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Assay Detail

CHEMBL2384040

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

Binding
Inhibition of human cathepsin-S
31
Total Activities
31
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 S (CHEMBL2954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of proline analogues as potent and selective cathepsin S inhibitors.
Kim M, Jeon J, Song J, Suh KH, Kim YH, Min KH, Lee KO.
Bioorg Med Chem Lett (2013) 23 : 3140 -3144
PubMed 23639544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.23 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2380725 1 8.96
CHEMBL222649 1 8.72
CHEMBL2380724 1 8.70
CHEMBL2380727 1 8.64
CHEMBL2380718 1 8.62
CHEMBL2380720 1 8.57
CHEMBL2380716 1 8.52
CHEMBL2380717 1 8.51
CHEMBL2380729 1 8.49
CHEMBL2380728 1 8.49
CHEMBL2380735 1 8.48
CHEMBL2380723 1 8.48
CHEMBL2380721 1 8.48
CHEMBL2380719 1 8.48
CHEMBL2380618 1 8.48
CHEMBL2380616 1 8.46
CHEMBL2380619 1 8.46
CHEMBL2380722 1 8.43
CHEMBL2380726 1 8.39
CHEMBL2380736 1 8.37
CHEMBL2380621 1 7.91
CHEMBL2380731 1 7.74
CHEMBL2380622 1 7.68
CHEMBL2380732 1 7.61
CHEMBL2380734 1 7.44
CHEMBL2380620 1 7.34
CHEMBL2380714 1 7.08
CHEMBL2380617 1 6.81
CHEMBL2380715 1 -
CHEMBL2380733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2380725 IC50 = 1.1 nM 8.96
CHEMBL222649 IC50 = 1.9 nM 8.72
CHEMBL2380724 IC50 = 2.0 nM 8.70
CHEMBL2380727 IC50 = 2.3 nM 8.64
CHEMBL2380718 IC50 = 2.4 nM 8.62
CHEMBL2380720 IC50 = 2.7 nM 8.57
CHEMBL2380716 IC50 = 3.0 nM 8.52
CHEMBL2380717 IC50 = 3.1 nM 8.51
CHEMBL2380729 IC50 = 3.2 nM 8.49
CHEMBL2380728 IC50 = 3.2 nM 8.49
CHEMBL2380735 IC50 = 3.3 nM 8.48
CHEMBL2380723 IC50 = 3.3 nM 8.48
CHEMBL2380721 IC50 = 3.3 nM 8.48
CHEMBL2380719 IC50 = 3.3 nM 8.48
CHEMBL2380618 IC50 = 3.3 nM 8.48
CHEMBL2380616 IC50 = 3.5 nM 8.46
CHEMBL2380619 IC50 = 3.5 nM 8.46
CHEMBL2380722 IC50 = 3.7 nM 8.43
CHEMBL2380726 IC50 = 4.1 nM 8.39
CHEMBL2380736 IC50 = 4.3 nM 8.37
CHEMBL2380621 IC50 = 12.4 nM 7.91
CHEMBL2380731 IC50 = 18.1 nM 7.74
CHEMBL2380622 IC50 = 20.7 nM 7.68
CHEMBL2380732 IC50 = 24.6 nM 7.61
CHEMBL2380734 IC50 = 36.6 nM 7.44
CHEMBL2380620 IC50 = 45.4 nM 7.34
CHEMBL2380714 IC50 = 83.7 nM 7.08
CHEMBL2380617 IC50 = 156.0 nM 6.81
CHEMBL2380715 IC50 > 1000.0 nM -
CHEMBL2380733 IC50 > 100.0 nM -
CHEMBL2380730 IC50 > 100.0 nM -