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

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ChEMBL ligand: CHEMBL1686 (2-Oxoglutarate, 2-Oxopentanedioic Acid, 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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  • Na+/dicarboxylate cotransporter 3/Solute carrier family 13 member 3 in Human [ChEMBL: CHEMBL3712947] [GtoPdb: 979] [UniProtKB: Q8WWT9]
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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 F 8.26 pEC50 5.5 nM EC50 US-20180116992-A1. Modulators of Prostate-Specific G-Protein Receptor (PSGR/OR51E2) and Methods of Using Same (2018)
Na+/dicarboxylate cotransporter 3/Solute carrier family 13 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712947] [GtoPdb: 979] [UniProtKB: Q8WWT9]
ChEMBL Substrate uptake by the Na(+)/Dicarboxylate Cotransporter 3 (NADC3, SLC13A3) as assessed by the fluorescent FLIPR membrane potential dye in HEK-293 JumpIN-SLC13A3 cells (PubChem AID: 1794820) F 4.27 pEC50 54000 nM EC50 Membrane potential based assay for SLC13A3 using HEK-293 SLC13A3 OE cells
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 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]