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Assay Detail

CHEMBL987288

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Binding
Inhibition of alpha-mannosidase in human HCEC
9
Total Activities
7
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

Lysosomal alpha-mannosidase (CHEMBL4059)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Functionalized pyrrolidine inhibitors of human type II alpha-mannosidases as anti-cancer agents: optimizing the fit to the active site.
Fiaux H, Kuntz DA, Hoffman D, Janzer RC, Gerber-Lemaire S, Rose DR, Juillerat-Jeanneret L.
Bioorg Med Chem (2008) 16 : 7337 -7346
PubMed 18599296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.34 8.00
Ki 2 5.40 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371197 TRIDOLGOSIR 2.0 1 8.00
CHEMBL476926 2 6.30
CHEMBL476343 1 6.12
CHEMBL425723 2 4.63
CHEMBL476927 1 4.12
CHEMBL476925 1 4.12
CHEMBL476718 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371197 TRIDOLGOSIR IC50 = 10.0 nM 8.00
CHEMBL476926 IC50 = 500.0 nM 6.30
CHEMBL476926 Ki = 670.0 nM 6.17
CHEMBL476343 IC50 = 750.0 nM 6.12
CHEMBL425723 Ki = 23300.0 nM 4.63
CHEMBL425723 IC50 = 25000.0 nM 4.60
CHEMBL476927 IC50 = 75000.0 nM 4.12
CHEMBL476925 IC50 = 75000.0 nM 4.12
CHEMBL476718 IC50 = 75000.0 nM 4.12