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Assay Detail

CHEMBL4365544

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

Binding
Inhibition of ERK5 in human HeLa cells by KiNativ profiling method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 7 (CHEMBL5332)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a novel orally bioavailable ERK5 inhibitor with selectivity over p38α and BRD4.
Myers SM, Miller DC, Molyneux L, Arasta M, Bawn RH, Blackburn TJ, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hammonds T, Hardcastle IR, Harnor SJ, Heptinstall AB, Lochhead PA, Martin MP, Martin NC, Newell DR, Owen PJ, Pang LC, Reuillon T, Rigoreau LJM, Thomas HD, Tucker JA, Wang LZ, Wong AC, Noble MEM, Wedge SR, Cano C.
Eur J Med Chem (2019) 178 : 530 -543
PubMed 31212132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.10 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4541479 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4541479 IC50 = 8.0 nM 8.10