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Assay Detail

CHEMBL731498

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

Binding
Inhibition of mitogen-activated protein kinase p38 alpha 2
27
Total Activities
27
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

1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors.
Dumas J, Hatoum-Mokdad H, Sibley R, Riedl B, Scott WJ, Monahan MK, Lowinger TB, Brennan C, Natero R, Turner T, Johnson JS, Schoenleber R, Bhargava A, Wilhelm SM, Housley TJ, Ranges GE, Shrikhande A.
Bioorg Med Chem Lett (2000) 10 : 2051 -2054
PubMed 10999468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.18 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64041 1 7.96
CHEMBL64040 1 7.89
CHEMBL10 SB-203580 1 7.70
CHEMBL62943 1 7.54
CHEMBL63071 1 7.52
CHEMBL418657 1 7.50
CHEMBL291835 1 7.48
CHEMBL64031 1 7.46
CHEMBL441793 1 7.41
CHEMBL65073 1 7.38
CHEMBL303798 1 7.37
CHEMBL62459 1 7.36
CHEMBL291826 1 7.28
CHEMBL41653 1 7.28
CHEMBL64192 1 7.25
CHEMBL304227 1 7.06
CHEMBL304256 1 6.98
CHEMBL64820 1 6.96
CHEMBL64432 1 6.92
CHEMBL62927 1 6.89
CHEMBL303562 1 6.89
CHEMBL61846 1 6.75
CHEMBL61735 1 6.60
CHEMBL61326 1 6.54
CHEMBL62859 1 6.49
CHEMBL293644 1 6.10
CHEMBL59876 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64041 IC50 = 11.0 nM 7.96
CHEMBL64040 IC50 = 13.0 nM 7.89
CHEMBL10 SB-203580 IC50 = 20.0 nM 7.70
CHEMBL62943 IC50 = 29.0 nM 7.54
CHEMBL63071 IC50 = 30.0 nM 7.52
CHEMBL418657 IC50 = 32.0 nM 7.50
CHEMBL291835 IC50 = 33.0 nM 7.48
CHEMBL64031 IC50 = 35.0 nM 7.46
CHEMBL441793 IC50 = 39.0 nM 7.41
CHEMBL65073 IC50 = 42.0 nM 7.38
CHEMBL303798 IC50 = 43.0 nM 7.37
CHEMBL62459 IC50 = 44.0 nM 7.36
CHEMBL291826 IC50 = 53.0 nM 7.28
CHEMBL41653 IC50 = 53.0 nM 7.28
CHEMBL64192 IC50 = 56.0 nM 7.25
CHEMBL304227 IC50 = 87.0 nM 7.06
CHEMBL304256 IC50 = 105.0 nM 6.98
CHEMBL64820 IC50 = 110.0 nM 6.96
CHEMBL64432 IC50 = 120.0 nM 6.92
CHEMBL62927 IC50 = 130.0 nM 6.89
CHEMBL303562 IC50 = 130.0 nM 6.89
CHEMBL61846 IC50 = 180.0 nM 6.75
CHEMBL61735 IC50 = 250.0 nM 6.60
CHEMBL61326 IC50 = 290.0 nM 6.54
CHEMBL62859 IC50 = 325.0 nM 6.49
CHEMBL293644 IC50 = 797.0 nM 6.10
CHEMBL59876 IC50 > 500.0 nM -