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Assay Detail

CHEMBL656676

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

Binding
Inhibitory activity against recombinant human cathepsin K
39
Total Activities
39
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 (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of the P1 SAR of aldehyde cathepsin K inhibitors.
Catalano JG, Deaton DN, Furfine ES, Hassell AM, McFadyen RB, Miller AB, Miller LR, Shewchuk LM, Willard DH, Wright LL.
Bioorg Med Chem Lett (2004) 14 : 275 -278
PubMed 14684342 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 7.10 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92708 CALPEPTIN 1 9.96
CHEMBL315651 1 7.82
CHEMBL96284 1 7.82
CHEMBL330718 1 7.80
CHEMBL313847 1 7.64
CHEMBL92567 1 7.58
CHEMBL94891 1 7.58
CHEMBL92972 1 7.54
CHEMBL92025 1 7.52
CHEMBL96823 1 7.51
CHEMBL447231 1 7.44
CHEMBL94616 1 7.42
CHEMBL96669 1 7.42
CHEMBL96508 1 7.40
CHEMBL92971 1 7.39
CHEMBL96341 1 7.39
CHEMBL92465 1 7.30
CHEMBL91968 1 7.29
CHEMBL96875 1 7.29
CHEMBL93420 1 7.24
CHEMBL91874 1 7.11
CHEMBL96482 1 7.10
CHEMBL93911 1 7.08
CHEMBL94820 1 7.06
CHEMBL92993 1 7.01
CHEMBL540696 1 6.96
CHEMBL94327 1 6.96
CHEMBL319662 1 6.89
CHEMBL94383 1 6.82
CHEMBL92826 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92708 CALPEPTIN IC50 = 0.11 nM 9.96
CHEMBL315651 IC50 = 15.0 nM 7.82
CHEMBL96284 IC50 = 15.0 nM 7.82
CHEMBL330718 IC50 = 16.0 nM 7.80
CHEMBL313847 IC50 = 23.0 nM 7.64
CHEMBL92567 IC50 = 26.0 nM 7.58
CHEMBL94891 IC50 = 26.0 nM 7.58
CHEMBL92972 IC50 = 29.0 nM 7.54
CHEMBL92025 IC50 = 30.0 nM 7.52
CHEMBL96823 IC50 = 31.0 nM 7.51
CHEMBL447231 IC50 = 36.0 nM 7.44
CHEMBL94616 IC50 = 38.0 nM 7.42
CHEMBL96669 IC50 = 38.0 nM 7.42
CHEMBL96508 IC50 = 40.0 nM 7.40
CHEMBL96341 IC50 = 41.0 nM 7.39
CHEMBL92971 IC50 = 41.0 nM 7.39
CHEMBL92465 IC50 = 50.0 nM 7.30
CHEMBL91968 IC50 = 51.0 nM 7.29
CHEMBL96875 IC50 = 51.0 nM 7.29
CHEMBL93420 IC50 = 58.0 nM 7.24
CHEMBL91874 IC50 = 78.0 nM 7.11
CHEMBL96482 IC50 = 79.0 nM 7.10
CHEMBL93911 IC50 = 83.0 nM 7.08
CHEMBL94820 IC50 = 87.0 nM 7.06
CHEMBL92993 IC50 = 98.0 nM 7.01
CHEMBL540696 IC50 = 110.0 nM 6.96
CHEMBL94327 IC50 = 110.0 nM 6.96
CHEMBL319662 IC50 = 130.0 nM 6.89
CHEMBL94383 IC50 = 150.0 nM 6.82
CHEMBL92826 IC50 = 160.0 nM 6.80
CHEMBL94727 IC50 = 200.0 nM 6.70
CHEMBL330046 IC50 = 250.0 nM 6.60
CHEMBL94150 IC50 = 250.0 nM 6.60
CHEMBL318817 IC50 = 370.0 nM 6.43
CHEMBL94695 IC50 = 410.0 nM 6.39
CHEMBL94253 IC50 = 660.0 nM 6.18
CHEMBL92991 IC50 = 680.0 nM 6.17
CHEMBL94805 IC50 = 5800.0 nM 5.24
CHEMBL94782 IC50 = 52000.0 nM 4.28