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Compile Data Set for Download or QSAR

Found 788 hits Enz. Inhib. hit(s) with Target = 'endothelial PAS domain-containing protein 1'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373041
PNG
(US10597366, Compound 292 | US9896418, Compound 292)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)C(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H11F4NO4S/c1-27(24,25)12-3-2-11(13-14(12)16(23)17(20,21)15(13)19)26-10-5-8(7-22)4-9(18)6-10/h2-6,15-16,23H,1H3/t15-,16+/m1/s1
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n/an/an/an/a 4n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373015
PNG
(US10597366, Compound 185 | US9896418, Compound 185)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)(F)F
Show InChI InChI=1S/C17H9F6NO4S/c18-9-3-8(7-24)4-10(5-9)28-12-1-2-13(29(26,27)17(21,22)23)14-11(12)6-16(19,20)15(14)25/h1-5,15,25H,6H2/t15-/m0/s1
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n/an/an/an/a<5n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372976
PNG
(US10597366, Compound 15 | US9896418, Compound 15)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1
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n/an/an/an/a 6n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372991
PNG
(US10597366, Compound 63 | US9896418, Compound 63)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)CF
Show InChI InChI=1S/C17H11F4NO4S/c18-8-27(24,25)14-2-1-13(12-6-17(20,21)16(23)15(12)14)26-11-4-9(7-22)3-10(19)5-11/h1-5,16,23H,6,8H2/t16-/m0/s1
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n/an/an/an/a 9n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282572
PNG
((R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy-...)
Show SMILES O[C@@H]1c2c(ccc(Oc3cc(F)cc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C16H8F5NO4S/c17-8-3-7(6-22)4-9(5-8)26-10-1-2-11-13(12(10)15(18)19)14(23)16(20,21)27(11,24)25/h1-5,14-15,23H/t14-/m1/s1
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n/an/an/an/a 10n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373040
PNG
(US10597366, Compound 289 | US9896418, Compound 289)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)[C@@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)12-3-2-11(13-14(12)17(22)16(20)15(13)19)25-10-5-8(7-21)4-9(18)6-10/h2-6,15-17,22H,1H3/t15-,16-,17+/m1/s1
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n/an/an/an/a 11n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282656
PNG
(4-(Difluoromethyl)-5-(3,5-difluorophenoxy)-2,2- di...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(F)c3)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C15H8F6O4S/c16-6-3-7(17)5-8(4-6)25-9-1-2-10-12(11(9)14(18)19)13(22)15(20,21)26(10,23)24/h1-5,13-14,22H
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n/an/an/an/a 13n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372976
PNG
(US10597366, Compound 15 | US9896418, Compound 15)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1
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n/an/an/an/a 14n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372972
PNG
(US10597366, Compound 11 | US9896418, Compound 11)
Show SMILES OC1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2
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n/an/an/an/a 15n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282572
PNG
((R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy-...)
Show SMILES O[C@@H]1c2c(ccc(Oc3cc(F)cc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C16H8F5NO4S/c17-8-3-7(6-22)4-9(5-8)26-10-1-2-11-13(12(10)15(18)19)14(23)16(20,21)27(11,24)25/h1-5,14-15,23H/t14-/m1/s1
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n/an/an/an/a 16n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373040
PNG
(US10597366, Compound 289 | US9896418, Compound 289)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)[C@@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)12-3-2-11(13-14(12)17(22)16(20)15(13)19)25-10-5-8(7-21)4-9(18)6-10/h2-6,15-17,22H,1H3/t15-,16-,17+/m1/s1
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n/an/an/an/a 17n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells assessed as reduction in VEGFA level incubated for 20 hrs prior to compound ...


