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=JHWDCJBLPGLDMI-UHFFFAOYSA-N

Data  44 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 44 hits for monomerid = 37953   

TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails PubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C9(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (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 DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 1A2(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2C19(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 2D6(Homo sapiens (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 DepthDetails ArticlePubMed
TargetCytochrome P450 3A4(Homo sapiens (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 DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Wuxi Apptec

Curated by ChEMBL
LigandPNGBDBM37953(US10093631, Compound Lesinurad | US10336710, Lesin...)
Affinity DataIC50: >3.00E+4nMAssay Description:Inhibition of human ERGMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetSolute carrier family 22 member 11(Homo sapiens (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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 11(Homo sapiens (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 DepthDetails ArticlePubMed
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails US Patent
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent
TargetSolute carrier family 22 member 12(Homo sapiens (Human))
Acquist

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 DepthDetails ArticlePubMed
TargetXanthine dehydrogenase/oxidase(Homo sapiens (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 DepthDetails US Patent