SLC22A6

Summary

SLC22A6 (solute carrier family 22 member 6, HGNC:10970) is a protein-coding gene on chromosome 11q12.3, encoding Solute carrier family 22 member 6 (Q4U2R8). Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate.

The protein encoded by this gene is involved in the sodium-dependent transport and excretion of organic anions, some of which are potentially toxic. The encoded protein is an integral membrane protein and may be localized to the basolateral membrane. Four transcript variants encoding four different isoforms have been found for this gene.

Source: NCBI Gene 9356 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 87 total
• Druggable target: yes — 32 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_153276

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10970
Approved symbol	SLC22A6
Name	solute carrier family 22 member 6
Location	11q12.3
Locus type	gene with protein product
Status	Approved
Aliases	ROAT1, PAHT, OAT1
Ensembl gene	ENSG00000197901
Ensembl biotype	protein_coding
OMIM	607582
Entrez	9356

Gene structure

Transcript identifiers

Ensembl transcripts: 7 — 5 protein_coding, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

ENST00000360421, ENST00000377871, ENST00000421062, ENST00000458333, ENST00000537349, ENST00000540654, ENST00000856538

RefSeq mRNA: 4 — MANE Select: NM_153276 NM_004790, NM_153276, NM_153277, NM_153278

CCDS: CCDS31591, CCDS44631, CCDS44632, CCDS8041

Canonical transcript exons

ENST00000360421 — 10 exons

Exon	Start	End
ENSE00001350481	62983944	62984047
ENSE00001388285	62984322	62984967
ENSE00001519126	62976597	62976881
ENSE00003523144	62979488	62979596
ENSE00003525889	62979734	62979948
ENSE00003548511	62981842	62982010
ENSE00003561177	62983537	62983691
ENSE00003575189	62977184	62977387
ENSE00003609081	62980985	62981100
ENSE00003690145	62981260	62981383

Expression profiles

Bgee: expression breadth broad, 63 present calls, max score 93.93.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.6831 / max 286.8650, expressed in 89 samples.

FANTOM5 promoters (7 alternative TSS)

Promoter ID	TPM avg	Samples expressed
120269	0.2990	10
120266	0.1966	80
120267	0.1130	46
120265	0.0351	20
120271	0.0147	9
120268	0.0142	8
120270	0.0105	6

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
adult mammalian kidney	UBERON:0000082	93.93	gold quality
nephron tubule	UBERON:0001231	92.49	gold quality
kidney epithelium	UBERON:0004819	91.69	gold quality
adult organism	UBERON:0007023	90.94	gold quality
renal glomerulus	UBERON:0000074	88.88	gold quality
metanephric glomerulus	UBERON:0004736	88.87	gold quality
kidney	UBERON:0002113	88.29	gold quality
renal medulla	UBERON:0000362	82.96	gold quality
cortex of kidney	UBERON:0001225	82.16	gold quality
metanephros	UBERON:0000081	79.10	gold quality
buccal mucosa cell	CL:0002336	78.71	silver quality
skeletal muscle tissue of rectus abdominis	UBERON:0004511	78.02	gold quality
endometrium epithelium	UBERON:0004811	74.71	gold quality
superficial temporal artery	UBERON:0001614	74.03	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	73.67	silver quality
gluteal muscle	UBERON:0002000	73.08	gold quality
inferior olivary complex	UBERON:0002127	72.57	gold quality
triceps brachii	UBERON:0001509	72.32	gold quality
pigmented layer of retina	UBERON:0001782	71.14	gold quality
diaphragm	UBERON:0001103	71.05	gold quality
type B pancreatic cell	CL:0000169	70.51	gold quality
skeletal muscle tissue of biceps brachii	UBERON:0004502	70.30	gold quality
substantia nigra	UBERON:0002038	70.22	gold quality
midbrain	UBERON:0001891	70.01	gold quality
olfactory bulb	UBERON:0002264	69.59	gold quality
pharyngeal mucosa	UBERON:0000355	69.38	gold quality
hypothalamus	UBERON:0001898	68.83	gold quality
pons	UBERON:0000988	68.78	gold quality
dorsal plus ventral thalamus	UBERON:0001897	68.66	gold quality
ventral tegmental area	UBERON:0002691	68.62	gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 3.

