SLC22A12

Summary

SLC22A12 (solute carrier family 22 member 12, HGNC:17989) is a protein-coding gene on chromosome 11q13.1, encoding Solute carrier family 22 member 12 (Q96S37). Electroneutral antiporter that translocates urate across the apical membrane of proximal tubular cells in exchange for monovalent organic or inorganic anions.

The protein encoded by this gene is a member of the organic anion transporter (OAT) family, and it acts as a urate transporter to regulate urate levels in blood. This protein is an integral membrane protein primarily found in epithelial cells of the proximal tubule of the kidney. An elevated level of serum urate, hyperuricemia, is associated with increased incidences of gout, and mutations in this gene cause renal hypouricemia type 1. Alternative splicing results in multiple transcript variants.

Source: NCBI Gene 116085 — RefSeq curated summary.

At a glance

• Gene–disease (curated): hypouricemia, renal 1 (Strong, GenCC) — +1 more curated relationship
• GWAS associations: 24
• Clinical variants (ClinVar): 337 total — 11 pathogenic, 9 likely-pathogenic
• Phenotypes (HPO): 27
• Druggable target: yes — 13 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_144585

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:17989
Approved symbol	SLC22A12
Name	solute carrier family 22 member 12
Location	11q13.1
Locus type	gene with protein product
Status	Approved
Aliases	OAT4L, RST, URAT1, hURAT1, UAT
Ensembl gene	ENSG00000197891
Ensembl biotype	protein_coding
OMIM	607096
Entrez	116085

Gene structure

Transcript identifiers

Ensembl transcripts: 5 — 5 protein_coding

ENST00000336464, ENST00000377567, ENST00000377572, ENST00000377574, ENST00000473690

RefSeq mRNA: 4 — MANE Select: NM_144585 NM_001276326, NM_001276327, NM_144585, NM_153378

CCDS: CCDS60835, CCDS60836, CCDS8075

Canonical transcript exons

ENST00000377574 — 10 exons

Exon	Start	End
ENSE00001120017	64599676	64599890
ENSE00001120018	64600367	64600475
ENSE00001172418	64598808	64598923
ENSE00001172424	64598516	64598639
ENSE00001340542	64600735	64600938
ENSE00001706205	64593405	64593559
ENSE00003487222	64593635	64593803
ENSE00003588678	64592779	64592882
ENSE00003847605	64601488	64602344
ENSE00003848955	64591220	64591958

Expression profiles

Bgee: expression breadth broad, 30 present calls, max score 98.60.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.1637 / max 124.5585, expressed in 5 samples.

FANTOM5 promoters (5 alternative TSS)

Promoter ID	TPM avg	Samples expressed
114979	0.0727	4
114981	0.0427	3
114980	0.0420	3
114978	0.0050	3
114977	0.0013	1

Top tissues by expression

243 total, by Bgee expression score (0-100, higher = more expressed):

Tissue	Anatomy ID	Expression score	Quality
kidney epithelium	UBERON:0004819	98.60	gold quality
adult mammalian kidney	UBERON:0000082	92.19	gold quality
kidney	UBERON:0002113	83.71	gold quality
left ventricle myocardium	UBERON:0006566	81.58	gold quality
cardiac muscle of right atrium	UBERON:0003379	81.06	gold quality
cortex of kidney	UBERON:0001225	77.28	gold quality
parotid gland	UBERON:0001831	75.04	gold quality
nasal cavity epithelium	UBERON:0005384	74.72	gold quality
renal medulla	UBERON:0000362	74.50	gold quality
epithelial cell of pancreas	CL:0000083	74.26	gold quality
myocardium	UBERON:0002349	72.21	gold quality
vena cava	UBERON:0004087	69.72	gold quality
quadriceps femoris	UBERON:0001377	68.88	gold quality
adult organism	UBERON:0007023	68.87	gold quality
cerebellar vermis	UBERON:0004720	68.70	gold quality
vastus lateralis	UBERON:0001379	68.46	gold quality
metanephros cortex	UBERON:0010533	68.19	gold quality
metanephros	UBERON:0000081	65.96	gold quality
lateral nuclear group of thalamus	UBERON:0002736	64.94	gold quality
upper arm skin	UBERON:0004263	64.24	gold quality
mucosa of paranasal sinus	UBERON:0005030	63.90	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	63.48	gold quality
layer of synovial tissue	UBERON:0007616	62.76	gold quality
biceps brachii	UBERON:0001507	62.72	gold quality
lateral globus pallidus	UBERON:0002476	62.27	gold quality
deltoid	UBERON:0001476	61.97	gold quality
secondary oocyte	CL:0000655	61.87	gold quality
subthalamic nucleus	UBERON:0001906	61.56	gold quality
dorsal plus ventral thalamus	UBERON:0001897	61.52	gold quality
heart right ventricle	UBERON:0002080	61.27	gold quality

Single-cell (SCXA)

Detected in 1 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	5.49

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): HNF1A, HNF1B

miRNA regulators (miRDB)

35 targeting SLC22A12, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNA	Max score	Avg score	miRNA target_count
HSA-MIR-6870-5P	99.99	68.55	2115
HSA-MIR-10401-5P	99.99	65.79	948
HSA-MIR-6721-5P	99.93	68.92	2981
HSA-MIR-579-3P	99.86	71.66	3628
HSA-MIR-4447	99.85	67.81	2900
HSA-MIR-664B-3P	99.84	71.65	3590
HSA-MIR-6756-5P	99.82	67.97	2466
HSA-MIR-4429	99.77	69.62	2111
HSA-MIR-6766-5P	99.68	67.70	2325
HSA-MIR-875-3P	99.63	69.47	2548
HSA-MIR-6751-5P	99.56	64.99	1145
HSA-MIR-1207-5P	99.49	69.11	2983
HSA-MIR-1275	99.47	67.90	2749
HSA-MIR-3911	99.38	66.95	1087
HSA-MIR-6803-5P	99.19	63.90	1026
HSA-MIR-7109-5P	99.18	66.13	1057
HSA-MIR-4763-3P	99.10	67.83	2649
HSA-MIR-3127-3P	98.94	67.34	1055
HSA-MIR-6756-3P	98.94	66.79	1104
HSA-MIR-4260	98.78	65.37	848
HSA-MIR-330-5P	98.73	67.63	1788
HSA-MIR-16-1-3P	98.70	69.23	1538
HSA-MIR-2467-3P	98.65	67.18	1969
HSA-MIR-6887-5P	98.56	68.49	1295
HSA-MIR-6795-5P	98.52	68.51	1277
HSA-MIR-6804-5P	98.39	65.77	1084
HSA-MIR-326	98.25	66.44	1565
HSA-MIR-939-5P	97.10	65.80	1579
HSA-MIR-134-3P	96.83	66.22	1001
HSA-MIR-1343-5P	96.48	66.06	1506

Literature-anchored findings (GeneRIF, showing 40)