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282632
PNG
(5-(3-Chloro-5-fluorophenoxy)-4-(difluoromethyl)- 2...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(Cl)c3)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C15H8ClF5O4S/c16-6-3-7(17)5-8(4-6)25-9-1-2-10-12(11(9)14(18)19)13(22)15(20,21)26(10,23)24/h1-5,13-14,22H
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n/an/an/an/a 17n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372964
PNG
(US10597366, Compound 8 | US9896418, Compound 8)
Show SMILES OC1c2c(CC1(F)F)c(Oc1cc(F)cc(Cl)c1)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C16H10ClF5O4S/c17-7-3-8(18)5-9(4-7)26-11-1-2-12(27(24,25)15(19)20)13-10(11)6-16(21,22)14(13)23/h1-5,14-15,23H,6H2
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n/an/an/an/a 20n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372991
PNG
(US10597366, Compound 63 | US9896418, Compound 63)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)CF
Show InChI InChI=1S/C17H11F4NO4S/c18-8-27(24,25)14-2-1-13(12-6-17(20,21)16(23)15(12)14)26-11-4-9(7-22)3-10(19)5-11/h1-5,16,23H,6,8H2/t16-/m0/s1
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n/an/an/an/a 20n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373008
PNG
(US10597366, Compound 163 | US9896418, Compound 163)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
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n/an/an/an/a 27n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373008
PNG
(US10597366, Compound 163 | US9896418, Compound 163)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
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n/an/an/an/a 27n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282685
PNG
(3-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C16H8F5NO4S/c17-8-3-7(6-22)4-9(5-8)26-10-1-2-11-13(12(10)15(18)19)14(23)16(20,21)27(11,24)25/h1-5,14-15,23H
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n/an/an/an/a 32n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372986
PNG
(US10597366, Compound 25 | US9896418, Compound 25)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cncc(Cl)c1)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C15H10ClF4NO4S/c16-7-3-8(6-21-5-7)25-10-1-2-11(26(23,24)14(17)18)12-9(10)4-15(19,20)13(12)22/h1-3,5-6,13-14,22H,4H2/t13-/m0/s1
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n/an/an/an/a 37n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373027
PNG
(US10597366, Compound 231 | US9896418, Compound 231)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2C[C@@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(12-7-13(19)17(21)16(12)15)24-11-5-9(8-20)4-10(18)6-11/h2-6,13,17,21H,7H2,1H3/t13-,17-/m1/s1
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n/an/an/an/a 39n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373027
PNG
(US10597366, Compound 231 | US9896418, Compound 231)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2C[C@@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(12-7-13(19)17(21)16(12)15)24-11-5-9(8-20)4-10(18)6-11/h2-6,13,17,21H,7H2,1H3/t13-,17-/m1/s1
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n/an/an/an/a 39n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373008
PNG
(US10597366, Compound 163 | US9896418, Compound 163)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
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n/an/an/an/a 41n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISA


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282581
PNG
(4-Bromo-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro-...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(Cl)c3)c2Br)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C14H7BrClF3O4S/c15-12-9(23-8-4-6(16)3-7(17)5-8)1-2-10-11(12)13(20)14(18,19)24(10,21)22/h1-5,13,20H
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n/an/an/an/a 43n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373008
PNG
(US10597366, Compound 163 | US9896418, Compound 163)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
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n/an/an/an/a 46n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells assessed as reduction in VEGFA level incubated for 20 hrs prior to compound ...


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372986
PNG
(US10597366, Compound 25 | US9896418, Compound 25)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cncc(Cl)c1)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C15H10ClF4NO4S/c16-7-3-8(6-21-5-7)25-10-1-2-11(26(23,24)14(17)18)12-9(10)4-15(19,20)13(12)22/h1-3,5-6,13-14,22H,4H2/t13-/m0/s1
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n/an/an/an/a 65n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50450495
PNG
(CHEMBL4159016 | US10597366, Compound 206)
Show SMILES CCS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C18H14F3NO4S/c1-2-27(24,25)15-4-3-14(13-8-18(20,21)17(23)16(13)15)26-12-6-10(9-22)5-11(19)7-12/h3-7,17,23H,2,8H2,1H3/t17-/m0/s1
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n/an/an/an/a 88n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282598
PNG
(5-(3-Chloro-5-fluorophenoxy)-2,2-difluoro-3- hydro...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(Cl)c3)c2C(F)(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C15H7ClF6O4S/c16-6-3-7(17)5-8(4-6)26-9-1-2-10-11(12(9)14(18,19)20)13(23)15(21,22)27(10,24)25/h1-5,13,23H
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Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372960
PNG
(US10597366, Compound 1 | US9896418, Compound 1)
Show SMILES O[C@@H]1CCc2c1c(ccc2Oc1cc(F)cc(Cl)c1)S(=O)(=O)C(F)F
Show InChI InChI=1S/C16H12ClF3O4S/c17-8-5-9(18)7-10(6-8)24-13-3-4-14(25(22,23)16(19)20)15-11(13)1-2-12(15)21/h3-7,12,16,21H,1-2H2/t12-/m1/s1
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n/an/an/an/a 110n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282584
PNG
(4-Chloro-5-(3-chloro-5-fluorophenoxy)-2,2-difluoro...)
Show SMILES OC1c2c(ccc(Oc3cc(F)cc(Cl)c3)c2Cl)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C14H7Cl2F3O4S/c15-6-3-7(17)5-8(4-6)23-9-1-2-10-11(12(9)16)13(20)14(18,19)24(10,21)22/h1-5,13,20H
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Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282572
PNG
((R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy-...)
Show SMILES O[C@@H]1c2c(ccc(Oc3cc(F)cc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C16H8F5NO4S/c17-8-3-7(6-22)4-9(5-8)26-10-1-2-11-13(12(10)15(18)19)14(23)16(20,21)27(11,24)25/h1-5,14-15,23H/t14-/m1/s1
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n/an/an/an/a 145n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELI...


