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Assay Detail

CHEMBL2188499

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

Functional
Cytotoxicity against human FADU cells incubated for 72 hrs by MTT assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type FaDu
Confidence 1 — Organism
Curated By Autocuration

Target

FaDu (CHEMBL612250)
Type CELL-LINE
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
IC50 2 7.56 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178352 1 7.82
CHEMBL939 GEFITINIB 4.0 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178352 IC50 = 15.0 nM 7.82
CHEMBL939 GEFITINIB IC50 = 50.0 nM 7.30