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Assay Detail

CHEMBL3737962

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

Binding
Inhibition of EGFR T790M/del (746 to 750) deletion mutant phosphorylation in erlotinib-resistant human PC9 cells preincubated for 1 hr followed by stimulation with EGF for 8 mins by electrochemiluminescent immunoassay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.
Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP.
J Med Chem (2015) 58 : 8877 -8895
PubMed 26455919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.33 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3736121 1 7.57
CHEMBL3734988 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3736121 IC50 = 27.0 nM 7.57
CHEMBL3734988 IC50 = 81.0 nM 7.09