BDBM50012957 1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea::1-(p-(2-(5-chloro-2-methoxybenzamido)ethyl)benzenesulfonyl)-3-cyclohexylurea::5-chloro-N-(2-(4-((((cyclohexylamino)carbonyl)amino)sulfonyl)phenyl)ethyl)-2-methoxybenzamide::5-chloro-N-(2-{4-[N-(N-cyclohexylcarbamoyl)sulfamoyl]phenyl}ethyl)-2-methoxybenzamide::CHEMBL472::GLYBURIDE::Glibenclamide::US20230348371, Compound 5

SMILES COc1ccc(Cl)cc1C(=O)NCCc1ccc(cc1)S(=O)(=O)NC(=O)NC1CCCCC1

InChI Key InChIKey=ZNNLBTZKUZBEKO-UHFFFAOYSA-N

Data  8 KI  36 IC50  2 EC50

PDB links: 14 PDB IDs match this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 13 hits for monomerid = 50012957   

TargetBile salt export pump(Rattus norvegicus)
University Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataKi:  6.10E+3nMAssay Description:TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataKi:  2.75E+4nMAssay Description:TP_TRANSPORTER: inhibition of Taurocholate uptake(Glibenclamide 30uM, 50 % of control) in membrane vesicles prepared from High Five cells infected wi...More data for this Ligand-Target Pair
TargetBile salt export pump(Rattus norvegicus)
University Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  1.57E+4nMAssay Description:TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from female ratMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Rattus norvegicus)
University Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  8.60E+3nMAssay Description:TP_TRANSPORTER: inhibition of Taurocholate uptake (Taurocholate: 1 uM) in liver canalicular membrane vesicle from male ratMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  1.47E+5nMAssay Description:TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP)More data for this Ligand-Target Pair
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  2.60E+5nMAssay Description:TP_TRANSPORTER: increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP)More data for this Ligand-Target Pair
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  1.50E+3nMAssay Description:Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-...More data for this Ligand-Target Pair
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  6.10E+3nMAssay Description:Inhibition of human BSEP expressed in fall armyworm sf9 cell plasma membrane vesicles assessed as reduction in vesicle-associated [3H]-taurocholate t...More data for this Ligand-Target Pair
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50: <1.00E+4nMAssay Description:Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-...More data for this Ligand-Target Pair
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  5.00E+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
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  5.30E+3nMAssay Description:Inhibition of human BSEP expressed in HEK293 cell membrane vesicles assessed as reduction in 3H-TCA uptake incubated for 5 mins by radiodetection met...More data for this Ligand-Target Pair
TargetBile salt export pump(Rattus norvegicus)
University Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  2.80E+3nMAssay Description:Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetBile salt export pump(Homo sapiens (Human))
King'S College Hospital

Curated by ChEMBL
LigandPNGBDBM50012957(1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfon...)
Affinity DataIC50:  5.30E+3nMAssay Description:Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptakeMore data for this Ligand-Target Pair