BindingDB BDBM50158460 (3,5-dibromo-4-hydroxyphenyl)(2-ethyl-1-benzofuran-3-yl)methanone::2-ethyl-3-(3,5-dibrom-4-hydroxybenzoyl)benzofuran::3,5-dibromo-4-hydroxyphenyl-2-ethyl-3-benzofuranyl ketone::Benzbromarone::CHEMBL388590::US20240116873, Compound Benzbromarone::US9725430, Compound 1::US9856239, benzbromarone::US9962362, Compound 1::Uroleap (TN)::cid

BDBM50158460 (3,5-dibromo-4-hydroxyphenyl)(2-ethyl-1-benzofuran-3-yl)methanone::2-ethyl-3-(3,5-dibrom-4-hydroxybenzoyl)benzofuran::3,5-dibromo-4-hydroxyphenyl-2-ethyl-3-benzofuranyl ketone::Benzbromarone::CHEMBL388590::US20240116873, Compound Benzbromarone::US9725430, Compound 1::US9856239, benzbromarone::US9962362, Compound 1::Uroleap (TN)::cid_2333

SMILES CCc1c(c2ccccc2o1)C(=O)c3cc(c(c(c3)Br)O)Br

InChI Key InChIKey=WHQCHUCQKNIQEC-UHFFFAOYSA-N

Data 4 KI 58 IC50 2 Kd 5 EC50

PDB links: 5 PDB IDs match this monomer.

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 73 hits for monomerid = 50158460

Cytochrome P450 2C9(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

Ki: 19nMAssay Description:Inhibition of human CYP2C9More data for this Ligand-Target Pair

PDB KEGG
UniProtKB/SwissProt
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Date in BDB:
11/10/2009
Entry Details Article
PubMed

Cytochrome P450 2C9(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

Ki: 19nMAssay Description:Binding affinity to CYP2C9More data for this Ligand-Target Pair

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Date in BDB:
1/11/2010
Entry Details Article
PubMed

Cytochrome P450 2C9(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

Ki: 19nMAssay Description:Inhibition of CYP2C9More data for this Ligand-Target Pair

PDB KEGG
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Date in BDB:
11/11/2009
Entry Details Article
PubMed

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 26nMAssay Description:Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation cou...More data for this Ligand-Target Pair

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Date in BDB:
12/3/2011
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 35nMAssay Description:Inhibition of human URAT1 expressed in human MDCK cellsMore data for this Ligand-Target Pair

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Date in BDB:
12/3/2011
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 35nMAssay Description:Inhibition of URAT1 (unknown origin) transfected in dog MDCK cells assessed as inhibition of [14C]uric acid uptake by liquid scintillation counting m...More data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Cytochrome P450 2C9(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 41nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/29/2022
Entry Details Article
PubMed

Cytochrome P450 2C9(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 41nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed

Aldo-keto reductase family 1 member C1(Human)
Monash University (Parkville Campus)

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 48nMAssay Description:Inhibition of 20-alpha HSD (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
1/11/2010
Entry Details Article
PubMed

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 48nMAssay Description:Inhibition of URAT1 (unknown origin) by absorbance based assayMore data for this Ligand-Target Pair

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Date in BDB:
TBA
Entry Details
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 100nMAssay Description:Inhibition of human URAT1 expressed in Xenopus oocytes by [14C]urate uptake assayMore data for this Ligand-Target Pair

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Date in BDB:
2/21/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 120nMAssay Description:Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation cou...More data for this Ligand-Target Pair

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Date in BDB:
9/19/2019
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 190nMAssay Description:Inhibition of human URAT1 expressed in Xenopus laevis oocytes assessed as inhibition of [14C]uric acid uptake measured after 60 mins by liquid scinti...More data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
PubMed PDB

3D Structure (crystal)

Broad substrate specificity ATP-binding cassette transporter ABCG2(Human)
Federal University of Parana

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 200nMAssay Description:Inhibition of ABCG2 (unknown origin) expressed in human HEK293-A cells membrane vesicles assessed inhibition of ABCG2-mediated urate transport activi...More data for this Ligand-Target Pair

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Date in BDB:
6/21/2023
Entry Details
PubMed