Experiment	Marker?	Max mean expression
E-GEOD-131882	yes	978.32
E-CURD-119	yes	69.20
E-CURD-135	no	1003.19
E-ANND-3	no	0.00

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): BCL6, FOXC1, HNF4A, IRF1

miRNA regulators (miRDB)

10 targeting SLC22A6, 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-5193	100.00	67.26	1744
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-92A-2-5P	99.75	67.01	2164
HSA-MIR-6715B-3P	98.80	68.07	1204
HSA-MIR-629-5P	98.78	68.72	1032
HSA-MIR-193B-5P	97.91	65.88	837
HSA-MIR-4456	97.50	64.88	1678
HSA-MIR-152-5P	96.42	66.59	960
HSA-MIR-203A-5P	96.33	65.03	714
HSA-MIR-6742-5P	96.32	64.01	869

Literature-anchored findings (GeneRIF, showing 40)

• elucidation of the molecular mechanism for renal tetracycline transport by human organic anion transporters (hOATs) using proximal tubular cells stably expressing hOATs (PMID:11855680)
• cimetidine was found to be substrate for fROAT/hOAT1; organic anion transporters likely contribute to cimetidine excretion in proximal tubules (PMID:12429554)
• hOAT1 transports urate,and is not responsible for familial juvenile gouty nephropathy in the two sisters examined in this study. (PMID:12472777)
• PKC-induced hOAT1 downregulation is achieved through carrier retrieval from the cell membrane and does not involve phosphorylation of the predicted classic hOAT1 PKC consensus sites (PMID:12874449)
• stimulation of basolateral organic anion uptake by EGF or PGE2 is a widespread (if not general) regulatory mechanism, and the signal transduction pathway involved seems to be general (PMID:14644751)
• glycosylation has a role in the targeting of OAT1 onto the plasma membrane (PMID:14749323)
• The level of human OAT1 mRNA is significantly lower in the kidney of patients with renal diseases than in the normal controls. (PMID:14984259)
• “…provide evidence for a general expression of the recently identified splice-variants of hOTA1…Their expression is restricted to the kidney cortex.” p. 430 (PMID:15039295)
• Leu-30 and Thr-36 in transmembrane domain 1 are critical determinants of hOAT1 function (PMID:15145940)
• Organic anion transporter(s) likely play prominent role in basolateral transport of mercuric ions by proximal tubular cells and in nephropathy induced by Hg(2+). (PMID:15200431)
• mercuric conjugates of Hcy are potential transportable substrates of OAT1. (PMID:15284288)
• the coding region of OAT1 has low genetic and functional diversity and its variants may not contribute substantially to interindividual differences in renal elimination of xenobiotics (PMID:15864112)
• hOAT1 has been suggested as the basis of nephrotoxicity induced by nucleoside phosphonate analogs (PMID:15914676)
• hOAT1 exists in the plasma membrane as a homooligomer, possibly trimer, and higher order of oligomer (PMID:16046403)
• CH(3)Hg-Cys is transported by hOAT1 (PMID:16164645)
• The clustering of OAT genes in the genome raises the possibility that nucleotide polymorphisms in SLC22A6 could also effect SLC22A8 expression, and vice versa. (PMID:16648942)
• the C terminus of hOAT1 has a central role in its function (PMID:16920720)
• identified two new residues, Tyr(230) and Phe(438), which are important for substrate/protein interactions (PMID:17038320)
• this paper reports the first characterization of the human OAT1 promoter and the first gene in the kidney whose promoter activity is regulated by HNF-4alpha (PMID:17344191)
• it is concluded that Arg(466) influences the binding of glutarate, but not interaction with p-aminohippurate, and interacts with chloride, which is a major determinant in substrate translocation (PMID:17353191)
• Both hOAT1 and hOAT3 are responsible for the basolateral uptake of edaravone sulfate in the kidney. (PMID:17502342)
• hOAT1 did not mediate rosuvastatin uptake (PMID:17585018)
• The data provide a model for the concerted action of OAT1 mediating basolateral secretion of glutarate derivatives from proximal tubule cells (PMID:18365245)
• OAT1 undergoes constitutive and protein kinase C-regulated trafficking through a dynamin- and clathrin-dependent pathway (PMID:18818201)
• The renal expression of OAT1 and OAT3 should be taken into account in order to improve pharmacotherapeutic efficacy and to prevent drug toxicity during the onset of this hepatic disease. (PMID:19034961)
• Gaboxadol could be taken up into the kidney by hOAT1 followed by glucuronidation and efflux of the conjugate into urine via MRP4. (PMID:19082692)
• ANG II inhibited hOAT1 activity through activation of PKCalpha, which led to the redistribution of the transporter from the cell surface to the intracellular compartments. (PMID:19088254)
• OAT1 appears to be one of the major contributors to renal basolateral uptake of citrulline, and impaired activities of these transporters may contribute substantially to the increase in plasma citrulline in renal failure. (PMID:19403644)
• results suggest that genetic polymorphisms may not be a significant contributing factor to variations in the hOAT2 expression or hOAT2 transport activity (PMID:19854166)
• Our results are the first to highlight the central role of TM 12 in maintaining the stability and in promoting the maturation efficiency of hOAT1. (PMID:19892921)
• Intergenic polymorphism rs10792367 between OAT1 and OAT3 is not associated with hypertension, but appears to be involved in between-individual variations in antihypertensive responses to hydrochlorothiazide. (PMID:21164499)
• The data reveal alpha-ketoglutarate as a common high-affinity substrate of NaDC3, OAT1, and OAT3 (PMID:21865262)
• High urine OAT1 and OAT3 and low OAT4 is associated with early reversible proximal tubular damage. (PMID:21945944)
• Both hOAT1 and hOAT3 markedly stimulated the uptake of kynurenic acid into oocytes. (PMID:22108572)
• It was shown that human OAT3 and OAT1 cannot be involved in the renal extraction of glutathione from blood, but OAT1 could support intracellular glutathione synthesis by taking up cysteinyl glycine. (PMID:23255614)
• The results confirmed that OAT1, OAT3, OCT2, MATE1, and MATE2-K were coexpressed in tubular epithelial cells. (PMID:23630107)
• PKC isoform PKCalpha was responsible for OAT1 ubiquitination. (PMID:23640180)
• transport of xanthurenic acid by OAT1 and OAT3 (PMID:23832370)
• high capacity p-cresyl sulfate trasnporter (PMID:24185403)
• Clopidogrel/clopidogrel carboxylate are weak inhibitors of OAT1. (PMID:24530383)

