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Assay Detail

CHEMBL2188992

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

Functional
Cytotoxicity against human HuH7 cells after 48 hrs
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Huh-7
Confidence 1 — Organism
Curated By Autocuration

Target

Huh-7 (CHEMBL614039)
Type CELL-LINE
Organism Homo sapiens

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 7 6.15 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180855 1 6.92
CHEMBL2180862 1 6.62
CHEMBL2180844 1 6.30
CHEMBL2180863 1 6.08
CHEMBL2180849 1 5.70
CHEMBL2180854 1 5.30
CHEMBL2180852 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180855 IC50 = 120.0 nM 6.92
CHEMBL2180862 IC50 = 240.0 nM 6.62
CHEMBL2180844 IC50 = 500.0 nM 6.30
CHEMBL2180863 IC50 = 830.0 nM 6.08
CHEMBL2180849 IC50 = 2000.0 nM 5.70
CHEMBL2180854 IC50 = 5000.0 nM 5.30
CHEMBL2180852 IC50 > 25000.0 nM -