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Assay Detail

CHEMBL988573

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

Functional
Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MES-SA
Confidence 1 — Organism
Curated By Autocuration

Target

NON-PROTEIN TARGET (CHEMBL3879801) ↗
Type NON-MOLECULAR

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 6.67 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL489658 — — 1 7.55
CHEMBL521913 — — 1 7.52
CHEMBL489263 — — 1 7.33
CHEMBL489864 — — 1 7.27
CHEMBL484004 — — 1 7.18
CHEMBL500031 — — 1 7.16
CHEMBL521492 — — 1 7.12
CHEMBL522449 — — 1 7.11
CHEMBL483738 — — 1 7.09
CHEMBL484788 — — 1 7.09
CHEMBL520328 — — 1 6.96
CHEMBL484596 — — 1 6.92
CHEMBL484159 — — 1 6.91
CHEMBL482574 — — 1 6.90
CHEMBL484156 — — 1 6.84
CHEMBL451324 — — 1 6.83
CHEMBL484003 — — 1 6.81
CHEMBL484175 — — 1 6.80
CHEMBL471470 — — 1 6.79
CHEMBL482560 — — 1 6.74
CHEMBL490465 — — 1 6.69
CHEMBL449550 — — 1 6.66
CHEMBL484157 — — 1 6.58
CHEMBL483739 — — 1 6.57
CHEMBL445540 — — 1 6.57
CHEMBL484591 — — 1 6.56
CHEMBL491073 — — 1 6.54
CHEMBL491463 — — 1 6.51
CHEMBL521448 — — 1 6.45
CHEMBL484406 — — 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL489658 — IC50 = 28.0 nM 7.55
CHEMBL521913 — IC50 = 30.0 nM 7.52
CHEMBL489263 — IC50 = 47.0 nM 7.33
CHEMBL489864 — IC50 = 54.0 nM 7.27
CHEMBL484004 — IC50 = 66.0 nM 7.18
CHEMBL500031 — IC50 = 70.0 nM 7.16
CHEMBL521492 — IC50 = 75.0 nM 7.12
CHEMBL522449 — IC50 = 77.0 nM 7.11
CHEMBL483738 — IC50 = 82.0 nM 7.09
CHEMBL484788 — IC50 = 82.0 nM 7.09
CHEMBL520328 — IC50 = 110.0 nM 6.96
CHEMBL484596 — IC50 = 120.0 nM 6.92
CHEMBL484159 — IC50 = 123.0 nM 6.91
CHEMBL482574 — IC50 = 125.0 nM 6.90
CHEMBL484156 — IC50 = 145.0 nM 6.84
CHEMBL451324 — IC50 = 147.0 nM 6.83
CHEMBL484003 — IC50 = 155.0 nM 6.81
CHEMBL484175 — IC50 = 159.0 nM 6.80
CHEMBL471470 — IC50 = 164.0 nM 6.79
CHEMBL482560 — IC50 = 181.0 nM 6.74
CHEMBL490465 — IC50 = 205.0 nM 6.69
CHEMBL449550 — IC50 = 219.0 nM 6.66
CHEMBL484157 — IC50 = 260.0 nM 6.58
CHEMBL483739 — IC50 = 269.0 nM 6.57
CHEMBL445540 — IC50 = 271.0 nM 6.57
CHEMBL484591 — IC50 = 276.0 nM 6.56
CHEMBL491073 — IC50 = 286.0 nM 6.54
CHEMBL491463 — IC50 = 308.0 nM 6.51
CHEMBL521448 — IC50 = 353.0 nM 6.45
CHEMBL484406 — IC50 = 366.0 nM 6.44
CHEMBL483360 — IC50 = 367.0 nM 6.43
CHEMBL451887 CARFILZOMIB IC50 = 413.0 nM 6.38
CHEMBL505395 — IC50 = 421.0 nM 6.38
CHEMBL521174 — IC50 = 468.0 nM 6.33
CHEMBL484787 — IC50 = 505.0 nM 6.30
CHEMBL446227 — IC50 = 543.0 nM 6.26
CHEMBL483361 — IC50 = 636.0 nM 6.20
CHEMBL484002 — IC50 = 756.0 nM 6.12
CHEMBL501903 — IC50 = 841.0 nM 6.08
CHEMBL485150 — IC50 = 941.0 nM 6.03
CHEMBL509277 — IC50 = 1145.0 nM 5.94
CHEMBL483740 — IC50 = 1157.0 nM 5.94
CHEMBL483340 — IC50 = 1322.0 nM 5.88
CHEMBL504618 — IC50 > 1000.0 nM -
CHEMBL451371 — IC50 > 1000.0 nM -
CHEMBL507109 — IC50 > 1000.0 nM -
CHEMBL499471 — IC50 > 1000.0 nM -
CHEMBL508076 — IC50 > 1000.0 nM -
CHEMBL490466 — IC50 > 1000.0 nM -
CHEMBL483553 — IC50 > 1000.0 nM -