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Assay Detail

CHEMBL5159801

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

Functional
Antiproliferative activity against human RPMI-8226 cells after 72 hrs by MTS assay
14
Total Activities
14
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

Metabolism guided optimization of peptidomimetics as non-covalent proteasome inhibitors for cancer treatment.
Cao Y, Tu Y, Fu L, Yu Q, Gao L, Zhang M, Zeng L, Zhang C, Shao J, Zhu H, Zhou Y, Li J, Zhang J.
Eur J Med Chem (2022) 233 : 114211 -114211
PubMed 35218994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.64 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5204484 1 8.20
CHEMBL4102324 1 7.99
CHEMBL5197285 1 7.92
CHEMBL5179570 1 7.82
CHEMBL5208573 1 7.70
CHEMBL5188065 1 7.68
CHEMBL5202627 1 7.68
CHEMBL5172645 1 7.62
CHEMBL5201055 1 7.58
CHEMBL5173459 1 7.47
CHEMBL5171225 1 7.39
CHEMBL5186240 1 7.22
CHEMBL5209077 1 7.09
CHEMBL5196378 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5204484 IC50 = 6.347 nM 8.20
CHEMBL4102324 IC50 = 10.21 nM 7.99
CHEMBL5197285 IC50 = 12.08 nM 7.92
CHEMBL5179570 IC50 = 15.29 nM 7.82
CHEMBL5208573 IC50 = 19.94 nM 7.70
CHEMBL5188065 IC50 = 20.66 nM 7.68
CHEMBL5202627 IC50 = 20.81 nM 7.68
CHEMBL5172645 IC50 = 24.01 nM 7.62
CHEMBL5201055 IC50 = 26.18 nM 7.58
CHEMBL5173459 IC50 = 33.71 nM 7.47
CHEMBL5171225 IC50 = 40.73 nM 7.39
CHEMBL5186240 IC50 = 60.4 nM 7.22
CHEMBL5209077 IC50 = 81.69 nM 7.09
CHEMBL5196378 IC50 > 100.0 nM -