• Molecular identification of a renal urate anion exchanger that regulates blood urate levels (PMID:12024214)
• PDZK1 plays a role in regulating the functional activity of URAT1-mediated urate transport in the apical membrane of renal proximal tubules. (PMID:15304510)
• SLC22A12 is a major gene for hypouricemia but not hyperuricemia in Japanese. (PMID:15327384)
• heterozygous mutations of the URAT1 gene (Q297X and IVS2+1G>A) may be recurrent mutations of the URAT1 gene in a Japanese population (PMID:15772829)
• G774A mutation in SCL22A12 gene serves as a suppressing factor for development of gout. Mutation decreased uric acid levels. (PMID:16059895)
• A single nucleotide polymorphism (SNP) in the urate transporter gene SLC22CA12 was found to be associated with elevated serum uric acid levels (PMID:16920156)
• Report of patients with heterozygous and homozygous mutations in the hURAT1 gene in a family with renal hypouricemia associated with exercise-induced acute renal failure. (PMID:17445045)
• Functioning as an antiporter, hURAT1 mediates the uptake of urate from the lumen into proximal tubule cells in exchange for organic and inorganic anions. (PMID:17891408)
• This study was undertaken to elucidate whether SLC22A12 gene mutations are responsible for low serum uric acid levels in Greek people. No previously reported mutation of URAT1 was associated with primary renal hypouricaemia in Greek subjects. (PMID:17891652)
• is a urate anion exchanger regulating blood urate levels and proposed to be involved in the multimolecular complex “transportsome” that allows the cooperation of multiple transporters. (PMID:18409511)
• The G774A mutation in the SLC22A12 gene encoding URAT1 ( urate anion exchanger 1 ) predominates in Japanese renal hypouricemia. (PMID:18492088)
• losartan inhibited URAT1 and thereby it lowered Sur levels in hypertensive patients. (PMID:18670416)
• The in vivo role of GLUT9 is supported by the fact that a renal hypouricemia patient without any mutations in SLC22A12 was found to have a missense mutation in SLC2A9, which reduced urate transport activity in vitro. (PMID:18701466)
• polymorphism of the SLC22A12 gene may be involved in renal urate handling and the concentration of serum uric acid (PMID:18824160)
• Serial changes in serum levels of reactive oxygen species and antioxidant potentials were demonstrated after exercise stress testing in a girl with idiopathic renal hypouricemia due to a mutation in SLC22A12. (PMID:18936980)
• Prevalence of hypouricaemia and SLC22A12 mutations in healthy Korean subjects. (PMID:19019168)
• Single nucleotide polymorphism rs475688 within SLC22A12 gene contributed to the development of gout under the hypothesis of common disease/common variant. (PMID:19762362)
• There are multiple genetic variants within or near hURAT1 that are associated with susceptibility to hyperuricaemia in Han Chinese, including a novel SNP located in intron 3. (PMID:19833602)
• replicated the associations of the SLC2A9 and ABCG2 polymorphisms with serum UA and clarified the prognostic significance of the SLC22A12, SLC2A9 and ABCG2 genotypes for the development of hyperuricemia (PMID:20714133)
• URAT1 mutations cause renal hypouricemia type 1. (PMID:21148271)
• polymorphisms of the SLC22A12 gene were associated with primary hyperuricemia (PMID:21154327)
• The SNP of 11G > A in the intron 3 of hURAT1 gene was apparently associated with hyperuricemia in Han Chinese. (PMID:21211204)
• hURAT1 mediated a time- and dose-dependent uptake of orotate (K (m) 5.2 muM). (PMID:21350910)
• Although SLC22A12 W258X was a determining genetic factor on SUA, SUA of those with WX genotype distributed widely from 0.8 mg/dL to 7.8 mg/dL. (PMID:21366895)
• The novel G109T polymorphism of the SLC22A12 gene is related to serum uric acid level, but not to the development of metabolic syndrome. (PMID:21544634)
• SLC22A12 258WX was more common among those with a lower serum uric acid concentration; this allele is known to cause hypouricemia (PMID:21614936)
• two cases with the URAT1 gene, encoded by SLC22A12, found a homozygous mutation in exon 4 (PMID:21722610)
• we identified and replicated one novel locus in association with serum urate levels and experimentally characterize the novel G65W variant in URAT1 as a functional allele. (PMID:21768215)
• This data highlights the importance of the URAT1 renal urate transporter in determining serum urate concentrations and the clinical phenotypes. (PMID:22194875)
• present study confirmed the existence of OAT1-4 and URAT1 in the salivary gland (PMID:22564045)
• SLC22A12 polymorphisms are associated with obesity and metabolic syndrome in Caucasian hypertensive subjects. (PMID:22688828)
• Genetic analysis detected no mutations in the SLC22A12/URAT1 gene, except for the previously reported silent polymorphisms rs 3825016, 11231825, 1630320, 7932775, and the intronic polymorphism rs 79866595. (PMID:22942308)
• This report identifies a novel loss-of-function URAT1 mutations (c.151delG)which cause renal hypouricemia and renal dysfunction in two independent renal hypouricemia pedigrees. (PMID:23043931)
• Our study is the first one in Turkish population and suggests that there is no association between primary gout disease and SLC22A12 gene polymorphisms. (PMID:23129426)
• The strongest association was detected at SLC22A12 rs505802 for genetic loci and uric acid (p=2.4x10(-50)). (PMID:23238572)
• The findings suggest that loss-of-function mutations in URAT1 cause renal hypouricemia via loss of uric acid absorption partly by protein misfolding. (PMID:23386035)
• Report no association between serum uric acid and MTHFR C677T genotype, after the influences of ABCG2 Q126X and SLC22A12 W258X were removed. (PMID:23544272)
• Our study suggests that the URAT1 rs559946 polymorphism is associated with increased hyperuricemia risk and may also contribute to gout development in Han Chinese men. (PMID:23981340)
• analysis of mutations in genes SLC22A12 and SLC2A9 urate transporter genes in patients with exercise-induced acute kidney injury (PMID:24107611)
• Our analysis provides evidence for multiple ancestral-specific effects across the SLC22A11/SLC22A12 locus that presumably influence the activity of OAT4 and URAT1 and risk of gout. (PMID:24360580)

Cross-species orthologs

51 orthologs

Organism	Symbol	Gene ID
danio_rerio	slc22a4	ENSDARG00000005335
danio_rerio	oatx	ENSDARG00000019713
danio_rerio	si:dkey-166k12.1	ENSDARG00000054690
danio_rerio	si:dkey-119m7.4	ENSDARG00000071049
danio_rerio	si:dkey-119m7.8	ENSDARG00000096654
mus_musculus	Slc22a12	ENSMUSG00000061742
rattus_norvegicus	Slc22a12	ENSRNOG00000021108
drosophila_melanogaster	Orct	FBGN0019952
drosophila_melanogaster	CG15221	FBGN0030331
drosophila_melanogaster	Balat	FBGN0033778
drosophila_melanogaster	CG4630	FBGN0033809
drosophila_melanogaster	CG5592	FBGN0035645
drosophila_melanogaster	CG10486	FBGN0035647
drosophila_melanogaster	SLC22A	FBGN0037140
drosophila_melanogaster	CG7458	FBGN0037144
drosophila_melanogaster	CG14691	FBGN0037829
drosophila_melanogaster	CG14855	FBGN0038260
drosophila_melanogaster	CG14856	FBGN0038261
drosophila_melanogaster	CG14857	FBGN0038262
drosophila_melanogaster	CG12783	FBGN0038448
drosophila_melanogaster	CG7333	FBGN0038715
drosophila_melanogaster	CG7342	FBGN0038716
drosophila_melanogaster	CG17751	FBGN0038717
drosophila_melanogaster	CG17752	FBGN0038718
drosophila_melanogaster	CG16727	FBGN0038719
drosophila_melanogaster	CG6231	FBGN0038720
drosophila_melanogaster	CG4465	FBGN0038750
drosophila_melanogaster	CG4462	FBGN0038752
drosophila_melanogaster	CG4459	FBGN0038753
drosophila_melanogaster	CG6356	FBGN0039178
drosophila_melanogaster	CG3690	FBGN0040350
drosophila_melanogaster	CG31103	FBGN0051103
drosophila_melanogaster	CG31106	FBGN0051106
drosophila_melanogaster	CG31272	FBGN0051272
drosophila_melanogaster	CG33233	FBGN0053233
drosophila_melanogaster	CG33234	FBGN0053234
drosophila_melanogaster	Orct2	FBGN0086365
drosophila_melanogaster	CG42269	FBGN0259164
drosophila_melanogaster	CG44098	FBGN0264907
caenorhabditis_elegans		WBGENE00003837
caenorhabditis_elegans	oct-1	WBGENE00003842
caenorhabditis_elegans		WBGENE00003843
caenorhabditis_elegans		WBGENE00006220
caenorhabditis_elegans		WBGENE00008110
caenorhabditis_elegans		WBGENE00011456
caenorhabditis_elegans		WBGENE00014127
caenorhabditis_elegans		WBGENE00015088
caenorhabditis_elegans		WBGENE00017751
caenorhabditis_elegans		WBGENE00019408
caenorhabditis_elegans		WBGENE00020701
caenorhabditis_elegans		WBGENE00044455

