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Assay Detail

CHEMBL988568

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

Binding
Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MOLT-4
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Design and synthesis of an orally bioavailable and selective peptide epoxyketone proteasome inhibitor (PR-047).
Zhou HJ, Aujay MA, Bennett MK, Dajee M, Demo SD, Fang Y, Ho MN, Jiang J, Kirk CJ, Laidig GJ, Lewis ER, Lu Y, Muchamuel T, Parlati F, Ring E, Shenk KD, Shields J, Shwonek PJ, Stanton T, Sun CM, Sylvain C, Woo TM, Yang J.
J Med Chem (2009) 52 : 3028 -3038
PubMed 19348473 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 7.30 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489864 — — 1 8.52
CHEMBL451887 CARFILZOMIB 4.0 1 8.29
CHEMBL489658 — — 1 8.09
CHEMBL445540 — — 1 8.07
CHEMBL483739 — — 1 8.00
CHEMBL500031 — — 1 7.96
CHEMBL504618 — — 1 7.85
CHEMBL489263 — — 1 7.77
CHEMBL521913 — — 1 7.77
CHEMBL483360 — — 1 7.60
CHEMBL451324 — — 1 7.58
CHEMBL446227 — — 1 7.57
CHEMBL451371 — — 1 7.52
CHEMBL505395 — — 1 7.51
CHEMBL483738 — — 1 7.50
CHEMBL484003 — — 1 7.46
CHEMBL484004 — — 1 7.46
CHEMBL521492 — — 1 7.44
CHEMBL484596 — — 1 7.40
CHEMBL484406 — — 1 7.39
CHEMBL509277 — — 1 7.38
CHEMBL491463 — — 1 7.35
CHEMBL482560 — — 1 7.34
CHEMBL490466 — — 1 7.33
CHEMBL484002 — — 1 7.33
CHEMBL484156 — — 1 7.32
CHEMBL484159 — — 1 7.30
CHEMBL511313 — — 1 7.30
CHEMBL471674 — — 1 7.26
CHEMBL522449 — — 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489864 — IC50 = 3.0 nM 8.52
CHEMBL451887 CARFILZOMIB IC50 = 5.1 nM 8.29
CHEMBL489658 — IC50 = 8.1 nM 8.09
CHEMBL445540 — IC50 = 8.6 nM 8.07
CHEMBL483739 — IC50 = 10.0 nM 8.00
CHEMBL500031 — IC50 = 11.0 nM 7.96
CHEMBL504618 — IC50 = 14.0 nM 7.85
CHEMBL489263 — IC50 = 17.0 nM 7.77
CHEMBL521913 — IC50 = 17.0 nM 7.77
CHEMBL483360 — IC50 = 25.0 nM 7.60
CHEMBL451324 — IC50 = 26.0 nM 7.58
CHEMBL446227 — IC50 = 27.0 nM 7.57
CHEMBL451371 — IC50 = 30.0 nM 7.52
CHEMBL505395 — IC50 = 31.0 nM 7.51
CHEMBL483738 — IC50 = 32.0 nM 7.50
CHEMBL484003 — IC50 = 35.0 nM 7.46
CHEMBL484004 — IC50 = 35.0 nM 7.46
CHEMBL521492 — IC50 = 36.0 nM 7.44
CHEMBL484596 — IC50 = 40.0 nM 7.40
CHEMBL484406 — IC50 = 41.0 nM 7.39
CHEMBL509277 — IC50 = 42.0 nM 7.38
CHEMBL491463 — IC50 = 45.0 nM 7.35
CHEMBL482560 — IC50 = 46.0 nM 7.34
CHEMBL490466 — IC50 = 47.0 nM 7.33
CHEMBL484002 — IC50 = 47.0 nM 7.33
CHEMBL484156 — IC50 = 48.0 nM 7.32
CHEMBL511313 — IC50 = 50.0 nM 7.30
CHEMBL484159 — IC50 = 50.0 nM 7.30
CHEMBL471674 — IC50 = 55.0 nM 7.26
CHEMBL522449 — IC50 = 56.0 nM 7.25
CHEMBL484591 — IC50 = 57.0 nM 7.24
CHEMBL501903 — IC50 = 59.0 nM 7.23
CHEMBL499471 — IC50 = 59.0 nM 7.23
CHEMBL508076 — IC50 = 62.0 nM 7.21
CHEMBL484788 — IC50 = 65.0 nM 7.19
CHEMBL483340 — IC50 = 66.0 nM 7.18
CHEMBL491073 — IC50 = 69.0 nM 7.16
CHEMBL521448 — IC50 = 78.0 nM 7.11
CHEMBL449550 — IC50 = 78.0 nM 7.11
CHEMBL484787 — IC50 = 84.0 nM 7.08
CHEMBL485150 — IC50 = 91.0 nM 7.04
CHEMBL482574 — IC50 = 116.0 nM 6.94
CHEMBL507109 — IC50 = 124.0 nM 6.91
CHEMBL483361 — IC50 = 147.0 nM 6.83
CHEMBL520328 — IC50 = 154.0 nM 6.81
CHEMBL471470 — IC50 = 161.0 nM 6.79
CHEMBL483740 — IC50 = 164.0 nM 6.79
CHEMBL484157 — IC50 = 168.0 nM 6.78
CHEMBL484175 — IC50 = 180.0 nM 6.75
CHEMBL484920 — IC50 = 188.0 nM 6.73