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Assay Detail

CHEMBL2183186

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

Binding
Binding affinity to wild type EGFR L861Q mutant by KINOMEscan kinase binding assay
1
Total Activities
1
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

Structural optimization and structure-activity relationships of N2-(4-(4-Methylpiperazin-1-yl)phenyl)-N8-phenyl-9H-purine-2,8-diamine derivatives, a new class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations.
Yang J, Wang LJ, Liu JJ, Zhong L, Zheng RL, Xu Y, Ji P, Zhang CH, Wang WJ, Lin XD, Li LL, Wei YQ, Yang SY.
J Med Chem (2012) 55 : 10685 -10699
PubMed 23116168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.22 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178352 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178352 Kd = 0.6 nM 9.22