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Assay Detail

CHEMBL5342465

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

Binding
Inhibition of EGFR (unknown origin) in presence of ATP by Z-LYTE based FRET assay
12
Total Activities
12
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

Synthesis and Development of Highly Selective Pyrrolo[2,3-<i>d</i>]pyrimidine CSF1R Inhibitors Targeting the Autoinhibited Form.
Aarhus TI, Bjørnstad F, Wolowczyk C, Larsen KU, Rognstad L, Leithaug T, Unger A, Habenberger P, Wolf A, Bjørkøy G, Pridans C, Eickhoff J, Klebl B, Hoff BH, Sundby E.
J Med Chem (2023) 66 : 6959 -6980
PubMed 37191268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.89 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5418087 1 7.52
CHEMBL5439126 1 7.28
CHEMBL5411617 1 7.01
CHEMBL5406924 1 6.93
CHEMBL5425883 1 6.93
CHEMBL5404033 1 6.90
CHEMBL5436321 1 6.38
CHEMBL5397490 1 6.13
CHEMBL5398778 1 -
CHEMBL5420485 1 -
CHEMBL5397426 1 -
CHEMBL5415647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5418087 IC50 = 30.0 nM 7.52
CHEMBL5439126 IC50 = 53.0 nM 7.28
CHEMBL5411617 IC50 = 98.0 nM 7.01
CHEMBL5406924 IC50 = 118.0 nM 6.93
CHEMBL5425883 IC50 = 117.0 nM 6.93
CHEMBL5404033 IC50 = 127.0 nM 6.90
CHEMBL5436321 IC50 = 413.0 nM 6.38
CHEMBL5397490 IC50 = 745.0 nM 6.13
CHEMBL5398778 IC50 > 1000.0 nM -
CHEMBL5420485 IC50 > 1000.0 nM -
CHEMBL5397426 IC50 > 1000.0 nM -
CHEMBL5415647 IC50 > 1000.0 nM -