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Assay Detail

CHEMBL733338

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

Binding
Tested in vitro for filter plate binding versus gamma-[33P]ATP in active recombinant murine FLAG-P38 alpha fusion protein (GST-Activating transcription factor-2).
18
Total Activities
18
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 14 (CHEMBL2336)
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 18 7.25 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334215 1 8.10
CHEMBL325854 1 8.10
CHEMBL118651 1 8.05
CHEMBL118466 1 7.85
CHEMBL118768 1 7.85
CHEMBL325706 1 7.66
CHEMBL119385 NEFLAMAPIMOD 2.0 1 7.66
CHEMBL333243 1 7.66
CHEMBL118187 1 7.58
CHEMBL434409 1 7.38
CHEMBL117109 1 7.31
CHEMBL334184 1 7.12
CHEMBL119675 1 6.77
CHEMBL118917 1 6.68
CHEMBL331842 1 6.57
CHEMBL119406 1 6.46
CHEMBL332666 1 6.00
CHEMBL117228 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334215 IC50 = 8.0 nM 8.10
CHEMBL325854 IC50 = 8.0 nM 8.10
CHEMBL118651 IC50 = 9.0 nM 8.05
CHEMBL118466 IC50 = 14.0 nM 7.85
CHEMBL118768 IC50 = 14.0 nM 7.85
CHEMBL325706 IC50 = 22.0 nM 7.66
CHEMBL119385 NEFLAMAPIMOD IC50 = 22.0 nM 7.66
CHEMBL333243 IC50 = 22.0 nM 7.66
CHEMBL118187 IC50 = 26.0 nM 7.58
CHEMBL434409 IC50 = 42.0 nM 7.38
CHEMBL117109 IC50 = 49.0 nM 7.31
CHEMBL334184 IC50 = 76.0 nM 7.12
CHEMBL119675 IC50 = 171.0 nM 6.77
CHEMBL118917 IC50 = 208.0 nM 6.68
CHEMBL331842 IC50 = 270.0 nM 6.57
CHEMBL119406 IC50 = 344.0 nM 6.46
CHEMBL332666 IC50 = 1000.0 nM 6.00
CHEMBL117228 IC50 = 2000.0 nM 5.70