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Assay Detail

CHEMBL3226845

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

Binding
Inhibition of JNK in human U87MG cells overexpressing EGFR V3 mutant assessed as inhibition of c-jun phosphorylation after 6 hrs by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U-87MG ATCC
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

c-Jun N-terminal kinase, JNK (CHEMBL2096667)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors
Song X, He Y, Koenig M, Shin Y, Noel R, Chen W, Ling YY, Feurstein D, Lin L, Ruiz CH, Cameron MD, Duckett DR, Kamenecka TM
Medchemcomm (2012) 3 : 238 -243
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 7.52 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3220497 1 7.64
CHEMBL458997 1 7.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3220497 EC50 = 23.0 nM 7.64
CHEMBL458997 EC50 = 41.0 nM 7.39