BDBM50023198 8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5-yl)-4-oxo-4H-1-benzopyran::CHEMBL21333::N-(4-oxo-2-(1H-tetrazol-5-yl)-4H-chromen-8-yl)-4-(4-phenylbutoxy)benzamide::N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-chromen-8-yl]-4-(4-phenyl-butoxy)-benzamide::N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-chromen-8-yl]-4-(4-phenyl-butoxy)-benzamide (ONO-RS-411)::N-[4-Oxo-2-(1H-tetrazol-5-yl)-4H-chromen-8-yl]-4-(4-phenyl-butoxy)-benzamide(ONO-RS-411)::ONO-1078::PRANLUKAST

SMILES O=C(Nc1cccc2c1oc(cc2=O)-c1nnn[nH]1)c1ccc(OCCCCc2ccccc2)cc1

InChI Key InChIKey=NBQKINXMPLXUET-UHFFFAOYSA-N

Data  5 KI  17 IC50  2 Kd  1 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 50023198   

TargetCysteinyl leukotriene receptor 1(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKi:  0.800nMAssay Description:Compound was evaluated in vitro for the binding of Cysteinyl leukotriene receptor 1 to guinea pig lung membranesMore data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKi:  0.800nMAssay Description:Antagonism of Cysteinyl leukotriene receptor 1 from guinea pig lung membranesMore data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1/2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKi:  0.800nMAssay Description:Ability to antagonize LTD4 receptors isolated from guinea pig lung membranesMore data for this Ligand-Target Pair
TargetUracil nucleotide/cysteinyl leukotriene receptor(Homo sapiens (Human))
University Of Bonn

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKi:  4.06E+3nMAssay Description:Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 2(Rattus norvegicus)
University Of Tokyo

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKi:  4.11E+4nMAssay Description:TP_TRANSPORTER: inhibition of DNP-SG uptake in bile canalicular membrane vesicles from SD ratMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCysteinyl leukotriene receptor 1(Homo sapiens (Human))
Setsunan University

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  4.30nMAssay Description:Antagonist activity at human CysLT1More data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1(Homo sapiens (Human))
Setsunan University

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  23nMAssay Description:Antagonist activity against CysLT1 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pr...More data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 2(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  4.30E+4nMAssay Description:Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCruzipain(Trypanosoma cruzi)
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  6.80E+4nMAssay Description:Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in presence of 0.01% Triton X-100More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCruzipain(Trypanosoma cruzi)
University Of California San Francisco

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  7.00E+3nMAssay Description:Inhibition of Trypanosoma cruzi cruzaine preincubated for 5 mins before substrate addition by fluorescence assay in absence of Triton X-100More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCysteinyl leukotriene receptor 1(Homo sapiens (Human))
Setsunan University

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  0.800nMAssay Description:Antagonist activity at CysLT1 receptor in human dU937 cells assessed as inhibition of LTD4-induced increase of calcium level treated 30 mins before L...More data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1(Homo sapiens (Human))
Setsunan University

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  4.30nMAssay Description:Antagonist activity at human CysLT1 receptorMore data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 2(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50: >3.00E+3nMAssay Description:Antagonist activity at human CysLT2 receptorMore data for this Ligand-Target Pair
In DepthDetails PubMed
TargetCysteinyl leukotriene receptor 1(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  0.0440nMAssay Description:Displacement of [3H]ICI from cysteinyl leukotriene receptor 1 in Hartley guinea pig lung membrane after 30 mins by liquid scintillation counting meth...More data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1(Homo sapiens (Human))
Setsunan University

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  4.40nMAssay Description:Inhibition of cysteinyl leukotriene receptor 1 (unknown origin) expressed in HEK293 cell membranes after 45 mins by scintillation spectrometryMore data for this Ligand-Target Pair
TargetATP-binding cassette sub-family C member 2(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 3(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50: >1.33E+5nMAssay Description:Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  2.97E+3nMAssay Description:Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to ...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetATP-binding cassette sub-family C member 4(Homo sapiens (Human))
Amgen

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  2.70E+3nMAssay Description:Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCysteinyl leukotriene receptor 1/2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKd:  1nMAssay Description:Displacement of [3H]LTD4 from Cysteinyl leukotriene D4 receptor in guinea pig lung membranesMore data for this Ligand-Target Pair
TargetBile acid receptor(Homo sapiens (Human))
Universidad Nacional De Colombia

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataEC50:  1.50E+4nMAssay Description:Partial agonist activity at human full-length FXR expressed in human HeLa cells co-expressing pSG5-RXR measured after 24 hrs by dual-glo luciferase r...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCysteinyl leukotriene receptor 1(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  1nMAssay Description:Binding affinity of the compound towards Cysteinyl leukotriene D4 receptor (cysLT1) was measured by the displacement of [3H]-LTD4 radioligandMore data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 2(Homo sapiens (Human))
Shanghai Institute Of Materia Medica

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  3.62E+3nMAssay Description:Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 a...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCysteinyl leukotriene receptor 1(GUINEA PIG)
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataKd:  2.14E+5nMAssay Description:Dissociation constant for CysLT1 receptor was determined by the displacement of [3H]LTD4 from guinea pig lung membranesMore data for this Ligand-Target Pair
TargetCysteinyl leukotriene receptor 1/2(Homo sapiens (Human))
Pfizer

Curated by ChEMBL
LigandPNGBDBM50023198(8-[4-(4-phenylbutyloxy)benzoyl]amino-2-(tetrazol-5...)
Affinity DataIC50:  0.0440nMAssay Description:Inhibition of LTC4 induced smooth muscle contraction of guinea pig ileumMore data for this Ligand-Target Pair