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Assay Detail

CHEMBL864422

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Binding
Inhibition of Cathepsin L
28
Total Activities
28
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

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of a potent and selective non-basic cathepsin K inhibitor.
Li CS, Deschenes D, Desmarais S, Falgueyret JP, Gauthier JY, Kimmel DB, Léger S, Massé F, McGrath ME, McKay DJ, Percival MD, Riendeau D, Rodan SB, Thérien M, Truong VL, Wesolowski G, Zamboni R, Black WC.
Bioorg Med Chem Lett (2006) 16 : 1985 -1989
PubMed 16413777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.21 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL204277 1 7.89
CHEMBL204276 1 7.47
CHEMBL195454 1 7.33
CHEMBL206024 1 7.10
CHEMBL437501 1 6.58
CHEMBL382038 1 6.50
CHEMBL377285 1 6.47
CHEMBL380425 1 6.46
CHEMBL207554 1 6.33
CHEMBL437694 1 6.28
CHEMBL203944 1 6.25
CHEMBL206913 1 6.11
CHEMBL208278 1 6.09
CHEMBL381758 1 6.06
CHEMBL205929 1 6.05
CHEMBL205504 1 6.00
CHEMBL204792 1 5.83
CHEMBL206912 1 5.83
CHEMBL381621 1 5.83
CHEMBL382576 1 5.78
CHEMBL378583 1 5.73
CHEMBL426493 1 5.72
CHEMBL206169 1 5.71
CHEMBL382820 1 5.62
CHEMBL207769 1 5.55
CHEMBL207891 1 5.52
CHEMBL208481 1 5.52
CHEMBL206166 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL204277 IC50 = 13.0 nM 7.89
CHEMBL204276 IC50 = 34.0 nM 7.47
CHEMBL195454 IC50 = 47.0 nM 7.33
CHEMBL206024 IC50 = 80.0 nM 7.10
CHEMBL437501 IC50 = 264.0 nM 6.58
CHEMBL382038 IC50 = 314.0 nM 6.50
CHEMBL377285 IC50 = 342.0 nM 6.47
CHEMBL380425 IC50 = 344.0 nM 6.46
CHEMBL207554 IC50 = 470.0 nM 6.33
CHEMBL437694 IC50 = 524.0 nM 6.28
CHEMBL203944 IC50 = 560.0 nM 6.25
CHEMBL206913 IC50 = 771.0 nM 6.11
CHEMBL208278 IC50 = 809.0 nM 6.09
CHEMBL381758 IC50 = 878.0 nM 6.06
CHEMBL205929 IC50 = 887.0 nM 6.05
CHEMBL205504 IC50 = 1001.0 nM 6.00
CHEMBL204792 IC50 = 1473.0 nM 5.83
CHEMBL206912 IC50 = 1480.0 nM 5.83
CHEMBL381621 IC50 = 1475.0 nM 5.83
CHEMBL382576 IC50 = 1670.0 nM 5.78
CHEMBL378583 IC50 = 1857.0 nM 5.73
CHEMBL426493 IC50 = 1915.0 nM 5.72
CHEMBL206169 IC50 = 1950.0 nM 5.71
CHEMBL382820 IC50 = 2422.0 nM 5.62
CHEMBL207769 IC50 = 2792.0 nM 5.55
CHEMBL207891 IC50 = 3047.0 nM 5.52
CHEMBL208481 IC50 = 3002.0 nM 5.52
CHEMBL206166 IC50 > 10000.0 nM -