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Assay Detail

CHEMBL734079

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Binding
Inhibition of Mitogen-activated protein kinase p38
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
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 8 8.51 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305178 1 9.96
CHEMBL303144 1 9.72
CHEMBL308939 1 9.12
CHEMBL424418 1 8.15
CHEMBL307980 1 8.12
CHEMBL10 SB-203580 1 7.41
CHEMBL67658 1 7.07
CHEMBL431583 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305178 IC50 = 0.11 nM 9.96
CHEMBL303144 IC50 = 0.19 nM 9.72
CHEMBL308939 IC50 = 0.75 nM 9.12
CHEMBL424418 IC50 = 7.0 nM 8.15
CHEMBL307980 IC50 = 7.6 nM 8.12
CHEMBL10 SB-203580 IC50 = 39.0 nM 7.41
CHEMBL67658 IC50 = 86.0 nM 7.07
CHEMBL431583 IC50 > 10000.0 nM -