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 data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
