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Assay Detail

CHEMBL5166113

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

Binding
Inhibition of full-length ERK5 in HEK293 cells assessed as paradoxical activation of ERK5 transcriptional activity incubated for 20 hrs by dual luciferase reporter assay
1
Total Activities
1
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 7 (CHEMBL5332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C.
J Med Chem (2022) 65 : 6513 -6540
PubMed 35468293 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5193786 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5193786 IC50 = 1000.0 nM 6.00