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Assay Detail

CHEMBL942267

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

Binding
Inhibition of human recombinant NAT1 assessed as hydrolysis of acetyl coA using PABA as substrate by Ellman's method
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 Autocuration

Target

Arylamine N-acetyltransferase 1 (CHEMBL5101)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2.
Russell AJ, Westwood IM, Crawford MH, Robinson J, Kawamura A, Redfield C, Laurieri N, Lowe ED, Davies SG, Sim E.
Bioorg Med Chem (2009) 17 : 905 -918
PubMed 19059786 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.37 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458614 1 6.48
CHEMBL457919 1 6.22
CHEMBL431550 1 5.96
CHEMBL511165 1 5.96
CHEMBL506606 1 5.47
CHEMBL110470 1 5.44
CHEMBL458705 1 5.41
CHEMBL201467 1 5.33
CHEMBL456849 1 5.12
CHEMBL502693 1 5.09
CHEMBL387624 1 4.89
CHEMBL305763 1 4.89
CHEMBL458999 1 4.77
CHEMBL487697 1 4.77
CHEMBL512033 1 4.75
CHEMBL224521 1 -
CHEMBL402427 1 -
CHEMBL224172 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458614 IC50 = 330.0 nM 6.48
CHEMBL457919 IC50 = 600.0 nM 6.22
CHEMBL431550 IC50 = 1100.0 nM 5.96
CHEMBL511165 IC50 = 1100.0 nM 5.96
CHEMBL506606 IC50 = 3400.0 nM 5.47
CHEMBL110470 IC50 = 3600.0 nM 5.44
CHEMBL458705 IC50 = 3900.0 nM 5.41
CHEMBL201467 IC50 = 4700.0 nM 5.33
CHEMBL456849 IC50 = 7600.0 nM 5.12
CHEMBL502693 IC50 = 8100.0 nM 5.09
CHEMBL387624 IC50 = 12900.0 nM 4.89
CHEMBL305763 IC50 = 13000.0 nM 4.89
CHEMBL458999 IC50 = 17000.0 nM 4.77
CHEMBL487697 IC50 = 16900.0 nM 4.77
CHEMBL512033 IC50 = 17600.0 nM 4.75
CHEMBL224521 IC50 > 30000.0 nM -
CHEMBL402427 IC50 > 30000.0 nM -
CHEMBL224172 IC50 > 30000.0 nM -