Compile Data Set for Download or QSAR
Report error Found 25 Enz. Inhib. hit(s) for PDB: 8ZYO
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 0.900nMAssay Description:Inhibitory activity against Potassium channel HERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/27/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 0.900nMAssay Description:K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/26/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 0.900nMAssay Description:Inhibition of hERG potassium channel in HEK293 cells by patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 0.910nMAssay Description:Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open stateMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/23/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 0.912nMAssay Description:Inhibition of human ERG in MCF7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.5nMAssay Description:Inhibitory concentration against IKr potassium channelMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataEC50:  1.90nMAssay Description:Binding affinity to human ERG by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/2/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKi:  2.90nMAssay Description:Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.30nMAssay Description:Inhibition of human ERG assessed as reduction in channel current by automated patch-clamp electrophysiology assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/4/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 4nMAssay Description:Inhibition of human ERG expressed in CHO K1 cells measured after 4 min by QPatch assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 4.20nMAssay Description:Inhibition of human ERG stably expressed in CHO-K1 cells at -90 mV holding potential by automated Q-patch clamp methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 4.20nMAssay Description:Inhibition of human ERG expressed in CHO-K1 cells by Q-patch clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 6nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/8/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 6.03nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/8/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 8nMAssay Description:Inhibition of human ERG expressed in HEK293 cells coexpressing Kir2.3 after 30 mins by FluxOR based FLIPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/8/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 10nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/20/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 10nMAssay Description:Inhibition of human ERG expressed in CHO cells by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/21/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKi:  11nMAssay Description:Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 11.5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKi:  13nMAssay Description:Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/10/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 14nMAssay Description:Inhibition of [3H]-astemizole binding to human ERG expressed in HEK293 cell membranes by scintillation counting methodMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/28/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKi:  20nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/1/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 23nMAssay Description:Displacement of [3H] dofetilide from human ERG channel expressed in HEK293 cell membranes incubated for 2 hrs by scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/29/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 305nMAssay Description:Inhibition of human ERG expressed in Xenopus laevis oocytes by two-electrode voltage clamp assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/15/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
Aventis Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 2.60E+3nMAssay Description:Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)