BDBM50247053 1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine::CHEMBL462605::Tiprolisant
SMILES Clc1ccc(CCCOCCCN2CCCCC2)cc1
InChI Key InChIKey=NNACHAUCXXVJSP-UHFFFAOYSA-N
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 47 hits for monomerid = 50247053
Affinity DataKi: 0.160nMAssay Description:Antagonist activity at recombinant human H3 receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.160nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]gammaS binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.160nMAssay Description:Inhibition of Guinea Pig Ileum H3RMore data for this Ligand-Target Pair
Affinity DataKi: 0.160nMAssay Description:Inhibition of Guinea Pig Ileum H3RMore data for this Ligand-Target Pair
Affinity DataKi: 0.160nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Inhibition of human H3 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Binding affinity to human H3RMore data for this Ligand-Target Pair
Affinity DataKi: 0.300nMAssay Description:Binding affinity to human histamine H3 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 0.912nMAssay Description:Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 2.40nMAssay Description:Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in CHO-K1 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 2.5nMAssay Description:Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 2.5nMAssay Description:Antagonist activity at histamine H3 receptor (unknown origin)More data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in rat C6 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cellsMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [125I]iodoproxyfan human histamine H3 receptorMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cellsMore data for this Ligand-Target Pair
Affinity DataKi: 2.70nMAssay Description:Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor after 60 mins by gamma counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 3nMAssay Description:Displacement of N-alpha-[methyl-3H]-methylhistamine dihydrochloride from recombinant human histamine H3 receptor expressed in CHO-K1 cells assessed a...More data for this Ligand-Target Pair
Affinity DataKi: 8nMAssay Description:Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor stably transfected in HEK-293T cells membrane incubated for 9...More data for this Ligand-Target Pair
Affinity DataKi: 11nMAssay Description:Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells incubated for 90 mins by competitio...More data for this Ligand-Target Pair
Affinity DataKi: 11nMAssay Description:Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assayMore data for this Ligand-Target Pair
Affinity DataKi: 11nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in HEK-293 cell membrane after 90 mins by liquid scintillation counting ...More data for this Ligand-Target Pair
Affinity DataKi: 12nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from human histamine H3 receptor stably expressed in HEK293 cell membrane after 90 minsMore data for this Ligand-Target Pair
Affinity DataKi: 12nMAssay Description:Displacement of [3H]N-alpha-Methylhistamine from recombinant human histamine H3 receptor expressed in human HEK293 cells incubated for 90 mins by mic...More data for this Ligand-Target Pair
Affinity DataKi: 12nMAssay Description:Displacement of [3H]-N-alpha-methylhistamine from human recombinant full length H3R expressed in HEK293 cell membranes incubated for 90 mins by liqui...More data for this Ligand-Target Pair
Affinity DataKi: 14nMAssay Description:Displacement of [125I]-iodoproxyfan from mouse brain cortex H3 receptor after 60 mins by gamma counting methodMore data for this Ligand-Target Pair
Affinity DataKi: 14.8nMAssay Description:Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Binding affinity to rat histamine H3 receptorMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Binding affinity to histamine H3 receptor in rat cerebral cortexMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Displacement of [125I]-iodoproxyfan from rat brain cortex H3 receptor after 60 mins by gamma counting methodMore data for this Ligand-Target Pair
TargetHistamine H3 receptor(Rattus norvegicus (rat))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataKi: 17nMAssay Description:Binding affinity to rat H3RMore data for this Ligand-Target Pair
Affinity DataKi: 28nMAssay Description:Displacement of [3]-RAMH from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes after 60 mins by scintillation countingMore data for this Ligand-Target Pair
Affinity DataKi: 30nMAssay Description:Displacement of [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cells by microbeta scintillation analysi...More data for this Ligand-Target Pair
Affinity DataKi: 1.15E+3nMAssay Description:Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysisMore data for this Ligand-Target Pair
Affinity DataKi: <1.00E+4nMAssay Description:Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by li...More data for this Ligand-Target Pair
Affinity DataKi: 1.34E+4nMAssay Description:Binding affinity to human H3 receptor assessed as inhibition constant incubated for 90 mins by scintillation counting methodMore data for this Ligand-Target Pair
Affinity DataKi: >1.00E+5nMAssay Description:Inhibition of human H4 receptorMore data for this Ligand-Target Pair
Affinity DataKi: >1.00E+5nMAssay Description:Binding affinity to human H4RMore data for this Ligand-Target Pair
Affinity DataKd: 5.62nMAssay Description:Antagonist activity at histamine H3 receptor in isolated guinea pig ileumMore data for this Ligand-Target Pair
Affinity DataIC50: 12nMAssay Description:Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GT...More data for this Ligand-Target Pair
Affinity DataIC50: 19nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of imetit-stimulation ERK1/2 phosphorylation by E...More data for this Ligand-Target Pair
Affinity DataEC50: 8nMAssay Description:Inverse agonist activity at recombinant human histamine H3 receptor expressed in CHO-K1 cells preincubated for 10 mins followed by [35S]GTPgammaS add...More data for this Ligand-Target Pair
TargetCholinesterase(Equus caballus (Horse))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataIC50: 8.42E+3nMAssay Description:Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured...More data for this Ligand-Target Pair
TargetCholinesterase(Equus caballus (Horse))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataIC50: 8.40E+3nMAssay Description:Inhibition of equine serum BChE using BTCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophoto...More data for this Ligand-Target Pair
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Jagiellonian University Medical College
Curated by ChEMBL
Jagiellonian University Medical College
Curated by ChEMBL
Affinity DataIC50: 1.70E+3nMAssay Description:Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp methodMore data for this Ligand-Target Pair
Affinity DataEC50: 1.5nMAssay Description:Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayMore data for this Ligand-Target Pair