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(CCN2CCC(CC2)Nc2nc3ccccc3n2Cc2ccc(F)cc2)cc1
InChI Key InChIKey=GXDALQBWZGODGZ-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 66 hits for monomerid = 24226
TargetHistamine H1 receptor(Homo sapiens (Human))
Janssen Research Foundation
Curated by PDSP Ki Database
Janssen Research Foundation
Curated by PDSP Ki Database
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Janssen Research Foundation
Curated by PDSP Ki Database
Janssen Research Foundation
Curated by PDSP Ki Database
TargetHistamine H1 receptor(Homo sapiens (Human))
Janssen Research Foundation
Curated by PDSP Ki Database
Janssen Research Foundation
Curated by PDSP Ki Database
Affinity DataKi: 2.09nMAssay Description:Displacement of [3H]mepyramine from human H1R expressed in Sf9 cells co-expressing RGS4 after 90 mins by liquid scintillation countingMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataKi: 2.90nMAssay Description:Binding affinity at hERG expressed in HEK293 cells by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetHistamine H1 receptor(Homo sapiens (Human))
Janssen Research Foundation
Curated by PDSP Ki Database
Janssen Research Foundation
Curated by PDSP Ki Database
Affinity DataKi: 3nMAssay Description:Binding affinity towards histamine H1 receptorMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataKi: 13nMAssay Description:Displacement of [3H]dofetilide from hERG expressed in HEK293 cells by SPAMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataKi: 20nMAssay Description:Binding affinity to human ERGMore data for this Ligand-Target Pair
TargetSigma intracellular receptor 2(Homo sapiens (Human))
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
Affinity DataKi: 95nMAssay Description:Displacement of [3H]-DTG from the Sigma2 receptorMore data for this Ligand-Target Pair
TargetSigma intracellular receptor 2(Homo sapiens (Human))
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
Affinity DataKi: 95nMAssay Description:Displacement of [3H]-DTG from the Sigma2 receptorMore data for this Ligand-Target Pair
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
Affinity DataKi: 1.26E+3nMAssay Description:Displacement of [3H]-pentazocin from the Sigma1 receptorMore data for this Ligand-Target Pair
TargetSigma non-opioid intracellular receptor 1(Homo sapiens (Human))
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
QBI COVID-19 Research Group (QCRG)
Curated by ChEMBL
Affinity DataKi: 1.27E+3nMAssay Description:Displacement of [3H]-pentazocin from the Sigma1 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 4.07E+3nMAssay Description:Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 4.07E+3nMAssay Description:Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cellsMore data for this Ligand-Target Pair
Affinity DataKi: 7.94E+3nMAssay Description:Displacement of [3H]histamine from human H4R expressed in Sf9 cells co-expressing RGS19, Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillat...More data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of SST14 from human recombinant SST3 receptorMore data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of SST14 from human recombinant SST4 receptorMore data for this Ligand-Target Pair
Affinity DataKi: >1.00E+4nMAssay Description:Displacement of SST14 from human recombinant SST2 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 2.30E+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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 11.5nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
TargetUbiquitin-conjugating enzyme E2 N(Homo sapiens (Human))
Burnham Center for Chemical Genomics
Curated by PubChem BioAssay
Burnham Center for Chemical Genomics
Curated by PubChem BioAssay
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
TargetProtein farnesyltransferase subunit beta/geranylgeranyltransferase type-1 subunit alpha(Bos taurus (bovine))
Centre de Recherche Pierre Fabre
Curated by ChEMBL
Centre de Recherche Pierre Fabre
Curated by ChEMBL
Affinity DataIC50: 2nMAssay Description:Inhibit of purified bovine Farnesyl protein transferase.More data for this Ligand-Target Pair
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
TargetGlycine receptor subunit alpha-1(Homo sapiens (Human))
University of Pittsburgh
Curated by ChEMBL
University of Pittsburgh
Curated by ChEMBL
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibition of hERG potassium channel in HEK293 cells by patch clamp assayMore data for this Ligand-Target Pair
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
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
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
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
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
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 6.03nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:Inhibitory activity against Potassium channel HERGMore data for this Ligand-Target Pair
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
F. Hoffmann-La Roche Inc
Curated by ChEMBL
F. Hoffmann-La Roche Inc
Curated by ChEMBL
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
Affinity DataIC50: 3.30E+3nMAssay Description:Inhibition of human cytochrome P450 3A4More data for this Ligand-Target Pair
TargetATP-dependent translocase ABCB1(Mus musculus (Mouse))
F. Hoffmann-La Roche Inc
Curated by ChEMBL
F. Hoffmann-La Roche Inc
Curated by ChEMBL
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
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
F. Hoffmann-La Roche Inc
Curated by ChEMBL
F. Hoffmann-La Roche Inc
Curated by ChEMBL
Affinity DataIC50: 300nMAssay Description:Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCECMore data for this Ligand-Target Pair
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 1.5nMAssay Description:Inhibitory concentration against IKr potassium channelMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 6nMAssay Description:Inhibition of human Potassium channel HERG expressed in mammalian cellsMore data for this Ligand-Target Pair
TargetHeparanase(Homo sapiens (Human))
Structural Biochemistry Laboratory, Centro de Investigaci�n Pr�ncipe Felipe, 46012 Valencia, Spain. rgozalbes@cipf.es
Curated by ChEMBL
Structural Biochemistry Laboratory, Centro de Investigaci�n Pr�ncipe Felipe, 46012 Valencia, Spain. rgozalbes@cipf.es
Curated by ChEMBL
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
TargetHistamine H1 receptor(Cavia porcellus (domestic guinea pig))
Janssen Research Foundation
Curated by PDSP Ki Database
Janssen Research Foundation
Curated by PDSP Ki Database
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
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
TargetMultidrug and toxin extrusion protein 1(Homo sapiens (Human))
University of California
Curated by ChEMBL
University of California
Curated by ChEMBL
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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 0.912nMAssay Description:Inhibition of human ERG in MCF7 cellsMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 10nMAssay Description:Inhibition of human ERG expressed in CHO cells by whole cell patch clamp techniqueMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Pfizer Inc
Curated by ChEMBL
Pfizer Inc
Curated by ChEMBL
Affinity DataIC50: 0.900nMAssay Description:K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1More data for this Ligand-Target Pair
TargetATP-dependent translocase ABCB1(Homo sapiens (Human))
F. Hoffmann-La Roche Inc
Curated by ChEMBL
F. Hoffmann-La Roche Inc
Curated by ChEMBL
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