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	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	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	6.39	pIC50	410	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	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]
ChEMBL	Inhibition of N-terminal His tagged PHD2 (181 to 426 residues) (unknown origin) measured by MALDI-TOF MS analysis	B	7.54	pIC50	29	nM	IC50	J Med Chem (2021) 64: 7189-7209 [PMID:34029087]
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]
ChEMBL	Inhibition of FIH (unknown origin) by solid-phase extraction coupled to MS based assay	B	4.54	pIC50	29000	nM	IC50	J Med Chem (2021) 64: 7189-7209 [PMID:34029087]
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 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]