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Assay Detail

CHEMBL1112959

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Binding
Inhibition of mouse p38alpha after 3 hrs by SPA method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 14 (CHEMBL2336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.
Tynebor RM, Chen MH, Natarajan SR, O'Neill EA, Thompson JE, Fitzgerald CE, O'Keefe SJ, Doherty JB.
Bioorg Med Chem Lett (2010) 20 : 2765 -2769
PubMed 20378346 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 8.28 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219804 1 9.22
CHEMBL1098525 1 8.82
CHEMBL1096830 1 8.82
CHEMBL94417 1 8.59
CHEMBL1098822 1 8.28
CHEMBL1098551 1 8.17
CHEMBL1098524 1 8.15
CHEMBL1098552 1 8.06
CHEMBL1096192 1 7.89
CHEMBL1098546 1 7.85
CHEMBL1098554 1 7.83
CHEMBL1098797 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219804 IC50 = 0.6 nM 9.22
CHEMBL1098525 IC50 = 1.5 nM 8.82
CHEMBL1096830 IC50 = 1.5 nM 8.82
CHEMBL94417 IC50 = 2.6 nM 8.59
CHEMBL1098822 IC50 = 5.3 nM 8.28
CHEMBL1098551 IC50 = 6.8 nM 8.17
CHEMBL1098524 IC50 = 7.1 nM 8.15
CHEMBL1098552 IC50 = 8.8 nM 8.06
CHEMBL1096192 IC50 = 13.0 nM 7.89
CHEMBL1098546 IC50 = 14.0 nM 7.85
CHEMBL1098554 IC50 = 14.7 nM 7.83
CHEMBL1098797 IC50 = 20.0 nM 7.70