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Assay Detail

CHEMBL4413409

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
10
Total Activities
10
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

Exploration of novel macrocyclic dipeptide N-benzyl amides as proteasome inhibitors.
Yu J, Liu J, Li D, Xu L, Hong D, Chang S, Xu L, Li J, Liu T, Zhou Y.
Eur J Med Chem (2019) 164 : 423 -439
PubMed 30611983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.43 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451887 CARFILZOMIB 4.0 1 8.70
CHEMBL4442152 1 7.82
CHEMBL4542139 1 7.75
CHEMBL2103884 OPROZOMIB 2.0 1 7.72
CHEMBL4538960 1 7.57
CHEMBL4456389 1 7.24
CHEMBL4549674 1 7.23
CHEMBL4438865 1 7.01
CHEMBL4461175 1 6.76
CHEMBL4588117 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451887 CARFILZOMIB IC50 = 2.0 nM 8.70
CHEMBL4442152 IC50 = 15.0 nM 7.82
CHEMBL4542139 IC50 = 18.0 nM 7.75
CHEMBL2103884 OPROZOMIB IC50 = 19.0 nM 7.72
CHEMBL4538960 IC50 = 27.0 nM 7.57
CHEMBL4456389 IC50 = 58.0 nM 7.24
CHEMBL4549674 IC50 = 59.0 nM 7.23
CHEMBL4438865 IC50 = 97.0 nM 7.01
CHEMBL4461175 IC50 = 175.0 nM 6.76
CHEMBL4588117 IC50 = 301.0 nM 6.52