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Assay Detail

CHEMBL4416355

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

ADMET
Inhibition of human TPMT expressed in Escherichia coli assessed as reduction in SAH level using 6-mercaptopurine as substrate in presence of SAM incubated for 30 mins by LC-MS/MS analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Thiopurine S-methyltransferase (CHEMBL2500)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide <i>N</i>-Methyltransferase (NNMT).
Policarpo RL, Decultot L, May E, Kuzmič P, Carlson S, Huang D, Chu V, Wright BA, Dhakshinamoorthy S, Kannt A, Rani S, Dittakavi S, Panarese JD, Gaudet R, Shair MD.
J Med Chem (2019) 62 : 9837 -9873
PubMed 31589440 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 6.00 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4591248 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4591248 IC50 = 1000.0 nM 6.00