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	Slc22a6	ENSMUSG00000024650
rattus_norvegicus	Slc22a6	ENSRNOG00000018215
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), SLC22A12 (ENSG00000197891), SLC22A31 (ENSG00000259803)

Protein

Protein identifiers

Solute carrier family 22 member 6 — Q4U2R8 (reviewed: Q4U2R8)

Alternative names: Organic anion transporter 1, PAH transporter, Renal organic anion transporter 1

All UniProt accessions (2): F5H0T7, Q4U2R8

UniProt curated annotations — full annotation on UniProt →

Function. Secondary active transporter that functions as a Na(+)-independent organic anion (OA)/dicarboxylate antiporter where the uptake of one molecule of OA into the cell is coupled with an efflux of one molecule of intracellular dicarboxylate such as 2-oxoglutarate or glutarate. Mediates the uptake of OA across the basolateral side of proximal tubule epithelial cells, thereby contributing to the renal elimination of endogenous OA from the systemic circulation into the urine. Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins. Transports prostaglandin E2 (PGE2) and prostaglandin F2-alpha (PGF2-alpha) and may contribute to their renal excretion. Also mediates the uptake of cyclic nucleotides such as cAMP and cGMP. Involved in the transport of neuroactive tryptophan metabolites kynurenate (KYNA) and xanthurenate (XA) and may contribute to their secretion from the brain. May transport glutamate. Also involved in the disposition of uremic toxins and potentially toxic xenobiotics by the renal organic anion secretory pathway, helping reduce their undesired toxicological effects on the body. Uremic toxins include the indoxyl sulfate (IS), hippurate/N-benzoylglycine (HA), indole acetate (IA), 3-carboxy-4- methyl-5-propyl-2-furanpropionate (CMPF) and urate. Xenobiotics include the mycotoxin ochratoxin (OTA). May also contribute to the transport of organic compounds in testes across the blood-testis-barrier.

Subcellular location. Basolateral cell membrane. Basal cell membrane.

Tissue specificity. Strongly expressed in kidney. Expressed at lower level in liver, skeletal muscle, brain and placenta. In kidney, found at the basolateral membrane of the proximal tubule. In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and vascular endothelial cells.

Post-translational modifications. Glycosylated. Glycosylation at Asn-113 may occur at a secondary level. Glycosylation is necessary for proper targeting of the transporter to the plasma membrane.

