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Assay Detail

CHEMBL5378739

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Functional
Antiproliferative activity against human HCT-116 cells harboring p53 assessed inhibition of cell growth incubated for 4 days by CCK-8 assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HCT-116
Confidence 1 — Organism
Curated By Autocuration

Target

HCT-116 (CHEMBL394)
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 33 7.09 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5404903 1 8.89
CHEMBL5424005 1 8.82
CHEMBL5405147 1 8.44
CHEMBL5436246 1 8.31
CHEMBL5402394 1 8.27
CHEMBL5433398 1 8.00
CHEMBL5395046 1 7.96
CHEMBL5413376 1 7.96
CHEMBL5440363 1 7.66
CHEMBL5405392 1 7.66
CHEMBL5431530 1 7.59
CHEMBL5405110 1 7.51
CHEMBL5397752 1 7.49
CHEMBL5403772 1 7.43
CHEMBL5441014 1 7.37
CHEMBL5414460 1 7.29
CHEMBL5436528 1 7.12
CHEMBL5396046 1 6.99
CHEMBL5421232 1 6.86
CHEMBL5406959 1 6.84
CHEMBL5398827 1 6.83
CHEMBL5438528 1 6.50
CHEMBL5404372 1 6.25
CHEMBL5423725 1 6.25
CHEMBL5400878 1 6.18
CHEMBL5403609 1 6.06
CHEMBL5408617 1 6.03
CHEMBL5401273 1 6.02
CHEMBL191334 NUTLIN-3 1 5.98
CHEMBL5437702 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5404903 IC50 = 1.3 nM 8.89
CHEMBL5424005 IC50 = 1.5 nM 8.82
CHEMBL5405147 IC50 = 3.6 nM 8.44
CHEMBL5436246 IC50 = 4.9 nM 8.31
CHEMBL5402394 IC50 = 5.4 nM 8.27
CHEMBL5433398 IC50 = 10.0 nM 8.00
CHEMBL5395046 IC50 = 11.0 nM 7.96
CHEMBL5413376 IC50 = 11.0 nM 7.96
CHEMBL5440363 IC50 = 22.0 nM 7.66
CHEMBL5405392 IC50 = 21.7 nM 7.66
CHEMBL5431530 IC50 = 25.7 nM 7.59
CHEMBL5405110 IC50 = 31.0 nM 7.51
CHEMBL5397752 IC50 = 32.7 nM 7.49
CHEMBL5403772 IC50 = 37.3 nM 7.43
CHEMBL5441014 IC50 = 42.3 nM 7.37
CHEMBL5414460 IC50 = 51.7 nM 7.29
CHEMBL5436528 IC50 = 75.5 nM 7.12
CHEMBL5396046 IC50 = 103.0 nM 6.99
CHEMBL5421232 IC50 = 138.0 nM 6.86
CHEMBL5406959 IC50 = 144.0 nM 6.84
CHEMBL5398827 IC50 = 149.0 nM 6.83
CHEMBL5438528 IC50 = 318.0 nM 6.50
CHEMBL5404372 IC50 = 558.0 nM 6.25
CHEMBL5423725 IC50 = 565.0 nM 6.25
CHEMBL5400878 IC50 = 667.0 nM 6.18
CHEMBL5403609 IC50 = 865.0 nM 6.06
CHEMBL5408617 IC50 = 927.0 nM 6.03
CHEMBL5401273 IC50 = 951.0 nM 6.02
CHEMBL191334 NUTLIN-3 IC50 = 1038.0 nM 5.98
CHEMBL5437702 IC50 = 1043.0 nM 5.98
CHEMBL5423147 IC50 = 1400.0 nM 5.85
CHEMBL5411556 IC50 = 1559.0 nM 5.81
CHEMBL5394717 IC50 = 2038.0 nM 5.69