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Assay Detail

CHEMBL818992

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

Functional
Inhibition of Tumor necrosis factor alpha release from LPS-induced THP-1 cells by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

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 12 7.27 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325706 1 8.22
CHEMBL334215 1 8.00
CHEMBL325854 1 7.85
CHEMBL118651 1 7.70
CHEMBL118466 1 7.66
CHEMBL118187 1 7.17
CHEMBL117109 1 7.16
CHEMBL334184 1 6.79
CHEMBL118768 1 6.79
CHEMBL332391 1 6.77
CHEMBL434409 1 6.75
CHEMBL118917 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325706 IC50 = 6.0 nM 8.22
CHEMBL334215 IC50 = 10.0 nM 8.00
CHEMBL325854 IC50 = 14.0 nM 7.85
CHEMBL118651 IC50 = 20.0 nM 7.70
CHEMBL118466 IC50 = 22.0 nM 7.66
CHEMBL118187 IC50 = 68.0 nM 7.17
CHEMBL117109 IC50 = 70.0 nM 7.16
CHEMBL334184 IC50 = 161.0 nM 6.79
CHEMBL118768 IC50 = 161.0 nM 6.79
CHEMBL332391 IC50 = 170.0 nM 6.77
CHEMBL434409 IC50 = 180.0 nM 6.75
CHEMBL118917 IC50 = 400.0 nM 6.40