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Assay Detail

CHEMBL896194

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

Functional
Inhibition of P-EGFR expressed in A431 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Expert

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
Green N, Hu Y, Janz K, Li HQ, Kaila N, Guler S, Thomason J, Joseph-McCarthy D, Tam SY, Hotchandani R, Wu J, Huang A, Wang Q, Leung L, Pelker J, Marusic S, Hsu S, Telliez JB, Hall JP, Cuozzo JW, Lin LL.
J Med Chem (2007) 50 : 4728 -4745
PubMed 17715908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.05 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220037 1 7.52
CHEMBL397949 1 6.81
CHEMBL245212 1 6.30
CHEMBL436817 1 5.75
CHEMBL241990 1 5.68
CHEMBL395573 1 5.54
CHEMBL241988 1 5.48
CHEMBL242206 1 5.30
CHEMBL242426 1 -
CHEMBL242425 1 -
CHEMBL242207 1 -
CHEMBL425834 1 -
CHEMBL230232 1 -
CHEMBL395997 1 -
CHEMBL242208 1 -
CHEMBL241989 1 -
CHEMBL242852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220037 IC50 = 30.0 nM 7.52
CHEMBL397949 IC50 = 156.0 nM 6.81
CHEMBL245212 IC50 = 500.0 nM 6.30
CHEMBL436817 IC50 = 1800.0 nM 5.75
CHEMBL241990 IC50 = 2080.0 nM 5.68
CHEMBL395573 IC50 = 2900.0 nM 5.54
CHEMBL241988 IC50 = 3300.0 nM 5.48
CHEMBL242206 IC50 = 5000.0 nM 5.30
CHEMBL242426 IC50 - -
CHEMBL242425 IC50 - -
CHEMBL242207 IC50 - -
CHEMBL425834 IC50 > 5000.0 nM -
CHEMBL230232 IC50 > 5000.0 nM -
CHEMBL395997 IC50 - -
CHEMBL242208 IC50 > 20000.0 nM -
CHEMBL241989 IC50 > 20000.0 nM -
CHEMBL242852 IC50 > 5000.0 nM -