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Assay Detail

CHEMBL1279523

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

Binding
Inhibition of Trypanosoma brucei recombinant MBP-fused GSK-3 short isoform expressed in Escherichia coli by scintillation proximity assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Glycogen synthase kinase 3 is a potential drug target for African trypanosomiasis therapy.
Ojo KK, Gillespie JR, Riechers AJ, Napuli AJ, Verlinde CL, Buckner FS, Gelb MH, Domostoj MM, Wells SJ, Scheer A, Wells TN, Van Voorhis WC.
Antimicrob Agents Chemother (2008) 52 : 3710 -3717
PubMed 18644955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.37 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276446 1 9.00
CHEMBL1276514 1 8.40
CHEMBL1276447 1 7.89
CHEMBL1276544 1 7.66
CHEMBL1276515 1 7.52
CHEMBL1276574 1 7.52
CHEMBL1276543 1 7.34
CHEMBL1276575 1 6.78
CHEMBL260138 ALSTERPAULLONE 2 1 6.47
CHEMBL258805 SU-9516 1.0 1 6.45
CHEMBL322970 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276446 IC50 = 1.0 nM 9.00
CHEMBL1276514 IC50 = 4.0 nM 8.40
CHEMBL1276447 IC50 = 13.0 nM 7.89
CHEMBL1276544 IC50 = 22.0 nM 7.66
CHEMBL1276515 IC50 = 30.0 nM 7.52
CHEMBL1276574 IC50 = 30.0 nM 7.52
CHEMBL1276543 IC50 = 46.0 nM 7.34
CHEMBL1276575 IC50 = 168.0 nM 6.78
CHEMBL260138 ALSTERPAULLONE 2 IC50 = 336.0 nM 6.47
CHEMBL258805 SU-9516 IC50 = 352.0 nM 6.45
CHEMBL322970 IC50 = 1000.0 nM 6.00