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Assay Detail

CHEMBL4141000

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

Binding
Inhibition of human liver cathepsin D using Mca-Gly-Lys-Pro-Ile-Leu-PhePhe-Arg-Leu-Lys-(Dnp)-D-Arg-NH2 as substrate pretreated for 15 mins followed by substrate addition measured at 5 mins interval for 120 mins by fluorescence assay
9
Total Activities
9
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

Cathepsin D (CHEMBL2581)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Grassystatins D-F, Potent Aspartic Protease Inhibitors from Marine Cyanobacteria as Potential Antimetastatic Agents Targeting Invasive Breast Cancer.
Al-Awadhi FH, Law BK, Paul VJ, Luesch H.
J Nat Prod (2017) 80 : 2969 -2986
PubMed 29087712 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.17 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296588 PEPSTATIN 2.0 1 9.46
CHEMBL568553 GRASSYSTATIN B 1 8.14
CHEMBL567893 GRASSYSTATIN A 1 7.58
CHEMBL4167618 1 7.30
CHEMBL4163078 1 7.30
CHEMBL4159706 1 7.24
CHEMBL4170992 1 6.05
CHEMBL4174823 1 5.80
CHEMBL4173516 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296588 PEPSTATIN IC50 = 0.35 nM 9.46
CHEMBL568553 GRASSYSTATIN B IC50 = 7.3 nM 8.14
CHEMBL567893 GRASSYSTATIN A IC50 = 26.0 nM 7.58
CHEMBL4167618 IC50 = 50.0 nM 7.30
CHEMBL4163078 IC50 = 50.0 nM 7.30
CHEMBL4159706 IC50 = 57.0 nM 7.24
CHEMBL4170992 IC50 = 900.0 nM 6.05
CHEMBL4174823 IC50 = 1600.0 nM 5.80
CHEMBL4173516 IC50 = 2000.0 nM 5.70