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Assay Detail

CHEMBL864505

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

Binding
Inhibitory activity against human cathepsin K using Z-Leu-Arg-NHMec substrate
48
Total Activities
48
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Löser R, Schilling K, Dimmig E, Gütschow M.
J Med Chem (2005) 48 : 7688 -7707
PubMed 16302809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 5.40 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200161 1 7.46
CHEMBL200521 1 7.13
CHEMBL200160 1 6.92
CHEMBL344174 1 6.58
CHEMBL200235 1 6.52
CHEMBL381847 1 6.14
CHEMBL383816 1 5.96
CHEMBL200577 1 5.92
CHEMBL383584 1 5.90
CHEMBL371466 1 5.82
CHEMBL200181 1 5.68
CHEMBL200057 1 5.68
CHEMBL200549 1 5.48
CHEMBL371285 1 5.48
CHEMBL424669 1 5.39
CHEMBL200374 1 5.39
CHEMBL200427 1 5.38
CHEMBL200569 1 5.30
CHEMBL370188 1 5.28
CHEMBL197113 1 5.24
CHEMBL372154 1 5.20
CHEMBL371499 1 5.19
CHEMBL200004 1 5.19
CHEMBL197181 1 5.12
CHEMBL198570 1 5.07
CHEMBL200836 1 4.89
CHEMBL200558 1 4.80
CHEMBL380560 1 4.58
CHEMBL200724 1 4.55
CHEMBL381191 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200161 Ki = 35.0 nM 7.46
CHEMBL200521 Ki = 74.0 nM 7.13
CHEMBL200160 Ki = 120.0 nM 6.92
CHEMBL344174 Ki = 260.0 nM 6.58
CHEMBL200235 Ki = 300.0 nM 6.52
CHEMBL381847 Ki = 730.0 nM 6.14
CHEMBL383816 Ki = 1100.0 nM 5.96
CHEMBL200577 Ki = 1200.0 nM 5.92
CHEMBL383584 Ki = 1270.0 nM 5.90
CHEMBL371466 Ki = 1500.0 nM 5.82
CHEMBL200181 Ki = 2100.0 nM 5.68
CHEMBL200057 Ki = 2100.0 nM 5.68
CHEMBL371285 Ki = 3300.0 nM 5.48
CHEMBL200549 Ki = 3300.0 nM 5.48
CHEMBL200374 Ki = 4100.0 nM 5.39
CHEMBL424669 Ki = 4100.0 nM 5.39
CHEMBL200427 Ki = 4200.0 nM 5.38
CHEMBL200569 Ki = 5000.0 nM 5.30
CHEMBL370188 Ki = 5300.0 nM 5.28
CHEMBL197113 Ki = 5800.0 nM 5.24
CHEMBL372154 Ki = 6300.0 nM 5.20
CHEMBL371499 Ki = 6500.0 nM 5.19
CHEMBL200004 Ki = 6500.0 nM 5.19
CHEMBL197181 Ki = 7500.0 nM 5.12
CHEMBL198570 Ki = 8500.0 nM 5.07
CHEMBL200836 Ki = 13000.0 nM 4.89
CHEMBL200558 Ki = 16000.0 nM 4.80
CHEMBL380560 Ki = 26000.0 nM 4.58
CHEMBL200724 Ki = 28000.0 nM 4.55
CHEMBL381191 Ki = 29000.0 nM 4.54
CHEMBL371893 Ki = 30000.0 nM 4.52
CHEMBL383781 Ki = 34000.0 nM 4.47
CHEMBL200285 Ki = 66000.0 nM 4.18
CHEMBL200557 Ki = 83000.0 nM 4.08
CHEMBL200574 Ki = 90000.0 nM 4.05
CHEMBL200006 Ki > 1000000.0 nM -
CHEMBL200635 Ki = 136000.0 nM -
CHEMBL200007 Ki > 100000.0 nM -
CHEMBL197130 Ki > 100000.0 nM -
CHEMBL200576 Ki > 100000.0 nM -
CHEMBL200815 Ki > 100000.0 nM -
CHEMBL200743 Ki > 100000.0 nM -
CHEMBL200338 Ki > 100000.0 nM -
CHEMBL197498 Ki > 100000.0 nM -
CHEMBL197975 Ki > 1000000.0 nM -
CHEMBL200005 Ki > 1000000.0 nM -
CHEMBL200150 Ki > 1000000.0 nM -
CHEMBL381659 Ki > 100000.0 nM -