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Assay Detail

CHEMBL2176221

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

Binding
Inhibition of AGT in human HL60 cells assessed as AGT levels using [3H]AGT after 2 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methylated-DNA--protein-cysteine methyltransferase (CHEMBL2864)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of a hypoxia-activated prodrug inhibitor of O6-alkylguanine-DNA alkyltransferase.
Zhu R, Seow HA, Baumann RP, Ishiguro K, Penketh PG, Shyam K, Sartorelli AC.
Bioorg Med Chem Lett (2012) 22 : 6242 -6247
PubMed 22932317 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.53 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL485756 1 8.05
CHEMBL2171205 1 7.60
CHEMBL407874 6-O-BENZYLGUANINE 3.0 1 7.41
CHEMBL2171202 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL485756 IC50 = 9.0 nM 8.05
CHEMBL2171205 IC50 = 25.0 nM 7.60
CHEMBL407874 6-O-BENZYLGUANINE IC50 = 39.0 nM 7.41
CHEMBL2171202 IC50 = 86.0 nM 7.07