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Assay Detail

CHEMBL4371709

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

Functional
Antiproliferative activity against human RPMI8226 cells after 72 hrs by MTS assay
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RPMI-8226
Confidence 1 — Organism
Curated By Autocuration

Target

RPMI-8226 (CHEMBL614882)
Type CELL-LINE
Organism Homo sapiens

Publication

Development of Macrocyclic Peptides Containing Epoxyketone with Oral Availability as Proteasome Inhibitors.
Li D, Zhang X, Ma X, Xu L, Yu J, Gao L, Hu X, Zhang J, Dong X, Li J, Liu T, Zhou Y, Hu Y.
J Med Chem (2018) 61 : 9177 -9204
PubMed 30265557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 7.69 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4471209 1 8.70
CHEMBL4469081 1 8.52
CHEMBL4434719 1 8.52
CHEMBL4541096 1 8.30
CHEMBL4580102 1 8.30
CHEMBL4434736 1 8.30
CHEMBL4546156 1 8.00
CHEMBL4448256 1 7.89
CHEMBL2103884 OPROZOMIB 2.0 1 7.72
CHEMBL4559176 1 7.70
CHEMBL4465844 1 7.50
CHEMBL4453760 1 7.26
CHEMBL4472844 1 7.14
CHEMBL4585963 1 7.13
CHEMBL4536411 1 7.09
CHEMBL4536022 1 6.92
CHEMBL4536377 1 6.89
CHEMBL4466983 1 6.46
CHEMBL4440926 1 -
CHEMBL4565982 1 -
CHEMBL4449200 1 -
CHEMBL4560321 1 -
CHEMBL4592762 1 -
CHEMBL4458777 1 -
CHEMBL4591075 1 -
CHEMBL4444275 1 -
CHEMBL4530484 1 -
CHEMBL4464002 1 -
CHEMBL4449881 1 -
CHEMBL4447069 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4471209 IC50 = 2.0 nM 8.70
CHEMBL4469081 IC50 = 3.0 nM 8.52
CHEMBL4434719 IC50 = 3.0 nM 8.52
CHEMBL4541096 IC50 = 5.0 nM 8.30
CHEMBL4580102 IC50 = 5.0 nM 8.30
CHEMBL4434736 IC50 = 5.0 nM 8.30
CHEMBL4546156 IC50 = 10.0 nM 8.00
CHEMBL4448256 IC50 = 13.0 nM 7.89
CHEMBL2103884 OPROZOMIB IC50 = 19.0 nM 7.72
CHEMBL4559176 IC50 = 20.0 nM 7.70
CHEMBL4465844 IC50 = 32.0 nM 7.50
CHEMBL4453760 IC50 = 55.0 nM 7.26
CHEMBL4472844 IC50 = 73.0 nM 7.14
CHEMBL4585963 IC50 = 74.0 nM 7.13
CHEMBL4536411 IC50 = 82.0 nM 7.09
CHEMBL4536022 IC50 = 120.0 nM 6.92
CHEMBL4536377 IC50 = 128.0 nM 6.89
CHEMBL4466983 IC50 = 350.0 nM 6.46
CHEMBL4440926 IC50 > 100.0 nM -
CHEMBL4565982 IC50 > 100.0 nM -
CHEMBL4449200 IC50 > 100.0 nM -
CHEMBL4560321 IC50 > 100.0 nM -
CHEMBL4592762 IC50 - -
CHEMBL4458777 IC50 - -
CHEMBL4591075 IC50 > 100.0 nM -
CHEMBL4444275 IC50 > 100.0 nM -
CHEMBL4530484 IC50 > 100.0 nM -
CHEMBL4464002 IC50 > 100.0 nM -
CHEMBL4449881 IC50 > 100.0 nM -
CHEMBL4447069 IC50 - -
CHEMBL4461405 IC50 - -