Paralogs (22): SLC22A16 (ENSG00000004809), SLC22A17 (ENSG00000092096), SLC22A2 (ENSG00000112499), SLC22A7 (ENSG00000137204), SLC22A23 (ENSG00000137266), SLC22A14 (ENSG00000144671), SLC22A3 (ENSG00000146477), SLC22A8 (ENSG00000149452), SLC22A9 (ENSG00000149742), SVOPL (ENSG00000157703), SLC22A15 (ENSG00000163393), SVOP (ENSG00000166111), SLC22A11 (ENSG00000168065), SLC22A13 (ENSG00000172940), SLC22A1 (ENSG00000175003), SLC22A10 (ENSG00000184999), SLC22A25 (ENSG00000196600), SLC22A4 (ENSG00000197208), SLC22A5 (ENSG00000197375), SLC22A24 (ENSG00000197658), SLC22A6 (ENSG00000197901), SLC22A31 (ENSG00000259803)

Protein

Protein identifiers

Solute carrier family 22 member 12 — Q96S37 (reviewed: Q96S37)

Alternative names: Organic anion transporter 4-like protein, Renal-specific transporter, Urate anion exchanger 1, Urate:anion antiporter SLC22A12

All UniProt accessions (1): Q96S37

UniProt curated annotations — full annotation on UniProt →

Function. Electroneutral antiporter that translocates urate across the apical membrane of proximal tubular cells in exchange for monovalent organic or inorganic anions. Involved in renal reabsorption of urate and helps maintaining blood levels of uric acid. Mediates urate uptake by an exchange with organic anions such as (S)-lactate and nicotinate, and inorganic anion Cl(-). Other inorganic anions such as Br(-), I(-) and NO3(-) may also act as counteranions that exchange for urate. Also mediates orotate tubular uptake coupled with nicotinate efflux and to a lesser extent with lactate efflux, therefore displaying a potential role in orotate renal reabsorption. Orotate transport is Cl(-)-dependent.

Subunit / interactions. Interacts with PDZK1.

Subcellular location. Apical cell membrane.

Tissue specificity. Detected in kidney (at protein level). Detected in fetal and adult kidney. Detected in epithelial cells of proximal tubules in renal cortex.

Post-translational modifications. N-glycosylated.

Disease relevance. Hypouricemia renal 1 (RHUC1) [MIM:220150] A disorder characterized by impaired uric acid reabsorption at the apical membrane of proximal renal tubule cells, and high urinary urate excretion. Patients often appear asymptomatic, but may be subject to exercise-induced acute renal failure, chronic renal dysfunction and nephrolithiasis. The disease is caused by variants affecting the gene represented in this entry.

Similarity. Belongs to the major facilitator (TC 2.A.1) superfamily. Organic cation transporter (TC 2.A.1.19) family.

Isoforms (4)

UniProt ID	Names	Canonical?
Q96S37-1	1	yes
Q96S37-2	2
Q96S37-3	3
Q96S37-4	4

RefSeq proteins (4): NP_001263255, NP_001263256, NP_653186, NP_700357 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR011701	MFS	Family
IPR020846	MFS_dom	Domain
IPR036259	MFS_trans_sf	Homologous_superfamily

Pfam: PF07690

Catalyzed reactions (Rhea), 4 shown:

• urate(out) + (S)-lactate(in) = urate(in) + (S)-lactate(out) (RHEA:72003)
• nicotinate(in) + urate(out) = nicotinate(out) + urate(in) (RHEA:72023)
• orotate(out) + nicotinate(in) = orotate(in) + nicotinate(out) (RHEA:72039)
• urate(out) + n chloride(in) = urate(in) + n chloride(out) (RHEA:72319)

UniProt features (89 total): helix 33, sequence variant 24, transmembrane region 12, strand 9, splice variant 3, glycosylation site 2, sequence conflict 2, turn 2, chain 1, modified residue 1

Structure

Experimental structures (PDB)

28 structures.

PDB	Method	Resolution (Å)
9RXO	X-RAY DIFFRACTION	1.2
9RXR	X-RAY DIFFRACTION	1.69
9RXS	X-RAY DIFFRACTION	2
9DKC	ELECTRON MICROSCOPY	2.55
9DK9	ELECTRON MICROSCOPY	2.68
9B1G	ELECTRON MICROSCOPY	2.7
9DKB	ELECTRON MICROSCOPY	2.74
9B1F	ELECTRON MICROSCOPY	2.9
9B1H	ELECTRON MICROSCOPY	2.9
8WJG	ELECTRON MICROSCOPY	3
9B1J	ELECTRON MICROSCOPY	3
9B1M	ELECTRON MICROSCOPY	3
9DKA	ELECTRON MICROSCOPY	3
9IRX	ELECTRON MICROSCOPY	3
9B1L	ELECTRON MICROSCOPY	3.1
9B1N	ELECTRON MICROSCOPY	3.1
9B1O	ELECTRON MICROSCOPY	3.1
9IRY	ELECTRON MICROSCOPY	3.2
9JDY	ELECTRON MICROSCOPY	3.23
9JE0	ELECTRON MICROSCOPY	3.23
9IRW	ELECTRON MICROSCOPY	3.26
9B1K	ELECTRON MICROSCOPY	3.3
9JDV	ELECTRON MICROSCOPY	3.32
9US8	ELECTRON MICROSCOPY	3.32
9JDZ	ELECTRON MICROSCOPY	3.5
9JE1	ELECTRON MICROSCOPY	3.6
9B1I	ELECTRON MICROSCOPY	3.7
8WJQ	ELECTRON MICROSCOPY	3.8

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q96S37-F1	86.79	0.54

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Post-translational modifications (1): 542

Glycosylation sites (2): 56, 102

Function

Pathways and Gene Ontology

Reactome pathways

9 pathways

ID	Pathway
R-HSA-561048	Organic anion transport by SLC22 transporters
R-HSA-5619071	Defective SLC22A12 causes renal hypouricemia 1 (RHUC1)
R-HSA-1643685	Disease
R-HSA-382551	Transport of small molecules
R-HSA-425366
R-HSA-425407	SLC-mediated transmembrane transport
R-HSA-549132
R-HSA-5619102	SLC transporter disorders
R-HSA-5619115	Disorders of transmembrane transporters

MSigDB gene sets: 135 (showing top): GSE37336_LY6C_POS_VS_NEG_NAIVE_CD4_TCELL_DN, GSE45365_NK_CELL_VS_CD11B_DC_UP, GOBP_EXCRETION, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_CELLULAR_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, chr11q13, GOBP_CELLULAR_RESPONSE_TO_INSULIN_STIMULUS, FERREIRA_EWINGS_SARCOMA_UNSTABLE_VS_STABLE_DN, GOBP_CELLULAR_RESPONSE_TO_HORMONE_STIMULUS, GOBP_RESPONSE_TO_INSULIN, RYTAAWNNNTGAY_UNKNOWN, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_RESPONSE_TO_OXYGEN_CONTAINING_COMPOUND, GOBP_CELLULAR_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_RESPONSE_TO_HORMONE

GO Biological Process (9): monoatomic ion transport (GO:0006811), response to xenobiotic stimulus (GO:0009410), obsolete organic anion transport (GO:0015711), urate transport (GO:0015747), cellular homeostasis (GO:0019725), cellular response to insulin stimulus (GO:0032869), urate metabolic process (GO:0046415), renal urate salt excretion (GO:0097744), transmembrane transport (GO:0055085)

GO Molecular Function (3): urate transmembrane transporter activity (GO:0015143), PDZ domain binding (GO:0030165), transmembrane transporter activity (GO:0022857)

GO Cellular Component (5): plasma membrane (GO:0005886), membrane (GO:0016020), apical plasma membrane (GO:0016324), brush border membrane (GO:0031526), extracellular exosome (GO:0070062)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
SLC-mediated transport of organic anions	1
SLC transporter disorders	1
Transport of small molecules	1
Disorders of transmembrane transporters	1
Disease	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	2
response to chemical	1
nitrogen compound transport	1
homeostatic process	1
response to insulin	1
cellular response to peptide hormone stimulus	1
small molecule metabolic process	1
purine-containing compound metabolic process	1
renal tubular secretion	1
cellular process	1
urate transport	1
salt transmembrane transporter activity	1
protein domain specific binding	1
transporter activity	1
transmembrane transport	1
membrane	1
cell periphery	1
cellular anatomical structure	1
apical part of cell	1
plasma membrane region	1
brush border	1
apical plasma membrane	1
cell projection membrane	1
extracellular vesicle	1

