General Information of the Protein
Protein ID
PT01988
Protein Name
Prolyl hydroxylase EGLN2
Secondarily
Protein Name
Egl nine homolog 2
Estrogen-induced tag 6
HPH-3
Hypoxia-inducible factor prolyl hydroxylase 1
Prolyl hydroxylase domain-containing protein 1
Gene Name
EGLN2
Secondarily
Gene Name
EIT6
Sequence
MDSPCQPQPLSQALPQLPGSSSEPLEPEPGRARMGVESYLPCPLLPSYHCPGVPSEASAGSGTPRATATSTTASPLRDGFGGQDGGELRPLQSEGAAALVTKGCQRLAAQGARPEAPKRKWAEDGGDAPSPSKRPWARQENQEAEREGGMSCSCSSGSGEASAGLMEEALPSAPERLALDYIVPCMRYYGICVKDSFLGAALGGRVLAEVEALKRGGRLRDGQLVSQRAIPPRSIRGDQIAWVEGHEPGCRSIGALMAHVDAVIRHCAGRLGSYVINGRTKAMVACYPGNGLGYVRHVDNPHGDGRCITCIYYLNQNWDVKVHGGLLQIFPEGRPVVANIEPLFDRLLIFWSDRRNPHEVKPAYATRYAITVWYFDAKERAAAKDKYQLASGQKGVQVPVSQPPTPT
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Oxidoreductase
Function
Prolyl hydroxylase that mediates hydroxylation of proline residues in target proteins, such as ATF4, IKBKB, CEP192 and HIF1A (PubMed:11595184, PubMed:12039559, PubMed:15925519, PubMed:16509823, PubMed:17114296, PubMed:23932902). Target proteins are preferentially recognized via a LXXLAP motif (PubMed:11595184, PubMed:12039559, PubMed:15925519). Cellular oxygen sensor that catalyzes, under normoxic conditions, the post-translational formation of 4-hydroxyproline in hypoxia-inducible factor (HIF) alpha proteins (PubMed:11595184, PubMed:12039559, PubMed:12181324, PubMed:15925519, PubMed:19339211). Hydroxylates a specific proline found in each of the oxygen-dependent degradation (ODD) domains (N-terminal, NODD, and C-terminal, CODD) of HIF1A (PubMed:11595184, PubMed:12039559, PubMed:12181324, PubMed:15925519). Also hydroxylates HIF2A (PubMed:11595184, PubMed:12039559, PubMed:15925519). Has a preference for the CODD site for both HIF1A and HIF2A (PubMed:11595184, PubMed:12039559, PubMed:15925519). Hydroxylated HIFs are then targeted for proteasomal degradation via the von Hippel-Lindau ubiquitination complex (PubMed:11595184, PubMed:12039559, PubMed:15925519). Under hypoxic conditions, the hydroxylation reaction is attenuated allowing HIFs to escape degradation resulting in their translocation to the nucleus, heterodimerization with HIF1B, and increased expression of hypoxy-inducible genes (PubMed:11595184, PubMed:12039559, PubMed:15925519). EGLN2 is involved in regulating hypoxia tolerance and apoptosis in cardiac and skeletal muscle (PubMed:11595184, PubMed:12039559, PubMed:15925519). Also regulates susceptibility to normoxic oxidative neuronal death (PubMed:11595184, PubMed:12039559, PubMed:15925519). Links oxygen sensing to cell cycle and primary cilia formation by hydroxylating the critical centrosome component CEP192 which promotes its ubiquitination and subsequent proteasomal degradation (PubMed:23932902). Hydroxylates IKBKB, mediating NF-kappa-B activation in hypoxic conditions (PubMed:17114296). Also mediates hydroxylation of ATF4, leading to decreased protein stability of ATF4 (By similarity).
