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Assay Detail

CHEMBL2188994

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

Binding
Inhibition of porcine brain CK1delta/epsilon using RRKHAAIGpSAYSITA as substrate and [gamma-33P]-ATP after 30 mins by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.
Boulahjar R, Ouach A, Matteo C, Bourg S, Ravache M, le Guével R, Marionneau S, Oullier T, Lozach O, Meijer L, Guguen-Guillouzo C, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S.
J Med Chem (2012) 55 : 9589 -9606
PubMed 23083119 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.76 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180854 1 5.89
CHEMBL2180844 1 5.82
CHEMBL2180858 1 5.58
CHEMBL2180845 1 -
CHEMBL2180843 1 -
CHEMBL2180859 1 -
CHEMBL2180857 1 -
CHEMBL2180856 1 -
CHEMBL2180855 1 -
CHEMBL2180853 1 -
CHEMBL2180852 1 -
CHEMBL2180862 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180854 IC50 = 1300.0 nM 5.89
CHEMBL2180844 IC50 = 1500.0 nM 5.82
CHEMBL2180858 IC50 = 2600.0 nM 5.58
CHEMBL2180845 IC50 >= 10000.0 nM -
CHEMBL2180843 IC50 > 10000.0 nM -
CHEMBL2180859 IC50 > 10000.0 nM -
CHEMBL2180857 IC50 - -
CHEMBL2180856 IC50 > 10000.0 nM -
CHEMBL2180855 IC50 - -
CHEMBL2180853 IC50 - -
CHEMBL2180852 IC50 - -
CHEMBL2180862 IC50 - -