Domain organisation. Multiple cysteine residues are necessary for proper targeting to the plasma membrane.

Miscellaneous. Involved in the renal transport of a variety of drugs with well-known nephrotoxic potential, therefore may play a role in the etiology of the drug-associated nephrotoxicity. Uptakes the diagnostic agent PAH/para-aminohippurate and clinically used drugs. Mediates the pH- and chloride-dependent bidirectional transport of PAH/para-aminohippurate in exchange for 2-oxoglutarate or glutarate as counteranions. Can also mediate PAH/cGMP exchange.

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?
Q4U2R8-1	1, OAT1-1	yes
Q4U2R8-2	2, OAT1-2
Q4U2R8-3	3, OAT1-3
Q4U2R8-4	4, OAT1-4

RefSeq proteins (4): NP_004781, NP_695008, NP_695009, NP_695010 (=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR004749	Orgcat_transp/SVOP	Family
IPR005828	MFS_sugar_transport-like	Family
IPR020846	MFS_dom	Domain
IPR036259	MFS_trans_sf	Homologous_superfamily

Pfam: PF00083

Catalyzed reactions (Rhea), 12 shown:

• (indol-3-yl)acetate(out) + a dicarboxylate(in) = (indol-3-yl)acetate(in) + a dicarboxylate(out) (RHEA:75983)
• indoxyl sulfate(out) + a dicarboxylate(in) = indoxyl sulfate(in) + a dicarboxylate(out) (RHEA:75987)
• N-benzoylglycine(out) + a dicarboxylate(in) = N-benzoylglycine(in) + a dicarboxylate(out) (RHEA:75991)
• 3-carboxy-4-methyl-5-propyl-2-furanpropanoate(out) + a dicarboxylate(in) = 3-carboxy-4-methyl-5-propyl-2-furanpropanoate(in) + a dicarboxylate(out) (RHEA:75995)
• kynurenate(out) + glutarate(in) = kynurenate(in) + glutarate(out) (RHEA:75999)
• (6R)-L-erythro-5,6,7,8-tetrahydrobiopterin(out) + a dicarboxylate(in) = (6R)-L-erythro-5,6,7,8-tetrahydrobiopterin(in) + a dicarboxylate(out) (RHEA:76071)
• L-erythro-7,8-dihydrobiopterin(out) + a dicarboxylate(in) = L-erythro-7,8-dihydrobiopterin(in) + a dicarboxylate(out) (RHEA:76075)
• L-sepiapterin(out) + a dicarboxylate(in) = L-sepiapterin(in) + a dicarboxylate(out) (RHEA:76079)
• prostaglandin F2alpha(out) + a dicarboxylate(in) = prostaglandin F2alpha(in) + a dicarboxylate(out) (RHEA:76119)
• prostaglandin E2(out) + a dicarboxylate(in) = prostaglandin E2(in) + a dicarboxylate(out) (RHEA:76123)
• 3’,5’-cyclic AMP(out) + a dicarboxylate(in) = 3’,5’-cyclic AMP(in) + a dicarboxylate(out) (RHEA:76127)
• 3’,5’-cyclic GMP(out) + a dicarboxylate(in) = 3’,5’-cyclic GMP(in) + a dicarboxylate(out) (RHEA:76131)

UniProt features (48 total): topological domain 13, transmembrane region 12, mutagenesis site 6, glycosylation site 5, sequence variant 4, site 2, splice variant 2, sequence conflict 2, chain 1, region of interest 1

Structure

Experimental structures (PDB)

12 structures.

PDB	Method	Resolution (Å)
9MAU	ELECTRON MICROSCOPY	2.87
9J04	ELECTRON MICROSCOPY	3.15
9U55	ELECTRON MICROSCOPY	3.17
9M8Y	ELECTRON MICROSCOPY	3.27
9M9V	ELECTRON MICROSCOPY	3.31
9MC8	ELECTRON MICROSCOPY	3.31
9KL5	ELECTRON MICROSCOPY	3.33
9J02	ELECTRON MICROSCOPY	3.36
9UNX	ELECTRON MICROSCOPY	3.45
9J06	ELECTRON MICROSCOPY	3.68
9KKK	ELECTRON MICROSCOPY	3.85
9KLZ	ELECTRON MICROSCOPY	3.88

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q4U2R8-F1	83.07	0.40

Functional residue map

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

Catalytic / active sites (2): 230 (important for interaction with cidofovir); 438 (important for interaction with cidofovir and pah)