Protein interactions and networks

STRING

890 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLC22A12	SLC2A9	Q9NRM0	996
SLC22A12	SLC5A8	Q8N695	971
SLC22A12	SLC5A12	Q1EHB4	968
SLC22A12	SLC17A1	Q14916	924
SLC22A12	PDZK1	Q5T2W1	892
SLC22A12	ABCG2	Q9UNQ0	861
SLC22A12	SLC17A3	O00476	819
SLC22A12	CEBPD	P49716	763
SLC22A12	ABCC4	O15439	758
SLC22A12	SLC16A9	Q7RTY1	729
SLC22A12	XDH	P47989	720
SLC22A12	SLC2A5	P22732	716
SLC22A12	SLC5A6	Q9Y289	629
SLC22A12	LRP2	P98164	612
SLC22A12	CARMIL1	Q5VZK9	600

IntAct

130 interactions, top by confidence:

A	B	Type	Score
SLC22A12	PDZK1	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	SHANK1	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	PTPN3	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	NHERF2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	MAST1	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	DLG3	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	PARD3B	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	TIAM2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	NHERF4	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	TAMALIN	psi-mi:“MI:0407”(direct interaction)	0.440
PICK1	SLC22A12	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	PDZD7	psi-mi:“MI:0407”(direct interaction)	0.440
APBA3	SLC22A12	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	GRIP2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	MPP2	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	SNTA1	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	PDZRN4	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	TAX1BP3	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	ARHGAP21	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	AHNAK	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	PDLIM1	psi-mi:“MI:0407”(direct interaction)	0.440
SLC22A12	SNTB1	psi-mi:“MI:0407”(direct interaction)	0.440
PATJ	SLC22A12	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (13): SLC22A12 (Affinity Capture-MS), SMAP2 (Affinity Capture-MS), ATP5B (Affinity Capture-MS), SLC22A12 (Reconstituted Complex), SLC22A12 (Two-hybrid), SMAP2 (Affinity Capture-MS), CFL2 (Affinity Capture-MS), LIMA1 (Affinity Capture-MS), MYO5A (Affinity Capture-MS), OCIAD1 (Affinity Capture-MS), PPP1R12A (Affinity Capture-MS), SAP18 (Affinity Capture-MS), SPECC1L (Affinity Capture-MS)

ESM2 similar proteins: A0A3Q2IDB4, A0A8B7HA97, A4ZYQ5, A6NK97, A6QLW8, G1SZD9, O35956, O57379, O88909, Q05B81, Q1RPP5, Q2KIV1, Q3ZAV1, Q4U2R8, Q4W8A2, Q4W8A3, Q5R9C4, Q5RC45, Q5RCH6, Q5RLM2, Q63ZE4, Q66J52, Q6A4L0, Q6DFR1, Q6NUB3, Q6NYN7, Q6PXP3, Q6T423, Q6ZMD2, Q70BM6, Q76M72, Q76M99, Q80UJ1, Q864Z3, Q8CE47, Q8CFZ5, Q8HY24, Q8IVM8, Q8MK48, Q8N4F4

Diamond homologs: A0A3Q2IDB4, A0A8B7HA97, A6NK97, A6QLW8, B2GV36, G1SZD9, O34691, O35956, O57379, O75751, O88446, O88909, Q1RPP5, Q28ES4, Q2KIV1, Q3YAW7, Q3ZAV1, Q4U2R8, Q4W8A2, Q4W8A3, Q5R540, Q5R9C4, Q5RC45, Q5RCH6, Q5RLM2, Q63ZE4, Q66J52, Q66J54, Q6A4L0, Q6NYN7, Q6T423, Q70BM6, Q76M72, Q76M99, Q80UJ1, Q864Z3, Q8CFZ5, Q8HY24, Q8IVM8, Q8MK48

SIGNOR signaling

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 88 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	50.1×	2e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	47.7×	2e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	47.7×	2e-06
Long-term potentiation	5	41.7×	3e-06
Assembly and cell surface presentation of NMDA receptors	9	40.1×	9e-11
Neurexins and neuroligins	10	34.5×	4e-11
Protein-protein interactions at synapses	6	28.0×	2e-06
RHOB GTPase cycle	5	13.5×	6e-04

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	76.1×	4e-16
protein localization to synapse	6	54.7×	1e-07
receptor clustering	7	52.0×	1e-08
regulation of postsynaptic membrane neurotransmitter receptor levels	7	41.3×	5e-08
protein-containing complex assembly	9	12.2×	3e-06
cell-cell adhesion	10	12.1×	8e-07
regulation of small GTPase mediated signal transduction	5	8.6×	6e-03
chemical synaptic transmission	7	6.4×	3e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

337 variants total. Per-class counts are floors (≥ shown; pagination cap):

Classification	Count (floor)
Pathogenic	11
Likely pathogenic	9
Uncertain significance	175
Likely benign	65
Benign	42

Top pathogenic / likely-pathogenic (20)

Variant ID	HGVS	Classification
1177307	NM_144585.4(SLC22A12):c.502G>A (p.Asp168Asn)	Pathogenic
1356316	NM_144585.4(SLC22A12):c.743del (p.Thr248fs)	Pathogenic
1459519	NC_000011.9:g.(?64359029)(64359450_?)del	Pathogenic
2501006	NM_144585.4(SLC22A12):c.1523G>A (p.Ser508Asn)	Pathogenic
3512	NM_144585.4(SLC22A12):c.774G>A (p.Trp258Ter)	Pathogenic
3514	NM_144585.4(SLC22A12):c.894G>T (p.Glu298Asp)	Pathogenic
3515	NM_144585.4(SLC22A12):c.1253T>G (p.Leu418Arg)	Pathogenic
3516	NM_144585.4(SLC22A12):c.269G>A (p.Arg90His)	Pathogenic
3517	NM_144585.4(SLC22A12):c.1082G>T (p.Gly361Val)	Pathogenic
3599964	NM_144585.4(SLC22A12):c.506+1G>A	Pathogenic
3615385	NM_144585.4(SLC22A12):c.258_259delinsTT (p.Gln87Ter)	Pathogenic
1515855	NM_144585.4(SLC22A12):c.507-8_511del	Likely pathogenic
2137128	NM_144585.4(SLC22A12):c.1430G>A (p.Arg477His)	Likely pathogenic
3599958	NM_144585.4(SLC22A12):c.259C>T (p.Gln87Ter)	Likely pathogenic
3599969	NM_144585.4(SLC22A12):c.536del (p.Ser179fs)	Likely pathogenic
3599974	NM_144585.4(SLC22A12):c.667G>T (p.Glu223Ter)	Likely pathogenic
4277583	NM_144585.4(SLC22A12):c.693del (p.Leu232fs)	Likely pathogenic
493093	NM_144585.4(SLC22A12):c.103_104del (p.Ser35fs)	Likely pathogenic
631663	NM_144585.4(SLC22A12):c.661+1G>A	Likely pathogenic
632166	NM_144585.4(SLC22A12):c.1216C>T (p.Arg406Cys)	Likely pathogenic

SpliceAI

1621 predictions. Top by Δscore:

