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Assay Detail

CHEMBL733334

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

Binding
In vivo inhibition of murine Mitogen-activated protein kinase p38 alpha activity, GST-ATF-2 as substrate in the presence of 120 uM ATP
17
Total Activities
17
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 (CHEMBL2336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Revesz L, Di Padova FE, Buhl T, Feifel R, Gram H, Hiestand P, Manning U, Wolf R, Zimmerlin AG.
Bioorg Med Chem Lett (2002) 12 : 2109 -2112
PubMed 12127515 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.54 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304523 1 8.40
CHEMBL306667 1 8.40
CHEMBL66600 1 8.30
CHEMBL63983 1 7.80
CHEMBL63442 1 7.05
CHEMBL65541 1 6.85
CHEMBL291427 1 6.68
CHEMBL307336 1 6.40
CHEMBL304416 1 6.33
CHEMBL66601 1 6.17
CHEMBL66802 1 6.10
CHEMBL294052 1 6.10
CHEMBL63135 1 6.00
CHEMBL295787 1 5.89
CHEMBL291834 1 5.68
CHEMBL305797 1 5.00
CHEMBL419069 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304523 IC50 = 4.0 nM 8.40
CHEMBL306667 IC50 = 4.0 nM 8.40
CHEMBL66600 IC50 = 5.0 nM 8.30
CHEMBL63983 IC50 = 16.0 nM 7.80
CHEMBL63442 IC50 = 90.0 nM 7.05
CHEMBL65541 IC50 = 140.0 nM 6.85
CHEMBL291427 IC50 = 210.0 nM 6.68
CHEMBL307336 IC50 = 400.0 nM 6.40
CHEMBL304416 IC50 = 470.0 nM 6.33
CHEMBL66601 IC50 = 670.0 nM 6.17
CHEMBL66802 IC50 = 800.0 nM 6.10
CHEMBL294052 IC50 = 800.0 nM 6.10
CHEMBL63135 IC50 = 1000.0 nM 6.00
CHEMBL295787 IC50 = 1300.0 nM 5.89
CHEMBL291834 IC50 = 2100.0 nM 5.68
CHEMBL305797 IC50 = 10000.0 nM 5.00
CHEMBL419069 IC50 = 100000.0 nM 4.00