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Uniprot ID
Primary ID:
Q96KS0

Secondarily ID:
A8K5S0
Q8WWY4
Q9BV14
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HGNC ID
HGNC:14660
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000013 , Sf9
Compound ID Compound Name Compound Formula
CP0136665
N-[bis(4-methoxyphenyl)methyl]-6-oxo-2-pyridazin-3-yl-1H-pyrimidine-5-carboxamide
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C24H21N5O4
 1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CP0458164
2-[[3-(4-cyanophenyl)-10-hydroxy-12-oxo-7-(trifluoromethoxy)-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13),10-tetraene-11-carbonyl]amino]acetic acid
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C22H14F3N3O7
 1
1
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0521144
2-[[1-[(4-chlorophenyl)methyl]-4-hydroxy-2-oxo-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C17H15ClN2O6
 1
1
IC50 = 2.1 nM
   TI
   LI
   LO
   TS
CP0434449
2-[[1-[(2,4-difluorophenyl)methyl]-4-hydroxy-2-oxo-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C17H14F2N2O6
 1
1
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
CP0533798
2-[[10-hydroxy-12-oxo-3-[6-(trifluoromethyl)pyridin-3-yl]-1,4-diazatricyclo[7.3.1.05,13]trideca-5,7,9(13),10-tetraene-11-carbonyl]amino]acetic acid
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C20H15F3N4O5
 1
1
IC50 = 2.3 nM
   TI
   LI
   LO
   TS
CP0437857
2-[[4-hydroxy-2-oxo-1-[[4-(trifluoromethoxy)phenyl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C18H15F3N2O7
 1
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
CP0439910
2-[[4-hydroxy-2-oxo-1-[[2-(trifluoromethyl)-1,3-thiazol-5-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C15H12F3N3O6S
 1
1
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
CP0426003
2-[[4-hydroxy-2-oxo-1-[(2,4,5-trifluorophenyl)methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C17H13F3N2O6
 1
1
IC50 = 3.1 nM
   TI
   LI
   LO
   TS
CP0470796
2-[[7-chloro-4-hydroxy-2-oxo-1-[[4-(trifluoromethyl)phenyl]methyl]quinoline-3-carbonyl]amino]acetic acid
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C20H14ClF3N2O5
 1
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
CP0517636
2-[[4-hydroxy-2-oxo-1-[(1-phenylpyrazol-3-yl)methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C20H18N4O6
 1
1
IC50 = 3.2 nM
   TI
   LI
   LO
   TS
CP0458167
2-[[1-(1,3-benzothiazol-2-ylmethyl)-4-hydroxy-2-oxo-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonyl]amino]acetic acid
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C19H17N3O6S
 1
1
IC50 = 3.3 nM
   TI
   LI
   LO
   TS
CP0142820
2-[[4-hydroxy-2-oxo-1-[[4-(trifluoromethyl)phenyl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C18H15F3N2O6
 1
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
CP0426000
2-[[4-hydroxy-2-oxo-1-[[6-(trifluoromethyl)pyridin-3-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C17H14F3N3O6
 1
1
IC50 = 3.6 nM
   TI
   LI
   LO
   TS
CP0492051
2-[[4-hydroxy-2-oxo-1-[[4-(trifluoromethyl)-1,3-thiazol-2-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C15H12F3N3O6S
 1
1
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0470792
2-[[10-hydroxy-12-oxo-3-[4-(trifluoromethyl)phenyl]-4-thia-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13),10-tetraene-11-carbonyl]amino]acetic acid
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C21H15F3N2O5S
 1
1
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0426002
2-[[4-hydroxy-2-oxo-1-[[5-(trifluoromethyl)pyrazin-2-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C16H13F3N4O6
 1
1
IC50 = 4.9 nM
   TI
   LI
   LO
   TS
CP0559017
2-[[10-hydroxy-12-oxo-2-[6-(trifluoromethyl)pyridin-3-yl]-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13),10-tetraene-11-carbonyl]amino]acetic acid
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C20H14F3N3O6
 1
1
IC50 = 4.9 nM
   TI
   LI
   LO
   TS
CP0533783
2-[[1-(1,3-benzoxazol-2-ylmethyl)-4-hydroxy-2-oxo-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C18H15N3O7
 1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0533800
2-[[1-[(4-chlorophenyl)methyl]-4-hydroxy-2-oxo-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonyl]amino]acetic acid
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C18H17ClN2O6
 1
1
IC50 = 5.9 nM
   TI
   LI
   LO
   TS
CP0519246
2-[[4-hydroxy-1-[[4-(2-hydroxypropan-2-yl)phenyl]methyl]-2-oxo-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C20H22N2O7
 1
1
IC50 = 6.2 nM
   TI
   LI
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CP0533799
2-[[1-[(4-cyano-2-fluorophenyl)methyl]-4-hydroxy-2-oxo-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonyl]amino]acetic acid
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C19H16FN3O6
 1
1
IC50 = 6.3 nM
   TI
   LI
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CP0492050
