ChEMBL ligand: CHEMBL2338329 (ASP-1517, ASP1517, FG-4592, FG4592, Roxadustat)
Alpha-ketoglutarate-dependent dioxygenase FTO in Human [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1] There should be some charts here, you may need to enable JavaScript!
egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9] There should be some charts here, you may need to enable JavaScript!
Hypoxia-inducible factor 1-alpha inhibitor in Human [ChEMBL: CHEMBL5909] [UniProtKB: Q9NWT6] There should be some charts here, you may need to enable JavaScript!
Prolyl 3-hydroxylase OGFOD1 in Human [ChEMBL: CHEMBL4523398] [UniProtKB: Q8N543] There should be some charts here, you may need to enable JavaScript!
Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Alpha-ketoglutarate-dependent dioxygenase FTO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2331065] [UniProtKB: Q9C0B1]
ChEMBL	Inhibition of human hexahistidine-tagged full-length FTO expressed in Escherichia coli BL21 (DE3) using 3-methylthymidine as substrate assessed as inhibition of 3-methylthymidine conversion to thymidine after 1 hr by liquid chromatographic analysis	B	5.01	pIC50	9800	nM	IC50	J Med Chem (2013) 56: 3680-3688 [PMID:23547775]
egl-9 family hypoxia inducible factor 1/Egl nine homolog 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5697] [GtoPdb: 2833] [UniProtKB: Q9GZT9]
ChEMBL	Inhibition of HIF-PHD2 (181 to 426 residues) (unknown origin) using HIF1-alpha (556 to 574 residues) as substrate in presence of 2-OG preincubated for 30 mins followed by OPD addition measured after 10 mins by fluorescence assay	B	5.24	pIC50	5740	nM	IC50	J Med Chem (2018) 61: 5332-5349 [PMID:29856623]
ChEMBL	HIF-PH Assay: Ketoglutaric acid alpha -[1-14C]-sodium salt, alpha-ketoglutaric acid sodium salt, and HPLC purified peptide were obtained from commercial sources, e.g., Perkin-Elmer (Wellesley Mass.), Sigma-Aldrich, and SynPep Corp. (Dublin Calif.), respectively. Peptides for use in the assay were fragments of HIFalpha as described above or as disclosed in International Publication WO 2005/118836, incorporated by reference herein. For example, a HIF peptide for use in the HIF-PH assay was [methoxycoumarin]-DLDLEALAPYIPADDDFQL-amide. HIF-PH, e.g., HIF-PH2 (also known as EGLN1 or PHD2), was expressed in, e.g., insect Hi5 cells, and partially purified, e.g., through a SP ion exchange chromatography column. Enzyme activity was determined by capturing 14CO2 using an assay described by Kivirikko and Myllyla (1982, Methods Enzymol. 82:245-304). Assay reactions contained 50 mM HEPES (pH 7.4), 100 uM alpha -ketoglutaric acid sodium salt, 0.30 uCi/mL alpha -ketoglutaric acid alpha -[1-14C]-sodium.	B	5.68	pIC50	2100	nM	IC50	US-9115085-B2. Crystalline forms of a prolyl hydroxylase inhibitor (2015)
ChEMBL	HIF-PH Assay: Ketoglutaric acid α-[1-14C]-sodium salt, alpha-ketoglutaric acid sodium salt, and HPLC purified peptide were obtained from commercial sources, e.g., Perkin-Elmer (Wellesley Mass.), Sigma-Aldrich, and SynPep Corp. (Dublin Calif.), respectively. Peptides for use in the assay were fragments of HIFα as described above or as disclosed in International Publication WO 2005/118836, incorporated by reference herein. For example, a HIF peptide for use in the HIF-PH assay was [methoxycoumarin]-DLDLEALAPYIPADDDFQL-amide. HIF-PH, e.g., HIF-PH2 (also known as EGLN1 or PHD2), was expressed in, e.g., insect Hi5 cells, and partially purified, e.g., through a SP ion exchange chromatography column. Enzyme activity was determined by capturing 14CO2 using an assay described by Kivirikko and Myllyla (1982, Methods Enzymol. 82:245-304). Assay reactions contained 50 mM HEPES (pH 7.4), 100 μM α-ketoglutaric acid sodium salt, 0.30 μCi/mL α-ketoglutaric acid α-[1-14C]-sodium salt, 40 μM FeSO4, 1 mM ascorbate, 1541.8 units/mL Catalase, with or without 50 μM peptide substrate and various concentrations of compound of the invention. Reactions were initiated by addition of HIF-PH enzyme.	B	5.68	pIC50	2100	nM	IC50	US-9340511-B2. Process for making isoquinoline compounds (2016)
ChEMBL	Displacement of FITC-HIF-1alpha (556 to 574 residues) from PHD2 (181 to 426 residues) (unknown origin) after 60 mins by fluorescence polarization assay	B	6.23	pIC50	591.4	nM	IC50	ACS Med Chem Lett (2015) 6: 1236-1240 [PMID:26713111]
ChEMBL	Inhibition of HIF-PHD2 (181 to 426 residues) (unknown origin) using FITC-HIF1-alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay	B	6.23	pIC50	591.4	nM	IC50	J Med Chem (2018) 61: 5332-5349 [PMID:29856623]
ChEMBL	Inhibition of FITC-HIF1alpha (556 to 574 residues) binding to PHD2 (181 to 426 residues) (unknown origin) by fluorescence polarization assay	B	6.23	pIC50	591	nM	IC50	J Med Chem (2020) 63: 10045-10060 [PMID:32787144]
ChEMBL	Inhibition of PHD2 (181 to 426 residues) (unknown origin) using FITC-HIF1alpha (556 to 574 residues) as substrate after 60 mins by fluorescence polarization assay	B	6.24	pIC50	575.3	nM	IC50	J Med Chem (2019) 62: 7583-7588 [PMID:31244107]
ChEMBL	Inhibition of HIF-PHD2 (unknown origin)	B	7.49	pIC50	32	nM	IC50	J Med Chem (2016) 59: 11039-11049 [PMID:28002958]
ChEMBL	Inhibition of recombinant human PHD2 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by LC-MS analysis	B	7.57	pIC50	27	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
Hypoxia-inducible factor 1-alpha inhibitor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5909] [UniProtKB: Q9NWT6]
ChEMBL	Inhibition of recombinant human FIH using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by LC-MS analysis	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
Prolyl 3-hydroxylase OGFOD1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523398] [UniProtKB: Q8N543]
ChEMBL	Inhibition of recombinant human OGFOD1 using 2OG as substrate and Fe2 as co-factor assessed as hydroxylation incubated for 15 mins in presence of L-ascorbate by MALDI-TOF MS analysis	B	6	pIC50	<1000	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
Prolyl 4-hydroxylase in Paramecium bursaria Chlorella virus 1 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523368] [UniProtKB: Q84406]
ChEMBL	Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and measured after 5 mins MALDI TOF MS analysis	B	5.97	pKi	1070	nM	Ki	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
ChEMBL	Inhibition of N-terminal His6-tagged recombinant Paramecium bursaria chlorella virus 1 CPH expressed in Escherichia coli Rosetta 2 (DE3) cells pre-incubated for 5 mins before 2OG as substrate and Fe2 as co-factor addition in presence of L-ascorbate and measured after 5 mins MALDI TOF MS analysis	B	5.3	pIC50	5000	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]

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]