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Assay Detail

CHEMBL941183

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

Binding
Inhibition of human C-terminal His-tagged AdoMetDC assessed as release of 14CO2 from S-adenosyl-L-[carboxy-14C]methionine
24
Total Activities
24
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

S-adenosylmethionine decarboxylase proenzyme (CHEMBL4181)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

New insights into the design of inhibitors of human S-adenosylmethionine decarboxylase: studies of adenine C8 substitution in structural analogues of S-adenosylmethionine.
McCloskey DE, Bale S, Secrist JA, Tiwari A, Moss TH, Valiyaveettil J, Brooks WH, Guida WC, Pegg AE, Ealick SE.
J Med Chem (2009) 52 : 1388 -1407
PubMed 19209891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.30 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL517131 1 8.30
CHEMBL510356 1 8.15
CHEMBL461970 1 7.96
CHEMBL461779 1 7.82
CHEMBL516811 1 7.75
CHEMBL460719 1 7.31
CHEMBL461780 1 7.26
CHEMBL453372 1 7.07
CHEMBL517593 1 6.77
CHEMBL462656 1 6.40
CHEMBL516214 1 6.22
CHEMBL462138 1 5.82
CHEMBL473134 1 5.52
CHEMBL517908 1 5.40
CHEMBL473336 1 5.30
CHEMBL461969 1 5.16
CHEMBL472733 1 5.05
CHEMBL462139 1 4.51
CHEMBL515862 1 4.16
CHEMBL462660 1 4.06
CHEMBL474137 1 -
CHEMBL472730 1 -
CHEMBL460737 1 -
CHEMBL461966 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL517131 IC50 = 5.0 nM 8.30
CHEMBL510356 IC50 = 7.0 nM 8.15
CHEMBL461970 IC50 = 11.0 nM 7.96
CHEMBL461779 IC50 = 15.0 nM 7.82
CHEMBL516811 IC50 = 18.0 nM 7.75
CHEMBL460719 IC50 = 49.0 nM 7.31
CHEMBL461780 IC50 = 55.0 nM 7.26
CHEMBL453372 IC50 = 86.0 nM 7.07
CHEMBL517593 IC50 = 170.0 nM 6.77
CHEMBL462656 IC50 = 400.0 nM 6.40
CHEMBL516214 IC50 = 600.0 nM 6.22
CHEMBL462138 IC50 = 1500.0 nM 5.82
CHEMBL473134 IC50 = 3000.0 nM 5.52
CHEMBL517908 IC50 = 4000.0 nM 5.40
CHEMBL473336 IC50 = 5000.0 nM 5.30
CHEMBL461969 IC50 = 7000.0 nM 5.16
CHEMBL472733 IC50 = 9000.0 nM 5.05
CHEMBL462139 IC50 = 31000.0 nM 4.51
CHEMBL515862 IC50 = 70000.0 nM 4.16
CHEMBL462660 IC50 = 88000.0 nM 4.06
CHEMBL474137 IC50 = 157000.0 nM -
CHEMBL472730 IC50 = 420000.0 nM -
CHEMBL460737 IC50 = 500000.0 nM -
CHEMBL461966 IC50 = 440000.0 nM -