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Assay Detail

CHEMBL2383983

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

Functional
Cytotoxicity against gefitinib-resistant human NCI-H1975 cells harboring EGFR L858R/T90M double mutant assessed as growth inhibition after 72 hrs by MTT assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1975
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1975 (CHEMBL614348)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel hybrids of (phenylsulfonyl)furoxan and anilinopyrimidine as potent and selective epidermal growth factor receptor inhibitors for intervention of non-small-cell lung cancer.
Han C, Huang Z, Zheng C, Wan L, Zhang L, Peng S, Ding K, Ding K, Ji H, Tian J, Zhang Y.
J Med Chem (2013) 56 : 4738 -4748
PubMed 23668441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.43 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2381511 1 7.54
CHEMBL2381509 1 7.37
CHEMBL1229592 1 7.34
CHEMBL2381506 1 7.20
CHEMBL2381508 1 7.16
CHEMBL2381505 1 6.61
CHEMBL2381516 1 6.51
CHEMBL2381507 1 6.40
CHEMBL2381510 1 6.33
CHEMBL2381504 1 6.07
CHEMBL2381515 1 5.99
CHEMBL2381513 1 5.82
CHEMBL2381514 1 5.70
CHEMBL2381512 1 5.23
CHEMBL939 GEFITINIB 4.0 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2381511 IC50 = 29.0 nM 7.54
CHEMBL2381509 IC50 = 43.0 nM 7.37
CHEMBL1229592 IC50 = 46.0 nM 7.34
CHEMBL2381506 IC50 = 63.0 nM 7.20
CHEMBL2381508 IC50 = 69.0 nM 7.16
CHEMBL2381505 IC50 = 245.0 nM 6.61
CHEMBL2381516 IC50 = 311.0 nM 6.51
CHEMBL2381507 IC50 = 396.0 nM 6.40
CHEMBL2381510 IC50 = 471.0 nM 6.33
CHEMBL2381504 IC50 = 855.0 nM 6.07
CHEMBL2381515 IC50 = 1027.0 nM 5.99
CHEMBL2381513 IC50 = 1514.0 nM 5.82
CHEMBL2381514 IC50 = 2017.0 nM 5.70
CHEMBL2381512 IC50 = 5931.0 nM 5.23
CHEMBL939 GEFITINIB IC50 = 6917.0 nM 5.16