BDBM373008 US10597366, Compound 163::US9896418, Compound 163
SMILES CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12
InChI Key InChIKey=ONBSHRSJOPSEGS-INIZCTEOSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 20 hits for monomerid = 373008
Affinity DataEC50: 42nMAssay Description:Four hours later, serial dilutions of 10× compound stocks were made in growth medium from 500×DMSO stocks, and 20 μL of those 10× stocks were ad...More data for this Ligand-Target Pair
Affinity DataEC50: 42nMAssay Description:VEGF: Four hours later, serial dilutions of 10x compound stocks were made in growth medium from 500xDMSO stocks, and 20 uL of those 10x stocks were a...More data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of of CYP2C8 in human liver microsomes using amodiaquine as substrate after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 4.60E+4nMAssay Description:Inhibition of of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 20 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
3D Structure (crystal)TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of of CYP1A2 in human liver microsomes using phenacetin after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of of CYP2B6 in human liver microsomes using bupropion as substrate after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: 2.30E+4nMAssay Description:Inhibition of of CYP2C9 in human liver microsomes using diclofenac as substrate after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
Affinity DataIC50: >5.00E+4nMAssay Description:Inhibition of of CYP3A4 in human liver microsomes using midazolam as substrate after 10 mins in presence of NADPH by LC-MS/MS analysisMore data for this Ligand-Target Pair
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
TargetEndothelial PAS domain-containing protein 1(Homo sapiens (Human))
Peloton Therapeutics
Curated by ChEMBL
Peloton Therapeutics
Curated by ChEMBL
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
Affinity DataEC50: 42nMAssay Description:About 7500 of 786-0 cells in 180 μL of growth medium were seeded into each well of a 96 well plate with white clear bottom on the first day (07-...More data for this Ligand-Target Pair