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Assay Detail

CHEMBL832299

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

Binding
Inhibition of human recombinant Mitogen activated protein kinase p38 alpha activity using ATP[gamma-33P] and EGFR 21mer-peptide
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design of potent and selective 2-aminobenzimidazole-based p38alpha MAP kinase inhibitors with excellent in vivo efficacy.
de Dios A, Shih C, López de Uralde B, Sánchez C, del Prado M, Martín Cabrejas LM, Pleite S, Blanco-Urgoiti J, Lorite MJ, Nevill CR, Bonjouklian R, York J, Vieth M, Wang Y, Magnus N, Campbell RM, Anderson BD, McCann DJ, Giera DD, Lee PA, Schultz RM, Li LC, Johnson LM, Wolos JA.
J Med Chem (2005) 48 : 2270 -2273
PubMed 15801819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 8.05 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191113 1 8.57
CHEMBL192848 1 8.38
CHEMBL192850 1 8.37
CHEMBL363831 1 8.36
CHEMBL364925 1 8.35
CHEMBL191053 1 8.33
CHEMBL190514 1 8.32
CHEMBL364572 1 8.31
CHEMBL371145 1 8.26
CHEMBL192889 1 7.82
CHEMBL193055 1 7.80
CHEMBL193247 1 7.70
CHEMBL193305 1 7.68
CHEMBL363852 1 7.64
CHEMBL434957 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191113 IC50 = 2.7 nM 8.57
CHEMBL192848 IC50 = 4.2 nM 8.38
CHEMBL192850 IC50 = 4.3 nM 8.37
CHEMBL363831 IC50 = 4.4 nM 8.36
CHEMBL364925 IC50 = 4.5 nM 8.35
CHEMBL191053 IC50 = 4.7 nM 8.33
CHEMBL190514 IC50 = 4.8 nM 8.32
CHEMBL364572 IC50 = 4.9 nM 8.31
CHEMBL371145 IC50 = 5.5 nM 8.26
CHEMBL192889 IC50 = 15.3 nM 7.82
CHEMBL193055 IC50 = 15.9 nM 7.80
CHEMBL193247 IC50 = 19.9 nM 7.70
CHEMBL193305 IC50 = 20.7 nM 7.68
CHEMBL363852 IC50 = 22.8 nM 7.64
CHEMBL434957 IC50 = 125.0 nM 6.90