BDBM24226 1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine::ASTEMIZOLE::Astemizole, [O-Methyl-3H]::CHEMBL296419::Hismanal::Histaminos::[3H]-ASTEMIZOLE::[3H]Astemizole::cid_2247::med.21724, Compound Astemizole

SMILES COc1ccc(cc1)CCN2CCC(CC2)Nc3nc4ccccc4n3Cc5ccc(cc5)F

InChI Key InChIKey=GXDALQBWZGODGZ-UHFFFAOYSA-N

Data  19 KI  42 IC50  3 Kd  4 EC50

PDB links: 3 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 68 hits for monomerid = 24226   

LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetATP-dependent translocase ABCB1(Mouse)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetHeparanase(Human)
Centro De Investigaci�N Pr�Ncipe Felipe

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKd: >1.00E+6nMAssay Description:Binding affinity to recombinant heparanase catalytic stie (unknown origin) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assa...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetHistamine H1 receptor(Guinea pig)
University of Regensburg

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKd:  3.80nMAssay Description:Antagonist activity at H1R in guinea pig ileum assessed as inhibition of histamine-induced muscle contraction after 15 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
TargetMultidrug and toxin extrusion protein 1(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 2.64E+4nMAssay Description:Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetATP-dependent translocase ABCB1(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.30E+3nMAssay Description:TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.00E+4nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/28/2019
Entry Details Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 5.88E+4nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2019
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
TargetHLA class I histocompatibility antigen, A alpha chain(Human)
University of Illinois At Chicago

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKd:  2.50E+3nMAssay Description:Binding affinity to human biotinylated HLA-A2 by surface plasmon resonance assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.10E+3nMAssay Description:Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunitsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/3/2020
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetOrf1a protein(MERS-CoV)
University of Bonn

LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataEC50:  4.88E+3nMAssay Description:This is a review article.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2020
Entry Details Article
PubMed
TargetReplicase polyprotein 1ab(SARS-CoV)
University of Bonn

LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataEC50:  5.59E+3nMAssay Description:This is a review article.More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/7/2020
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetCytochrome P450 3A4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.06E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetUbiquitin-conjugating enzyme E2 N(Human)
Burnham Center For Chemical Genomics

Curated by PubChem BioAssay
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 2.00E+4nMAssay Description:Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG) Source Affiliation: Sanford-Burnham Medical Research Institute (SBMRI, San Diego CA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/2/2011
Entry Details
PCBioAssay
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 2nMAssay Description:Inhibit of purified bovine Farnesyl protein transferase.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/9/2012
Entry Details Article
PubMed
TargetPolycomb protein EED(Human)
Chinese Academy of Sciences

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 9.38E+4nMAssay Description:Displacement of FITC-labeled EZH2 peptide from recombinant N-terminal 6His-tagged EED (residues 81 to 441) (unknown origin) expressed in Escherichia ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/12/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGlycine receptor subunit alpha-1(Human)
University of Pittsburgh

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataEC50:  4.20E+3nMAssay Description:Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-el...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
TargetCytochrome P450 2C8(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of CYP2D6 in human liver microsomes using dextromethorphan as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetCytochrome P450 2C19(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.37E+4nMAssay Description:Inhibition of CYP2C19 in human liver microsomes using S-mephenytoin as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetATP-dependent translocase ABCB1(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 300nMAssay Description:Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCECMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of CYP2C9 in human liver microsomes using diclofenac as substrate after 8 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/3/2016
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
TargetATP-dependent translocase ABCB1(Mouse)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.30E+3nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetPotassium voltage-gated channel subfamily H member 2(Human)
China Pharmaceutical University

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)
China Pharmaceutical University

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)
TargetATP-dependent translocase ABCB1(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 1.30E+3nMAssay Description:Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Pfizer

Curated by ChEMBL
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataIC50: 3.30E+3nMAssay Description:Inhibition of human cytochrome P450 3A4More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMed
TargetHistamine H1 receptor(Human)
Janssen Research Foundation

Curated by PDSP Ki Database
LigandPNGBDBM24226(cid_2247 | [3H]-ASTEMIZOLE | Hismanal | ASTEMIZOLE...)
Affinity DataKi:  0.800nMMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2012
Entry Details Article
PubMed
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