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Assay Detail

CHEMBL684976

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Binding
Inhibitory activity against glycogen synthase kinase-3 beta purified from insect sf9 cells
ChEMBL ↗
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism insect
Cell Type Sf9
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glycogen synthase kinase-3 beta (CHEMBL262) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Evaluation and comparison of 3D-QSAR CoMSIA models for CDK1, CDK5, and GSK-3 inhibition by paullones.
Kunick C, Lauenroth K, Wieking K, Xie X, Schultz C, Gussio R, Zaharevitz D, Leost M, Meijer L, Weber A, Jørgensen FS, Lemcke T.
J Med Chem (2004) 47 : 22 -36
PubMed 14695817 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 66 6.31 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL299756 PAULLONE 2 — 1 8.00
CHEMBL331190 — — 1 7.89
CHEMBL325654 — — 1 7.75
CHEMBL331000 — — 1 7.75
CHEMBL325403 — — 1 7.66
CHEMBL329505 — — 1 7.52
CHEMBL545053 — — 1 7.52
CHEMBL121492 — — 1 7.48
CHEMBL119963 — — 1 7.46
CHEMBL116545 — — 1 7.16
CHEMBL332678 — — 1 7.12
CHEMBL328194 — — 1 7.12
CHEMBL99037 — — 1 7.10
CHEMBL333894 — — 1 7.05
CHEMBL319373 — — 1 7.00
CHEMBL323657 — — 1 6.92
CHEMBL329063 — — 1 6.92
CHEMBL317964 — — 1 6.89
CHEMBL332359 — — 1 6.89
CHEMBL333006 — — 1 6.70
CHEMBL121543 — — 1 6.70
CHEMBL334084 — — 1 6.62
CHEMBL116832 — — 1 6.60
CHEMBL99803 — — 1 6.52
CHEMBL118162 — — 1 6.48
CHEMBL121958 — — 1 6.46
CHEMBL419054 — — 1 6.40
CHEMBL334031 — — 1 6.40
CHEMBL318208 — — 1 6.40
CHEMBL120030 — — 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL299756 PAULLONE 2 IC50 = 10.0 nM 8.00
CHEMBL331190 — IC50 = 13.0 nM 7.89
CHEMBL331000 — IC50 = 17.99 nM 7.75
CHEMBL325654 — IC50 = 17.99 nM 7.75
CHEMBL325403 — IC50 = 21.98 nM 7.66
CHEMBL329505 — IC50 = 29.99 nM 7.52
CHEMBL545053 — IC50 = 29.99 nM 7.52
CHEMBL121492 — IC50 = 33.04 nM 7.48
CHEMBL119963 — IC50 = 34.99 nM 7.46
CHEMBL116545 — IC50 = 69.98 nM 7.16
CHEMBL332678 — IC50 = 74.99 nM 7.12
CHEMBL328194 — IC50 = 74.99 nM 7.12
CHEMBL99037 — IC50 = 79.98 nM 7.10
CHEMBL333894 — IC50 = 89.95 nM 7.05
CHEMBL319373 — IC50 = 100.0 nM 7.00
CHEMBL323657 — IC50 = 119.95 nM 6.92
CHEMBL329063 — IC50 = 119.95 nM 6.92
CHEMBL317964 — IC50 = 130.02 nM 6.89
CHEMBL332359 — IC50 = 130.02 nM 6.89
CHEMBL333006 — IC50 = 199.99 nM 6.70
CHEMBL121543 — IC50 = 199.99 nM 6.70
CHEMBL334084 — IC50 = 239.88 nM 6.62
CHEMBL116832 — IC50 = 250.03 nM 6.60
CHEMBL99803 — IC50 = 299.92 nM 6.52
CHEMBL118162 — IC50 = 330.37 nM 6.48
CHEMBL121958 — IC50 = 349.95 nM 6.46
CHEMBL334031 — IC50 = 399.94 nM 6.40
CHEMBL318208 — IC50 = 399.94 nM 6.40
CHEMBL419054 — IC50 = 399.94 nM 6.40
CHEMBL120030 — IC50 = 500.03 nM 6.30
CHEMBL98501 — IC50 = 500.03 nM 6.30
CHEMBL318911 — IC50 = 599.79 nM 6.22
CHEMBL120497 — IC50 = 599.79 nM 6.22
CHEMBL430574 PAULLONE IC50 = 619.44 nM 6.21
CHEMBL317150 — IC50 = 699.84 nM 6.16
CHEMBL98360 — IC50 = 799.83 nM 6.10
CHEMBL431634 — IC50 = 899.5 nM 6.05
CHEMBL328164 — IC50 = 1199.5 nM 5.92
CHEMBL119932 — IC50 = 1300.17 nM 5.89
CHEMBL118406 — IC50 = 1300.17 nM 5.89
CHEMBL119989 — IC50 = 1399.59 nM 5.85
CHEMBL328627 — IC50 = 1499.68 nM 5.82
CHEMBL120664 — IC50 = 1999.86 nM 5.70
CHEMBL52551 — IC50 = 1999.86 nM 5.70
CHEMBL100309 — IC50 = 1999.86 nM 5.70
CHEMBL316485 — IC50 = 2098.94 nM 5.68
CHEMBL121957 — IC50 = 2197.86 nM 5.66
CHEMBL95827 — IC50 = 2197.86 nM 5.66
CHEMBL100312 — IC50 = 2301.44 nM 5.64
CHEMBL324064 — IC50 = 3999.45 nM 5.40