Transthyretin(Human)
University of Toyama

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

Kd: 200nMAssay Description:Binding affinity to thyroxin binding site of TTR V30M mutant (unknown origin) expressed in Escherichia coli assessed as quenching of intrinsic trypto...More data for this Ligand-Target Pair

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Date in BDB:
12/14/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 220nMAssay Description:Inhibition of URAT1 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
8/12/2021
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 300nMAssay Description:Inhibition of human URAT1-mediated urate uptake in HEK293 cellsMore data for this Ligand-Target Pair

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Date in BDB:
12/15/2012
Entry Details Article
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 300nMAssay Description:Inhibition of human URAT1-mediated [8-14C]uric acid uptake expressed in HEK293 cells using [8-14C]uric acid as substrate by liquid scintillation coun...More data for this Ligand-Target Pair

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Date in BDB:
4/19/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Broad substrate specificity ATP-binding cassette transporter ABCG2(Human)
Federal University of Parana

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 340nMAssay Description:Inhibition of ABCG2 (unknown origin) transfected in HEK293 cell membrane vesicle assessed as inhibition of 14C-uric acid uptake incubated for 15 mins...More data for this Ligand-Target Pair

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Date in BDB:
12/17/2024
Entry Details
PubMed

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 530nMAssay Description:Inhibition of URAT1 (unknown origin)More data for this Ligand-Target Pair

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Date in BDB:
TBA
Entry Details
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 530nMAssay Description:Inhibition of human URAT1 stably overexpressing in human HEK293 cells assessed as inhibition of 14C-uric acid uptake preincubated for 30 mins followe...More data for this Ligand-Target Pair

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Date in BDB:
12/17/2024
Entry Details
PubMed PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 550nMAssay Description:Human kidney embryonic cells HEK-293T were grown in a petri dish (diameter=10 cm) containing DMEM and 10% of bovine fetal serum culture solution, and...More data for this Ligand-Target Pair

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Date in BDB:
11/21/2019
Entry Details
US Patent
PDB

3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 585nMAssay Description:Experimental results: The compounds had no obvious inhibitory effect on the drug transporter OAT3, and when the compounds were used clinically in com...More data for this Ligand-Target Pair

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Date in BDB:
6/29/2024
Entry Details
US Patent
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3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 750nMAssay Description:URAT1 (Uric Acid Transporter 1) is expressed on the apical membrane in renal tubules. It mediates the re-uptake of uric acid from the urine into the ...More data for this Ligand-Target Pair

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Date in BDB:
4/27/2015
Entry Details
US Patent
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3D Structure (crystal)

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.09E+3nMAssay Description:Experimental results: The compounds had no obvious inhibitory effect on the drug transporter OAT3, and when the compounds were used clinically in com...More data for this Ligand-Target Pair

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Date in BDB:
6/29/2024
Entry Details
US Patent
PDB

3D Structure (crystal)

cAMP-specific 3',5'-cyclic phosphodiesterase 4D(Human)TBA

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 2.10E+3nMAssay Description:Inhibition of his-tagged recombinant human PDE4D catalytic domain (T86 to S413 residues) expressed in Escherichia coli BL21(DE3) using [3H]-cAMP as s...More data for this Ligand-Target Pair

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Date in BDB:
TBA
Entry Details
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3D Structure (crystal)

Solute carrier family 22 member 6(Human)
Southern Medical University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 2.12E+3nMAssay Description:Inhibition of OAT1 (unknown origin) transfected in HEK293 cells assessed as inhibition of 6-CFL uptake preincubated for 30 mins followed by 6-CFL add...More data for this Ligand-Target Pair

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Date in BDB:
12/17/2024
Entry Details
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Cytochrome P450 2C19(Human)
Washington State University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

Ki: 3.70E+3nMAssay Description:Inhibition of human CYP2C19More data for this Ligand-Target Pair

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Date in BDB:
11/10/2009
Entry Details Article
PubMed

Multidrug resistance-associated protein 1(Human)TBA

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 4.00E+3nMAssay Description:Inhibition of Homo sapiens (human) MRP1 expressed in Sf9 cell membranes assessed as decrease in N-ethyl-maleimide-glutathione-induced inorganic phosp...More data for this Ligand-Target Pair

