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Assay Detail

CHEMBL3762136

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

Binding
Inhibition of wild type EGFR (unknown origin)
6
Total Activities
6
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

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.
Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP.
Bioorg Med Chem Lett (2016) 26 : 534 -539
PubMed 26639762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.94 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 10.00
CHEMBL3758502 1 9.22
CHEMBL3759096 1 8.96
CHEMBL3758602 1 8.82
CHEMBL3353410 OSIMERTINIB 4.0 1 8.46
CHEMBL3758739 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB Ki = 0.1 nM 10.00
CHEMBL3758502 Ki = 0.6 nM 9.22
CHEMBL3759096 Ki = 1.1 nM 8.96
CHEMBL3758602 Ki = 1.5 nM 8.82
CHEMBL3353410 OSIMERTINIB Ki = 3.5 nM 8.46
CHEMBL3758739 Ki = 6.5 nM 8.19