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Assay Detail

CHEMBL4705469

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

Binding
Inhibition of N-terminal GST tagged wild-type human ALK cytoplasmic domain (1058-1620 amino acids) expressed Sf9 cells pre-incubated for 30 mins before addition of Ulight-CKKSRGDYMTMQIG substrate and measured after 90 mins by fluorescence based assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of CJ-2360 as a Potent and Orally Active Inhibitor of Anaplastic Lymphoma Kinase Capable of Achieving Complete Tumor Regression.
Chen J,Zhou Y,Dong X,Liu L,Bai L,McEachern D,Przybranowski S,Yang CY,Stuckey J,Li X,Wen B,Zhao T,Sun S,Sun D,Jiao L,Jing Y,Guo M,Yang D,Wang S
J Med Chem (2020) 63 : 13994 -14016
PubMed 33185101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 8.30 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790570 1 9.31
CHEMBL1738797 ALECTINIB 4.0 1 9.23
CHEMBL2403108 CERITINIB 4.0 1 9.21
CHEMBL4799217 1 9.21
CHEMBL4754012 1 9.00
CHEMBL4761644 1 8.89
CHEMBL4778565 1 8.89
CHEMBL4778853 1 8.82
CHEMBL4798441 1 8.80
CHEMBL4764107 1 8.68
CHEMBL4764610 1 8.66
CHEMBL4747806 1 8.66
CHEMBL4756825 1 8.60
CHEMBL4787453 1 8.60
CHEMBL4779307 1 8.59
CHEMBL4747053 1 8.59
CHEMBL4749002 1 8.43
CHEMBL4745824 1 8.41
CHEMBL4777376 1 8.40
CHEMBL4755960 1 8.32
CHEMBL4741360 1 8.32
CHEMBL4797642 1 8.31
CHEMBL4760756 1 8.28
CHEMBL4788534 1 8.28
CHEMBL4781855 1 8.27
CHEMBL4776403 1 8.26
CHEMBL4795124 1 8.24
CHEMBL4795844 1 8.24
CHEMBL4785020 1 8.18
CHEMBL4753546 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790570 IC50 = 0.49 nM 9.31
CHEMBL1738797 ALECTINIB IC50 = 0.59 nM 9.23
CHEMBL4799217 IC50 = 0.62 nM 9.21
CHEMBL2403108 CERITINIB IC50 = 0.61 nM 9.21
CHEMBL4754012 IC50 = 1.0 nM 9.00
CHEMBL4761644 IC50 = 1.3 nM 8.89
CHEMBL4778565 IC50 = 1.3 nM 8.89
CHEMBL4778853 IC50 = 1.5 nM 8.82
CHEMBL4798441 IC50 = 1.6 nM 8.80
CHEMBL4764107 IC50 = 2.1 nM 8.68
CHEMBL4764610 IC50 = 2.2 nM 8.66
CHEMBL4747806 IC50 = 2.2 nM 8.66
CHEMBL4756825 IC50 = 2.5 nM 8.60
CHEMBL4787453 IC50 = 2.5 nM 8.60
CHEMBL4747053 IC50 = 2.6 nM 8.59
CHEMBL4779307 IC50 = 2.6 nM 8.59
CHEMBL4749002 IC50 = 3.7 nM 8.43
CHEMBL4745824 IC50 = 3.9 nM 8.41
CHEMBL4777376 IC50 = 4.0 nM 8.40
CHEMBL4755960 IC50 = 4.8 nM 8.32
CHEMBL4741360 IC50 = 4.8 nM 8.32
CHEMBL4797642 IC50 = 4.9 nM 8.31
CHEMBL4788534 IC50 = 5.2 nM 8.28
CHEMBL4760756 IC50 = 5.3 nM 8.28
CHEMBL4781855 IC50 = 5.4 nM 8.27
CHEMBL4776403 IC50 = 5.5 nM 8.26
CHEMBL4795124 IC50 = 5.8 nM 8.24
CHEMBL4795844 IC50 = 5.8 nM 8.24
CHEMBL4785020 IC50 = 6.6 nM 8.18
CHEMBL4753546 IC50 = 8.2 nM 8.09
CHEMBL4781439 IC50 = 8.9 nM 8.05
CHEMBL4744052 IC50 = 12.7 nM 7.90
CHEMBL4780297 IC50 = 13.5 nM 7.87
CHEMBL4744640 IC50 = 16.5 nM 7.78
CHEMBL4787543 IC50 = 19.8 nM 7.70
CHEMBL4789803 IC50 = 20.6 nM 7.69
CHEMBL4741676 IC50 = 21.3 nM 7.67
CHEMBL4748562 IC50 = 28.6 nM 7.54
CHEMBL601719 CRIZOTINIB IC50 = 34.5 nM 7.46
CHEMBL4796970 IC50 = 40.5 nM 7.39
CHEMBL4743395 IC50 = 2503.0 nM 5.60
CHEMBL4757803 IC50 > 50000.0 nM -