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Assay Detail

CHEMBL829134

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

Binding
Inhibition of 10 lM Cbz-Phe-Arg-AMC binding to human cathepsin B activity in fluorescence assay with 100 mM NaOAc
17
Total Activities
17
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 B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Barrett DG, Boncek VM, Catalano JG, Deaton DN, Hassell AM, Jurgensen CH, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Ray JA, Samano V, Shewchuk LM, Tavares FX, Wells-Knecht KJ, Willard DH, Wright LL, Zhou HQ.
Bioorg Med Chem Lett (2005) 15 : 3540 -3546
PubMed 15982880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.71 5.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365822 1 5.28
CHEMBL426617 1 5.21
CHEMBL188438 1 5.01
CHEMBL190053 1 5.00
CHEMBL186778 1 4.92
CHEMBL189417 1 4.75
CHEMBL234367 1 4.70
CHEMBL191584 1 4.57
CHEMBL189604 1 4.51
CHEMBL363773 1 4.50
CHEMBL188400 1 4.35
CHEMBL188563 1 4.25
CHEMBL191178 1 4.22
CHEMBL186149 1 -
CHEMBL188929 1 -
CHEMBL187864 1 -
CHEMBL365049 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365822 IC50 = 5200.0 nM 5.28
CHEMBL426617 IC50 = 6200.0 nM 5.21
CHEMBL188438 IC50 = 9800.0 nM 5.01
CHEMBL190053 IC50 = 10000.0 nM 5.00
CHEMBL186778 IC50 = 12000.0 nM 4.92
CHEMBL189417 IC50 = 18000.0 nM 4.75
CHEMBL234367 IC50 = 20000.0 nM 4.70
CHEMBL191584 IC50 = 27000.0 nM 4.57
CHEMBL189604 IC50 = 31000.0 nM 4.51
CHEMBL363773 IC50 = 32000.0 nM 4.50
CHEMBL188400 IC50 = 45000.0 nM 4.35
CHEMBL188563 IC50 = 56000.0 nM 4.25
CHEMBL191178 IC50 = 60000.0 nM 4.22
CHEMBL186149 IC50 = 3500000.0 nM -
CHEMBL188929 IC50 = 107000.0 nM -
CHEMBL187864 IC50 = 870000.0 nM -
CHEMBL365049 IC50 = 870000.0 nM -