RG7112 [Ligand Id: 9599] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2386346 (Mdm2 antagonist ro5045337, R 7112, RG-7112, RG7112, Ro-5045337, RO-5045337, RO5045337) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| MDM2 proto-oncogene/p53-binding protein Mdm-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5023] [GtoPdb: 3136] [UniProtKB: Q00987] | ||||||||
| ChEMBL | Binding affinity to recombinant human GST-tagged HDM2 | B | 7.97 | pKd | 10.7 | nM | Kd | J Med Chem (2021) 64: 16213-16241 [PMID:34714078] |
| ChEMBL | Binding affinity to human MDM2 by by Surface Plasmon Resonace (SPR) spectroscopy binding assay | B | 8.54 | pKd | 2.9 | nM | Kd | J Med Chem (2014) 57: 1454-1472 [PMID:24456472] |
| ChEMBL | Inhibition of N-terminal human recombinant MDM2 assessed as inhibition of protein interaction with p53 by HTRF assay | B | 7.74 | pIC50 | 18 | nM | IC50 | ACS Med Chem Lett (2013) 4: 466-469 [PMID:24900694] |
| ChEMBL | Binding affinity to GST-tagged MDM2 (unknown origin) assessed as inhibition of interaction with p53 after 1 hr by HTRF assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2013) 56: 5979-5983 [PMID:23808545] |
| ChEMBL | Inhibition of MDM2 (unknown origin) by HTRF assay | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2020) 63: 7957-7985 [PMID:32142281] |
| ChEMBL | Inhibition of MDM2 (unknown origin) | B | 7.74 | pIC50 | 18 | nM | IC50 | J Med Chem (2022) 65: 6207-6230 [PMID:35420431] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