Variant	Effect	Δscore
11:64592777:A:AG	acceptor_gain	1.0000
11:64592777:AGT:A	acceptor_gain	1.0000
11:64592778:G:GG	acceptor_gain	1.0000
11:64592778:GT:G	acceptor_gain	1.0000
11:64592778:GTG:G	acceptor_gain	1.0000
11:64599888:ACGGT:A	donor_loss	1.0000
11:64599889:CGG:C	donor_loss	1.0000
11:64599890:GGTGA:G	donor_loss	1.0000
11:64599891:G:GG	donor_gain	1.0000
11:64600939:G:GG	donor_gain	1.0000
11:64591958:G:GC	donor_loss	0.9900
11:64591959:G:GA	donor_loss	0.9900
11:64592773:CATCA:C	acceptor_loss	0.9900
11:64592774:ATCAG:A	acceptor_loss	0.9900
11:64592776:CAG:C	acceptor_loss	0.9900
11:64592777:A:C	acceptor_loss	0.9900
11:64592777:AGTG:A	acceptor_gain	0.9900
11:64592778:GTGG:G	acceptor_gain	0.9900
11:64592778:GTGGA:G	acceptor_gain	0.9900
11:64592878:GACAG:G	donor_gain	0.9900
11:64592880:CAGG:C	donor_loss	0.9900
11:64592881:AGG:A	donor_loss	0.9900
11:64592883:G:GA	donor_loss	0.9900
11:64592883:G:GG	donor_gain	0.9900
11:64592884:T:G	donor_loss	0.9900
11:64593560:G:GG	donor_gain	0.9900
11:64593633:A:AG	acceptor_gain	0.9900
11:64593634:G:GG	acceptor_gain	0.9900
11:64598803:CACA:C	acceptor_loss	0.9900
11:64598805:CAGGT:C	acceptor_loss	0.9900

AlphaMissense

3544 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:64593697:A:C	S242R	0.982
11:64593699:C:A	S242R	0.982
11:64593699:C:G	S242R	0.982
11:64591602:T:C	F16L	0.977
11:64591604:C:A	F16L	0.977
11:64591604:C:G	F16L	0.977
11:64591827:T:C	F91L	0.975
11:64591829:C:A	F91L	0.975
11:64591829:C:G	F91L	0.975
11:64591674:T:C	F40L	0.974
11:64591676:C:A	F40L	0.974
11:64591676:C:G	F40L	0.974
11:64591563:T:C	F3L	0.968
11:64591565:T:A	F3L	0.968
11:64591565:T:G	F3L	0.968
11:64591916:G:C	W120C	0.966
11:64591916:G:T	W120C	0.966
11:64591701:T:A	C49S	0.961
11:64591702:G:C	C49S	0.961
11:64600866:G:A	G509D	0.961
11:64591935:T:C	F127L	0.960
11:64591937:C:A	F127L	0.960
11:64591937:C:G	F127L	0.960
11:64600862:A:C	S508R	0.960
11:64600864:T:A	S508R	0.960
11:64600864:T:G	S508R	0.960
11:64593704:G:A	G244D	0.952
11:64600865:G:C	G509R	0.951
11:64591828:T:G	F91C	0.948
11:64592781:G:C	W135C	0.948

dbSNP variants (sampled 300 via entrez): RS1000417463 (11:64593221 C>T), RS1000696326 (11:64594776 G>A), RS1000696796 (11:64599525 C>A,T), RS1000748706 (11:64594653 T>C), RS1000812258 (11:64602808 G>A,C), RS1000843602 (11:64599625 A>C,T), RS1000881389 (11:64589510 A>G), RS1000927186 (11:64589221 A>G), RS1001099955 (11:64596709 G>C), RS1001555231 (11:64601286 C>A), RS1001582833 (11:64593831 C>T), RS1001915048 (11:64596208 T>A,C), RS1001968922 (11:64595677 T>C), RS1002300241 (11:64590102 G>A), RS1002426830 (11:64589326 C>T)

Disease associations

OMIM: gene MIM:607096 | disease phenotypes: MIM:220150

GenCC curated gene-disease

Disease	Classification	Inheritance
hypouricemia, renal 1	Strong	Autosomal recessive
hereditary renal hypouricemia	Supportive	Autosomal recessive

Mondo (2): hypouricemia, renal 1 (MONDO:0020728), hereditary renal hypouricemia (MONDO:0009071)

Orphanet (1): Hereditary renal hypouricemia (Orphanet:94088)

HPO phenotypes

27 total (27 of 27 shown, HPO-id order):

HPO	Term
HP:0000007	Autosomal recessive inheritance
HP:0000091	Abnormal renal tubule morphology
HP:0000093	Proteinuria
HP:0000790	Hematuria
HP:0000791	Uric acid nephrolithiasis
HP:0001919	Acute kidney injury
HP:0002013	Vomiting
HP:0002018	Nausea
HP:0002150	Hypercalciuria
HP:0003138	Increased blood urea nitrogen
HP:0003149	Hyperuricosuria
HP:0003259	Elevated circulating creatinine concentration
HP:0003418	Back pain
HP:0003537	Hypouricemia
HP:0008651	Uric acid urolithiasis independent of gout
HP:0008682	Renal tubular epithelial necrosis
HP:0012211	Abnormal renal physiology
HP:0012213	Decreased glomerular filtration rate
HP:0012595	Mild proteinuria
HP:0012622	Chronic kidney disease
HP:0025709	Intermediate young adult onset
HP:0025710	Late young adult onset
HP:0030973	Postexertional symptom exacerbation
HP:0033132	Renal cortical hyperechogenicity
HP:0034368	Urolithiasis
HP:0100520	Oliguria
HP:6000746	Elevated fractional excretion of urate

GWAS associations

24 associations (top):

Study	Trait	p-value
GCST000418_2	Uric acid levels	2.000000e-09
GCST000581_2	Urate levels	2.000000e-31
GCST001163_4	Urate levels	3.000000e-16
GCST001608_4	Renal function-related traits (urate)	3.000000e-63
GCST001791_47	Urate levels	4.000000e-11
GCST002828_2	Urate levels in obese individuals	2.000000e-06
GCST002829_34	Urate levels in overweight individuals	9.000000e-14
GCST002829_43	Urate levels in overweight individuals	1.000000e-09
GCST002830_27	Urate levels in lean individuals	1.000000e-06
GCST003252_23	Systemic lupus erythematosus	7.000000e-07
GCST003359_4	Serum uric acid levels	5.000000e-06
GCST003924_4	Renal overload gout	2.000000e-06
GCST003925_9	Gout	5.000000e-11
GCST003926_7	Renal underexcretion gout	9.000000e-10
GCST007733_64	Serum uric acid levels	1.000000e-300
GCST007733_7	Serum uric acid levels	7.000000e-31
GCST007916_18	Hyperuricemia	2.000000e-16
GCST007918_7	Serum uric acid levels	2.000000e-16
GCST008971_38	Urate levels	5.000000e-48
GCST008972_170	Urate levels	2.000000e-246
GCST008972_96	Urate levels	1.000000e-101
GCST010274_8	Gout (combined type)	8.000000e-10
GCST010512_12	Serum uric acid levels	7.000000e-54
GCST010637_17	Urate levels	4.000000e-36

EFO canonical traits (3, from GWAS)

EFO ID	Trait name
EFO:0004761	uric acid measurement
EFO:0004531	urate measurement
EFO:0009104	hyperuricemia

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
C537757	Renal hypouricemia (supp.)

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL6120 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

13 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 135,703 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

Molecule	Name	Phase	Patents
CHEMBL1474963	BENZARONE	4	358
CHEMBL2105720	LESINURAD	4	604
CHEMBL388590	BENZBROMARONE	4	8,245
CHEMBL832	SULFINPYRAZONE	4	13,780
CHEMBL897	PROBENECID	4	105,640
CHEMBL981	FENOFIBRIC ACID	4	6,353
CHEMBL3746329	SHR-4640	3	32
CHEMBL4594446	DOTINURAD	3	68
CHEMBL2103824	ARHALOFENATE	2	170
CHEMBL2325014	PF-05089771	2	219
CHEMBL3707347	VERINURAD	2	184
CHEMBL5314438	PULIGINURAD	2	12
CHEMBL4640580	EPAMINURAD	1	38

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

1 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs11231825	Toxicity	3	cytarabine;fludarabine;gemtuzumab ozogamicin;idarubicin	Leukemia;Myeloid;Acute

PharmGKB variants

6 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs1529909	SLC22A12		0.00	0
rs3825016	SLC22A12		0.00	0
rs11231825	SLC22A12	3	2.75	1	cytarabine;fludarabine;gemtuzumab ozogamicin;idarubicin
rs3825018	SLC22A12		0.00	0
rs3825017	SLC22A12		0.00	0
rs505802	SLC22A12		0.00	0

