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Assay Detail

CHEMBL861978

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Functional
Antiproliferative activity against human PC3 cell line
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-3
Confidence 1 — Organism
Curated By Expert

Target

PC-3 (CHEMBL390)
Type CELL-LINE
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 30 6.10 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207990 EPOXOMYCIN 1 9.00
CHEMBL383674 1 6.70
CHEMBL382203 1 6.70
CHEMBL207591 1 6.43
CHEMBL379772 1 6.35
CHEMBL376815 1 6.30
CHEMBL207016 1 6.30
CHEMBL381735 1 6.26
CHEMBL64925 MG-132 1 6.22
CHEMBL446443 1 6.22
CHEMBL207403 1 6.10
CHEMBL207336 1 5.76
CHEMBL207162 1 5.70
CHEMBL204946 1 5.62
CHEMBL206206 1 5.52
CHEMBL379669 1 5.52
CHEMBL379771 1 5.49
CHEMBL204992 1 5.40
CHEMBL208015 1 5.19
CHEMBL383529 1 5.12
CHEMBL207196 1 -
CHEMBL205757 1 -
CHEMBL205687 1 -
CHEMBL206413 1 -
CHEMBL437115 1 -
CHEMBL438612 1 -
CHEMBL206001 1 -
CHEMBL207669 1 -
CHEMBL208372 1 -
CHEMBL377532 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207990 EPOXOMYCIN IC50 = 1.0 nM 9.00
CHEMBL383674 IC50 = 200.0 nM 6.70
CHEMBL382203 IC50 = 200.0 nM 6.70
CHEMBL207591 IC50 = 375.0 nM 6.43
CHEMBL379772 IC50 = 450.0 nM 6.35
CHEMBL376815 IC50 = 500.0 nM 6.30
CHEMBL207016 IC50 = 500.0 nM 6.30
CHEMBL381735 IC50 = 550.0 nM 6.26
CHEMBL64925 MG-132 IC50 = 600.0 nM 6.22
CHEMBL446443 IC50 = 600.0 nM 6.22
CHEMBL207403 IC50 = 800.0 nM 6.10
CHEMBL207336 IC50 = 1750.0 nM 5.76
CHEMBL207162 IC50 = 2000.0 nM 5.70
CHEMBL204946 IC50 = 2400.0 nM 5.62
CHEMBL206206 IC50 = 3000.0 nM 5.52
CHEMBL379669 IC50 = 3000.0 nM 5.52
CHEMBL379771 IC50 = 3250.0 nM 5.49
CHEMBL204992 IC50 = 4000.0 nM 5.40
CHEMBL208015 IC50 = 6500.0 nM 5.19
CHEMBL383529 IC50 = 7500.0 nM 5.12
CHEMBL207196 IC50 - -
CHEMBL205757 IC50 - -
CHEMBL205687 IC50 - -
CHEMBL206413 IC50 - -
CHEMBL437115 IC50 = 3000000.0 nM -
CHEMBL438612 IC50 = 5000000.0 nM -
CHEMBL206001 IC50 - -
CHEMBL207669 IC50 - -
CHEMBL208372 IC50 - -
CHEMBL377532 IC50 - -