Compile Data Set for Download or QSAR
Report error Found 13 Enz. Inhib. hit(s) with all data for entry = 50010008
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50051007(4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2...)
Affinity DataKi:  0.0340nMAssay Description:Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50051007(4-Benzo[1,3]dioxol-5-yl-1-dibutylcarbamoylmethyl-2...)
Affinity DataIC50: 0.0550nMAssay Description:Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membraneMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Rat)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50112678((R)-2-Benzo[1,3]dioxol-5-yl-6-isopropoxy-4-(4-meth...)
Affinity DataIC50: 0.190nMAssay Description:Displacement of [125I]ET-1 from ET-A receptor in RASMC incubated for 60 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50105051(N-{6-[2-(5-Bromo-pyrimidin-2-yloxy)-ethoxy]-5-p-to...)
Affinity DataIC50: 0.400nMAssay Description:Antagonist activity at ET-A receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin receptor type B(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50534382(CHEMBL4568795)
Affinity DataIC50: 1.20nMAssay Description:Displacement of [125I]ET-1 from ET-B receptor in human Girardi heart cells incubated for 4 hrs by gamma counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin receptor type B(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50071433((S)-2-{(R)-3-Biphenyl-4-yl-2-[(3,5-dimethyl-benzoy...)
Affinity DataIC50: 1.30nMAssay Description:Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50079424((S)-3-[2-(3,4-Dimethoxy-phenyl)-ethoxy]-2-(4,6-dim...)
Affinity DataKi:  2.20nMAssay Description:Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin receptor type B(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50079424((S)-3-[2-(3,4-Dimethoxy-phenyl)-ethoxy]-2-(4,6-dim...)
Affinity DataKi:  4.80nMAssay Description:Displacement of [125I]ET-3 from human ET-B receptor expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin receptor type B(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50105051(N-{6-[2-(5-Bromo-pyrimidin-2-yloxy)-ethoxy]-5-p-to...)
Affinity DataIC50: 12nMAssay Description:Antagonist activity at ET-B receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50061101(4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyph...)
Affinity DataIC50: 45nMAssay Description:Antagonist activity at ET-A receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50071433((S)-2-{(R)-3-Biphenyl-4-yl-2-[(3,5-dimethyl-benzoy...)
Affinity DataIC50: 94nMAssay Description:Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetEndothelin receptor type B(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50061101(4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyph...)
Affinity DataIC50: 202nMAssay Description:Antagonist activity at ET-B receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEndothelin-1 receptor(Human)
Centre Hospitalier Universitaire Vaudois (Chuv)

Curated by ChEMBL
LigandPNGBDBM50534382(CHEMBL4568795)
Affinity DataIC50: 1.30E+3nMAssay Description:Displacement of [125I]ET-1 from ET-A receptor in human SK-N-MC cells incubated for 4 hrs by gamma counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed