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Assay Detail

CHEMBL900179

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

Binding
Inhibition of p38 MAPK activity assessed as EGFR phosphorylation
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis, crystal structure, and activity of pyrazole-based inhibitors of p38 kinase.
Graneto MJ, Kurumbail RG, Vazquez ML, Shieh HS, Pawlitz JL, Williams JM, Stallings WC, Geng L, Naraian AS, Koszyk FJ, Stealey MA, Xu XD, Weier RM, Hanson GJ, Mourey RJ, Compton RP, Mnich SJ, Anderson GD, Monahan JB, Devraj R.
J Med Chem (2007) 50 : 5712 -5719
PubMed 17948975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.18 7.92
Kd 1 7.82 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237817 1 7.92
CHEMBL279416 VK-19911 1 7.82
CHEMBL396320 1 7.80
CHEMBL274064 SB-220025 1 7.72
CHEMBL236559 1 7.40
CHEMBL237606 1 7.30
CHEMBL237602 1 7.21
CHEMBL391277 1 6.96
CHEMBL236356 1 6.89
CHEMBL236557 1 6.89
CHEMBL400030 1 6.72
CHEMBL236558 1 6.72
CHEMBL400029 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237817 IC50 = 12.0 nM 7.92
CHEMBL279416 VK-19911 Kd = 15.0 nM 7.82
CHEMBL396320 IC50 = 16.0 nM 7.80
CHEMBL274064 SB-220025 IC50 = 19.0 nM 7.72
CHEMBL236559 IC50 = 40.0 nM 7.40
CHEMBL237606 IC50 = 50.0 nM 7.30
CHEMBL237602 IC50 = 62.0 nM 7.21
CHEMBL391277 IC50 = 110.0 nM 6.96
CHEMBL236356 IC50 = 130.0 nM 6.89
CHEMBL236557 IC50 = 130.0 nM 6.89
CHEMBL400030 IC50 = 190.0 nM 6.72
CHEMBL236558 IC50 = 190.0 nM 6.72
CHEMBL400029 IC50 = 260.0 nM 6.58