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Assay Detail

CHEMBL2393733

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

Binding
Inhibition of JNK-mediated c-Jun activation in TNFalpha-induced human SW1353 cells preincubated for 30 mins prior to TNFalpha treatment measured after 20 mins
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SW1353
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

c-Jun N-terminal kinase, JNK (CHEMBL2096667)
Type PROTEIN FAMILY
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 14 6.29 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2392831 1 6.98
CHEMBL2392827 1 6.70
CHEMBL2392840 1 6.66
CHEMBL2392833 1 6.62
CHEMBL2392832 1 6.54
CHEMBL2392839 1 6.38
CHEMBL2392838 1 6.19
CHEMBL2392834 1 6.16
CHEMBL2392825 1 6.15
CHEMBL2392828 1 6.09
CHEMBL2390974 1 6.00
CHEMBL2392837 1 5.89
CHEMBL2392835 1 5.89
CHEMBL2392836 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2392831 IC50 = 104.0 nM 6.98
CHEMBL2392827 IC50 = 200.0 nM 6.70
CHEMBL2392840 IC50 = 220.0 nM 6.66
CHEMBL2392833 IC50 = 240.0 nM 6.62
CHEMBL2392832 IC50 = 290.0 nM 6.54
CHEMBL2392839 IC50 = 420.0 nM 6.38
CHEMBL2392838 IC50 = 650.0 nM 6.19
CHEMBL2392834 IC50 = 700.0 nM 6.16
CHEMBL2392825 IC50 = 710.0 nM 6.15
CHEMBL2392828 IC50 = 820.0 nM 6.09
CHEMBL2390974 IC50 = 1000.0 nM 6.00
CHEMBL2392837 IC50 = 1300.0 nM 5.89
CHEMBL2392835 IC50 = 1300.0 nM 5.89
CHEMBL2392836 IC50 = 1700.0 nM 5.77