2-[[4-hydroxy-2-oxo-1-[[6-(trifluoromethyl)pyridin-3-yl]methyl]-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonyl]amino]acetic acid
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C18H16F3N3O6
 1
1
IC50 = 6.8 nM
   TI
   LI
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CP0546260
N-[5-(4-cyanophenyl)-[1,2,4]triazolo[1,5-a]pyridin-7-yl]acetamide
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C15H11N5O
 1
1
IC50 = 8 nM
   TI
   LI
   LO
   TS
CP0543106
2-fluoro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H7FN4
 1
1
IC50 = 10 nM
   TI
   LI
   LO
   TS
CP0426423
2-[[4-hydroxy-2-oxo-1-[[2-(trifluoromethyl)pyrimidin-5-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C16H13F3N4O6
 1
1
IC50 = 11 nM
   TI
   LI
   LO
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CP0437858
2-[[4-hydroxy-2-oxo-1-[[4-(trifluoromethyl)phenyl]methyl]-6,8-dihydro-5H-pyrano[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C19H17F3N2O6
 1
1
IC50 = 11 nM
   TI
   LI
   LO
   TS
CP0426422
2-[[4-hydroxy-2-oxo-1-[[5-(trifluoromethyl)pyrimidin-2-yl]methyl]-5,7-dihydrofuro[3,4-b]pyridine-3-carbonyl]amino]acetic acid
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C16H13F3N4O6
 1
1
IC50 = 12 nM
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   LI
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CP0565175
4-(7-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H9N5
 1
1
IC50 = 13 nM
   TI
   LI
   LO
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CP0492049
2-[[4-hydroxy-2-oxo-1-[[4-(trifluoromethyl)phenyl]methyl]-7,8-dihydro-5H-pyrano[4,3-b]pyridine-3-carbonyl]amino]acetic acid
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C19H17F3N2O6
 1
1
IC50 = 14 nM
   TI
   LI
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CP0551667
4-[7-(ethylamino)-[1,2,4]triazolo[1,5-a]pyridin-5-yl]benzonitrile
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C15H13N5
 1
1
IC50 = 25 nM
   TI
   LI
   LO
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CP0425999
2-[[10-hydroxy-2-(4-methoxyphenyl)-12-oxo-4-oxa-1-azatricyclo[7.3.1.05,13]trideca-5,7,9(13),10-tetraene-11-carbonyl]amino]acetic acid
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C21H18N2O7
 1
1
IC50 = 27 nM
   TI
   LI
   LO
   TS
CP0458272
2,6-difluoro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H6F2N4
 1
1
IC50 = 34 nM
   TI
   LI
   LO
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CP0469866
4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H8N4
 1
1
IC50 = 34 nM
   TI
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CP0461702
4-(7-methyl-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4
 1
1
IC50 = 39 nM
   TI
   LI
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CP0546951
3-fluoro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H7FN4
 1
1
IC50 = 50 nM
   TI
   LI
   LO
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CP0461706
2-fluoro-3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H9FN4
 1
1
IC50 = 52 nM
   TI
   LI
   LO
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CP0469871
3-amino-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H9N5
 1
1
IC50 = 57 nM
   TI
   LI
   LO
   TS
CP0458271
2,3-difluoro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H6F2N4
 1
1
IC50 = 67 nM
   TI
   LI
   LO
   TS
CP0407937
N-[5-(4-cyano-2-methylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-7-yl]acetamide
   Show/Hide
C16H13N5O
 1
1
IC50 = 70 nM
   TI
   LI
   LO
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CP0393896
3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4
 1
1
IC50 = 74 nM
   TI
   LI
   LO
   TS
CP0565178
5-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyrimidine-2-carbonitrile
   Show/Hide
C11H6N6
 1
1
IC50 = 84 nM
   TI
   LI
   LO
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CP0469870
4-(7-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)-3-methylbenzonitrile
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C14H11N5
 1
1
IC50 = 90 nM
   TI
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CP0479683
3-chloro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H7ClN4
 1
1
IC50 = 140 nM
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CP0543085
3-methoxy-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4O
 1
1
IC50 = 140 nM
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CP0573920
2-fluoro-5-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H9FN4
 1
1
IC50 = 140 nM
   TI
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CP0458270
3,5-difluoro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H6F2N4
 1
1
IC50 = 160 nM
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   LI
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CP0565184
5-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyridine-2-carbonitrile