Glycosylation sites (5): 39, 56, 92, 97, 113

Mutagenesis-validated functional residues (6):

Position	Phenotype
30	complete loss of pah transport activity.
36	complete loss of pah transport activity.
39	complete loss of pah transport activity.
230	loss of membrane protein expression and little uptake of cidofovir.
431	decrease in the level of membrane protein expression and 70 % loss of pah uptake.
438	decrease in the level of membrane protein expression, 70 % loss of pah uptake, increased affinity for cidofovir, lower v

Function

Pathways and Gene Ontology

Reactome pathways

5 pathways

ID	Pathway
R-HSA-561048	Organic anion transport by SLC22 transporters
R-HSA-382551	Transport of small molecules
R-HSA-425366
R-HSA-425407	SLC-mediated transmembrane transport
R-HSA-549132

MSigDB gene sets: 144 (showing top): GOBP_EXCRETION, GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, GOBP_EPITHELIUM_DEVELOPMENT, MORF_FLT1, GOBP_METANEPHROS_DEVELOPMENT, MORF_MSH3, RORA1_01, GOBP_METANEPHRIC_EPITHELIUM_DEVELOPMENT, MODULE_64, MORF_BRCA1, MORF_ESR1, GOBP_KIDNEY_EPITHELIUM_DEVELOPMENT, MORF_RAD51L3, GOBP_ORGANIC_ACID_TRANSPORT, MODULE_379

GO Biological Process (10): monoatomic anion transport (GO:0006820), obsolete organic anion transport (GO:0015711), prostaglandin transport (GO:0015732), alpha-ketoglutarate transport (GO:0015742), sodium-independent organic anion transport (GO:0043252), metanephric proximal tubule development (GO:0072237), renal tubular secretion (GO:0097254), inorganic anion transport (GO:0015698), xenobiotic transport (GO:0042908), transmembrane transport (GO:0055085)

GO Molecular Function (11): solute:inorganic anion antiporter activity (GO:0005452), obsolete organic anion transmembrane transporter activity (GO:0008514), prostaglandin transmembrane transporter activity (GO:0015132), alpha-ketoglutarate transmembrane transporter activity (GO:0015139), antiporter activity (GO:0015297), obsolete sodium-independent organic anion transmembrane transporter activity (GO:0015347), transmembrane transporter activity (GO:0022857), chloride ion binding (GO:0031404), identical protein binding (GO:0042802), xenobiotic transmembrane transporter activity (GO:0042910), protein binding (GO:0005515)

GO Cellular Component (7): plasma membrane (GO:0005886), caveola (GO:0005901), basal plasma membrane (GO:0009925), basolateral plasma membrane (GO:0016323), protein-containing complex (GO:0032991), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-2 pathways:

Category	Pathways
SLC-mediated transport of organic anions	1
Transport of small molecules	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	3
transmembrane transport	2
plasma membrane region	2
monoatomic ion transport	1
fatty acid transport	1
icosanoid transport	1
dicarboxylic acid transport	1
proximal tubule development	1
metanephric nephron tubule development	1
renal system process	1
excretion	1
cellular process	1
antiporter activity	1
prostaglandin transport	1
icosanoid transmembrane transporter activity	1
dicarboxylic acid transmembrane transporter activity	1
alpha-ketoglutarate transport	1
secondary active transmembrane transporter activity	1
transporter activity	1
anion binding	1
protein binding	1
transmembrane transporter activity	1
xenobiotic transport	1
binding	1
membrane	1
cell periphery	1
plasma membrane raft	1
basal part of cell	1
basal plasma membrane	1
cellular_component	1
extracellular vesicle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1300 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLC22A6	SLC2A9	Q9NRM0	780
SLC22A6	YRDC	Q86U90	771
SLC22A6	SLC47A1	Q96FL8	733
SLC22A6	Q92681	Q92681	722
SLC22A6	ABCC4	O15439	722
SLC22A6	SLC6A2	P23975	714
SLC22A6	SLC47A2	Q86VL8	712
SLC22A6	SLCO1B3	Q9NPD5	706
SLC22A6	SLC15A1	P46059	704
SLC22A6	ABCC2	Q92887	704
SLC22A6	SLCO1B1	Q9Y6L6	685
SLC22A6	ABCG2	Q9UNQ0	677
SLC22A6	SLC17A3	O00476	657
SLC22A6	SLC15A2	Q16348	648
SLC22A6	SLC17A1	Q14916	647

