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Assay Detail

CHEMBL3787890

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Functional
Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 3342 staining analysis
28
Total Activities
28
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

Publication

Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.
Ouach A, Boulahjar R, Vala C, Bourg S, Bonnet P, Guguen-Guillouzo C, Ravache M, Le Guevel R, Lozach O, Lazar S, Troin Y, Meijer L, Ruchaud S, Akssira M, Guillaumet G, Routier S.
Eur J Med Chem (2016) 115 : 311 -325
PubMed 27019296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.20 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3786430 1 7.70
CHEMBL3786276 1 7.40
CHEMBL3787480 1 7.30
CHEMBL3785408 1 7.22
CHEMBL3787512 1 7.00
CHEMBL3787135 1 6.92
CHEMBL3787557 1 6.82
CHEMBL3786536 1 6.82
CHEMBL3785575 1 6.82
CHEMBL3785571 1 6.82
CHEMBL3787081 1 6.72
CHEMBL2180862 1 6.62
CHEMBL3787033 1 6.40
CHEMBL3787093 1 6.30
CHEMBL3785771 1 6.22
CHEMBL2180863 1 6.08
CHEMBL3786332 1 5.92
CHEMBL3785795 1 5.70
CHEMBL3785804 1 5.52
CHEMBL3785596 1 5.40
CHEMBL14762 SELICICLIB 2.0 1 5.30
CHEMBL3786624 1 5.10
CHEMBL3787292 1 5.10
CHEMBL3786745 1 4.70
CHEMBL3787061 1 4.70
CHEMBL3785573 1 4.70
CHEMBL3787584 1 -
CHEMBL3786657 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3786430 IC50 = 20.0 nM 7.70
CHEMBL3786276 IC50 = 40.0 nM 7.40
CHEMBL3787480 IC50 = 50.0 nM 7.30
CHEMBL3785408 IC50 = 60.0 nM 7.22
CHEMBL3787512 IC50 = 100.0 nM 7.00
CHEMBL3787135 IC50 = 120.0 nM 6.92
CHEMBL3787557 IC50 = 150.0 nM 6.82
CHEMBL3786536 IC50 = 150.0 nM 6.82
CHEMBL3785575 IC50 = 150.0 nM 6.82
CHEMBL3785571 IC50 = 150.0 nM 6.82
CHEMBL3787081 IC50 = 190.0 nM 6.72
CHEMBL2180862 IC50 = 240.0 nM 6.62
CHEMBL3787033 IC50 = 400.0 nM 6.40
CHEMBL3787093 IC50 = 500.0 nM 6.30
CHEMBL3785771 IC50 = 600.0 nM 6.22
CHEMBL2180863 IC50 = 830.0 nM 6.08
CHEMBL3786332 IC50 = 1200.0 nM 5.92
CHEMBL3785795 IC50 = 2000.0 nM 5.70
CHEMBL3785804 IC50 = 3000.0 nM 5.52
CHEMBL3785596 IC50 = 4000.0 nM 5.40
CHEMBL14762 SELICICLIB IC50 = 5000.0 nM 5.30
CHEMBL3786624 IC50 = 8000.0 nM 5.10
CHEMBL3787292 IC50 = 8000.0 nM 5.10
CHEMBL3786745 IC50 = 20000.0 nM 4.70
CHEMBL3787061 IC50 = 20000.0 nM 4.70
CHEMBL3785573 IC50 = 20000.0 nM 4.70
CHEMBL3787584 IC50 > 25000.0 nM -
CHEMBL3786657 IC50 > 25000.0 nM -