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Date in BDB:
8/31/2020
Entry Details Article

Multidrug resistance-associated protein 1(Human)TBA

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 4.00E+3nMAssay Description:Inhibition of human MRP1 expressed in Spodoptera frugiperda Sf9 cells assessed as inhibition of NEM-GS-induced vanadate-sensitive ATPase activity mea...More data for this Ligand-Target Pair

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Date in BDB:
3/23/2012
Entry Details Article
PubMed

Cytochrome P450 2J2(Human)
Tongji University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 4.26E+3nMAssay Description:Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS methodMore data for this Ligand-Target Pair

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Date in BDB:
11/3/2016
Entry Details Article
PubMed

Solute carrier family 22 member 6(Human)
Southern Medical University

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 4.60E+3nMAssay Description:TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cellsMore data for this Ligand-Target Pair

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Date in BDB:
8/30/2020
Entry Details Article
PubMed

Isoform 2 of Nuclear receptor corepressor 2 (TRAC-1)(Human)
The Scripps Research Institute Molecular Screening Center

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 4.81E+3nMAssay Description:Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center Affiliation: The Scripps Research Institute, TSRI Assay Provide...More data for this Ligand-Target Pair

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Date in BDB:
7/11/2011
Entry Details
PCBioAssay

Sphingosine 1-phosphate receptor 1(Human)
The Scripps Research Institute Molecular Screening Center

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

EC50: 5.13E+3nMAssay Description:Source (MLSCN Center Name): The Scripps Research Institute Molecular Screening Center Center Affiliation: The Scripps Research Institute, TSRI Assay ...More data for this Ligand-Target Pair

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Date in BDB:
4/28/2011
Entry Details
PCBioAssay

Transthyretin(Human)
University of Toyama

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 5.70E+3nMAssay Description:Inhibition of acid mediated TTR V30M mutant aggregation (unknown origin) expressed in Escherichia coli preincubated for 30 mins followed by acetic bu...More data for this Ligand-Target Pair

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Date in BDB:
12/14/2024
Entry Details
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3D Structure (crystal)

Sphingosine 1-phosphate receptor 1(Human)
The Scripps Research Institute Molecular Screening Center

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

EC50: 5.94E+3nMAssay Description:Source (MLSCN Center Name): The Scripps Research Institute Molecular Screening Center Center Affiliation: The Scripps Research Institute, TSRI Assay ...More data for this Ligand-Target Pair

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Date in BDB:
4/29/2011
Entry Details
PCBioAssay

Solute carrier family 22 member 12(Human)
University of Colorado Anschutz Medical Campus

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 6.80E+3nMAssay Description:Inhibition of URAT1 in human RPTEC assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition and i...More data for this Ligand-Target Pair

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Date in BDB:
3/28/2022
Entry Details Article
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3D Structure (crystal)

Eyes absent homolog 3(Human)
Cincinnati Childrens Hospital Medical Center

US Patent

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 8.30E+3nMAssay Description:An inhibitory assay was conducted using the previously described p-nitrophenylphosphate assay (Rayapureddi, J. P. et al. Nature 426, 295-298 (2003))....More data for this Ligand-Target Pair

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Date in BDB:
6/12/2019
Entry Details
US Patent

Eyes absent homolog 3(Human)
Cincinnati Childrens Hospital Medical Center

US Patent

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 8.30E+3nMAssay Description:The compounds were then tested using full-length human recombinant, purified EYA3 and pNPP as a substrate. Compounds were dissolved in DMSO and dilut...More data for this Ligand-Target Pair

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Date in BDB:
3/30/2020
Entry Details
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Monocarboxylate transporter 2(Rat)
Physiologisch-Chemisches Institut Der Eberhard-Karls-Universit£T T£Bingen

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 9.00E+3nMAssay Description:TP_TRANSPORTER: inhibition of lactate uptake in Xenopus laevis oocytesMore data for this Ligand-Target Pair

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Date in BDB:
2/8/2013
Entry Details Article
PubMed

60 kDa heat shock protein, mitochondrial(Human)
Indiana University School of Medicine

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 9.10E+3nMAssay Description:Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Roset...More data for this Ligand-Target Pair

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Date in BDB:
2/24/2021
Entry Details Article
PubMed