IntAct

7 interactions, top by confidence:

A	B	Type	Score
APPBP2	SLC22A6	psi-mi:“MI:0915”(physical association)	0.620
SLC22A6	APPBP2	psi-mi:“MI:0915”(physical association)	0.620
IL3RA	STX7	psi-mi:“MI:0914”(association)	0.350
SLC22A6	YIF1A	psi-mi:“MI:0914”(association)	0.350
SLC22A6	CLGN	psi-mi:“MI:0914”(association)	0.350

BioGRID (76): APPBP2 (Two-hybrid), SLC25A23 (Affinity Capture-MS), SLC25A46 (Affinity Capture-MS), SLC20A2 (Affinity Capture-MS), SLC25A24 (Affinity Capture-MS), LPCAT3 (Affinity Capture-MS), GK (Affinity Capture-MS), RAB32 (Affinity Capture-MS), SLC38A7 (Affinity Capture-MS), ERGIC3 (Affinity Capture-MS), ERGIC2 (Affinity Capture-MS), MCU (Affinity Capture-MS), PDXDC1 (Affinity Capture-MS), CHPT1 (Affinity Capture-MS), SFXN5 (Affinity Capture-MS)

ESM2 similar proteins: A0A3Q2IDB4, A0A8B7HA97, A4ZYQ5, A6NK97, G1SZD9, O35956, O57379, O88909, P22732, P23945, P43427, Q0IHM1, Q2KIV1, Q3ZAV1, Q4U2R8, Q4W8A2, Q4W8A3, Q5R9C4, Q5RC45, Q5RCH6, Q5RET7, Q63ZE4, Q66J52, Q6DFR1, Q6NUB3, Q6NYN7, Q6PXP3, Q6T423, Q70BM6, Q76M72, Q76M99, Q80UJ1, Q863Y9, Q864Z3, Q8CFZ5, Q8HY24, Q8IVM8, Q8MK48, Q8N4F4, Q8R0S9

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.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	78
Likely benign	7
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

1529 predictions. Top by Δscore:

Variant	Effect	Δscore
11:62979597:C:CC	acceptor_gain	1.0000
11:62979728:GCTCA:G	donor_loss	1.0000
11:62979730:TCA:T	donor_loss	1.0000
11:62979731:CA:C	donor_loss	1.0000
11:62979732:A:AC	donor_gain	1.0000
11:62979732:AC:A	donor_gain	1.0000
11:62979733:C:CC	donor_gain	1.0000
11:62979733:C:CT	donor_loss	1.0000
11:62979733:CC:C	donor_gain	1.0000
11:62979944:CAAAC:C	acceptor_gain	1.0000
11:62979946:AAC:A	acceptor_gain	1.0000
11:62979946:AACC:A	acceptor_loss	1.0000
11:62979947:AC:A	acceptor_gain	1.0000
11:62979948:CC:C	acceptor_gain	1.0000
11:62979948:CCT:C	acceptor_loss	1.0000
11:62979949:C:CC	acceptor_gain	1.0000
11:62979949:CTA:C	acceptor_loss	1.0000
11:62979950:T:C	acceptor_loss	1.0000
11:62979953:C:CT	acceptor_gain	1.0000
11:62981256:TCA:T	donor_loss	1.0000
11:62981257:CACCT:C	donor_loss	1.0000
11:62981258:A:AG	donor_loss	1.0000
11:62981259:C:A	donor_loss	1.0000
11:62981261:T:TA	donor_gain	1.0000
11:62981270:A:AC	donor_gain	1.0000
11:62981271:A:C	donor_gain	1.0000
11:62981379:AGAAC:A	acceptor_gain	1.0000
11:62981380:GAAC:G	acceptor_gain	1.0000
11:62981381:AAC:A	acceptor_gain	1.0000
11:62981381:AACC:A	acceptor_loss	1.0000

