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Assay Detail

CHEMBL872473

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Binding
Inhibition of Human Cathepsin K
13
Total Activities
13
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

Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.
Wieczerzak E, Drabik P, Łankiewicz L, Ołdziej S, Grzonka Z, Abrahamson M, Grubb A, Brömme D.
J Med Chem (2002) 45 : 4202 -4211
PubMed 12213061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.13 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2028910 1 9.74
CHEMBL2028921 1 9.07
CHEMBL2028911 1 8.67
CHEMBL2028909 1 8.67
CHEMBL2028919 1 8.61
CHEMBL2028920 1 8.24
CHEMBL2028908 1 8.17
CHEMBL2028912 1 8.07
CHEMBL2028907 1 7.68
CHEMBL3143135 1 7.47
CHEMBL3143130 1 7.21
CHEMBL2028906 1 7.14
CHEMBL2028913 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2028910 Ki = 0.18 nM 9.74
CHEMBL2028921 Ki = 0.86 nM 9.07
CHEMBL2028911 Ki = 2.12 nM 8.67
CHEMBL2028909 Ki = 2.13 nM 8.67
CHEMBL2028919 Ki = 2.45 nM 8.61
CHEMBL2028920 Ki = 5.75 nM 8.24
CHEMBL2028908 Ki = 6.76 nM 8.17
CHEMBL2028912 Ki = 8.42 nM 8.07
CHEMBL2028907 Ki = 21.0 nM 7.68
CHEMBL3143135 Ki = 34.0 nM 7.47
CHEMBL3143130 Ki = 61.0 nM 7.21
CHEMBL2028906 Ki = 72.0 nM 7.14
CHEMBL2028913 Ki = 100.0 nM 7.00