Reaction Details
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Epidermal growth factor receptor [696-1022,L858R]
Ligand
BDBM5447
Substrate
BDBM10852
Meas. Tech.
Fluorescence Binding Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Kd
2.4±.1 nM
Citation
Yun, CH; Mengwasser, KE; Toms, AV; Woo, MS; Greulich, H; Wong, KK; Meyerson, M; Eck, MJ The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A 105:2070-5 (2008) [PubMed] Article More Info.:
Target
Name:
Epidermal growth factor receptor [696-1022,L858R]
Synonyms:
EGF-R Tyrosine Kinase Mutant (L858R) | EGFR | EGFR_HUMAN | ERBB | ERBB1 | Epidermal growth factor receptor [696-1022,L858R] | HER1 | c-raf
Type:
Tyrosine-protein kinase
Mol. Mass.:
37296.75
Organism:
Homo sapiens (Human)
Description:
P00533[696-1022,L858R]
Residue:
327
Sequence:
GEAPNQALLRILKETEFKKIKVLGSGAFGTVYKGLWIPEGEKVKIPVAIKELREATSPKANKEILDEAYVMASVDNPHVCRLLGICLTSTVQLITQLMPFGCLLDYVREHKDNIGSQYLLNWCVQIAKGMNYLEDRRLVHRDLAARNVLVKTPQHVKITDFGRAKLLGAEEKEYHAEGGKVPIKWMALESILHRIYTHQSDVWSYGVTVWELMTFGSKPYDGIPASEISSILEKGERLPQPPICTIDVYMIMVKCWMIDADSRPKFRELIIEFSKMARDPQRYLVIQGDERMHLPSPTDSNFYRALMDEEDMDDVVDADEYLIPQQG
Inhibitor
Name:
BDBM5447
Synonyms:
CHEMBL939 | GEFITINIB | Iressa | N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-4-quinazolinamine | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine | US10106508, Gefitinib | US10507209, Compound Gefitinib | US9416123, Gefitinib | US9730934, Gefitinib | US9783524, Gefitinib | WO2022090481, Example gefitinib | ZD1839 | cid_123631
Type:
Small organic molecule
Emp. Form.:
C22H24ClFN4O3
Mol. Mass.:
446.902
SMILES:
COc1cc2ncnc(Nc3ccc(F)c(Cl)c3)c2cc1OCCCN1CCOCC1
Structure:
Substrate