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Assay Detail

CHEMBL4194794

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Binding
Inhibition of APN (unknown origin)
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aminopeptidase N (CHEMBL1907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Aminopeptidase N Inhibitors as Anti-cancer Agents.
Amin SA, Adhikari N, Jha T.
J Med Chem (2018) 61 : 6468 -6490
PubMed 29630364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.90 7.96
Ki 1 6.92 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1159812 1 7.96
CHEMBL4216928 1 7.70
CHEMBL4208547 1 7.70
CHEMBL1159809 1 7.70
CHEMBL1159811 1 7.70
CHEMBL1159810 1 7.68
CHEMBL4213478 1 7.60
CHEMBL4204214 1 7.40
CHEMBL88645 1 6.92
CHEMBL4209822 1 6.72
CHEMBL4206158 1 6.66
CHEMBL4217158 1 5.02
CHEMBL4213272 1 4.99
CHEMBL140 CURCUMIN 3.0 1 4.81

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1159812 IC50 = 11.0 nM 7.96
CHEMBL4216928 IC50 = 20.0 nM 7.70
CHEMBL4208547 IC50 = 20.0 nM 7.70
CHEMBL1159809 IC50 = 20.0 nM 7.70
CHEMBL1159811 IC50 = 20.0 nM 7.70
CHEMBL1159810 IC50 = 21.0 nM 7.68
CHEMBL4213478 IC50 = 25.0 nM 7.60
CHEMBL4204214 IC50 = 40.0 nM 7.40
CHEMBL88645 Ki = 120.0 nM 6.92
CHEMBL4209822 IC50 = 190.0 nM 6.72
CHEMBL4206158 IC50 = 220.0 nM 6.66
CHEMBL4217158 IC50 = 9600.0 nM 5.02
CHEMBL4213272 IC50 = 10200.0 nM 4.99
CHEMBL140 CURCUMIN IC50 = 15500.0 nM 4.81