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Assay Detail

CHEMBL5378737

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Binding
Inhibition of MDM2 (1 to 118 residues)/p53 (unknown origin) interaction expressed in Escherichia coli BL21(DE3) cells assessed as inhibition constant incubated for 1.5 hrs by competitive fluorescence polarization assay
ChEMBL ↗
57
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

E3 ubiquitin-protein ligase Mdm2 (CHEMBL5023) ↗
Type SINGLE PROTEIN
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
Ki 57 8.00 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425989 — — 2 9.15
CHEMBL5438520 — — 1 8.92
CHEMBL5405110 — — 1 8.89
CHEMBL5395046 — — 1 8.89
CHEMBL5413376 — — 1 8.89
CHEMBL5424005 — — 1 8.89
CHEMBL2381408 SAR-405838 1.0 1 8.89
CHEMBL5431530 — — 1 8.85
CHEMBL5407963 — — 1 8.85
CHEMBL5402394 — — 1 8.85
CHEMBL5404903 — — 1 8.85
CHEMBL5433398 — — 1 8.82
CHEMBL5441014 — — 1 8.77
CHEMBL5430850 — — 1 8.74
CHEMBL5403772 — — 1 8.74
CHEMBL5436528 — — 1 8.70
CHEMBL5405880 — — 1 8.70
CHEMBL5421232 — — 1 8.70
CHEMBL5405147 — — 1 8.68
CHEMBL5414460 — — 1 8.64
CHEMBL5436246 — — 1 8.64
CHEMBL5440363 — — 1 8.60
CHEMBL5406959 — — 1 8.59
CHEMBL5405392 — — 1 8.59
CHEMBL5398827 — — 1 8.57
CHEMBL5396046 — — 1 8.54
CHEMBL5438528 — — 1 8.49
CHEMBL5403609 — — 1 8.34
CHEMBL5400878 — — 1 8.27
CHEMBL5411556 — — 1 8.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425989 — Ki = 0.7 nM 9.15
CHEMBL5438520 — Ki = 1.2 nM 8.92
CHEMBL5395046 — Ki = 1.3 nM 8.89
CHEMBL5413376 — Ki = 1.3 nM 8.89
CHEMBL5424005 — Ki = 1.3 nM 8.89
CHEMBL2381408 SAR-405838 Ki = 1.3 nM 8.89
CHEMBL5405110 — Ki = 1.3 nM 8.89
CHEMBL5404903 — Ki = 1.4 nM 8.85
CHEMBL5431530 — Ki = 1.4 nM 8.85
CHEMBL5402394 — Ki = 1.4 nM 8.85
CHEMBL5407963 — Ki = 1.4 nM 8.85
CHEMBL5433398 — Ki = 1.5 nM 8.82
CHEMBL5425989 — Ki = 1.6 nM 8.80
CHEMBL5441014 — Ki = 1.7 nM 8.77
CHEMBL5430850 — Ki = 1.8 nM 8.74
CHEMBL5403772 — Ki = 1.8 nM 8.74
CHEMBL5421232 — Ki = 2.0 nM 8.70
CHEMBL5436528 — Ki = 2.0 nM 8.70
CHEMBL5405880 — Ki = 2.0 nM 8.70
CHEMBL5405147 — Ki = 2.1 nM 8.68
CHEMBL5414460 — Ki = 2.3 nM 8.64
CHEMBL5436246 — Ki = 2.3 nM 8.64
CHEMBL5440363 — Ki = 2.5 nM 8.60
CHEMBL5406959 — Ki = 2.6 nM 8.59
CHEMBL5405392 — Ki = 2.6 nM 8.59
CHEMBL5398827 — Ki = 2.7 nM 8.57
CHEMBL5396046 — Ki = 2.9 nM 8.54
CHEMBL5438528 — Ki = 3.2 nM 8.49
CHEMBL5403609 — Ki = 4.6 nM 8.34
CHEMBL5400878 — Ki = 5.4 nM 8.27
CHEMBL5411556 — Ki = 7.8 nM 8.11
CHEMBL5401273 — Ki = 7.7 nM 8.11
CHEMBL5413534 — Ki = 7.7 nM 8.11
CHEMBL5394717 — Ki = 8.3 nM 8.08
CHEMBL5415765 — Ki = 8.6 nM 8.07
CHEMBL5200857 — Ki = 9.5 nM 8.02
CHEMBL5423725 — Ki = 10.7 nM 7.97
CHEMBL5394822 — Ki = 10.9 nM 7.96
CHEMBL5423147 — Ki = 11.4 nM 7.94
CHEMBL5437702 — Ki = 12.9 nM 7.89
CHEMBL5404372 — Ki = 16.3 nM 7.79
CHEMBL5413325 — Ki = 18.0 nM 7.75
CHEMBL5396529 — Ki = 31.8 nM 7.50
CHEMBL191334 NUTLIN-3 Ki = 42.6 nM 7.37
CHEMBL5421177 — Ki = 46.7 nM 7.33
CHEMBL5400925 — Ki = 53.1 nM 7.28
CHEMBL5397420 — Ki = 73.4 nM 7.13
CHEMBL5408617 — Ki = 105.0 nM 6.98
CHEMBL5430636 — Ki = 115.0 nM 6.94
CHEMBL5405535 — Ki = 132.0 nM 6.88