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Assay Detail

CHEMBL636819

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

Binding
concentration required to reduce AGT activity to 50% of control rate in intact HT-29 human colorectal carcinoma cells.
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-29
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Resistance-modifying agents. 8. Inhibition of O(6)-alkylguanine-DNA alkyltransferase by O(6)-alkenyl-, O(6)-cycloalkenyl-, and O(6)-(2-oxoalkyl)guanines and potentiation of temozolomide cytotoxicity in vitro by O(6)-(1-cyclopentenylmethyl)guanine.
Griffin RJ, Arris CE, Bleasdale C, Boyle FT, Calvert AH, Curtin NJ, Dalby C, Kanugula S, Lembicz NK, Newell DR, Pegg AE, Golding BT.
J Med Chem (2000) 43 : 4071 -4083
PubMed 11063604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.29 5.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325053 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325053 IC50 = 5100.0 nM 5.29