BDBM50000483 (BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide::(granisetron)1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide::1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl)-amide::1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide::1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide(BRL 43694)::1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide(Granisetron)::1-methyl-N-((1S,5R)-9-methyl-9-aza-bicyclo[3.3.1]nonan-3-yl)-1H-indazole-3-carboxamide::2-(9-Methyl-3,9-diaza-bicyclo[3.3.1]non-3-yl)-1-(1-methyl-1H-indol-3-yl)-ethanone(Granisetron)::BRL 43694::BRL-43694::CHEMBL519643::GRANISETRON::LY-278584

SMILES CN1C2CCCC1CC(C2)NC(=O)c1nn(C)c2ccccc12

InChI Key InChIKey=MFWNKCLOYSRHCJ-UHFFFAOYSA-N

Data  26 KI  10 IC50  2 Kd

PDB links: 2 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 38 hits for monomerid = 50000483   

Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  0.251nMAssay Description:Displacement of [3H]granisetron from 5-hydroxytryptamine 3 receptor of rat cortexMore data for this Ligand-Target Pair
In DepthDetails PDB3D3D Structure (crystal)
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  0.589nMAssay Description:Potency at neuronal 5-hydroxytryptamine 3 receptor in the rabbit heartMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  0.590nMAssay Description:Binding affinity for central 5-hydroxytryptamine 3 receptor was determined by displacement of [3H]-ketanserinMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  0.780nMAssay Description:Displacement of [3H]- GR-65,630 binding to 5-hydroxytryptamine 3 receptor in rat brain cortical membranesMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
University Of Warwick

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.45nMAssay Description:Displacement of [3H]granisetron from human 5HT3A receptor expressed in HEK293 cells by scintillation countingMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
University Of Warwick

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.45nMAssay Description:Displacement of [3H]granisetron from human 5HT3A expressed in HEK293 cells after 1 hr by scintillation countingMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.60nMAssay Description:pKi value for inhibition of [3H]LY-278584 binding to 5-hydroxytryptamine 3 receptorMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.60nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-a...More data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.70nMAssay Description:Displacement of the 5-hydroxytryptamine 3 receptor ligand [3H]GR-65630 from rat brain cortical membranes.More data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  2nMAssay Description:In vitro by displacement of [3H]LY-278584 from 5-hydroxytryptamine 3 receptor on rat entorhinal cortexMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  2.10nMAssay Description:Compound was evaluated for its ability to displace [3H]quipazine binding to 5-hydroxytryptamine 3 receptor sites in NG 108-15. More data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A(Homo sapiens (Human))
University Of Warwick

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  3.98nMAssay Description:Binding affinity to 5HT3A receptorMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A(GUINEA PIG)
Czech Republic

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  4nMAssay Description:Antagonist activity at 5-HT3 receptor in guinea-pig ileum assessed as inhibition of 5HT-induced contractionMore data for this Ligand-Target Pair
In DepthDetails PubMed
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  9.10nMAssay Description:Binding affinity to 5-hydroxytryptamine 3 receptor of neuronal in the afferent rabbit vagusMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 1B(Rattus norvegicus (Rat))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 1B receptor in rat cortical membranes using [3H]5-HT as a radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSerotonin 2 (5-HT2) receptor(RAT)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 2 receptor in rat cortical membranes using [3H]ketanserin as a radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 1A(Rattus norvegicus (rat))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 1A receptor in rat cortical membranes using [3H]8-OH-DPAT as a radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 1D(RAT)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 3 receptor in rat cortical membranes using [3H]- 1-Methyl-1H-indazole-3-carboxylic acid (8-methyl-8-a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 2C(Rattus norvegicus (Rat))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Inhibitory activity against 5-hydroxytryptamine 1C receptor in rat cortical membranes using [3H]mesulergine as a radioligandMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 7(Rattus norvegicus (rat))
National Institute Of Neurological Disorders And Stroke

Curated by PDSP Ki Database
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
Target5-hydroxytryptamine receptor 7(Rattus norvegicus (rat))
National Institute Of Neurological Disorders And Stroke

Curated by PDSP Ki Database
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  1.00E+3nMMore data for this Ligand-Target Pair
In DepthDetails PubMed
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+3nMAssay Description:Binding affinity for central 5-hydroxytryptamine 3 receptor was determined by displacement of [3H]GR-65630More data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: <1.00E+4nMAssay Description:5-hydroxytryptamine 3 receptor antagonist activity was confirmed by its ability to antagonize 5-HT evoked tachycardia of rabbit isolated heartMore data for this Ligand-Target Pair
TargetNeuronal acetylcholine receptor subunit alpha-7(Mus musculus)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi: >1.00E+4nMAssay Description:In vitro Binding affinity towards alpha-7 nAChR was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-4/beta-2(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  3.80E+4nMAssay Description:In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetNeuronal acetylcholine receptor subunit alpha-3(Homo sapiens (Human))
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKi:  6.70E+4nMAssay Description:In vitro Binding affinity towards 5-hydroxytryptamine 3 receptor was determinedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  3.80E+3nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
Target5-hydroxytryptamine receptor 3A/3B(Rattus norvegicus)TBA
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  1.76E+3nMAssay Description:Binding affinity towards 5-HT3 receptor in rat was evaluatedMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Mus musculus (house mouse))
Merrell Dow Research Institute

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKd:  1.40nMAssay Description:Binding affinity towards 5-hydroxytryptamine 3 receptor was determined by using [3H]-ICS 205-930 as radioligand in mouse N1E 115 cellsMore data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 3A/3B(Mus musculus (house mouse))
Merrell Dow Research Institute

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataKd:  1.30nMAssay Description:Antagonistic activity against Serotonin 5-hydroxytryptamine 3 receptor in isolated rabbit vagus nerve (RVN)More data for this Ligand-Target Pair
Target5-hydroxytryptamine receptor 4(GUINEA PIG)
Universidad De Alcal£

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50: >1.00E+3nMAssay Description:Binding affinity towards 5-HT3 receptor in rat was evaluatedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetD(2) dopamine receptor(Rattus norvegicus (rat))
Universidad De Alcal£

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50: >1.00E+3nMAssay Description:Binding affinity towards 5-HT3 receptor in rat was evaluatedMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  3.80E+3nMAssay Description:Inhibition of human ERG in MCF7 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMultidrug and toxin extrusion protein 2(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  3.11E+5nMAssay Description:Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  3.73E+3nMAssay Description:K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 2(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  4.30E+3nMAssay Description:Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Tcg Lifesciences

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  3.72E+3nMAssay Description:Inhibitory concentration against potassium channel HERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetMultidrug and toxin extrusion protein 1(Homo sapiens (Human))
University Of California

Curated by ChEMBL
LigandPNGBDBM50000483((BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid ...)
Affinity DataIC50:  5.00E+3nMAssay 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 DepthDetails ArticlePubMed