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: transporter — Urate transporter

Most potent curated ligand interactions (2 total), top 2:

Ligand	Action	Affinity	Parameter
dotinurad	Inhibition	6.4	pIC50
sufinpyrazone	Inhibition	4.0	pIC50

Binding affinities (BindingDB)

456 measured of 564 human assays (565 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
4-[3-chloro-4-(hydroxymethyl)phenoxy]-3-cyano-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	1 nM	US-9067922: Chemical compounds
4-[[5-chloro-6-(hydroxymethyl)-3-pyridinyl]oxy]-2-fluoro-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	2 nM	US-9067922: Chemical compounds
3-cyano-4-(3,5-dichloro-4-cyanophenoxy)-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	3 nM	US-9067922: Chemical compounds
4-(3-chloro-4-cyano-5-fluorophenoxy)-3-cyano-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	8 nM	US-9067922: Chemical compounds
2{[4-(4-Cyanonaphthalen)isoquinolin-6-yl]thio}-2-methylpropionic acid	IC50	8 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
3-[1-[(2,6-dichlorophenyl)methyl]-3-methylindazol-6-yl]propanoic acid	IC50	10 nM	US-8987473: Ring-fused compound
5-[[1-[(2,6-dichlorophenyl)methyl]-3-methylindazol-6-yl]methyl]-3H-1,3,4-oxadiazole-2-thione	IC50	10 nM	US-8987473: Ring-fused compound
(3S)-3-[7-(4-cyanonaphthalen-1-yl)thieno[3,2-c]pyridin-2-yl]butanoic acid	IC50	10 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
(3R)-3-[4-(4-cyanonaphthalen-1-yl)thieno[2,3-c]pyridin-2-yl]butanoic acid	IC50	11 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
4-(3-chloro-4-cyanophenoxy)-N-(5-chloro-2-pyridinyl)-3-cyanobenzenesulfonamide	IC50	12 nM	US-9067922: Chemical compounds
3-[4-(4-Cyanonaphthalen-1-yl)isoquinolin-6-yl]-2,2-dimethyl propionic Acid	IC50	12 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
3-[4-(4-Cyanophenyl)thieno[2,3-c]pyridin-2-yl]-2,2-dimethyl propionic Acid	IC50	12 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
2-methyl-2-[[7-(4-nitrophenyl)-1,2-benzothiazol-6-yl]sulfanyl]propanoic acid	IC50	12 nM	US-10173990: URAT1 inhibitor
1-[(2,6-dichlorophenyl)methyl]-3-methyl-6-(2H-tetrazol-5-ylmethyl)indazole	IC50	13 nM	US-8987473: Ring-fused compound
4-(3-chloro-4-cyanophenoxy)-3-cyano-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	13 nM	US-9067922: Chemical compounds
3-cyano-4-(4-cyano-3,5-dimethylphenoxy)-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	13 nM	US-9067922: Chemical compounds
4-(2-chloro-6-cyano-1-benzofuran-4-yl)-2-hydroxybenzoic acid	IC50	14 nM	US-10266496: Carboxy substituted (hetero) aromatic ring derivatives and preparation method and uses thereof
2-[1-[(2,6-dichlorophenyl)methyl]-3-methylindol-6-yl]acetic acid	IC50	15 nM	US-8987473: Ring-fused compound
2-[1-[(2,6-dichlorophenyl)methyl]-3-methylindazol-6-yl]-2,2-difluoroacetic acid	IC50	15 nM	US-8987473: Ring-fused compound
4-(3-chloro-4-cyanophenoxy)-3-cyano-N-(4-fluoro-2-pyridinyl)benzenesulfonamide	IC50	15 nM	US-9067922: Chemical compounds
2{[4-(4-Cyanophenyl)isoquinolin-6-yl]thio-2-methylpropionic Acid	IC50	15 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
3-[4-(4-Cyanonaphthalen-1-yl)isoquinolin-6-yl]-2-methyl propionic acid	IC50	15 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
4-(6-cyano-2-fluoro-1-benzothiophen-4-yl)-2-hydroxybenzoic acid	IC50	15 nM	US-10266496: Carboxy substituted (hetero) aromatic ring derivatives and preparation method and uses thereof
4-[1-[(2,6-dichlorophenyl)methyl]-3-methylindazol-6-yl]butanoic acid	IC50	16 nM	US-8987473: Ring-fused compound
3-[1-[(2-chloro-6-cyclopropylphenyl)methyl]-3-methylindazol-6-yl]propanoic acid	IC50	17 nM	US-8987473: Ring-fused compound
2-[1-[(2,6-dimethylphenyl)methyl]-3,3-dimethyl-2H-indol-6-yl]acetic acid	IC50	18 nM	US-8987473: Ring-fused compound
2-[1-[(2,6-dichlorophenyl)methyl]-3-methylindazol-6-yl]acetic acid	IC50	18 nM	US-8987473: Ring-fused compound
3-[4-(4-Cyanonaphthalen-1-yl)thieno[2,3-c]pyridin-2-yl]-2,2-dimethyl propionic Acid	IC50	18 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
2-{[4-(2-Chloro-4-cyanophenyl)isoquinolin-6-yl]thio}-2-methyl propionic Acid	IC50	18 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
1-{[4-(4-cyanonaphthalen-1-yl)isoquinolin-6-yl]thio}cyclobutane-1-carboxylic Acid	IC50	18 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
4-(3-chloro-4-fluorophenoxy)-3-cyano-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	19 nM	US-9067922: Chemical compounds
2{[4-(5-Cyanonaphthalen-1-yl)isoquinolin-6-yl]thio}-2-methylpropionic Acid	IC50	19 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
3-[4-(4-Cyanophenyl)isoquinolin-6-yl]-2,2-dimethyl propionic Acid	IC50	19 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
4-(3-cyanonaphthalen-1-yl)-2-hydroxybenzoic acid	IC50	19 nM	US-10266496: Carboxy substituted (hetero) aromatic ring derivatives and preparation method and uses thereof
1-(6-bromoquinolin-4-yl)sulfanylcyclobutane-1-carboxylic acid	IC50	19 nM	US-9637484: Cycloalkyl acid derivative, preparation method thereof, and pharmaceutical application thereof
2-[[7-(4-cyanophenyl)-1,2-benzothiazol-6-yl]sulfanyl]-2-ethylbutanoic acid	IC50	21 nM	US-10173990: URAT1 inhibitor
4-(4-cyano-3,5-dimethylphenoxy)-2-fluoro-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	21 nM	US-9067922: Chemical compounds
1-[[7-(4-cyanophenyl)-1,2-benzothiazol-6-yl]sulfanyl]cyclobutane-1-carboxylic acid	IC50	21.5 nM	US-10173990: URAT1 inhibitor
2-[1-[(2,6-dimethylphenyl)methyl]-3-methylindol-6-yl]acetic acid	IC50	22 nM	US-8987473: Ring-fused compound
3-[1-[(2,6-dichlorophenyl)methyl]-3-methylindol-6-yl]propanoic acid	IC50	23 nM	US-8987473: Ring-fused compound
1-[(2,6-dichlorophenyl)methyl]-3-methyl-6-[2-(2H-tetrazol-5-yl)ethyl]indazole	IC50	23 nM	US-8987473: Ring-fused compound
2-[1-[(2,6-dimethylphenyl)methyl]-3-methyl-2,3-dihydroindol-6-yl]acetic acid	IC50	24 nM	US-8987473: Ring-fused compound
2-[1-[(2,6-dichlorophenyl)methyl]-3-ethylindazol-6-yl]acetic acid	IC50	24 nM	US-8987473: Ring-fused compound
3-cyano-N-(5-fluoro-2-pyridinyl)-4-(2-methoxy-6-methylphenoxy)benzenesulfonamide	IC50	24 nM	US-9067922: Chemical compounds
3-[4-(4-Cyanonaphthalen-1-yl)thieno[2,3-c]pyridin-2-yl] butyric Acid	IC50	24 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
3-[4-(4-Cyanonaphthalen-1-yl)isoquinolin-6-yl]butyric Acid	IC50	24 nM	US-10100016: Condensed ring derivative, and preparation method, intermediate, pharmaceutical composition and use thereof
4-[(5-chloro-6-methoxy-3-pyridinyl)oxy]-3-cyano-N-(5-fluoro-2-pyridinyl)benzenesulfonamide	IC50	25 nM	US-9067922: Chemical compounds
(E)-3-[1-(4-cyanophenyl)naphthalen-2-yl]sulfanylbut-2-enoic acid	IC50	25 nM	US-10173990: URAT1 inhibitor
3-[1-[(2,6-dichlorophenyl)methyl]-3-ethylindazol-6-yl]propanoic acid	IC50	26 nM	US-8987473: Ring-fused compound
RDEA3170	EC50	26 nM	US-10266493: Thioacetate compounds, compositions and methods of use

