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Assay Detail

CHEMBL929902

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

Binding
Inhibition of purified human p38alpha
9
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenyl amide p38 kinase inhibitors 1: Discovery and binding mode.
Angell RM, Bamborough P, Cleasby A, Cockerill SG, Jones KL, Mooney CJ, Somers DO, Walker AL.
Bioorg Med Chem Lett (2008) 18 : 318 -323
PubMed 18006306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.58 7.75
IC50 4 5.49 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10 SB-203580 1 7.75
CHEMBL270164 GW607117X 2 6.62
CHEMBL237127 2 6.40
CHEMBL273158 2 6.32
CHEMBL270608 2 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10 SB-203580 Ki = 18.0 nM 7.75
CHEMBL270164 GW607117X Ki = 240.0 nM 6.62
CHEMBL237127 Ki = 400.0 nM 6.40
CHEMBL273158 Ki = 480.0 nM 6.32
CHEMBL270164 GW607117X IC50 = 1500.0 nM 5.82
CHEMBL270608 Ki = 1600.0 nM 5.80
CHEMBL237127 IC50 = 2500.0 nM 5.60
CHEMBL273158 IC50 = 3000.0 nM 5.52
CHEMBL270608 IC50 = 10000.0 nM 5.00