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Assay Detail

CHEMBL880234

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

Binding
Inhibitory activity against p38 at a concentration of 1.0 uM
6
Total Activities
6
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

The neuroprotective action of JNK3 inhibitors based on the 6,7-dihydro-5H-pyrrolo[1,2-a]imidazole scaffold.
Graczyk PP, Khan A, Bhatia GS, Palmer V, Medland D, Numata H, Oinuma H, Catchick J, Dunne A, Ellis M, Smales C, Whitfield J, Neame SJ, Shah B, Wilton D, Morgan L, Patel T, Chung R, Desmond H, Staddon JM, Sato N, Inoue A.
Bioorg Med Chem Lett (2005) 15 : 4666 -4670
PubMed 16153829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.08 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL198756 1 7.55
CHEMBL383799 1 7.51
CHEMBL383348 1 7.27
CHEMBL198427 1 6.94
CHEMBL198261 1 6.66
CHEMBL372082 1 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL198756 IC50 = 28.0 nM 7.55
CHEMBL383799 IC50 = 31.0 nM 7.51
CHEMBL383348 IC50 = 54.0 nM 7.27
CHEMBL198427 IC50 = 116.0 nM 6.94
CHEMBL198261 IC50 = 217.0 nM 6.66
CHEMBL372082 IC50 = 295.0 nM 6.53