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Assay Detail

CHEMBL731909

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

Binding
Displacement of [gamma-33P]-ATP binding from active recombinant murine FLAG-Mitogen-activated protein kinase p38 beta fusion protein (GST-ATF2)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mitogen-activated protein kinase 11 (CHEMBL4335)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Colletti SL, Frie JL, Dixon EC, Singh SB, Choi BK, Scapin G, Fitzgerald CE, Kumar S, Nichols EA, O'Keefe SJ, O'Neill EA, Porter G, Samuel K, Schmatz DM, Schwartz CD, Shoop WL, Thompson CM, Thompson JE, Wang R, Woods A, Zaller DM, Doherty JB.
J Med Chem (2003) 46 : 349 -352
PubMed 12540232 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.79 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL118651 1 7.55
CHEMBL325706 1 7.36
CHEMBL334215 1 7.20
CHEMBL118768 1 7.19
CHEMBL325854 1 7.11
CHEMBL118466 1 7.03
CHEMBL333243 1 6.95
CHEMBL118187 1 6.85
CHEMBL117109 1 6.82
CHEMBL334184 1 6.77
CHEMBL119675 1 6.45
CHEMBL434409 1 6.17
CHEMBL331842 1 6.05
CHEMBL118917 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL118651 IC50 = 28.0 nM 7.55
CHEMBL325706 IC50 = 44.0 nM 7.36
CHEMBL334215 IC50 = 63.0 nM 7.20
CHEMBL118768 IC50 = 64.0 nM 7.19
CHEMBL325854 IC50 = 78.0 nM 7.11
CHEMBL118466 IC50 = 94.0 nM 7.03
CHEMBL333243 IC50 = 112.0 nM 6.95
CHEMBL118187 IC50 = 140.0 nM 6.85
CHEMBL117109 IC50 = 153.0 nM 6.82
CHEMBL334184 IC50 = 171.0 nM 6.77
CHEMBL119675 IC50 = 355.0 nM 6.45
CHEMBL434409 IC50 = 670.0 nM 6.17
CHEMBL331842 IC50 = 890.0 nM 6.05
CHEMBL118917 IC50 = 2600.0 nM 5.58