ChEMBL bioactivities

992 potent at pChembl≥5 of 1085 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
9.00	IC50	1	nM	CHEMBL3688197
8.70	IC50	2	nM	CHEMBL3688190
8.70	IC50	2	nM	CHEMBL4087516
8.52	IC50	3	nM	CHEMBL3688192
8.40	IC50	4	nM	CHEMBL5414132
8.22	IC50	6	nM	CHEMBL5399348
8.15	IC50	7	nM	CHEMBL3971610
8.15	IC50	7	nM	CHEMBL3683365
8.10	IC50	8	nM	CHEMBL3688188
8.10	IC50	8	nM	CHEMBL5759161
8.00	IC50	10	nM	CHEMBL3692018
8.00	IC50	10	nM	CHEMBL3692028
8.00	IC50	10	nM	CHEMBL4088988
8.00	IC50	10	nM	CHEMBL5965801
7.96	IC50	11	nM	CHEMBL6056778
7.92	IC50	12	nM	CHEMBL3683287
7.92	IC50	12	nM	CHEMBL3688185
7.92	IC50	12	nM	CHEMBL6049501
7.92	IC50	12	nM	PULIGINURAD
7.92	IC50	12	nM	CHEMBL5962505
7.89	IC50	13	nM	CHEMBL3683365
7.89	IC50	13	nM	CHEMBL3692025
7.89	IC50	13	nM	CHEMBL3683287
7.85	IC50	14	nM	CHEMBL5885206
7.82	IC50	15	nM	CHEMBL3691994
7.82	IC50	15	nM	CHEMBL3692056
7.82	IC50	15	nM	CHEMBL3683388
7.82	IC50	15	nM	CHEMBL5791883
7.82	IC50	15	nM	CHEMBL5926965
7.82	IC50	15	nM	CHEMBL5860948
7.80	IC50	16	nM	CHEMBL3692024
7.77	IC50	17	nM	CHEMBL3692057
7.75	IC50	18	nM	CHEMBL3902309
7.75	IC50	18	nM	CHEMBL3899557
7.75	IC50	18	nM	CHEMBL3691993
7.75	IC50	18	nM	CHEMBL3692003
7.75	IC50	18	nM	CHEMBL5874127
7.75	IC50	18	nM	CHEMBL5793003
7.75	IC50	18	nM	CHEMBL5745494
7.72	IC50	19	nM	CHEMBL3683364
7.72	IC50	19	nM	CHEMBL5786822
7.72	IC50	19	nM	CHEMBL5960864
7.72	IC50	19	nM	SHR-4640
7.72	IC50	19	nM	CHEMBL5993875
7.71	IC50	19.7	nM	CHEMBL5396351
7.70	IC50	20	nM	CHEMBL3947681
7.68	IC50	21	nM	CHEMBL3948311
7.68	IC50	21	nM	CHEMBL5937449
7.67	IC50	21.5	nM	CHEMBL5948551
7.66	IC50	22	nM	BENZBROMARONE

PubChem BioAssay actives

288 with measured affinity, of 766 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