Eyes absent homolog 3 [223-510](Mouse)
Cincinnati Childrens Hospital Medical Center

US Patent

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.10E+4nMAssay Description:The compounds were then tested using full-length human recombinant, purified EYA3 and pNPP as a substrate. Compounds were dissolved in DMSO and dilut...More data for this Ligand-Target Pair

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Date in BDB:
3/30/2020
Entry Details
US Patent

Eyes absent homolog 3 [223-510](Human)
Cincinnati Childrens Hospital Medical Center

US Patent

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.10E+4nMAssay Description:An inhibitory assay was conducted using the previously described p-nitrophenylphosphate assay (Rayapureddi, J. P. et al. Nature 426, 295-298 (2003))....More data for this Ligand-Target Pair

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Date in BDB:
6/12/2019
Entry Details
US Patent

Sphingosine 1-phosphate receptor 1(Human)
The Scripps Research Institute Molecular Screening Center

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

EC50: 1.35E+4nMAssay Description:Source (MLSCN Center Name): The Scripps Research Institute Molecular Screening Center Center Affiliation: The Scripps Research Institute, TSRI Assay ...More data for this Ligand-Target Pair

PDB KEGG
UniProtKB/SwissProt
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Date in BDB:
4/28/2011
Entry Details
PCBioAssay

Perilipin-1(Human)
The Scripps Research Institute Molecular Screening Center

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.50E+4nMAssay Description:Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Affiliation: The Scripps Research Institute, TSRI Assa...More data for this Ligand-Target Pair

KEGG
UniProtKB/SwissProt
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Date in BDB:
8/2/2011
Entry Details
PCBioAssay

Bile salt export pump(Human)
Pfizer

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.59E+4nMAssay 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

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Date in BDB:
8/19/2019
Entry Details Article
PubMed

ATP-binding cassette sub-family C member 4(Human)
Amgen

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.70E+4nMAssay 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

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Date in BDB:
11/3/2019
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PubMed

Streptokinase A(Streptococcus pyogenes M1 GAS)
Broad Institute

Curated by PubChem BioAssay

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

EC50: 1.72E+4nMAssay Description:Keywords: Group A streptococcus, GAS, streptokinase, expression, virulence, inhibition, dose response, EC50 Assay Overview: The goal of this assa...More data for this Ligand-Target Pair

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Date in BDB:
6/8/2011
Entry Details
PCBioAssay

Bile salt export pump(Human)
Pfizer

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.75E+4nMAssay 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

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Date in BDB:
11/3/2019
Entry Details Article
PubMed

Bile salt export pump(Human)
Pfizer

Curated by ChEMBL

BDBM50158460(cid_2333 | Benzbromarone | 3,5-dibromo-4-hydroxyph...)

IC50: 1.75E+4nMAssay 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

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Date in BDB:
8/17/2019
Entry Details Article
PubMed

