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Assay Detail

CHEMBL5378748

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Functional
Antiproliferative activity against human U2OS cells harboring p53 assessed inhibition of cell growth incubated for 4 days by celltiter-glo assay
19
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U2OS
Confidence 1 — Organism
Curated By Autocuration

Target

U2OS (CHEMBL615023)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
Cheng J, Yan Z, Jiang K, Liu C, Xu D, Lyu X, Hu X, Zhang S, Zhou Y, Li J, Zhao Y.
J Med Chem (2023) 66 : 16991 -17025
PubMed 38062557 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.41 7.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425989 2 7.97
CHEMBL5408617 1 7.97
CHEMBL5438520 1 6.96
CHEMBL5413376 1 6.81
CHEMBL5395046 1 6.59
CHEMBL5431530 1 6.52
CHEMBL5405147 1 6.42
CHEMBL5402394 1 6.24
CHEMBL5406959 1 6.20
CHEMBL5405110 1 6.20
CHEMBL5436528 1 6.19
CHEMBL5403772 1 6.12
CHEMBL5398827 1 6.01
CHEMBL5400878 1 5.90
CHEMBL5421232 1 5.80
CHEMBL5423147 1 5.73
CHEMBL5394717 1 5.55
CHEMBL5403609 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425989 IC50 = 10.8 nM 7.97
CHEMBL5408617 IC50 = 10.8 nM 7.97
CHEMBL5425989 IC50 = 67.0 nM 7.17
CHEMBL5438520 IC50 = 109.0 nM 6.96
CHEMBL5413376 IC50 = 156.0 nM 6.81
CHEMBL5395046 IC50 = 254.0 nM 6.59
CHEMBL5431530 IC50 = 304.0 nM 6.52
CHEMBL5405147 IC50 = 376.0 nM 6.42
CHEMBL5402394 IC50 = 574.0 nM 6.24
CHEMBL5406959 IC50 = 625.0 nM 6.20
CHEMBL5405110 IC50 = 634.0 nM 6.20
CHEMBL5436528 IC50 = 647.0 nM 6.19
CHEMBL5403772 IC50 = 752.0 nM 6.12
CHEMBL5398827 IC50 = 985.0 nM 6.01
CHEMBL5400878 IC50 = 1271.0 nM 5.90
CHEMBL5421232 IC50 = 1580.0 nM 5.80
CHEMBL5423147 IC50 = 1845.0 nM 5.73
CHEMBL5394717 IC50 = 2820.0 nM 5.55
CHEMBL5403609 IC50 = 3410.0 nM 5.47