BDBM37953 US10093631, Compound Lesinurad::US10336710, Lesinurad::US10752613, Compound Lesinurad::US11020397, Compound Lesinurad::US11149013, Compound lesinurad::US11161835, Compound Lesinurad

SMILES OC(=O)CSc1nnc(Br)n1-c1ccc(C2CC2)c2ccccc12

InChI Key InChIKey=FGQFOYHRJSUHMR-UHFFFAOYSA-N

Data  48 IC50

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

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 48 hits for monomerid = 37953   

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.18E+3nMAssay Description:The IC50 value of URAT1 inhibition for the crystalline form A of TY706 of the present invention was determined according to the following method:Afte...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2022
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.30E+3nMAssay Description:Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric ac...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 6.50E+4nMAssay Description:A plasmid (EX-T4563-M03, GeneCopoeia) containing the full-length human URAT1 gene (SLC22A12) was transfected into Flp-InT-REx-293 cells to construct ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/31/2020
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.86E+4nMAssay Description:URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was use...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/11/2021
Entry Details
Go to US Patent

TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+5nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/11/2021
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 11(Human)
The Scripps Research Institute

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 2.03E+3nMAssay Description:Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.53E+3nMAssay Description:Inhibition of human URAT1 expressed in HEK293T cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and mea...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/21/2021
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.30E+3nMAssay Description:Inhibition of human URAT1More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.20E+3nMAssay Description:Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptakeMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/23/2021
Entry Details Article
PubMed
TargetSolute carrier family 22 member 11(Human)
The Scripps Research Institute

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.30E+3nMAssay Description:Inhibition of OAT4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.70E+3nMAssay Description:Inhibition of URAT1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/12/2021
Entry Details Article
PubMed
TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+5nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/27/2022
Entry Details
Go to US Patent

LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.86E+4nMAssay Description:URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was use...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2021
Entry Details
Go to US Patent

TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 300nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2021
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.86E+4nMAssay Description:URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was use...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2021
Entry Details
Go to US Patent

TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 300nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/28/2021
Entry Details
Go to US Patent

TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+5nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan MP: ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/20/2022
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.32E+4nMAssay Description:Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric ac...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 5.54E+3nMAssay Description:Inhibition of human URAT1 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid sc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/24/2023
Entry Details
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.56E+3nMAssay 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
In Depth
Date in BDB:
12/17/2024
Entry Details
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.30nMAssay Description:Inhibition of URAT1 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetSolute carrier family 22 member 11(Human)
The Scripps Research Institute

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.70nMAssay Description:Inhibition of OAT4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/22/2024
Entry Details
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 9.40nMAssay Description:Inhibition of human URAT1 mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate incubated for 30 mins by liquid sc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/21/2024
Entry Details
PubMed
TargetCytochrome P450 2C19(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 6.17E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+5nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/22/2019
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 5.25E+4nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/22/2019
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.86E+4nMAssay Description:URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was use...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/22/2019
Entry Details
Go to US Patent

TargetXanthine dehydrogenase/oxidase(Human)
Acquist

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+5nMAssay Description:Xanthine oxidase inhibition was determined using a standard fluorescence-based assay for xanthine oxidase activity (McHale A, Grimes H, Coughlan M P:...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/22/2019
Entry Details
Go to US Patent

TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.30E+3nMAssay Description:Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric ac...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.51E+4nMAssay Description:Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric ac...More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.73E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.73E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.87E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2C9(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.87E+4nMAssay Description:Inhibition of CYP2C9 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetSolute carrier family 22 member 12(Human)
Tianjin Institute of Pharmaceutical Research

US Patent
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.86E+4nMAssay Description:URAT1 (SLC22A12) activity was evaluated in a cellular uptake assay using a 96-well plate with stably transfected URAT-1/CHO cells. 3H-orotate was use...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/22/2019
Entry Details
Go to US Patent

TargetCytochrome P450 2C19(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 6.17E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.26E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 1.00E+5nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.44E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.44E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 1A2(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.93E+4nMAssay Description:Inhibition of CYP1A2 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2C19(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 6.17E+4nMAssay Description:Inhibition of CYP2C19 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 3.26E+4nMAssay Description:Inhibition of CYP2D6 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: 7.44E+4nMAssay Description:Inhibition of CYP3A4 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
6/15/2019
Entry Details Article
PubMed