BDBM50247054 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylnicotinamide::CHEMBL517140::GSK-189254

SMILES CNC(=O)c1ccc(Oc2ccc3CCN(CCc3c2)C2CCC2)nc1

InChI Key InChIKey=WROHEWWOCPRMIA-UHFFFAOYSA-N

Data  8 KI  1 IC50

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 9 hits for monomerid = 50247054   

TargetHistamine H3 receptor(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  0.120nMAssay Description:Binding affinity to histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  0.126nMAssay Description:Binding affinity to human histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  0.260nMAssay Description:Displacement of [3H]-N-R-methylhistamine from human H3 receptor isolated from C6 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  0.631nMAssay Description:Binding affinity to rat cortical histamine H3 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  0.676nMAssay Description:Displacement of [3H]-R-alpha-ethylhistamine from rat histamine H3 receptor expressed in HEK293 cells after 45 mins by liquid scintillation spectromet...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Rattus norvegicus (rat))
TBA

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi:  2.60nMAssay Description:Displacement of [3H]-R-alpha-ethylhistamine from histamine H3 receptor in rat cerebral cortical tissue membranes after 45 mins by liquid scintillatio...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H1 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi: >2.51E+3nMAssay Description:Binding affinity to human histamine H1 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H2 receptor(Homo sapiens (Human))
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataKi: >3.16E+3nMAssay Description:Binding affinity to human histamine H2 receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetHistamine H3 receptor(Homo sapiens (Human))
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM50247054(6-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azep...)
Affinity DataIC50:  0.550nMAssay 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
In DepthDetails ArticlePubMed