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Assay Detail

CHEMBL1670879

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

Binding
Inhibition of human recombinant cathepsin V expressed in Pichia pastoris
11
Total Activities
11
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 L2 (CHEMBL3272)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acridone alkaloids as potent inhibitors of cathepsin V.
Severino RP, Guido RV, Marques EF, Brömme D, da Silva MF, Fernandes JB, Andricopulo AD, Vieira PC.
Bioorg Med Chem (2011) 19 : 1477 -1481
PubMed 21277783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.21 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1668599 CITIBRASINE 1 5.92
CHEMBL463652 GLYCOCITRINE-IV 1 5.66
CHEMBL451705 CITRUSININE-I 1 5.66
CHEMBL1668597 1 5.60
CHEMBL1668602 1 5.55
CHEMBL464846 1 5.41
CHEMBL1668601 1 5.28
CHEMBL465847 CITRUSININE-II 1 5.00
CHEMBL1668598 GLYCOCITRINE-I 1 4.60
CHEMBL1668600 PYRANOFOLINE 1 4.36
CHEMBL447169 1 4.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1668599 CITIBRASINE IC50 = 1200.0 nM 5.92
CHEMBL463652 GLYCOCITRINE-IV IC50 = 2200.0 nM 5.66
CHEMBL451705 CITRUSININE-I IC50 = 2200.0 nM 5.66
CHEMBL1668597 IC50 = 2500.0 nM 5.60
CHEMBL1668602 IC50 = 2800.0 nM 5.55
CHEMBL464846 IC50 = 3900.0 nM 5.41
CHEMBL1668601 IC50 = 5200.0 nM 5.28
CHEMBL465847 CITRUSININE-II IC50 = 10000.0 nM 5.00
CHEMBL1668598 GLYCOCITRINE-I IC50 = 25000.0 nM 4.60
CHEMBL1668600 PYRANOFOLINE IC50 = 44000.0 nM 4.36
CHEMBL447169 IC50 = 48000.0 nM 4.32