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Assay Detail

CHEMBL4382304

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

Binding
Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

EML4-ALK (CHEMBL3883330)
Type CHIMERIC PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent dual ALK and EGFR T790M inhibitor.
Jang J, Son JB, To C, Bahcall M, Kim SY, Kang SY, Mushajiang M, Lee Y, Jänne PA, Choi HG, Gray NS.
Eur J Med Chem (2017) 136 : 497 -510
PubMed 28528303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.73 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4473365 1 8.15
CHEMBL4449391 1 8.10
CHEMBL4448107 1 7.70
CHEMBL4467561 1 7.68
CHEMBL2403108 CERITINIB 4.0 1 7.58
CHEMBL4565984 1 7.41
CHEMBL4531697 1 7.06
CHEMBL4540442 1 6.66
CHEMBL4520341 1 6.02
CHEMBL3353410 OSIMERTINIB 4.0 1 5.76
CHEMBL4516287 1 5.66
CHEMBL4581316 1 5.63
CHEMBL4558227 1 5.60
CHEMBL1229592 1 5.20
CHEMBL4465103 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4473365 EC50 = 7.0 nM 8.15
CHEMBL4449391 EC50 = 8.0 nM 8.10
CHEMBL4448107 EC50 = 20.0 nM 7.70
CHEMBL4467561 EC50 = 21.0 nM 7.68
CHEMBL2403108 CERITINIB EC50 = 26.0 nM 7.58
CHEMBL4565984 EC50 = 39.0 nM 7.41
CHEMBL4531697 EC50 = 87.0 nM 7.06
CHEMBL4540442 EC50 = 217.0 nM 6.66
CHEMBL4520341 EC50 = 961.0 nM 6.02
CHEMBL3353410 OSIMERTINIB EC50 = 1748.0 nM 5.76
CHEMBL4516287 EC50 = 2182.0 nM 5.66
CHEMBL4581316 EC50 = 2357.0 nM 5.63
CHEMBL4558227 EC50 = 2506.0 nM 5.60
CHEMBL1229592 EC50 = 6258.0 nM 5.20
CHEMBL4465103 EC50 > 5000.0 nM -