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Assay Detail

CHEMBL1825474

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

Binding
Inhibition of human p38alpha using biotinylated ATF2 substrate by FRET assay
19
Total Activities
19
Compounds Tested
1
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

Indolin-2-one p38α inhibitors II: Lead optimisation.
Eastwood P, González J, Gómez E, Caturla F, Balagué C, Orellana A, Domínguez M.
Bioorg Med Chem Lett (2011) 21 : 5270 -5273
PubMed 21813275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 8.44 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1825149 1 10.10
CHEMBL1825148 1 10.05
CHEMBL1825157 1 9.10
CHEMBL1825154 1 9.05
CHEMBL1825146 1 9.00
CHEMBL1825151 1 8.85
CHEMBL1825152 1 8.85
CHEMBL1825147 1 8.78
CHEMBL1825158 1 8.74
CHEMBL1825153 1 8.74
CHEMBL1825160 1 8.64
CHEMBL1825145 1 8.28
CHEMBL1825156 1 8.25
CHEMBL1825150 1 8.17
CHEMBL1825155 1 8.13
CHEMBL1825159 1 7.89
CHEMBL1825161 1 7.21
CHEMBL1825162 1 7.14
CHEMBL1825144 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1825149 IC50 = 0.08 nM 10.10
CHEMBL1825148 IC50 = 0.09 nM 10.05
CHEMBL1825157 IC50 = 0.8 nM 9.10
CHEMBL1825154 IC50 = 0.9 nM 9.05
CHEMBL1825146 IC50 = 1.0 nM 9.00
CHEMBL1825151 IC50 = 1.4 nM 8.85
CHEMBL1825152 IC50 = 1.4 nM 8.85
CHEMBL1825147 IC50 = 1.65 nM 8.78
CHEMBL1825158 IC50 = 1.8 nM 8.74
CHEMBL1825153 IC50 = 1.8 nM 8.74
CHEMBL1825160 IC50 = 2.3 nM 8.64
CHEMBL1825145 IC50 = 5.2 nM 8.28
CHEMBL1825156 IC50 = 5.6 nM 8.25
CHEMBL1825150 IC50 = 6.7 nM 8.17
CHEMBL1825155 IC50 = 7.4 nM 8.13
CHEMBL1825159 IC50 = 13.0 nM 7.89
CHEMBL1825161 IC50 = 62.0 nM 7.21
CHEMBL1825162 IC50 = 72.0 nM 7.14
CHEMBL1825144 IC50 = 4570.0 nM 5.34