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Assay Detail

CHEMBL2393734

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

Binding
Inhibition of human JNK2alpha2 using GST-tagged ATF2 as substrate preincubated for 10 mins prior to substrate addition measured after 30 mins by microplate scintillation counting analysis
17
Total Activities
17
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

Mitogen-activated protein kinase 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties.
Gong L, Han X, Silva T, Tan YC, Goyal B, Tivitmahaisoon P, Trejo A, Palmer W, Hogg H, Jahagir A, Alam M, Wagner P, Stein K, Filonova L, Loe B, Makra F, Rotstein D, Rapatova L, Dunn J, Zuo F, Dal Porto J, Wong B, Jin S, Chang A, Tran P, Hsieh G, Niu L, Shao A, Reuter D, Hermann J, Kuglstatter A, Goldstein D.
Bioorg Med Chem Lett (2013) 23 : 3565 -3569
PubMed 23664880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.31 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2392840 1 7.92
CHEMBL2392832 1 7.77
CHEMBL2392833 1 7.70
CHEMBL2390974 1 7.62
CHEMBL2392825 1 7.62
CHEMBL2392836 1 7.57
CHEMBL2392838 1 7.48
CHEMBL2392831 1 7.46
CHEMBL2392827 1 7.44
CHEMBL2392837 1 7.40
CHEMBL2392834 1 7.31
CHEMBL2392835 1 7.18
CHEMBL2392828 1 7.17
CHEMBL2392839 1 7.07
CHEMBL2392826 1 6.75
CHEMBL2392830 1 6.55
CHEMBL2392829 1 6.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2392840 IC50 = 12.0 nM 7.92
CHEMBL2392832 IC50 = 17.0 nM 7.77
CHEMBL2392833 IC50 = 20.0 nM 7.70
CHEMBL2390974 IC50 = 24.0 nM 7.62
CHEMBL2392825 IC50 = 24.0 nM 7.62
CHEMBL2392836 IC50 = 27.0 nM 7.57
CHEMBL2392838 IC50 = 33.0 nM 7.48
CHEMBL2392831 IC50 = 35.0 nM 7.46
CHEMBL2392827 IC50 = 36.0 nM 7.44
CHEMBL2392837 IC50 = 40.0 nM 7.40
CHEMBL2392834 IC50 = 49.0 nM 7.31
CHEMBL2392835 IC50 = 66.0 nM 7.18
CHEMBL2392828 IC50 = 68.0 nM 7.17
CHEMBL2392839 IC50 = 86.0 nM 7.07
CHEMBL2392826 IC50 = 180.0 nM 6.75
CHEMBL2392830 IC50 = 280.0 nM 6.55
CHEMBL2392829 IC50 = 650.0 nM 6.19