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C12H7N5
 1
1
IC50 = 170 nM
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CP0412957
3,5-dimethyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C15H12N4
 1
1
IC50 = 200 nM
   TI
   LI
   LO
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CP0569627
3-fluoro-5-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H9FN4
 1
1
IC50 = 220 nM
   TI
   LI
   LO
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CP0565201
4-(2-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H9N5
 1
1
IC50 = 240 nM
   TI
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CP0546264
6-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyridine-3-carbonitrile
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C12H7N5
 1
1
IC50 = 270 nM
   TI
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CP0458269
1-([1,2,4]triazolo[1,5-a]pyridin-5-yl)piperidine-4-carbonitrile
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C12H13N5
 1
1
IC50 = 280 nM
   TI
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CP0513613
4-(6-methyl-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4
 1
1
IC50 = 460 nM
   TI
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CP0546259
4-(6-fluoro-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H7FN4
 1
1
IC50 = 460 nM
   TI
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CP0393900
5-(4-chlorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
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C12H8ClN3
 1
1
IC50 = 550 nM
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CP0407936
4-(2-methyl-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4
 1
1
IC50 = 570 nM
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CP0546262
5-(2,4-dichlorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
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C12H7Cl2N3
 1
1
IC50 = 670 nM
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CP0548492
4-(6-amino-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C13H9N5
 1
1
IC50 = 770 nM
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CP0393897
2-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
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C14H10N4
 1
1
IC50 = 830 nM
   TI
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CP0543084
5-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyrazine-2-carbonitrile
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C11H6N6
 1
1
IC50 = 1280 nM
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CP0510308
5-(4-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
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C12H8FN3
 1
1
IC50 = 1300 nM
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CP0565177
6-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyridazine-3-carbonitrile
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C11H6N6
 1
1
IC50 = 1370 nM
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CP0035875
2,4 PDCA
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C7H5NO4
 1
1
IC50 = 1500 nM
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CP0565533
4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)piperazine-1-carbonitrile
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C11H12N6
 1
1
IC50 = 1800 nM
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CP0544156
4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)-2-(trifluoromethyl)benzonitrile
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C14H7F3N4
 1
1
IC50 = 1870 nM
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CP0039003
2-(carboxymethylamino)-2-oxoacetic acid
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C4H5NO5
 1
1
IC50 = 2100 nM
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CP0461703
N-[5-(4-cyanophenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]acetamide
   Show/Hide
C15H11N5O
 1
1
IC50 = 2500 nM
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   TS
CP0565531
2-chloro-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
   Show/Hide
C13H7ClN4
 1
1
IC50 = 3900 nM
   TI
   LI
   LO
   TS
CP0469864
5-(4-methylphenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C13H11N3
 1
1
IC50 = 5600 nM
   TI
   LI
   LO
   TS
CP0393679
3-ethyl-4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
   Show/Hide
C15H12N4
 1
1
IC50 = 6100 nM
   TI
   LI
   LO
   TS
CP0546926
4-(8-fluoro-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
   Show/Hide
C13H7FN4
 1
1
IC50 = 9600 nM
   TI
   LI
   LO
   TS
CP0407938
N-[5-cyano-2-([1,2,4]triazolo[1,5-a]pyridin-5-yl)phenyl]acetamide
   Show/Hide
C15H11N5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0420475
5-([1,2,4]triazolo[1,5-a]pyridin-5-yl)furan-2-carbonitrile
   Show/Hide
C11H6N4O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0469869
4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)thiophene-2-carbonitrile