Compound	Assay	Type	Value	Unit
N-[3-(4-cyanophenyl)-4-pyridinyl]-1,1,1-trifluoromethanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.0020	uM
N-(3,5-dichloro-4-cyanophenyl)-2-(trifluoromethoxy)benzenesulfonamide	2004198: Inhibition of URAT1 (unknown origin) assessed as decrease in uric acid level measured after 15 mins	ic50	0.0040	uM
N-(3-chloro-4-cyanophenyl)-2-(trifluoromethoxy)benzenesulfonamide	2004198: Inhibition of URAT1 (unknown origin) assessed as decrease in uric acid level measured after 15 mins	ic50	0.0060	uM
N-[3-(4-cyanonaphthalen-1-yl)-4-pyridinyl]-1,1,1-trifluoromethanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.0100	uM
dimethyl 2-[[5-bromo-4-(4-bromonaphthalen-1-yl)-1,2,4-triazol-3-yl]sulfanyl]propanedioate	2004197: Inhibition of human URAT1	ic50	0.0197	uM
2-[[3-(4-cyanonaphthalen-1-yl)-4-pyridinyl]sulfanyl]-2-methylpropanoic acid	1649928: Inhibition of human URAT1	ic50	0.0230	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-1-benzofuran-3-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.0260	uM
4-(5-cyano-2-fluoro-1-benzofuran-7-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.0310	uM
1-[[5-bromo-4-[(4-bromonaphthalen-1-yl)methyl]-1,2,4-triazol-3-yl]sulfanyl]-N-pyridin-3-ylmethanesulfonamide	1575209: Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptake	ic50	0.0320	uM
1-(6-bromoquinolin-4-yl)sulfanylcyclobutane-1-carboxylic acid	1447359: Inhibition of human URAT1	ic50	0.0330	uM
sodium 2-[[5-bromo-4-(thiophen-2-ylmethyl)-1,2,4-triazol-3-yl]sulfanyl]acetate	2037824: Inhibition of URAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction of uric acid uptake measured after 48 hrs	ic50	0.0350	uM
4-(2-chloro-5-cyano-1-benzofuran-7-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.0370	uM
(3,5-dichloro-4-hydroxyphenyl)-(1,1-dioxo-2H-1,3-benzothiazol-3-yl)methanone	1725612: Inhibition of human URAT1 expressed in Xenopus laevis oocytes assessed as inhibition of [14C]uric acid uptake measured after 60 mins by liquid scintillation counter method	ic50	0.0372	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-5-methoxy-1-benzofuran-3-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.0420	uM
4-(6-cyano-1-benzothiophen-4-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.0450	uM
1-[2-(4-cyanophenyl)phenyl]sulfanylcyclobutane-1-carboxylic acid	1447360: Inhibition of URAT1 (unknown origin) expressed in HEK293 cells assessed as reduction in [14C]uric acid uptake after 10 mins by liquid scintillation counting method	ic50	0.0500	uM
2-[[3-(4-cyanophenyl)-4-pyridinyl]sulfanyl]-2-methylpropanoic acid	1447359: Inhibition of human URAT1	ic50	0.0500	uM
N-[[(2S)-1-(6-cyclopropylquinoline-4-carbonyl)pyrrolidin-2-yl]methyl]-1,1,1-trifluoromethanesulfonamide	2075628: Inhibition of human URAT1 expressed in HEK-293T cells assessed as inhibition rate by measuring [C14}-uric acid uptake measured after 8 mins by MicroBeta2 scintillation counting analysis	ic50	0.0520	uM
(3,5-dibromo-4-hydroxyphenyl)-(2,3-dihydropyrido[4,3-b][1,4]oxazin-4-yl)methanone	1649928: Inhibition of human URAT1	ki	0.0570	uM
1-[6-(trifluoromethyl)quinolin-4-yl]sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.0612	uM
2-[3-[(2,6-dimethylphenyl)methoxy]-4-methylphenyl]acetic acid	1447359: Inhibition of human URAT1	ic50	0.0800	uM
N-(6-bromoquinolin-4-yl)-1,1,1-trifluoromethanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.0830	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-5-hydroxy-1-benzofuran-4-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.0830	uM
sodium 2-[[5-bromo-4-[(4-bromonaphthalen-1-yl)methyl]-1,2,4-triazol-3-yl]sulfanyl]acetate	1575209: Inhibition of human URAT1 expressed in HEK293 cells assessed as reduction in [8-14C]uric acid uptake	ic50	0.0940	uM
4-[5-cyano-2-(trifluoromethyl)-1-benzofuran-7-yl]-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.1040	uM
4-(6-cyano-2,3-dihydro-1H-inden-4-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.1070	uM
1,1,1-trifluoro-N-[[(2S)-1-[6-(1,2-oxazol-4-yl)quinoline-4-carbonyl]pyrrolidin-2-yl]methyl]methanesulfonamide	2075628: Inhibition of human URAT1 expressed in HEK-293T cells assessed as inhibition rate by measuring [C14}-uric acid uptake measured after 8 mins by MicroBeta2 scintillation counting analysis	ic50	0.1100	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-6-methoxy-1-benzofuran-3-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.1110	uM
1-[6-[2-(trifluoromethyl)phenyl]quinolin-4-yl]sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.1153	uM
N-[3-(4-cyanonaphthalen-1-yl)-4-pyridinyl]benzenesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.1270	uM
1-(7-bromoquinolin-4-yl)sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.1298	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-6-hydroxy-1-benzofuran-3-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.1380	uM
4-(5-cyano-1-benzofuran-7-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.1400	uM
1-[6-(4-fluorophenyl)quinolin-4-yl]sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.1588	uM
(E)-4-[2-(4-bromonaphthalen-1-yl)-4-oxo-2,3-dihydrochromen-8-yl]-2-methylbut-2-enoic acid	2129091: Inhibition of human URAT1 transfected in HEK293 cells by measuring 14C-uric acid uptake preincubated for 30 mins followed by 14–uric acid addition and measured after 15 mins by liquid scintillation counter analysis	ic50	0.1600	uM
sodium 2-[[3-(4-cyanonaphthalen-1-yl)-4-pyridinyl]sulfanyl]-2-methylpropanoate	1900867: Inhibition of URAT1 (unknown origin)-mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by liquid scintillation counting analysis	ic50	0.1700	uM
4-(6-cyano-1-benzofuran-4-yl)-2-hydroxybenzoic acid	2121183: Inhibition of URAT1 (unknown origin) by absorbance based assay	ic50	0.1720	uM
(6-bromo-2-ethyl-7-hydroxy-1-benzofuran-4-yl)-(3,5-dibromo-4-hydroxyphenyl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.1770	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-5-hydroxy-1-benzofuran-3-yl)methanone	593714: Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting	ic50	0.1890	uM
(E)-4-[2-(4-bromonaphthalen-1-yl)-7-hydroxy-4-oxo-2,3-dihydrochromen-8-yl]-2-methylbut-2-enoic acid	2129091: Inhibition of human URAT1 transfected in HEK293 cells by measuring 14C-uric acid uptake preincubated for 30 mins followed by 14–uric acid addition and measured after 15 mins by liquid scintillation counter analysis	ic50	0.1900	uM
1-[6-(methoxymethyl)quinolin-4-yl]sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.1978	uM
N-[3-(4-cyanophenyl)-4-pyridinyl]methanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.2030	uM
1-[6-(2-methoxyethoxy)quinolin-4-yl]sulfanylcyclobutane-1-carboxylic acid	1269088: Inhibition of human URAT1 expressed in HEK293 cells assessed as [14C]uric acid uptake after 12 mins by scintillation counter	ic50	0.2069	uM
1,1,1-trifluoro-N-[3-(4-methoxyphenyl)-4-pyridinyl]methanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.2150	uM
7-hydroxy-2-(4-hydroxyphenyl)-8-(3-methylbut-2-enyl)-2,3-dihydrochromen-4-one	2129111: Inhibition of URAT1 (unknown origin)	ic50	0.2200	uM
sodium 4-[5-bromo-4-[(4-bromonaphthalen-1-yl)methyl]-1,2,4-triazol-3-yl]butanoate	2037824: Inhibition of URAT1 (unknown origin) stably expressed in HEK293 cells assessed as reduction of uric acid uptake measured after 48 hrs	ic50	0.2300	uM
(E)-4-[2-(1-benzothiophen-3-yl)-7-hydroxy-4-oxo-2,3-dihydrochromen-8-yl]-2-methylbut-2-enoic acid	2129091: Inhibition of human URAT1 transfected in HEK293 cells by measuring 14C-uric acid uptake preincubated for 30 mins followed by 14–uric acid addition and measured after 15 mins by liquid scintillation counter analysis	ic50	0.2300	uM
sodium 2-[[3-[(4-cyanonaphthalen-1-yl)amino]-4-pyridinyl]sulfanylmethyl]benzoate	1900867: Inhibition of URAT1 (unknown origin)-mediated 14C-uric acid uptake expressed in HEK293 cells using 14C-uric acid as substrate preincubated for 30 mins followed by substrate addition and measured after 15 mins by liquid scintillation counting analysis	ic50	0.2400	uM
1,1,1-trifluoro-N-[3-(2-methoxyphenyl)-4-pyridinyl]methanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.2410	uM
N-[3-(4-cyanonaphthalen-1-yl)-4-pyridinyl]methanesulfonamide	1447335: Inhibition of human URAT1 expressed in HEK293T cells assessed as reduction in [14C]uric acid uptake measured after 5 mins by liquid scintillation counting method	ic50	0.2610	uM

CTD chemical–gene interactions

29 total (human), top 29 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
Uric Acid	decreases reaction, increases uptake, affects cotreatment, increases import, increases expression (+2 more)	8
Benzbromarone	decreases activity, affects response to substance, affects activity, decreases reaction, increases uptake	6
6-hydroxybenzbromarone	decreases reaction, increases uptake, decreases activity	2
Probenecid	affects activity, decreases reaction, increases uptake	2
Losartan	decreases activity, decreases abundance, decreases expression, affects response to substance	2
benzarone	decreases reaction, increases uptake	1
honokiol	decreases reaction, increases expression	1
bisphenol A	decreases methylation	1
nuciferine	increases expression, affects binding, decreases reaction	1
estrone sulfate	increases uptake	1
sodium arsenite	increases expression	1
perfluorooctanoic acid	decreases reaction, increases import, affects cotreatment	1
perfluorodecanoic acid	affects cotreatment, decreases reaction, increases import	1
CGP 52608	affects binding, increases reaction	1
E 3040	decreases reaction, increases uptake	1
perfluoro-n-heptanoic acid	affects cotreatment, decreases reaction, increases import	1
perfluoro-n-nonanoic acid	affects cotreatment, decreases reaction, increases import	1
perfluorohexanoic acid	affects uptake	1
Arsenic	affects methylation	1
Chlorine	affects cotreatment, decreases reaction, increases import	1
Enalapril	decreases reaction, increases uptake	1
Indomethacin	decreases reaction, increases uptake	1
Oxypurinol	decreases reaction, increases uptake	1
Phenylbutazone	decreases reaction, increases uptake	1
Pyrazinamide	affects activity	1
Salicylates	increases uptake, decreases reaction	1
Sulfinpyrazone	increases uptake, decreases reaction	1
Valproic Acid	increases methylation	1
Cadmium Chloride	increases expression	1

ChEMBL screening assays

108 unique, capped per target: 108 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1638722	Binding	Inhibition of human URAT-1 assessed as increase in renal uric acid excretion	Phase 2a randomized controlled trial of short-term activity, safety, and pharmacokinetics of a novel nonnucleoside reverse transcriptase inhibitor, RDEA806, in HIV-1-positive, antiretroviral-naive subjects. — Antimicrob Agents Chemother

Clinical trials (associated diseases)

3 trials via MONDO — disease-level, not drug-specific.

Trial	Phase	Status	Title
NCT04398251	PHASE4	UNKNOWN	A Randomized Clinical Trail of The Effect of Postoperative Uric Acid Control on Stone Recurrence and Renal Function in Patients With Hyperuricemia of Urolithiasis.
NCT06310967	PHASE1/PHASE2	RECRUITING	A Dose Escalation Study of IG3018 in Subjects With Hyperuricemia With or Without Chronic Kidney Disease
NCT06065852	Not specified	RECRUITING	National Registry of Rare Kidney Diseases