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Assay Detail

CHEMBL820306

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

Binding
Inhibition of c-Jun N-terminal kinase 2-alpha 1
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ.
J Med Chem (1999) 42 : 2180 -2190
PubMed 10377223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.68 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69331 1 7.54
CHEMBL68572 1 7.01
CHEMBL69228 1 6.89
CHEMBL67874 1 6.85
CHEMBL67633 1 6.76
CHEMBL302728 1 6.75
CHEMBL63135 1 6.71
CHEMBL69764 1 6.68
CHEMBL446404 1 6.53
CHEMBL307435 1 6.52
CHEMBL67658 1 6.04
CHEMBL302805 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69331 IC50 = 29.0 nM 7.54
CHEMBL68572 IC50 = 98.0 nM 7.01
CHEMBL69228 IC50 = 130.0 nM 6.89
CHEMBL67874 IC50 = 140.0 nM 6.85
CHEMBL67633 IC50 = 175.0 nM 6.76
CHEMBL302728 IC50 = 180.0 nM 6.75
CHEMBL63135 IC50 = 195.0 nM 6.71
CHEMBL69764 IC50 = 210.0 nM 6.68
CHEMBL446404 IC50 = 295.0 nM 6.53
CHEMBL307435 IC50 = 300.0 nM 6.52
CHEMBL67658 IC50 = 910.0 nM 6.04
CHEMBL302805 IC50 = 1420.0 nM 5.85