 nM 7.19
CHEMBL2064662 IC50 = 65.0 nM 7.19
CHEMBL2064667 IC50 = 120.0 nM 6.92
CHEMBL2064665 IC50 = 120.0 nM 6.92
CHEMBL2064723 IC50 = 150.0 nM 6.82
CHEMBL2064723 IC50 = 150.0 nM 6.82
CHEMBL2064722 IC50 = 200.0 nM 6.70