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373008
PNG
(US10597366, Compound 163 | US9896418, Compound 163)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1
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n/an/an/an/a 158n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELI...


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282693
PNG
(5-((4-(Difluoromethyl)-2,2-difluoro-3-hydroxy-1,1-...)
Show SMILES OC1c2c(ccc(Oc3cncc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C15H8F4N2O4S/c16-14(17)11-9(25-8-3-7(4-20)5-21-6-8)1-2-10-12(11)13(22)15(18,19)26(10,23)24/h1-3,5-6,13-14,22H
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n/an/an/an/a 180n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372979
PNG
(US10597366, Compound 17 | US9896418, Compound 17)
Show SMILES OC1CCc2c1c(ccc2Oc1cc(F)cc(Cl)c1)S(=O)(=O)C(F)F
Show InChI InChI=1S/C16H12ClF3O4S/c17-8-5-9(18)7-10(6-8)24-13-3-4-14(25(22,23)16(19)20)15-11(13)1-2-12(15)21/h3-7,12,16,21H,1-2H2
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n/an/an/an/a 180n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372991
PNG
(US10597366, Compound 63 | US9896418, Compound 63)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)CF
Show InChI InChI=1S/C17H11F4NO4S/c18-8-27(24,25)14-2-1-13(12-6-17(20,21)16(23)15(12)14)26-11-4-9(7-22)3-10(19)5-11/h1-5,16,23H,6,8H2/t16-/m0/s1
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n/an/an/an/a 182n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELI...


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372976
PNG
(US10597366, Compound 15 | US9896418, Compound 15)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cc(F)cc(c1)C#N)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C17H10F5NO4S/c18-9-3-8(7-23)4-10(5-9)27-12-1-2-13(28(25,26)16(19)20)14-11(12)6-17(21,22)15(14)24/h1-5,15-16,24H,6H2/t15-/m0/s1
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n/an/an/an/a 233n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELI...


