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Assay Detail

CHEMBL1806288

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Binding
Inhibition of ERK2
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 1 (CHEMBL4040)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration.
Heathcote DA, Patel H, Kroll SH, Hazel P, Periyasamy M, Alikian M, Kanneganti SK, Jogalekar AS, Scheiper B, Barbazanges M, Blum A, Brackow J, Siwicka A, Pace RD, Fuchter MJ, Snyder JP, Liotta DC, Freemont PS, Aboagye EO, Coombes RC, Barrett AG, Ali S.
J Med Chem (2010) 53 : 8508 -8522
PubMed 21080703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.51 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1234833 1 5.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1234833 IC50 = 3110.0 nM 5.51