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Assay Detail

CHEMBL2429341

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

Binding
Inhibition of human JNK2 assessed as inhibition of GST-tagged ATF2 (19 to 96) phosphorylation incubated for 10 mins prior to substrate addition measured after 30 mins by scintillation counting analysis in presence of [gamma-33P]-ATP
30
Total Activities
30
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 amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): kinase profiling guided optimization of a 1,2,3-benzotriazole lead.
Palmer WS, Alam M, Arzeno HB, Chang KC, Dunn JP, Goldstein DM, Gong L, Goyal B, Hermann JC, Hogg JH, Hsieh G, Jahangir A, Janson C, Jin S, Ursula Kammlott R, Kuglstatter A, Lukacs C, Michoud C, Niu L, Reuter DC, Shao A, Silva T, Trejo-Martin TA, Stein K, Tan YC, Tivitmahaisoon P, Tran P, Wagner P, Weller P, Wu SY.
Bioorg Med Chem Lett (2013) 23 : 1486 -1492
PubMed 23352510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 6.83 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2425635 1 7.68
CHEMBL2390974 1 7.62
CHEMBL2425634 1 7.57
CHEMBL2425630 1 7.55
CHEMBL2425629 1 7.33
CHEMBL2425631 1 7.29
CHEMBL2425633 1 7.24
CHEMBL2425632 1 7.19
CHEMBL2425628 1 7.18
CHEMBL2425653 1 7.12
CHEMBL2425639 1 7.10
CHEMBL2425655 1 7.01
CHEMBL2425654 1 6.96
CHEMBL2425640 1 6.86
CHEMBL2425636 1 6.82
CHEMBL2425652 1 6.77
CHEMBL2425649 1 6.75
CHEMBL2425641 1 6.75
CHEMBL2425638 1 6.71
CHEMBL2425651 1 6.64
CHEMBL2425637 1 6.61
CHEMBL2425648 1 6.60
CHEMBL2425645 1 6.46
CHEMBL2425646 1 6.44
CHEMBL2425656 1 6.41
CHEMBL2425650 1 6.40
CHEMBL2425644 1 6.19
CHEMBL2425642 1 6.14
CHEMBL2425647 1 5.92
CHEMBL2425643 1 5.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2425635 IC50 = 21.0 nM 7.68
CHEMBL2390974 IC50 = 24.0 nM 7.62
CHEMBL2425634 IC50 = 27.0 nM 7.57
CHEMBL2425630 IC50 = 28.0 nM 7.55
CHEMBL2425629 IC50 = 47.0 nM 7.33
CHEMBL2425631 IC50 = 51.0 nM 7.29
CHEMBL2425633 IC50 = 57.0 nM 7.24
CHEMBL2425632 IC50 = 64.0 nM 7.19
CHEMBL2425628 IC50 = 66.0 nM 7.18
CHEMBL2425653 IC50 = 76.0 nM 7.12
CHEMBL2425639 IC50 = 79.0 nM 7.10
CHEMBL2425655 IC50 = 97.0 nM 7.01
CHEMBL2425654 IC50 = 110.0 nM 6.96
CHEMBL2425640 IC50 = 139.0 nM 6.86
CHEMBL2425636 IC50 = 151.0 nM 6.82
CHEMBL2425652 IC50 = 170.0 nM 6.77
CHEMBL2425649 IC50 = 180.0 nM 6.75
CHEMBL2425641 IC50 = 178.0 nM 6.75
CHEMBL2425638 IC50 = 194.0 nM 6.71
CHEMBL2425651 IC50 = 230.0 nM 6.64
CHEMBL2425637 IC50 = 246.0 nM 6.61
CHEMBL2425648 IC50 = 250.0 nM 6.60
CHEMBL2425645 IC50 = 350.0 nM 6.46
CHEMBL2425646 IC50 = 360.0 nM 6.44
CHEMBL2425656 IC50 = 390.0 nM 6.41
CHEMBL2425650 IC50 = 400.0 nM 6.40
CHEMBL2425644 IC50 = 650.0 nM 6.19
CHEMBL2425642 IC50 = 720.0 nM 6.14
CHEMBL2425647 IC50 = 1200.0 nM 5.92
CHEMBL2425643 IC50 = 2900.0 nM 5.54