α-ketoglutaric acid [Ligand Id: 3636] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1686 (2-Oxopentanedioic Acid, 2-Oxoglutarate, Alpha-Ketoglutarate)
  • egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9]
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  • oxoglutarate receptor in Human [GtoPdb: 162] [UniProtKB: Q96P68]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9]
ChEMBL Binding affinity to human PHD2-Mn(II) using 12.5% H2O/87.5% D2O MQC spectrometer operated at 500 MHz at 313K temperature B 5.66 pKd 2200 nM Kd J. Med. Chem. (2010) 53: 867-875 [PMID:20025281]
ChEMBL Binding affinity to human PHD2 catalytic domain (181 to 426) Zn2 expressed in Escherichia coli by 1H-15N HSQC titration assay B 5.7 pKd <2000 nM Kd J. Med. Chem. (2013) 56: 547-555 [PMID:23234607]
ChEMBL Binding affinity to human PHD2-Mn(II) using 100% H2O MQC spectrometer operated at 23 MHz at 313K temperature B 5.77 pKd 1700 nM Kd J. Med. Chem. (2010) 53: 867-875 [PMID:20025281]
ChEMBL Binding affinity to human PHD2-Mn(II) using 12.5% H2O/87.5% D2O MQC spectrometer operated at 500 MHz at 298K temperature in presence of HIF1alpha (556-574) CODD fragment B 6 pKd 1000 nM Kd J. Med. Chem. (2010) 53: 867-875 [PMID:20025281]
ChEMBL Binding affinity to human PHD2-Mn(II) using 12.5% H2O/87.5% D2O MQC spectrometer operated at 500 MHz at 298K temperature B 6.05 pKd 900 nM Kd J. Med. Chem. (2010) 53: 867-875 [PMID:20025281]
ChEMBL Binding affinity to human PHD2 by nondenaturing ESI-MS B 6.05 pKd 900 nM Kd J. Med. Chem. (2010) 53: 867-875 [PMID:20025281]
ChEMBL Binding affinity to human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by 1H-15N HSQC titration assay B 6.05 pKd 900 nM Kd J. Med. Chem. (2013) 56: 547-555 [PMID:23234607]
Olfactory receptor 51E2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523454] [UniProtKB: Q9H255]
ChEMBL Agonist activity at PSGR/OR51E2 (unknown origin) expressed in human Hana3A cells co-transfected with CRE-Luc by luciferase reporter gene assay B 8.26 pEC50 5.5 nM EC50 US-20180116992-A1. Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same (null)
oxoglutarate receptor in Human [GtoPdb: 162] [UniProtKB: Q96P68]
GtoPdb - - 4.49 pEC50 32000 nM EC50 Nature (2004) 429: 188-93 [PMID:15141213];
J Biomol Screen (2013) 18: 599-609 [PMID:23396314]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]