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM373000
PNG
(US10597366, Compound 124 | US9896418, Compound 124)
Show SMILES FC(F)c1cc(ccc1Oc1cc(F)cc(Cl)c1)S(=O)(=O)C(F)(F)F
Show InChI InChI=1S/C14H7ClF6O3S/c15-7-3-8(16)5-9(4-7)24-12-2-1-10(6-11(12)13(17)18)25(22,23)14(19,20)21/h1-6,13H
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n/an/an/an/a 240n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372994
PNG
(US10597366, Compound 74 | US9896418, Compound 74)
Show SMILES OCc1c(Br)c(Oc2cc(F)cc(Cl)c2)ccc1S(=O)(=O)C(F)F
Show InChI InChI=1S/C14H9BrClF3O4S/c15-13-10(6-20)12(24(21,22)14(18)19)2-1-11(13)23-9-4-7(16)3-8(17)5-9/h1-5,14,20H,6H2
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n/an/an/an/a 330n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282597
PNG
(US9884843, Compound 13)
Show SMILES Cc1c2C(O)C(F)(F)S(=O)(=O)c2ccc1Oc1cc(F)cc(Cl)c1
Show InChI InChI=1S/C15H10ClF3O4S/c1-7-11(23-10-5-8(16)4-9(17)6-10)2-3-12-13(7)14(20)15(18,19)24(12,21)22/h2-6,14,20H,1H3
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Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372988
PNG
(US10597366, Compound 41 | US9896418, Compound 41)
Show SMILES OCc1c(Cl)c(Oc2cc(F)cc(Cl)c2)ccc1S(=O)(=O)C(F)F
Show InChI InChI=1S/C14H9Cl2F3O4S/c15-7-3-8(17)5-9(4-7)23-11-1-2-12(10(6-20)13(11)16)24(21,22)14(18)19/h1-5,14,20H,6H2
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Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM438040
PNG
(US10597366, Compound 295)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)C[C@@H](O)c12
Show InChI InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(16-12(19)7-13(21)17(15)16)24-11-5-9(8-20)4-10(18)6-11/h2-6,12-13,21H,7H2,1H3/t12-,13+/m0/s1
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n/an/an/an/a 460n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50450496
PNG
(CHEMBL4170809 | US10597366, Compound 271)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2C[C@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(12-7-13(19)17(21)16(12)15)24-11-5-9(8-20)4-10(18)6-11/h2-6,13,17,21H,7H2,1H3/t13-,17+/m0/s1
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n/an/an/an/a 490n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50450496
PNG
(CHEMBL4170809 | US10597366, Compound 271)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2C[C@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H13F2NO4S/c1-25(22,23)15-3-2-14(12-7-13(19)17(21)16(12)15)24-11-5-9(8-20)4-10(18)6-11/h2-6,13,17,21H,7H2,1H3/t13-,17+/m0/s1
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n/an/an/an/a 490n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM372986
PNG
(US10597366, Compound 25 | US9896418, Compound 25)
Show SMILES O[C@H]1c2c(CC1(F)F)c(Oc1cncc(Cl)c1)ccc2S(=O)(=O)C(F)F
Show InChI InChI=1S/C15H10ClF4NO4S/c16-7-3-8(6-21-5-7)25-10-1-2-11(26(23,24)14(17)18)12-9(10)4-15(19,20)13(12)22/h1-3,5-6,13-14,22H,4H2/t13-/m0/s1
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n/an/an/an/a 617n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells assessed as free plasma adjusted EC50 for reduction in VEGFA concentration after 24 hrs by ELI...


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM282691
PNG
(5-((5-Chloropyridin-3-yl)oxy)-4-(difluoromethyl)- ...)
Show SMILES OC1c2c(ccc(Oc3cncc(Cl)c3)c2C(F)F)S(=O)(=O)C1(F)F
Show InChI InChI=1S/C14H8ClF4NO4S/c15-6-3-7(5-20-4-6)24-8-1-2-9-11(10(8)13(16)17)12(21)14(18,19)25(9,22)23/h1-5,12-13,21H
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n/an/an/an/a 630n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50398327
PNG
(VARIOLIN B)
Show SMILES Nc1nccc(n1)-c1c2ccnc(N)n2c2nccc(O)c12
Show InChI InChI=1S/C14H11N7O/c15-13-18-4-1-7(20-13)10-8-2-5-19-14(16)21(8)12-11(10)9(22)3-6-17-12/h1-6H,(H2,16,19)(H,17,22)(H2,15,18,20)
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n/an/an/an/a 700n/an/an/an/a



National Cancer Institute-Frederick

Curated by ChEMBL


Assay Description
Inhibition of HIF2alpha in human 786-0 cells expresseing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter ge...


