BDBM50341448 4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one::AZELASTINE::Astelin::Astepro::CHEMBL639::Optilast::Optivar::Rhinolast::US20230414632, Compound II-a::rac-Azelastine
SMILES CN1CCCC(CC1)n1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
InChI Key InChIKey=MBUVEWMHONZEQD-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 23 hits for monomerid = 50341448
Affinity DataKi: 1.20nMAssay Description:Antagonist activity at human Histamine H1 receptor expressed in CHO cells assessed as inhibition of histamine-induced calcium flux preincubated for 3...More data for this Ligand-Target Pair
Affinity DataKi: 1.20nMAssay Description:Antagonist activity at human H1 receptor expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assayMore data for this Ligand-Target Pair
Affinity DataKi: 1.26nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair
Affinity DataKi: 20nMAssay Description:Displacement of [3H]mesulergine from recombinant human 5-ht2B expressed in CHO cellsMore data for this Ligand-Target Pair
Affinity DataKi: 50nMAssay Description:Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptorMore data for this Ligand-Target Pair
Affinity DataKi: 50nMAssay Description:Antagonist activity at adrenergic alpha1A receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux...More data for this Ligand-Target Pair
Affinity DataKi: 50nMAssay Description:Antagonist activity at adrenergic alpha1B receptor (unknown origin) expressed in Rat1 cells assessed as inhibition of phenylephrine-induced Ca2+ flux...More data for this Ligand-Target Pair
Affinity DataKi: 50.1nMAssay Description:Antagonist activity at human adrenergic alpha1B receptor expressed in rat fibroblasts by by plate-based calcium imagingMore data for this Ligand-Target Pair
Affinity DataKi: 50.1nMAssay Description:Antagonist activity at human adrenergic alpha1A receptor expressed in rat fibroblasts by by plate-based calcium imagingMore data for this Ligand-Target Pair
Affinity DataKi: 148nMAssay Description:Antagonist activity at human H3 receptor expressed in CHO cells assessed as inhibition of histamine-induced GTPgamma[S] binding by scintillation prox...More data for this Ligand-Target Pair
Affinity DataKi: 148nMAssay Description:Antagonist activity at human Histamine H3 receptor expressed in CHO cell membranes assessed as inhibition of histamine-induced [35S]GTPgammaS binding...More data for this Ligand-Target Pair
Affinity DataKi: 501nMAssay Description:Displacement of [3H]mesulergine from recombinant human 5-ht2C expressed in CHO cellsMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Glaxosmithkline
Curated by ChEMBL
Glaxosmithkline
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Displacement of [3H]-Dofetilide from recombinant human ERG expressed in CHOK1 cell membranes incubated for 4 hrs under dark condition by luminescence...More data for this Ligand-Target Pair
Affinity DataIC50: 6.31E+3nMAssay Description:Displacement of [3H]AF-DX 384 from recombinant human M1 receptor expressed in CHO cellsMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Glaxosmithkline
Curated by ChEMBL
Glaxosmithkline
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Displacement of [3H]dofetilide from human ERGMore data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Glaxosmithkline
Curated by ChEMBL
Glaxosmithkline
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Displacement of [3H]-dofetilide from human ERG expressed in CHOK1 cell membranes incubated for 4 hrs in dark by luminescent assayMore data for this Ligand-Target Pair
Affinity DataIC50: 1.60E+4nMAssay Description:TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 3.00E+4nMAssay Description:TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cellsMore data for this Ligand-Target Pair
Affinity DataIC50: 1.00E+3nMAssay Description:Inhibition of CYP2D6More data for this Ligand-Target Pair
TargetVoltage-dependent L-type calcium channel subunit alpha-1C(Cavia porcellus)
Jagiellonian University
Curated by ChEMBL
Jagiellonian University
Curated by ChEMBL
Affinity DataIC50: 2.02E+4nMAssay Description:Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytesMore data for this Ligand-Target Pair
TargetLysine--tRNA ligase(Homo sapiens (Human))
Centre National De La Recherche Scientifique
US Patent
Centre National De La Recherche Scientifique
US Patent
Affinity DataIC50: 3.00E+5nMAssay Description:Homogeneous time-resolved fluorescence (HTRF) assays were performed in black, half-area, flat bottom, 96-well microplates (Costar #3694). Human mitoc...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Glaxosmithkline
Curated by ChEMBL
Glaxosmithkline
Curated by ChEMBL
Affinity DataIC50: 100nMAssay Description:Displacement of labeled dofetilide human ERGMore data for this Ligand-Target Pair
Affinity DataKd: 0.200nMAssay Description:Antagonist activity at human recombinant histamine H1 receptor expressed in intact CHO cells assessed as inhibition of histamine-induced cellular cal...More data for this Ligand-Target Pair