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Assay Detail

CHEMBL4313396

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

Binding
Inhibition of recombinant Nanoluc-tagged p38alpha (unknown origin) expressed in HEK293 cells incubated for 2 to 3 mins by NanoBRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a potent p38α/MAPK14 kinase inhibitor: Synthesis, in vitro/in vivo biological evaluation, and docking studies.
El-Gamal MI, Anbar HS, Tarazi H, Oh CH.
Eur J Med Chem (2019) 183 : 111684 -111684
PubMed 31520926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.39 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10 SB-203580 1 7.22
CHEMBL5416410 DASATINIB 4.0 1 6.33
CHEMBL4553144 1 6.28
CHEMBL4559825 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10 SB-203580 EC50 = 60.0 nM 7.22
CHEMBL5416410 DASATINIB EC50 = 470.0 nM 6.33
CHEMBL4553144 EC50 = 520.0 nM 6.28
CHEMBL4559825 EC50 = 1940.0 nM 5.71