J Nat Prod 75: 1632-6 (2012)


Article DOI: 10.1021/np300211x
BindingDB Entry DOI: 10.7270/Q2HM59KQ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM438032
PNG
(US10597366, Compound 287)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC[C@@H](O)c12
Show InChI InChI=1S/C17H14FNO4S/c1-24(21,22)16-5-4-15(13-2-3-14(20)17(13)16)23-12-7-10(9-19)6-11(18)8-12/h4-8,14,20H,2-3H2,1H3/t14-/m1/s1
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n/an/an/an/a 930n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50398322
PNG
(HETERONEMIN)
Show SMILES CC(=O)O[C@@H]1OC=C2[C@H]1[C@@]1(C)[C@H](O)C[C@@H]3[C@@]4(C)CCCC(C)(C)[C@@H]4CC[C@@]3(C)[C@@H]1C[C@@H]2OC(C)=O
Show InChI InChI=1S/C29H44O6/c1-16(30)34-19-13-22-28(6)12-9-20-26(3,4)10-8-11-27(20,5)21(28)14-23(32)29(22,7)24-18(19)15-33-25(24)35-17(2)31/h15,19-25,32H,8-14H2,1-7H3/t19-,20-,21+,22-,23+,24+,25-,27-,28+,29+/m0/s1
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n/an/an/an/a 1.20E+3n/an/an/an/a



National Cancer Institute-Frederick

Curated by ChEMBL


Assay Description
Inhibition of HIF2alpha in human 786-0 cells expresseing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter ge...


J Nat Prod 75: 1632-6 (2012)


Article DOI: 10.1021/np300211x
BindingDB Entry DOI: 10.7270/Q2HM59KQ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM438039
PNG
(US10597366, Compound 294)
Show SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@H](F)[C@@H](F)[C@@H](O)c12
Show InChI InChI=1S/C17H12F3NO4S/c1-26(23,24)12-3-2-11(13-14(12)17(22)16(20)15(13)19)25-10-5-8(7-21)4-9(18)6-10/h2-6,15-17,22H,1H3/t15-,16+,17-/m0/s1
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n/an/an/an/a 1.90E+3n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assay


J Med Chem 62: 6876-6893 (2019)


Article DOI: 10.1021/acs.jmedchem.9b00719
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50450493
PNG
(CHEMBL4164152 | US10597366, Compound 131)
Show SMILES FC(F)S(=O)(=O)c1ccc(Oc2cc(F)cc(Cl)c2)c(Br)c1
Show InChI InChI=1S/C13H7BrClF3O3S/c14-11-6-10(22(19,20)13(17)18)1-2-12(11)21-9-4-7(15)3-8(16)5-9/h1-6,13H
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n/an/an/an/a 2.20E+3n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50398328
PNG
(CHEMBL2177348)
Show SMILES COC1=C(C)C(=O)C2=C(C(COC(=O)C(\C)=C/C)N(C=O)C=C2)C1=O
Show InChI InChI=1S/C18H19NO6/c1-5-10(2)18(23)25-8-13-14-12(6-7-19(13)9-20)15(21)11(3)17(24-4)16(14)22/h5-7,9,13H,8H2,1-4H3/b10-5-
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n/an/an/an/a 2.70E+3n/an/an/an/a



National Cancer Institute-Frederick

Curated by ChEMBL


Assay Description
Inhibition of HIF2alpha in human 786-0 cells expresseing truncated HIF1alpha assessed as reduction in luciferase activity after 24 hrs by reporter ge...


J Nat Prod 75: 1632-6 (2012)


Article DOI: 10.1021/np300211x
BindingDB Entry DOI: 10.7270/Q2HM59KQ
More data for this
Ligand-Target Pair
Endothelial PAS domain-containing protein 1


(Homo sapiens (Human))
BDBM50450477
PNG
(CHEMBL4164767 | US10597366, Compound 16)
Show SMILES O[C@H]1CCc2c1c(ccc2Oc1cc(F)cc(Cl)c1)S(=O)(=O)C(F)F
Show InChI InChI=1S/C16H12ClF3O4S/c17-8-5-9(18)7-10(6-8)24-13-3-4-14(25(22,23)16(19)20)15-11(13)1-2-12(15)21/h3-7,12,16,21H,1-2H2/t12-/m0/s1
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n/an/an/an/a 2.90E+3n/an/an/an/a



Peloton Therapeutics, Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at HIF-2alpha in human 786-O cells co-expressing HIF responsive element after 24 hrs by ONE-Glo luciferase reporter gene assay


J Med Chem 61: 9691-9721 (2018)


Article DOI: 10.1021/acs.jmedchem.8b01196
BindingDB Entry DOI: 10.7270/Q2H997RJ
More data for this
Ligand-Target Pair
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