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Assay Detail

CHEMBL871199

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

Binding
Inhibition of human cathepsin B
25
Total Activities
25
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

Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.
Palmer JT, Hirschbein BL, Cheung H, McCarter J, Janc JW, Yu ZW, Wesolowski G.
Bioorg Med Chem Lett (2006) 16 : 2909 -2914
PubMed 16546382 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 5.73 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207347 1 8.70
CHEMBL378899 1 7.12
CHEMBL379622 1 7.03
CHEMBL405602 1 7.01
CHEMBL209215 1 6.66
CHEMBL209114 1 6.57
CHEMBL210535 1 6.37
CHEMBL209293 1 6.14
CHEMBL379157 1 6.02
CHEMBL208566 1 5.96
CHEMBL376994 1 5.68
CHEMBL209216 1 5.14
CHEMBL209181 1 5.00
CHEMBL210702 1 4.80
CHEMBL208577 1 4.64
CHEMBL210712 1 4.60
CHEMBL210759 1 4.47
CHEMBL210625 1 4.32
CHEMBL210198 1 4.24
CHEMBL211050 1 4.14
CHEMBL210523 1 -
CHEMBL209294 1 -
CHEMBL210315 1 -
CHEMBL378780 1 -
CHEMBL209766 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207347 Ki = 2.0 nM 8.70
CHEMBL378899 Ki = 75.0 nM 7.12
CHEMBL379622 Ki = 93.0 nM 7.03
CHEMBL405602 Ki = 98.0 nM 7.01
CHEMBL209215 Ki = 220.0 nM 6.66
CHEMBL209114 Ki = 270.0 nM 6.57
CHEMBL210535 Ki = 430.0 nM 6.37
CHEMBL209293 Ki = 730.0 nM 6.14
CHEMBL379157 Ki = 950.0 nM 6.02
CHEMBL208566 Ki = 1100.0 nM 5.96
CHEMBL376994 Ki = 2100.0 nM 5.68
CHEMBL209216 Ki = 7300.0 nM 5.14
CHEMBL209181 Ki = 10000.0 nM 5.00
CHEMBL210702 Ki = 16000.0 nM 4.80
CHEMBL208577 Ki = 23000.0 nM 4.64
CHEMBL210712 Ki = 25000.0 nM 4.60
CHEMBL210759 Ki = 34000.0 nM 4.47
CHEMBL210625 Ki = 48000.0 nM 4.32
CHEMBL210198 Ki = 57000.0 nM 4.24
CHEMBL211050 Ki = 73000.0 nM 4.14
CHEMBL210523 Ki > 150000.0 nM -
CHEMBL209294 Ki = 110000.0 nM -
CHEMBL210315 Ki = 120000.0 nM -
CHEMBL378780 Ki > 150000.0 nM -
CHEMBL209766 Ki > 150000.0 nM -