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Assay Detail

CHEMBL861977

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Binding
Inhibition of cathepsin S
ChEMBL ↗
56
Total Activities
56
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin S (CHEMBL2954) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of subsite binding to the beta5 subunit of the human 20S proteasome using vinyl sulfones and 2-keto-1,3,4-oxadiazoles: syntheses and cellular properties of potent, selective proteasome inhibitors.
Rydzewski RM, Burrill L, Mendonca R, Palmer JT, Rice M, Tahilramani R, Bass KE, Leung L, Gjerstad E, Janc JW, Pan L.
J Med Chem (2006) 49 : 2953 -2968
PubMed 16686537 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 4.96 6.82
Ki app 14 - -
Ki 3 5.61 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206525 — — 1 7.34
CHEMBL379669 — — 1 6.82
CHEMBL207403 — — 1 6.16
CHEMBL208015 — — 1 5.52
CHEMBL438612 — — 1 5.48
CHEMBL207579 — — 1 5.16
CHEMBL207196 — — 1 5.15
CHEMBL377532 — — 1 5.09
CHEMBL207284 — — 1 5.05
CHEMBL446443 — — 1 5.00
CHEMBL377123 — — 1 4.92
CHEMBL209243 — — 1 4.92
CHEMBL207670 — — 1 4.89
CHEMBL383730 — — 1 4.89
CHEMBL208019 — — 1 4.68
CHEMBL207990 EPOXOMYCIN — 1 4.60
CHEMBL379772 — — 1 4.46
CHEMBL207162 — — 1 4.44
CHEMBL383674 — — 1 4.41
CHEMBL437115 — — 1 4.39
CHEMBL382180 — — 1 4.32
CHEMBL207016 — — 1 4.17
CHEMBL438442 — — 1 4.11
CHEMBL381089 — — 1 -
CHEMBL383673 — — 1 -
CHEMBL207394 — — 1 -
CHEMBL381884 — — 1 -
CHEMBL376815 — — 1 -
CHEMBL204992 — — 1 -
CHEMBL206206 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206525 — Ki = 46.0 nM 7.34
CHEMBL379669 — IC50 = 150.0 nM 6.82
CHEMBL207403 — IC50 = 700.0 nM 6.16
CHEMBL208015 — IC50 = 3000.0 nM 5.52
CHEMBL438612 — IC50 = 3300.0 nM 5.48
CHEMBL207579 — IC50 = 6900.0 nM 5.16
CHEMBL207196 — IC50 = 7100.0 nM 5.15
CHEMBL377532 — Ki = 8100.0 nM 5.09
CHEMBL207284 — IC50 = 9000.0 nM 5.05
CHEMBL446443 — IC50 = 10000.0 nM 5.00
CHEMBL377123 — IC50 = 12000.0 nM 4.92
CHEMBL209243 — IC50 = 12000.0 nM 4.92
CHEMBL207670 — IC50 = 13000.0 nM 4.89
CHEMBL383730 — IC50 = 13000.0 nM 4.89
CHEMBL208019 — IC50 = 21000.0 nM 4.68
CHEMBL207990 EPOXOMYCIN IC50 = 25000.0 nM 4.60
CHEMBL379772 — IC50 = 35000.0 nM 4.46
CHEMBL207162 — IC50 = 36000.0 nM 4.44
CHEMBL383674 — Ki = 39000.0 nM 4.41
CHEMBL437115 — IC50 = 41000.0 nM 4.39
CHEMBL382180 — IC50 = 48000.0 nM 4.32
CHEMBL207016 — IC50 = 67000.0 nM 4.17
CHEMBL438442 — IC50 = 77000.0 nM 4.11
CHEMBL208159 — IC50 - — -
CHEMBL379771 — IC50 - — -
CHEMBL207425 — Ki app - — -
CHEMBL204946 — IC50 > 150000.0 nM -
CHEMBL383529 — IC50 = 170000.0 nM -
CHEMBL207591 — Ki app - — -
CHEMBL64925 MG-132 Ki app - — -
CHEMBL114388 — Ki app - — -
CHEMBL379476 — Ki app - — -
CHEMBL381931 — Ki app - — -
CHEMBL437311 — Ki app - — -
CHEMBL206001 — IC50 - — -
CHEMBL207598 — Ki app - — -
CHEMBL204518 — IC50 - — -
CHEMBL207669 — IC50 - — -
CHEMBL437882 — IC50 - — -
CHEMBL382203 — IC50 - — -
CHEMBL378901 — IC50 - — -
CHEMBL381735 — IC50 - — -
CHEMBL207336 — IC50 - — -
CHEMBL206206 — IC50 - — -
CHEMBL204992 — IC50 - — -
CHEMBL376815 — IC50 - — -
CHEMBL381884 — IC50 - — -
CHEMBL207394 — IC50 - — -
CHEMBL383673 — IC50 - — -
CHEMBL381089 — IC50 - — -