Displayed 1 to 50 (of 73 total ) | Next | Last >>

Filter my 73 hits

Targets 38▿
- Solute carrier family 22 member 12 18
- Cytochrome P450 2C9 6
- Sphingosine 1-phosphate receptor 1 3
- Bile salt export pump 3
- Multidrug resistance-associated protein 1 2
- Eyes absent homolog 3 2
- Co-chaperonin GroES 2
- Solute carrier family 22 member 6 2
- Tyrosine-protein phosphatase non-receptor type 1 2
- Transthyretin 2
- Eyes absent homolog 3 [223-510] 2
- Broad substrate specificity ATP-binding cassette transporter ABCG2 2
- Cytochrome P450 2C19 2
- Monocarboxylate transporter 2 1
- Monocarboxylate transporter 1 1
- Thiosulfate sulfurtransferase 1
- Solute carrier family 2, facilitated glucose transporter member 9 1
- Photoreceptor-specific nuclear receptor 1
- 60 kDa heat shock protein, mitochondrial 1
- M1 family aminopeptidase 1
- Cytochrome P450 1A2 1
- Streptokinase A 1
- Inosine-5'-monophosphate dehydrogenase 1
- Cytochrome P450 3A4 1
- Aldo-keto reductase family 1 member C1 1
- Cytochrome P450 2J2 1
- Chaperonin GroEL 1
- M17 leucyl aminopeptidase 1
- cAMP-specific 3',5'-cyclic phosphodiesterase 4D 1
- ATP-binding cassette sub-family C member 3 1
- ATP-binding cassette sub-family C member 4 1
- Bile acid receptor 1
- ATP-binding cassette sub-family C member 2 1
- Isoform 2 of Nuclear receptor corepressor 2 (TRAC-1) 1
- Perilipin-5 1
- Polymerase acidic protein 1
- Cytochrome P450 2D6 1
- Perilipin-1 1
Publications 41▿
- Drug Metab Dispos 41: 60-71 (2012) 6
- Bioorg Med Chem Lett 29: 1106-1112 (2019) 5
- Toxicol Sci 136: 216-41 (2013) 4
- Eur J Med Chem 242: (2022) 4
- ACS Med Chem Lett 11: 2017-2023 (2020) 4
- US Patent US9725430 (2017) 3
- US Patent US9962362 (2018) 3
- J Med Chem 47: 6768-76 (2004) 2
- US Patent US20240116873 (2024) 2
- Bioorg Med Chem 90: (2023) 2
- J Med Chem 54: 2701-13 (2011) 2
- Biochem J 341: 529-35 (1999) 2
- US Patent US8889724 (2014) 1
- PubChem Bioassay (2008) 1
- PubChem Bioassay (2007) 1
- Bioorg Med Chem 19: 3249-54 (2011) 1
- Eur J Med Chem 167: 124-132 (2019) 1
- Bioorg Med Chem 16: 4064-74 (2008) 1
- PubChem Bioassay (2009) 1
- Bioorg Med Chem Lett 27: 1919-1922 (2017) 1
- Kidney Int 63: 143-55 (2003) 1
- US Patent US9856239 (2018) 1
- PubChem Bioassay (2011) 1
- PubChem Bioassay (2007) 1
- PubChem Bioassay (2011) 1
- PubChem Bioassay (2009) 1
- PubChem Bioassay (2007) 1
- J Med Chem 52: 3259-64 (2009) 1
- Hepatology 60: 1015-22 (2014) 1
- Eur J Med Chem 166: 186-196 (2019) 1
- PubChem Bioassay (2010) 1
- Drug Metab Dispos 35: 981-6 (2007) 1
- PubChem Bioassay (2010) 1
- J Nat Prod 86: 24-33 (2023) 1
- Eur J Med Chem 237: (2022) 1
- J Med Chem 59: 7699-718 (2016) 1
- J Med Chem 51: 648-54 (2008) 1
- Bioorg Med Chem 75: (2022) 1
- J Med Chem 63: 3834-3867 (2020) 1
- Toxicol Sci 118: 485-500 (2010) 1
- Bioorg Med Chem Lett 40: (2021) 1
Institutions 29▿
- The Scripps Research Institute Molecular Screening Center 7
- Tongji University 6
- Cincinnati Childrens Hospital Medical Center 6
- Amgen 5
- Indiana University School of Medicine 5
- Fuji Yakuhin 5
- Washington State University 4
- Southern Medical University 4
- University of Colorado Anschutz Medical Campus 2
- Physiologisch-Chemisches Institut Der Eberhard-Karls-Universit£T T£Bingen 2
- Srmlsc 2
- University of Toyama 2
- JIANGSU CHIATAI QINGJIANG PHARMACEUTICAL CO., LTD. 2
- Chinese Academy of Sciences 1
- West China Hospital of Sichuan University 1
- The Scripps Research Institute 1
- Pfizer 1
- Guangdong Pharmaceutical University 1
- Inventisbio Shanghai 1
- Kakatiya University 1
- Broad Institute 1
- Kunming Medical University 1
- The Chinese University of Hong Kong 1
- Jikei University School of Medicine 1
- Monash University (Parkville Campus) 1
- France 1
- Wellstat Therapeutics 1
- University of Perugia 1
- Federal University of Parana 1
Affinity: 19 to 2.5E+5 nM▿
- Ki 4
- IC50 62
- Kd 2
- EC50 5
- Affinity ≤ nM
Xtal structures: 1
Docked structures: 0
Catalog Cmpds: 1