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Assay Detail

CHEMBL1798415

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Binding
Inhibition of p38alpha kinase
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Devadas B, Selness SR, Xing L, Madsen HM, Marrufo LD, Shieh H, Messing DM, Yang JZ, Morgan HM, Anderson GD, Webb EG, Zhang J, Devraj RV, Monahan JB.
Bioorg Med Chem Lett (2011) 21 : 3856 -3860
PubMed 21620699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.56 8.22
Ki 2 7.63 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1088751 PH-797804 2.0 1 8.54
CHEMBL1795684 1 8.22
CHEMBL1795686 1 7.96
CHEMBL1795683 1 7.92
CHEMBL1795682 1 7.57
CHEMBL1738710 2 7.54
CHEMBL1795681 1 7.52
CHEMBL1795685 1 7.42
CHEMBL1795687 1 7.22
CHEMBL1795688 1 6.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1088751 PH-797804 Ki = 2.9 nM 8.54
CHEMBL1795684 IC50 = 6.0 nM 8.22
CHEMBL1795686 IC50 = 11.0 nM 7.96
CHEMBL1795683 IC50 = 12.0 nM 7.92
CHEMBL1795682 IC50 = 27.0 nM 7.57
CHEMBL1738710 IC50 = 29.0 nM 7.54
CHEMBL1795681 IC50 = 30.0 nM 7.52
CHEMBL1795685 IC50 = 38.0 nM 7.42
CHEMBL1795687 IC50 = 60.0 nM 7.22
CHEMBL1738710 Ki = 193.0 nM 6.71
CHEMBL1795688 IC50 = 193.0 nM 6.71