Found 11 hits Enzyme Inhibition Constant Data Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 70 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford
Curated by ChEMBL
| Assay Description Inhibition of human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis |
J Med Chem 56: 547-55 (2013)
Article DOI: 10.1021/jm301583m BindingDB Entry DOI: 10.7270/Q26Q1ZJV |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 73 | n/a | n/a | n/a | n/a | n/a | n/a |
University of Oxford
Curated by ChEMBL
| Assay Description Inhibition of human PHD2 at 293K temperature by solvent relaxation technique |
J Med Chem 53: 867-75 (2010)
Article DOI: 10.1021/jm901537q BindingDB Entry DOI: 10.7270/Q2JD4WWN |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
China Pharmaceutical University
Curated by ChEMBL
| Assay Description Inhibition of recombinant PHD2 (unknown origin) catalytic domain (181 to 426 residues) expressed in Escherichia coli BL21 (DE3) cells using boitinyla... |
ACS Med Chem Lett 6: 1236-40 (2015)
Article DOI: 10.1021/acsmedchemlett.5b00394 BindingDB Entry DOI: 10.7270/Q2RB76G9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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| PDB Article PubMed
| n/a | n/a | 300 | n/a | n/a | n/a | n/a | n/a | n/a |
Japan Tobacco Inc.
Curated by ChEMBL
| Assay Description Inhibition of PHD2 (181 to 426 residues) (unknown origin) using biotinylated CODD peptide as substrate preincubated for 15 mins followed by substrate... |
ACS Med Chem Lett 8: 1320-1325 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00404 BindingDB Entry DOI: 10.7270/Q21N83N8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| n/a | n/a | 424 | n/a | n/a | n/a | n/a | n/a | n/a |
China Pharmaceutical University
Curated by ChEMBL
| Assay Description Displacement of FITC-HIF-1alpha (556 to 574 residues) from PHD2 (181 to 426 residues) (unknown origin) after 60 mins by fluorescence polarization ass... |
ACS Med Chem Lett 6: 1236-40 (2015)
Article DOI: 10.1021/acsmedchemlett.5b00394 BindingDB Entry DOI: 10.7270/Q2RB76G9 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
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| PDB Article PubMed
| n/a | n/a | 1.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Procter and Gamble Pharmaceuticals Inc
Curated by ChEMBL
| Assay Description Inhibition of human EGLN1 |
Bioorg Med Chem Lett 16: 5687-90 (2006)
Article DOI: 10.1016/j.bmcl.2006.08.017 BindingDB Entry DOI: 10.7270/Q25Q4WXS |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
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| PDB Article PubMed
| n/a | n/a | 3.90E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Sungkyunkwan University
Curated by ChEMBL
| Assay Description Inhibition of PHD2 in human Hep3B cells assessed as erythropoietin secretion by ELISA |
Bioorg Med Chem Lett 24: 3142-5 (2014)
Article DOI: 10.1016/j.bmcl.2014.05.003 BindingDB Entry DOI: 10.7270/Q2QN68F3 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL DrugBank MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | 3.90E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Sungkyunkwan University
Curated by ChEMBL
| Assay Description Inhibition of PHD2 (unknown origin) after 30 mins by fluorescence polarization assay |
Bioorg Med Chem Lett 23: 5953-7 (2013)
Article DOI: 10.1016/j.bmcl.2013.08.067 BindingDB Entry DOI: 10.7270/Q2XK8H1J |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
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CHEMBL DrugBank MCE MMDB PC cid PC sid PDB UniChem
Patents
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| PDB Article PubMed
| n/a | n/a | 7.50E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
Japan Tobacco Inc.
Curated by ChEMBL
| Assay Description Inhibition of human HIF-PHD2 assessed as reduction in HIF1-alpha binding to VBC complex using biotin-labeled HIF1-alpha peptide as substrate preincub... |
ACS Med Chem Lett 8: 1320-1325 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00404 BindingDB Entry DOI: 10.7270/Q21N83N8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | n/a | n/a | 7.90E+4 | n/a | n/a | n/a | n/a |
Japan Tobacco Inc.
Curated by ChEMBL
| Assay Description Inhibition of PHD2 in human Hep3B cells assessed as increase in EPO release after 24 hrs by ELISA |
ACS Med Chem Lett 8: 1320-1325 (2017)
Article DOI: 10.1021/acsmedchemlett.7b00404 BindingDB Entry DOI: 10.7270/Q21N83N8 |
More data for this Ligand-Target Pair | 3D Structure (crystal) |
Egl nine homolog 1
(246/246 = 100%)† (Homo sapiens (Human)) | BDBM50193145
(2-(1-chloro-4-hydroxyisoquinoline-3-carboxamido)ac...)Show InChI InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17) | PDB MMDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank antibodypedia GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE MMDB PC cid PC sid PDB UniChem
Patents
Similars
| PDB Article PubMed
| n/a | n/a | n/a | 80 | n/a | n/a | n/a | n/a | n/a |
University of Oxford
Curated by ChEMBL
| Assay Description Binding affinity to human PHD2 catalytic domain (181 to 426) Mn2 expressed in Escherichia coli by NMR spectroscopic analysis |
J Med Chem 56: 547-55 (2013)
Article DOI: 10.1021/jm301583m BindingDB Entry DOI: 10.7270/Q26Q1ZJV |
More data for this Ligand-Target Pair | 3D Structure (crystal) |