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Assay Detail

CHEMBL3857034

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

Binding
Inhibition of recombinant human GST-tagged EGFR cytoplasmic domain (668 to 1210 residues) expressed in baculovirus by Z'-LYTE assay
31
Total Activities
31
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

Chiral 6-aryl-furo[2,3-d]pyrimidin-4-amines as EGFR inhibitors.
Han J, Kaspersen SJ, Nervik S, Nørsett KG, Sundby E, Hoff BH.
Eur J Med Chem (2016) 119 : 278 -299
PubMed 27235841 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.12 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3901622 1 9.40
CHEMBL553 ERLOTINIB 4.0 1 9.40
CHEMBL3891846 1 9.22
CHEMBL3960853 1 8.96
CHEMBL3919609 1 8.82
CHEMBL3928512 1 8.70
CHEMBL3961553 1 8.70
CHEMBL3952157 1 8.57
CHEMBL3892567 1 8.41
CHEMBL3961961 1 8.40
CHEMBL3947406 1 8.40
CHEMBL3956112 1 8.34
CHEMBL3933539 1 8.28
CHEMBL3946396 1 8.15
CHEMBL3908303 1 7.96
CHEMBL3967219 1 7.89
CHEMBL3943438 1 7.85
CHEMBL3934461 1 7.66
CHEMBL3972981 1 7.66
CHEMBL3925584 1 7.62
CHEMBL3953210 1 7.62
CHEMBL3973601 1 7.57
CHEMBL3952877 1 7.55
CHEMBL3929584 1 7.54
CHEMBL3975699 1 7.36
CHEMBL3937527 1 7.25
CHEMBL3939429 1 7.13
CHEMBL3981621 1 7.03
CHEMBL3944121 1 -
CHEMBL3962640 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3901622 IC50 = 0.4 nM 9.40
CHEMBL553 ERLOTINIB IC50 = 0.4 nM 9.40
CHEMBL3891846 IC50 = 0.6 nM 9.22
CHEMBL3960853 IC50 = 1.1 nM 8.96
CHEMBL3919609 IC50 = 1.5 nM 8.82
CHEMBL3928512 IC50 = 2.0 nM 8.70
CHEMBL3961553 IC50 = 2.0 nM 8.70
CHEMBL3952157 IC50 = 2.7 nM 8.57
CHEMBL3892567 IC50 = 3.9 nM 8.41
CHEMBL3961961 IC50 = 4.0 nM 8.40
CHEMBL3947406 IC50 = 4.0 nM 8.40
CHEMBL3956112 IC50 = 4.6 nM 8.34
CHEMBL3933539 IC50 = 5.3 nM 8.28
CHEMBL3946396 IC50 = 7.0 nM 8.15
CHEMBL3908303 IC50 = 11.0 nM 7.96
CHEMBL3967219 IC50 = 13.0 nM 7.89
CHEMBL3943438 IC50 = 14.0 nM 7.85
CHEMBL3934461 IC50 = 22.0 nM 7.66
CHEMBL3972981 IC50 = 22.0 nM 7.66
CHEMBL3925584 IC50 = 24.0 nM 7.62
CHEMBL3953210 IC50 = 24.0 nM 7.62
CHEMBL3973601 IC50 = 27.0 nM 7.57
CHEMBL3952877 IC50 = 28.0 nM 7.55
CHEMBL3929584 IC50 = 29.0 nM 7.54
CHEMBL3975699 IC50 = 44.0 nM 7.36
CHEMBL3937527 IC50 = 56.0 nM 7.25
CHEMBL3939429 IC50 = 74.0 nM 7.13
CHEMBL3981621 IC50 = 93.0 nM 7.03
CHEMBL3944121 IC50 > 100.0 nM -
CHEMBL3962640 IC50 > 100.0 nM -
CHEMBL3935149 IC50 > 1000.0 nM -