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Assay Detail

CHEMBL934611

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

Binding
Inhibition of human recombinant p38alpha-mediated myelin basic protein phosphorylation
27
Total Activities
26
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Das J, Moquin RV, Pitt S, Zhang R, Shen DR, McIntyre KW, Gillooly K, Doweyko AM, Sack JS, Zhang H, Kiefer SE, Kish K, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.
Bioorg Med Chem Lett (2008) 18 : 2652 -2657
PubMed 18359226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.89 8.52
Ki 1 9.70 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL259922 2 9.70
CHEMBL410136 1 8.52
CHEMBL261021 1 8.52
CHEMBL409916 1 8.40
CHEMBL259007 1 8.40
CHEMBL260807 1 8.30
CHEMBL429863 1 8.22
CHEMBL260134 1 8.22
CHEMBL439267 1 8.15
CHEMBL258974 1 8.10
CHEMBL265710 1 8.10
CHEMBL259212 1 8.05
CHEMBL409329 1 8.05
CHEMBL410668 1 8.00
CHEMBL412265 1 7.96
CHEMBL258851 1 7.92
CHEMBL440406 1 7.89
CHEMBL407046 1 7.89
CHEMBL412281 1 7.85
CHEMBL261075 1 7.75
CHEMBL410667 1 7.68
CHEMBL409328 1 7.62
CHEMBL258653 1 7.17
CHEMBL260383 1 6.74
CHEMBL261235 1 6.62
CHEMBL407047 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL259922 Ki = 0.2 nM 9.70
CHEMBL261021 IC50 = 3.0 nM 8.52
CHEMBL410136 IC50 = 3.0 nM 8.52
CHEMBL259007 IC50 = 4.0 nM 8.40
CHEMBL409916 IC50 = 4.0 nM 8.40
CHEMBL259922 IC50 = 5.0 nM 8.30
CHEMBL260807 IC50 = 5.0 nM 8.30
CHEMBL429863 IC50 = 6.0 nM 8.22
CHEMBL260134 IC50 = 6.0 nM 8.22
CHEMBL439267 IC50 = 7.0 nM 8.15
CHEMBL258974 IC50 = 8.0 nM 8.10
CHEMBL265710 IC50 = 8.0 nM 8.10
CHEMBL259212 IC50 = 9.0 nM 8.05
CHEMBL409329 IC50 = 9.0 nM 8.05
CHEMBL410668 IC50 = 10.0 nM 8.00
CHEMBL412265 IC50 = 11.0 nM 7.96
CHEMBL258851 IC50 = 12.0 nM 7.92
CHEMBL440406 IC50 = 13.0 nM 7.89
CHEMBL407046 IC50 = 13.0 nM 7.89
CHEMBL412281 IC50 = 14.0 nM 7.85
CHEMBL261075 IC50 = 18.0 nM 7.75
CHEMBL410667 IC50 = 21.0 nM 7.68
CHEMBL409328 IC50 = 24.0 nM 7.62
CHEMBL258653 IC50 = 67.0 nM 7.17
CHEMBL260383 IC50 = 184.0 nM 6.74
CHEMBL261235 IC50 = 240.0 nM 6.62
CHEMBL407047 IC50 = 253.0 nM 6.60