AlphaMissense

3548 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:62979936:G:C	S350R	0.997
11:62979936:G:T	S350R	0.997
11:62979938:T:G	S350R	0.997
11:62977277:C:T	G491D	0.996
11:62977342:G:C	S469R	0.996
11:62977342:G:T	S469R	0.996
11:62977344:T:G	S469R	0.996
11:62977333:G:C	S472R	0.995
11:62977333:G:T	S472R	0.995
11:62977335:T:G	S472R	0.995
11:62977346:C:T	G468D	0.995
11:62981946:G:C	S231R	0.995
11:62981946:G:T	S231R	0.995
11:62981948:T:G	S231R	0.995
11:62977347:C:G	G468R	0.994
11:62979555:C:G	G432R	0.994
11:62979556:C:A	K431N	0.994
11:62979556:C:G	K431N	0.994
11:62979769:C:T	G406D	0.994
11:62979770:C:G	G406R	0.994
11:62977255:G:C	S498R	0.993
11:62977255:G:T	S498R	0.993
11:62977257:T:G	S498R	0.993
11:62979506:A:G	L448P	0.993
11:62979561:C:G	G430R	0.993
11:62979561:C:T	G430R	0.993
11:62979806:G:T	R394S	0.993
11:62979864:A:C	F374L	0.993
11:62979864:A:T	F374L	0.993
11:62979866:A:G	F374L	0.993

dbSNP variants (sampled 300 via entrez): RS1000108104 (11:62984914 T>C), RS1000387451 (11:62978773 G>A,C), RS1000989446 (11:62976974 G>A), RS1000998373 (11:62983798 T>C), RS1001114593 (11:62983421 C>G), RS1001289761 (11:62986487 C>A), RS1001306753 (11:62984585 T>C,G), RS1001771656 (11:62977928 A>G), RS1002316364 (11:62982872 G>A), RS1002952689 (11:62983246 A>G), RS1003012861 (11:62976368 A>G), RS1003538281 (11:62976738 G>A), RS1004597530 (11:62980866 T>C), RS1005168971 (11:62977438 C>T), RS1005196698 (11:62982308 G>A,T)

Disease associations

OMIM: gene MIM:607582 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

0 total (0 of 0 shown, HPO-id order):

GWAS associations

2 associations (top):

Study	Trait	p-value
GCST008963_3	Glucose homeostasis traits	4.000000e-07
GCST008972_29	Urate levels	2.000000e-16

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004468	glucose measurement
EFO:0004531	urate measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1641347 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

32 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,334,765 (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
CHEMBL1146	CEFAMANDOLE	4	21,886
CHEMBL139	DICLOFENAC	4	125,009
CHEMBL1435	CEFAZOLIN	4	37,670
CHEMBL154	NAPROXEN	4	136,434
CHEMBL161	CEFTRIAXONE	4	71,135
CHEMBL1644	CEFADROXIL	4	6,102
CHEMBL1730	CEFOTAXIME	4	480
CHEMBL316157	CEPHALORIDINE	4	45,474
CHEMBL388590	BENZBROMARONE	4	8,245
CHEMBL463	AMINOHIPPURIC ACID	4	2,260
CHEMBL507674	CEFOPERAZONE	4	23,712
CHEMBL521	IBUPROFEN	4	228,490
CHEMBL527	PIROXICAM	4	107,554
CHEMBL5314375	CIDOFOVIR	4	120
CHEMBL563	FLURBIPROFEN	4	71,809
CHEMBL571	KETOPROFEN	4	103,580
CHEMBL6	INDOMETHACIN	4	156,366
CHEMBL617	CEPHALOTHIN	4	24,927
CHEMBL622	ETODOLAC	4	57,872
CHEMBL897	PROBENECID	4	105,640
CHEMBL898	DIFLUNISAL	4
CHEMBL922	ADEFOVIR DIPIVOXIL	4
CHEMBL4112930	PAMIPARIB	3
CHEMBL484	ADEFOVIR	3
CHEMBL52333	ROLOFYLLINE	3
CHEMBL119625	ZONAMPANEL	2
CHEMBL1231530	BETAMIPRON	2
CHEMBL324846	OCTANOIC ACID	2
CHEMBL3707347	VERINURAD	2
CHEMBL6246	ELLAGIC ACID	2

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

PharmGKB clinical annotations

2 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs11568626	Other	4	adefovir dipivoxil;cidofovir;tenofovir
rs11568634	Other	4	adefovir dipivoxil

PharmGKB variants

4 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs4149170	SLC22A6		0.00	0
rs11568626	SLC22A6	4	-1.75	1	adefovir dipivoxil;cidofovir;tenofovir
rs11568634	SLC22A6	4	-1.25	1	adefovir dipivoxil
rs4149171	SLC22A6		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: transporter — Organic anion transporters (OATs)

Most potent curated ligand interactions (1 total), top 1:

