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Assay Detail

CHEMBL663327

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

Binding
Inhibition of cysteine protease cathepsin K of rat
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL3034)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin k.
Tavares FX, Boncek V, Deaton DN, Hassell AM, Long ST, Miller AB, Payne AA, Miller LR, Shewchuk LM, Wells-Knecht K, Willard DH, Wright LL, Zhou HQ.
J Med Chem (2004) 47 : 588 -599
PubMed 14736240 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.61 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL154579 1 8.74
CHEMBL154959 1 8.26
CHEMBL156764 1 7.96
CHEMBL345982 1 7.92
CHEMBL154862 1 7.89
CHEMBL157911 1 6.33
CHEMBL345356 1 6.10
CHEMBL157224 1 6.00
CHEMBL155148 1 5.96
CHEMBL155123 1 5.96
CHEMBL155297 1 5.92
CHEMBL345136 1 5.82
CHEMBL155183 1 5.80
CHEMBL152633 1 5.77
CHEMBL155592 1 5.77
CHEMBL346739 1 5.57
CHEMBL346102 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL154579 IC50 = 1.8 nM 8.74
CHEMBL154959 IC50 = 5.5 nM 8.26
CHEMBL156764 IC50 = 11.0 nM 7.96
CHEMBL345982 IC50 = 12.0 nM 7.92
CHEMBL154862 IC50 = 13.0 nM 7.89
CHEMBL157911 IC50 = 470.0 nM 6.33
CHEMBL345356 IC50 = 790.0 nM 6.10
CHEMBL157224 IC50 = 1000.0 nM 6.00
CHEMBL155148 IC50 = 1100.0 nM 5.96
CHEMBL155123 IC50 = 1100.0 nM 5.96
CHEMBL155297 IC50 = 1200.0 nM 5.92
CHEMBL345136 IC50 = 1500.0 nM 5.82
CHEMBL155183 IC50 = 1600.0 nM 5.80
CHEMBL152633 IC50 = 1700.0 nM 5.77
CHEMBL155592 IC50 = 1700.0 nM 5.77
CHEMBL346739 IC50 = 2700.0 nM 5.57
CHEMBL346102 IC50 > 1200.0 nM -