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Assay Detail

CHEMBL926489

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

Binding
Inhibition of human recombinant GSKbeta
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease.
Hamann M, Alonso D, Martín-Aparicio E, Fuertes A, Pérez-Puerto MJ, Castro A, Morales S, Navarro ML, Del Monte-Millán M, Medina M, Pennaka H, Balaiah A, Peng J, Cook J, Wahyuono S, Martínez A.
J Nat Prod (2007) 70 : 1397 -1405
PubMed 17708655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.01 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL612054 1 5.32
CHEMBL252520 12,13-DEHYDRO-8-O-ACETYLMANZAMINE A 1 5.32
CHEMBL268202 12,13-DEHYDROMANZAMINE A 1 5.27
CHEMBL400717 1 5.14
CHEMBL399696 1 5.07
CHEMBL403233 MANZAMINE A 1 4.99
CHEMBL403562 9-N-ETHYL-8-ETHOXY-MANZAMINE A 1 4.98
CHEMBL252672 1 4.78
CHEMBL414128 1 4.64
CHEMBL399493 MANZAMINE E 1 4.60
CHEMBL437596 TETRAHYDROMANZAMINE A 1 -
CHEMBL399694 MANZAMINE F 1 -
CHEMBL253510 TETRAHYDRO-8-HYDROXYMANZAMINE A 1 -
CHEMBL253548 6-Deoxymanzamine X 1 -
CHEMBL254391 1 -
CHEMBL592630 1 -
CHEMBL402273 9-N-ISOBUTYL-8-ISOBUTYLOXY-MANZAMINE A 1 -
CHEMBL267700 9-N-METHYL-8-METHOXY-MANZAMINE A 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL612054 IC50 = 4800.0 nM 5.32
CHEMBL252520 12,13-DEHYDRO-8-O-ACETYLMANZAMINE A IC50 = 4800.0 nM 5.32
CHEMBL268202 12,13-DEHYDROMANZAMINE A IC50 = 5400.0 nM 5.27
CHEMBL400717 IC50 = 7200.0 nM 5.14
CHEMBL399696 IC50 = 8500.0 nM 5.07
CHEMBL403233 MANZAMINE A IC50 = 10200.0 nM 4.99
CHEMBL403562 9-N-ETHYL-8-ETHOXY-MANZAMINE A IC50 = 10400.0 nM 4.98
CHEMBL252672 IC50 = 16600.0 nM 4.78
CHEMBL414128 IC50 = 23000.0 nM 4.64
CHEMBL399493 MANZAMINE E IC50 = 25000.0 nM 4.60
CHEMBL437596 TETRAHYDROMANZAMINE A IC50 - -
CHEMBL399694 MANZAMINE F IC50 - -
CHEMBL253510 TETRAHYDRO-8-HYDROXYMANZAMINE A IC50 - -
CHEMBL253548 6-Deoxymanzamine X IC50 - -
CHEMBL254391 IC50 - -
CHEMBL592630 IC50 - -
CHEMBL402273 9-N-ISOBUTYL-8-ISOBUTYLOXY-MANZAMINE A IC50 - -
CHEMBL267700 9-N-METHYL-8-METHOXY-MANZAMINE A IC50 - -