ChEMBL ligand: CHEMBL3646221 (AKB-6548, B-506, B506, PG-1016548, PG1016548, Vadadustat)
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!
egl-9 family hypoxia inducible factor 3/Egl nine homolog 3 in Human [ChEMBL: CHEMBL5705] [GtoPdb: 2834] [UniProtKB: Q9H6Z9] 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!
Vascular endothelial growth factor A in Human [ChEMBL: CHEMBL1783] [UniProtKB: P15692] 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
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 (unknown origin) by fluorescence polarization assay	B	4.86	pIC50	13700	nM	IC50	J Med Chem (2018) 61: 6964-6982 [PMID:29712435]
ChEMBL	Enzyme Assay: The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al., 2006).	B	5.96	pIC50	1100	nM	IC50	US-8598210-B2. Prolyl hydroxylase inhibitors and methods of use (2013)
ChEMBL	Mass Spectrometry Assay : The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al, 2006). The reaction is conducted in a total volume of 50 uL containing TrisCl (5 mM, pH7.5), ascorbate (120 μM), 2-oxoglutarate (3.2 μM), HIF-1α (8.6 μM), and bovine serum albumin (0.01%). The enzyme, quantity predetermined to hydroxylate 20% of substrate in 20 minutes, is added to start the reaction. Compounds are prepared in dimethyl sulfoxide at 10-fold final assay concentration. After 20 minutes at room temperature, the reaction is stopped by transferring 10 μL of reaction mixture to 50 μL of a mass spectrometry matrix solution (α-cyano-4-hydroxycinnamic acid, 5 mg/mL in 50% acetonitrile/0.1% TFA, 5 mM NH4PO4). Two microliters of the mixture is spotted onto a MALDI-TOF MS target plate for analysis with an Applied Biosystems.	B	5.96	pIC50	1100	nM	IC50	US-8722895-B2. Prolyl hydroxylase inhibitors and method of use (2014)
ChEMBL	Enzyme Assay: The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al., 2006).	B	6.39	pIC50	410	nM	IC50	US-8598210-B2. Prolyl hydroxylase inhibitors and methods of use (2013)
ChEMBL	Mass Spectrometry Assay : The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al, 2006). The reaction is conducted in a total volume of 50 uL containing TrisCl (5 mM, pH7.5), ascorbate (120 μM), 2-oxoglutarate (3.2 μM), HIF-1α (8.6 μM), and bovine serum albumin (0.01%). The enzyme, quantity predetermined to hydroxylate 20% of substrate in 20 minutes, is added to start the reaction. Compounds are prepared in dimethyl sulfoxide at 10-fold final assay concentration. After 20 minutes at room temperature, the reaction is stopped by transferring 10 μL of reaction mixture to 50 μL of a mass spectrometry matrix solution (α-cyano-4-hydroxycinnamic acid, 5 mg/mL in 50% acetonitrile/0.1% TFA, 5 mM NH4PO4). Two microliters of the mixture is spotted onto a MALDI-TOF MS target plate for analysis with an Applied Biosystems.	B	6.39	pIC50	410	nM	IC50	US-8722895-B2. Prolyl hydroxylase inhibitors and method of use (2014)
ChEMBL	Inhibition of recombinant human HIF-PHD2 using DLDLEALAPYIPADDDFQL as substrate after 20 mins by mass spectrometry	B	6.41	pIC50	390	nM	IC50	Medchemcomm (2016) 7: 1271-1284
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	7.54	pIC50	29	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
GtoPdb	-	-	7.54	pIC50	29	nM	IC50	Chem Sci (2017) 8: 7651-7668 [PMID:29435217]; Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
egl-9 family hypoxia inducible factor 3/Egl nine homolog 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5705] [GtoPdb: 2834] [UniProtKB: Q9H6Z9]
ChEMBL	Mass Spectrometry Assay : The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al, 2006). The reaction is conducted in a total volume of 50 uL containing TrisCl (5 mM, pH7.5), ascorbate (120 μM), 2-oxoglutarate (3.2 μM), HIF-1α (8.6 μM), and bovine serum albumin (0.01%). The enzyme, quantity predetermined to hydroxylate 20% of substrate in 20 minutes, is added to start the reaction. Compounds are prepared in dimethyl sulfoxide at 10-fold final assay concentration. After 20 minutes at room temperature, the reaction is stopped by transferring 10 μL of reaction mixture to 50 μL of a mass spectrometry matrix solution (α-cyano-4-hydroxycinnamic acid, 5 mg/mL in 50% acetonitrile/0.1% TFA, 5 mM NH4PO4). Two microliters of the mixture is spotted onto a MALDI-TOF MS target plate for analysis with an Applied Biosystems.	B	6.41	pIC50	390	nM	IC50	US-8722895-B2. Prolyl hydroxylase inhibitors and method of use (2014)
ChEMBL	Enzyme Assay: The EGLN-1 (or EGLN-3) enzyme activity is determined using mass spectrometry (matrix-assisted laser desorption ionization, time-of-flight MS, MALDI-TOF MS—for assay details, see reference (Greis et al., 2006).	B	6.41	pIC50	390	nM	IC50	US-8598210-B2. Prolyl hydroxylase inhibitors and methods of use (2013)
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	4.54	pIC50	29000	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	5.85	pIC50	1400	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	6.55	pKi	280	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	6	pIC50	<1000	nM	IC50	Bioorg Med Chem (2019) 27: 2405-2412 [PMID:30737136]
Vascular endothelial growth factor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1783] [UniProtKB: P15692]
ChEMBL	ELISA Assay: HEK293 cells are seeded in 96-well poly-lysine coated plates at 20,000 cells per well in DMEM (10% FBS, 1% NEAA, 0.1% glutamine). Following overnight incubation, the cells are washed with 100 uL of Opti-MEM (Gibco, Carlsbad, Calif.) to remove serum. Compound in DMSO is serially diluted (beginning with 100 μM) in Opti-MEM and added to the cells. The conditioned media is analyzed for VEGF with a Quantikine human VEGF immunoassay kit (R&D Systems, Minneapolis, Minn.).	B	5.12	pEC50	7600	nM	EC50	US-8598210-B2. Prolyl hydroxylase inhibitors and methods of use (2013)

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]