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Assay Detail

CHEMBL4338384

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Binding
Inhibition of human Cathepsin L assessed as inhibition constant using Cbz-Phe-Arg-AMC as substrate by fluorescence assay
15
Total Activities
15
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

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization Strategy of Novel Peptide-Based Michael Acceptors for the Treatment of Human African Trypanosomiasis.
Ettari R, Previti S, Maiorana S, Amendola G, Wagner A, Cosconati S, Schirmeister T, Hellmich UA, Zappalà M.
J Med Chem (2019) 62 : 10617 -10629
PubMed 31714776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.53 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4584291 1 9.22
CHEMBL4475066 1 8.82
CHEMBL4587965 1 8.39
CHEMBL4515298 1 8.28
CHEMBL4437914 1 7.99
CHEMBL4436812 1 7.83
CHEMBL4566436 1 7.46
CHEMBL4453415 1 7.33
CHEMBL4456010 1 7.11
CHEMBL4454883 1 7.04
CHEMBL4459413 1 6.97
CHEMBL4456727 1 6.80
CHEMBL4464737 1 6.76
CHEMBL4441635 1 6.64
CHEMBL4438444 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4584291 Ki = 0.6 nM 9.22
CHEMBL4475066 Ki = 1.5 nM 8.82
CHEMBL4587965 Ki = 4.1 nM 8.39
CHEMBL4515298 Ki = 5.3 nM 8.28
CHEMBL4437914 Ki = 10.2 nM 7.99
CHEMBL4436812 Ki = 14.8 nM 7.83
CHEMBL4566436 Ki = 35.0 nM 7.46
CHEMBL4453415 Ki = 47.0 nM 7.33
CHEMBL4456010 Ki = 78.2 nM 7.11
CHEMBL4454883 Ki = 90.3 nM 7.04
CHEMBL4459413 Ki = 108.2 nM 6.97
CHEMBL4456727 Ki = 158.3 nM 6.80
CHEMBL4464737 Ki = 174.8 nM 6.76
CHEMBL4441635 Ki = 230.0 nM 6.64
CHEMBL4438444 Ki = 453.0 nM 6.34