Compile Data Set for Download or QSAR
Report error Found 13 Enz. Inhib. hit(s) for PDB: 5TBM
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 5nMAssay Description:HIF-2a: The total assay volume was about 100 uL in the following configuration: 2 uL compound in 100% DMSO, 88 uL buffer with protein and probe and 1...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 8.5nMAssay Description:HIF-2a: The total assay volume was about 100 uL in the following configuration: 2 uL compound in 100% DMSO, 88 uL buffer with protein and probe and 1...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 12nMAssay Description:Inhibition of N-(3-Chlorophenyl-4,6-t2)-4-nitrobenzo[c][1,2,5]oxadiazol-5-amine binding to his-tagged HIF-2alpha PAS-B domain (unknown origin) measur...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 12nMAssay Description:Binding affinity to His-tagged HIF-2alpha PAS-B domain (unknown origin) after 2 hrs by scintillation proximity assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataKd:  17nMAssay Description:Binding affinity to human recombinant HIF-2alpha (240 to 350 residues) assessed as as dissociation constant by ITC analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 17nMAssay Description:HIF-2a: The total assay volume was about 100 uL in the following configuration: 2 uL compound in 100% DMSO, 88 uL buffer with protein and probe and 1...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/13/2020
Entry Details
Go to US Patent
PDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataEC50:  27nMAssay 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 assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataEC50:  27nMAssay Description:Inhibition of HIF-2alpha (unknown origin) expressed in human 786-O cells measured after 24 hrs by one-glo luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 27nMAssay Description:Inhibition of HIF-2alpha transcriptional activity in human 786-0 cells transfected with HRE-luc2P assessed as decrease in luminescence incubated for ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataIC50: 39nMAssay Description:Inhibition of HIF-2alpha transcriptional activity in human 786-0 cells assessed as decrease in VEGF production incubated for 48 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataEC50:  41nMAssay Description:Antagonist activity at HIF-2alpha in human 786-O cells assessed as reduction in VEGFA concentration after 24 hrs by ELISAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataEC50:  46nMAssay 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 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/18/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelial PAS domain-containing protein 1(Human)
Peloton Therapeutics

US Patent
LigandPNGBDBM373008(US9896418, Compound 163 | US10597366, Compound 163)
Affinity DataEC50:  158nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)