   Show/Hide
C11H6N4S
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0510310
1-([1,2,4]triazolo[1,5-a]pyridin-5-yl)imidazole-4-carbonitrile
   Show/Hide
C10H6N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0544158
N-[5-(4-cyanophenyl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]acetamide
   Show/Hide
C15H11N5O
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0546265
4-([1,2,4]triazolo[1,5-a]pyridin-5-yl)-3-(trifluoromethyl)benzonitrile
   Show/Hide
C14H7F3N4
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0547991
1-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyrrolidine-3-carbonitrile
   Show/Hide
C11H11N5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0548491
4-[6-(dimethylamino)-[1,2,4]triazolo[1,5-a]pyridin-5-yl]benzonitrile
   Show/Hide
C15H13N5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0565534
1-([1,2,4]triazolo[1,5-a]pyridin-5-yl)pyrazole-4-carbonitrile
   Show/Hide
C10H6N6
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0573827
2-([1,2,4]triazolo[1,5-a]pyridin-5-yl)-2-azaspiro[3.3]heptane-6-carbonitrile
   Show/Hide
C13H13N5
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0547990
4-[2-(dimethylamino)-[1,2,4]triazolo[1,5-a]pyridin-5-yl]benzonitrile
   Show/Hide
C15H13N5
 1
1
IC50 = 18000 nM
   TI
   LI
   LO
   TS
CP0408179
5-(2-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C12H8FN3
 1
1
IC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0547855
5-(2,4-dichlorophenyl)imidazo[1,2-a]pyrimidine
   Show/Hide
C12H7Cl2N3
 1
1
IC50 = 24000 nM
   TI
   LI
   LO
   TS
CP0407934
5-(3-chlorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C12H8ClN3
 1
1
IC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0469867
5-(4-methoxyphenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C13H11N3O
 1
1
IC50 = 26000 nM
   TI
   LI
   LO
   TS
CP0551668
5-(3-fluorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C12H8FN3
 1
1
IC50 = 28000 nM
   TI
   LI
   LO
   TS
CP0407935
5-phenyl-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C12H9N3
 1
1
IC50 = 30000 nM
   TI
   LI
   LO
   TS
CP0546261
5-(2-chlorophenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C12H8ClN3
 1
1
IC50 = 48000 nM
   TI
   LI
   LO
   TS
CP0546263
5-(3-methoxyphenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C13H11N3O
 1
1
IC50 = 55000 nM
   TI
   LI
   LO
   TS
CP0469865
3-([1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
   Show/Hide
C13H8N4
 1
1
IC50 = 61000 nM
   TI
   LI
   LO
   TS
CP0547989
4-(8-methyl-[1,2,4]triazolo[1,5-a]pyridin-5-yl)benzonitrile
   Show/Hide
C14H10N4
 1
1
IC50 = 80000 nM
   TI
   LI
   LO
   TS
CP0373189
3-(N-hydroxyacetamido)propanoic acid
   Show/Hide
C5H9NO4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0700054
4-[(8-Dimethylaminooctyl)-(hydroxyl)amino]-4-oxobutanoic Acid Hydrochloride
   Show/Hide
C14H29ClN2O4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0836970
3-{[8-(Dimethylamino)octanoyl](hydroxy)amino}propanoic Acid Hydrochloride
   Show/Hide
C13H27ClN2O4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0852013
3-({9-[Butyl(methyl)]amino}nonanoyl(hydroxy)amino)propanoic acid Hydrochloride
   Show/Hide
C17H35ClN2O4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0905853
3-{[9-(Dimethylamino)nonanoyl](hydroxy)amino}propanoic acid Hydrochloride
   Show/Hide
C14H29ClN2O4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0906772
3-{[10-(Dimethylamino)decanoyl](hydroxy)amino}propanoic acid Hydrochloride
   Show/Hide
C15H31ClN2O4
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0469868
5-(3-methylphenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C13H11N3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0510309
7-(2,4-dichlorophenyl)pyrazolo[1,5-a]pyrimidine
   Show/Hide
C12H7Cl2N3
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
CP0513614
5-(2-methoxyphenyl)-[1,2,4]triazolo[1,5-a]pyridine
   Show/Hide
C13H11N3O
 1
1
IC50 > 100000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0138757
3-methyl-4-[4-[8-[(3-methylpyridin-2-yl)methyl]-2,4-dioxo-1-pyrimidin-4-yl-1,3,8-triazaspiro[4.5]decan-3-yl]phenyl]benzoic acid
   Show/Hide
C32H30N6O4
 1
1 IC50 = 0.2 nM
CP0231640
US8653111, 72
   Show/Hide
C13H14N8O2
 1
1 IC50 = 490 nM
CP0039003
2-(carboxymethylamino)-2-oxoacetic acid
   Show/Hide
C4H5NO5
 2
1 IC50 = 842 nM
2 IC50 = 2100 nM
CP0035875
2,4 PDCA
   Show/Hide
C7H5NO4
 1
1 Ki = 7000 nM
Clinical Information about the Protein
Target 1 ( HIF-prolyl hydroxylase 1 (HPH-1) )
Target Type Successful Target
Disease 3 Target-related Diseases  3
1 Kidney disease [ICD-11: GC2Z]
2 Anemia [ICD-11: 3A00-3A9Z]
3 Anaemia [ICD-11: 3A90]
Approved Drug(s) 1 Approved Drug  1
1 Daprodustat Approved
Anaemia
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 FG-4592 Phase 3
Kidney disease
2 BAY-85-3934 Phase 2
Anemia