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Assay Detail

CHEMBL4009503

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

Binding
Inhibition of EGFR delE746_A750 mutant in human HCC827 cells assessed as reduction in cell viability after 96 hrs by CellTiterGlo assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Indazole-Based Covalent Inhibitors To Target Drug-Resistant Epidermal Growth Factor Receptor.
Tomassi S, Lategahn J, Engel J, Keul M, Tumbrink HL, Ketzer J, Mühlenberg T, Baumann M, Schultz-Fademrecht C, Bauer S, Rauh D.
J Med Chem (2017) 60 : 2361 -2372
PubMed 28225269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.29 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4068763 1 7.66
CHEMBL3545308 ROCILETINIB 3.0 1 7.35
CHEMBL4071463 1 7.01
CHEMBL4079501 1 6.97
CHEMBL4060039 1 6.92
CHEMBL4088277 1 6.79
CHEMBL4098444 1 6.40
CHEMBL4097594 1 6.34
CHEMBL4080424 1 6.14
CHEMBL4103757 1 6.13
CHEMBL4060103 1 6.12
CHEMBL4082000 1 6.07
CHEMBL4089863 1 5.96
CHEMBL4079566 1 5.73
CHEMBL4061043 1 5.63
CHEMBL4098500 1 5.60
CHEMBL4074766 1 5.33
CHEMBL4090330 1 5.01
CHEMBL3353410 OSIMERTINIB 4.0 1 -
CHEMBL939 GEFITINIB 4.0 1 -
CHEMBL4065517 1 -
CHEMBL4069284 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4068763 EC50 = 22.0 nM 7.66
CHEMBL3545308 ROCILETINIB EC50 = 45.0 nM 7.35
CHEMBL4071463 EC50 = 97.0 nM 7.01
CHEMBL4079501 EC50 = 106.0 nM 6.97
CHEMBL4060039 EC50 = 121.0 nM 6.92
CHEMBL4088277 EC50 = 162.0 nM 6.79
CHEMBL4098444 EC50 = 400.0 nM 6.40
CHEMBL4097594 EC50 = 459.0 nM 6.34
CHEMBL4080424 EC50 = 730.0 nM 6.14
CHEMBL4103757 EC50 = 734.0 nM 6.13
CHEMBL4060103 EC50 = 765.0 nM 6.12
CHEMBL4082000 EC50 = 856.0 nM 6.07
CHEMBL4089863 EC50 = 1095.0 nM 5.96
CHEMBL4079566 EC50 = 1846.0 nM 5.73
CHEMBL4061043 EC50 = 2348.0 nM 5.63
CHEMBL4098500 EC50 = 2522.0 nM 5.60
CHEMBL4074766 EC50 = 4650.0 nM 5.33
CHEMBL4090330 EC50 = 9813.0 nM 5.01
CHEMBL3353410 OSIMERTINIB EC50 < 14.0 nM -
CHEMBL939 GEFITINIB EC50 < 14.0 nM -
CHEMBL4065517 EC50 > 30000.0 nM -
CHEMBL4069284 EC50 > 30000.0 nM -