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Assay Detail

CHEMBL4189612

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ADMET
Inhibition of recombinant human meprin alpha expressed in insect cells using Abz-YVADAPK(Dnp)G-OH as substrate by fluorescence assay
6
Total Activities
6
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

Meprin A subunit alpha (CHEMBL4105775)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Guided Design, Synthesis, and Characterization of Next-Generation Meprin β Inhibitors.
Ramsbeck D, Hamann A, Richter G, Schlenzig D, Geissler S, Nykiel V, Cynis H, Schilling S, Buchholz M.
J Med Chem (2018) 61 : 4578 -4592
PubMed 29694039 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.69 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205925 1 6.43
CHEMBL4209993 1 6.20
CHEMBL4206683 1 5.75
CHEMBL4078433 1 5.48
CHEMBL4217240 1 5.47
CHEMBL4216076 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205925 IC50 = 368.0 nM 6.43
CHEMBL4209993 IC50 = 626.0 nM 6.20
CHEMBL4206683 IC50 = 1795.0 nM 5.75
CHEMBL4078433 IC50 = 3293.0 nM 5.48
CHEMBL4217240 IC50 = 3420.0 nM 5.47
CHEMBL4216076 IC50 = 16050.0 nM 4.79