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Assay Detail

CHEMBL735050

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Binding
Inhibition against Mitogen-activated protein kinase p38 alpha
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrimidinylimidazole inhibitors of p38: cyclic N-1 imidazole substituents enhance p38 kinase inhibition and oral activity.
Adams JL, Boehm JC, Gallagher TF, Kassis S, Webb EF, Hall R, Sorenson M, Garigipati R, Griswold DE, Lee JC.
Bioorg Med Chem Lett (2001) 11 : 2867 -2870
PubMed 11597418 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.39 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97550 1 8.85
CHEMBL408876 1 8.82
CHEMBL318892 1 8.52
CHEMBL329049 1 8.07
CHEMBL420081 1 8.02
CHEMBL329080 1 7.92
CHEMBL319716 1 7.75
CHEMBL95692 SB-242235 1 7.72
CHEMBL275798 1 7.70
CHEMBL274064 SB-220025 1 7.70
CHEMBL419149 1 7.57
CHEMBL95931 1 7.48
CHEMBL97162 1 7.47
CHEMBL95521 1 7.38
CHEMBL95365 1 7.35
CHEMBL95797 1 7.28
CHEMBL330422 1 7.28
CHEMBL95502 1 7.24
CHEMBL327949 1 7.10
CHEMBL319988 1 7.08
CHEMBL95207 1 7.07
CHEMBL329447 1 7.00
CHEMBL97604 1 6.80
CHEMBL316917 1 6.77
CHEMBL95206 1 6.77
CHEMBL330196 1 6.64
CHEMBL97451 1 6.41
CHEMBL274863 1 6.32
CHEMBL329469 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97550 IC50 = 1.4 nM 8.85
CHEMBL408876 IC50 = 1.5 nM 8.82
CHEMBL318892 IC50 = 3.0 nM 8.52
CHEMBL329049 IC50 = 8.5 nM 8.07
CHEMBL420081 IC50 = 9.6 nM 8.02
CHEMBL329080 IC50 = 12.0 nM 7.92
CHEMBL319716 IC50 = 18.0 nM 7.75
CHEMBL95692 SB-242235 IC50 = 19.0 nM 7.72
CHEMBL275798 IC50 = 20.0 nM 7.70
CHEMBL274064 SB-220025 IC50 = 20.0 nM 7.70
CHEMBL419149 IC50 = 27.0 nM 7.57
CHEMBL95931 IC50 = 33.0 nM 7.48
CHEMBL97162 IC50 = 34.0 nM 7.47
CHEMBL95521 IC50 = 42.0 nM 7.38
CHEMBL95365 IC50 = 45.0 nM 7.35
CHEMBL95797 IC50 = 53.0 nM 7.28
CHEMBL330422 IC50 = 53.0 nM 7.28
CHEMBL95502 IC50 = 58.0 nM 7.24
CHEMBL327949 IC50 = 79.0 nM 7.10
CHEMBL319988 IC50 = 83.0 nM 7.08
CHEMBL95207 IC50 = 86.0 nM 7.07
CHEMBL329447 IC50 = 100.0 nM 7.00
CHEMBL97604 IC50 = 160.0 nM 6.80
CHEMBL316917 IC50 = 170.0 nM 6.77
CHEMBL95206 IC50 = 170.0 nM 6.77
CHEMBL330196 IC50 = 230.0 nM 6.64
CHEMBL97451 IC50 = 390.0 nM 6.41
CHEMBL274863 IC50 = 480.0 nM 6.32
CHEMBL329469 IC50 = 610.0 nM 6.21