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Assay Detail

CHEMBL3748842

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Functional
Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type SMS-KCNR
Confidence 1 — Organism
Curated By Autocuration

Publication

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation.
Hatcher JM, Bahcall M, Choi HG, Gao Y, Sim T, George R, Jänne PA, Gray NS.
J Med Chem (2015) 58 : 9296 -9308
PubMed 26568289 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.73 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3746678 1 7.13
CHEMBL2403108 CERITINIB 4.0 1 7.04
CHEMBL3746522 1 6.89
CHEMBL3735401 1 6.88
CHEMBL601719 CRIZOTINIB 4.0 1 6.75
CHEMBL3397300 1 6.27
CHEMBL1738797 ALECTINIB 4.0 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3746678 EC50 = 74.0 nM 7.13
CHEMBL2403108 CERITINIB EC50 = 92.0 nM 7.04
CHEMBL3746522 EC50 = 129.0 nM 6.89
CHEMBL3735401 EC50 = 133.0 nM 6.88
CHEMBL601719 CRIZOTINIB EC50 = 179.0 nM 6.75
CHEMBL3397300 EC50 = 535.0 nM 6.27
CHEMBL1738797 ALECTINIB EC50 = 765.0 nM 6.12