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Assay Detail

CHEMBL998555

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Binding
Inhibition of GST-fused p38alpha expressed in Escherichia coli
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The identification of pyrazolo[1,5-a]pyridines as potent p38 kinase inhibitors.
Cheung M, Harris PA, Badiang JG, Peckham GE, Chamberlain SD, Alberti MJ, Jung DK, Harris SS, Bramson NH, Epperly AH, Stimpson SA, Peel MR.
Bioorg Med Chem Lett (2008) 18 : 5428 -5430
PubMed 18818075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.84 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520564 1 7.30
CHEMBL518890 1 7.16
CHEMBL485745 GW434756X 1 6.92
CHEMBL488183 1 6.85
CHEMBL487581 1 6.82
CHEMBL487780 1 6.82
CHEMBL501070 1 6.82
CHEMBL520563 1 6.82
CHEMBL518917 1 6.80
CHEMBL524530 1 6.80
CHEMBL488184 1 6.77
CHEMBL487781 1 6.70
CHEMBL509189 1 6.62
CHEMBL487577 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520564 IC50 = 50.0 nM 7.30
CHEMBL518890 IC50 = 70.0 nM 7.16
CHEMBL485745 GW434756X IC50 = 120.0 nM 6.92
CHEMBL488183 IC50 = 140.0 nM 6.85
CHEMBL487581 IC50 = 150.0 nM 6.82
CHEMBL487780 IC50 = 150.0 nM 6.82
CHEMBL501070 IC50 = 150.0 nM 6.82
CHEMBL520563 IC50 = 150.0 nM 6.82
CHEMBL518917 IC50 = 160.0 nM 6.80
CHEMBL524530 IC50 = 160.0 nM 6.80
CHEMBL488184 IC50 = 170.0 nM 6.77
CHEMBL487781 IC50 = 200.0 nM 6.70
CHEMBL509189 IC50 = 240.0 nM 6.62
CHEMBL487577 IC50 = 280.0 nM 6.55