Assay Detail
Binding
CHEMBL5378738
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MDM4 (14 to 111 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
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 |
Publication
Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein-Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 57 | 5.71 | 6.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423147 | — | — | 1 | 6.59 |
| CHEMBL5437702 | — | — | 1 | 6.53 |
| CHEMBL5394717 | — | — | 1 | 6.46 |
| CHEMBL5411556 | — | — | 1 | 6.41 |
| CHEMBL5395046 | — | — | 1 | 6.34 |
| CHEMBL5425989 | — | — | 2 | 6.28 |
| CHEMBL5436528 | — | — | 1 | 6.28 |
| CHEMBL5438520 | — | — | 1 | 6.28 |
| CHEMBL5438528 | — | — | 1 | 6.22 |
| CHEMBL5424005 | — | — | 1 | 6.21 |
| CHEMBL5405880 | — | — | 1 | 6.21 |
| CHEMBL5414460 | — | — | 1 | 6.14 |
| CHEMBL5396046 | — | — | 1 | 6.13 |
| CHEMBL5405147 | — | — | 1 | 6.11 |
| CHEMBL5421232 | — | — | 1 | 6.10 |
| CHEMBL5398827 | — | — | 1 | 6.06 |
| CHEMBL5407963 | — | — | 1 | 6.06 |
| CHEMBL5405110 | — | — | 1 | 6.05 |
| CHEMBL5407556 | — | — | 1 | 6.05 |
| CHEMBL5408617 | — | — | 1 | 6.04 |
| CHEMBL5406959 | — | — | 1 | 6.01 |
| CHEMBL5401273 | — | — | 1 | 6.00 |
| CHEMBL5403772 | — | — | 1 | 5.99 |
| CHEMBL5431530 | — | — | 1 | 5.99 |
| CHEMBL5402394 | — | — | 1 | 5.98 |
| CHEMBL5423725 | — | — | 1 | 5.97 |
| CHEMBL5433398 | — | — | 1 | 5.97 |
| CHEMBL5405392 | — | — | 1 | 5.94 |
| CHEMBL5404903 | — | — | 1 | 5.92 |
| CHEMBL5441014 | — | — | 1 | 5.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423147 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL5437702 | — | Ki | = | 298.0 | nM | 6.53 |
| CHEMBL5394717 | — | Ki | = | 349.0 | nM | 6.46 |
| CHEMBL5411556 | — | Ki | = | 386.0 | nM | 6.41 |
| CHEMBL5395046 | — | Ki | = | 457.0 | nM | 6.34 |
| CHEMBL5425989 | — | Ki | = | 527.0 | nM | 6.28 |
| CHEMBL5436528 | — | Ki | = | 522.0 | nM | 6.28 |
| CHEMBL5438520 | — | Ki | = | 529.0 | nM | 6.28 |
| CHEMBL5438528 | — | Ki | = | 595.0 | nM | 6.22 |
| CHEMBL5405880 | — | Ki | = | 623.0 | nM | 6.21 |
| CHEMBL5424005 | — | Ki | = | 616.0 | nM | 6.21 |
| CHEMBL5414460 | — | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL5396046 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL5405147 | — | Ki | = | 786.0 | nM | 6.11 |
| CHEMBL5421232 | — | Ki | = | 802.0 | nM | 6.10 |
| CHEMBL5425989 | — | Ki | = | 795.0 | nM | 6.10 |
| CHEMBL5407963 | — | Ki | = | 877.0 | nM | 6.06 |
| CHEMBL5398827 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL5405110 | — | Ki | = | 885.0 | nM | 6.05 |
| CHEMBL5407556 | — | Ki | = | 886.0 | nM | 6.05 |
| CHEMBL5408617 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL5406959 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL5401273 | — | Ki | = | 1003.0 | nM | 6.00 |
| CHEMBL5403772 | — | Ki | = | 1035.0 | nM | 5.99 |
| CHEMBL5431530 | — | Ki | = | 1035.0 | nM | 5.99 |
| CHEMBL5402394 | — | Ki | = | 1038.0 | nM | 5.98 |
| CHEMBL5433398 | — | Ki | = | 1064.0 | nM | 5.97 |
| CHEMBL5423725 | — | Ki | = | 1067.0 | nM | 5.97 |
| CHEMBL5405392 | — | Ki | = | 1144.0 | nM | 5.94 |
| CHEMBL5404903 | — | Ki | = | 1214.0 | nM | 5.92 |
| CHEMBL5441014 | — | Ki | = | 1327.0 | nM | 5.88 |
| CHEMBL191334 | NUTLIN-3 | Ki | = | 1599.0 | nM | 5.80 |
| CHEMBL5400878 | — | Ki | = | 1589.0 | nM | 5.80 |
| CHEMBL5413376 | — | Ki | = | 1582.0 | nM | 5.80 |
| CHEMBL5403609 | — | Ki | = | 1698.0 | nM | 5.77 |
| CHEMBL5430850 | — | Ki | = | 1692.0 | nM | 5.77 |
| CHEMBL5394822 | — | Ki | = | 1981.0 | nM | 5.70 |
| CHEMBL5415765 | — | Ki | = | 2004.0 | nM | 5.70 |
| CHEMBL5405535 | — | Ki | = | 2207.0 | nM | 5.66 |
| CHEMBL5404372 | — | Ki | = | 2473.0 | nM | 5.61 |
| CHEMBL5396529 | — | Ki | = | 3341.0 | nM | 5.48 |
| CHEMBL5411415 | — | Ki | = | 3651.0 | nM | 5.44 |
| CHEMBL5413534 | — | Ki | = | 5238.0 | nM | 5.28 |
| CHEMBL5400925 | — | Ki | = | 6400.0 | nM | 5.19 |
| CHEMBL5200857 | — | Ki | = | 13300.0 | nM | 4.88 |
| CHEMBL5425619 | — | Ki | = | 15315.0 | nM | 4.82 |
| CHEMBL5397420 | — | Ki | = | 15403.0 | nM | 4.81 |
| CHEMBL5413325 | — | Ki | = | 17032.0 | nM | 4.77 |
| CHEMBL5438048 | — | Ki | = | 17621.0 | nM | 4.75 |
| CHEMBL5417541 | — | Ki | = | 17693.0 | nM | 4.75 |