Ligand	Action	Affinity	Parameter
probenecid	Inhibition	4.9	pIC50

ChEMBL bioactivities

42 potent at pChembl≥5 of 81 total, top 41 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
7.52	Ki	30	nM	CEFAMANDOLE
6.75	Ki	180	nM	CEFAZOLIN
6.68	Ki	210	nM	CEFOPERAZONE
6.66	Ki	220	nM	CEPHALOTHIN
6.64	Ki	230	nM	CEFTRIAXONE
6.57	IC50	270	nM	ELLAGIC ACID
6.13	Ki	740	nM	CEPHALORIDINE
6.07	IC50	850	nM	DIFLUNISAL
5.89	IC50	1300	nM	KETOPROFEN
5.85	IC50	1400	nM	KETOPROFEN
5.82	IC50	1500	nM	FLURBIPROFEN
5.67	IC50	2120	nM	BENZBROMARONE
5.52	IC50	3000	nM	INDOMETHACIN
5.52	IC50	3000	nM	ZONAMPANEL
5.50	Ki	3130	nM	CEFOTAXIME
5.48	IC50	3300	nM	CHEMBL6143249
5.46	IC50	3500	nM	CHEMBL4527448
5.40	IC50	4000	nM	DICLOFENAC
5.37	Ki	4300	nM	PROBENECID
5.36	Ki	4410	nM	PROBENECID
5.36	IC50	4400	nM	CHEMBL4562825
5.34	IC50	4600	nM	BENZBROMARONE
5.34	IC50	4600	nM	VERINURAD
5.31	IC50	4900	nM	GLUTARATE
5.27	Ki	5410	nM	OCTANOIC ACID
5.24	IC50	5800	nM	NAPROXEN
5.22	IC50	6000	nM	BETAMIPRON
5.22	Ki	6020	nM	AMINOHIPPURIC ACID
5.21	Ki	6140	nM	CEFADROXIL
5.21	IC50	6190	nM	CHEMBL5542977
5.20	IC50	6300	nM	PROBENECID
5.14	Ki	7200	nM	EPAMINURAD
5.13	IC50	7400	nM	PROBENECID
5.11	Ki	7820	nM	ROLOFYLLINE
5.10	IC50	8000	nM	IBUPROFEN
5.08	IC50	8400	nM	CHEMBL4584575
5.06	IC50	8800	nM	AMINOHIPPURIC ACID
5.04	IC50	9170	nM	CHEMBL5568246
5.03	IC50	9300	nM	CHEMBL3929544
5.00	IC50	9900	nM	CHEMBL2074983
5.00	IC50	9900	nM	BENZOTHIAZOLYLCYSTEINE

PubChem BioAssay actives

39 with measured affinity, of 270 total; 32 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
(6R,7R)-7-[[(2R)-2-hydroxy-2-phenylacetyl]amino]-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.0300	uM
Cefazolin	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.1800	uM
(6R,7R)-7-[[(2R)-2-[(4-ethyl-2,3-dioxopiperazine-1-carbonyl)amino]-2-(4-hydroxyphenyl)acetyl]amino]-3-[(1-methyltetrazol-5-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.2100	uM
(6R,7R)-3-(acetyloxymethyl)-8-oxo-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.2200	uM
Ceftriaxone	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.2300	uM
6,7,13,14-tetrahydroxy-2,9-dioxatetracyclo[6.6.2.04,16.011,15]hexadeca-1(15),4,6,8(16),11,13-hexaene-3,10-dione	679387: TP_TRANSPORTER: inhibition of ochratoxin A uptake (ochratoxin A / 1uM) in Xenopus laevis oocytes	ic50	0.2700	uM
(6R,7R)-8-oxo-3-(pyridin-1-ium-1-ylmethyl)-7-[(2-thiophen-2-ylacetyl)amino]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	0.7400	uM
Diflunisal	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	0.8500	uM
Ketoprofen	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	1.3000	uM
Flurbiprofen	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	1.5000	uM
(3,5-dibromo-4-hydroxyphenyl)-(2-ethyl-1-benzofuran-3-yl)methanone	1999811: Inhibition of OAT1 (unknown origin) transfected in HEK293 cells assessed as inhibition of 6-CFL uptake preincubated for 30 mins followed by 6-CFL addition and measured for 15 mins by fluorescence based microplate reader analysis	ic50	2.1200	uM
2-(7-imidazol-1-yl-6-nitro-2,3-dioxo-4H-quinoxalin-1-yl)acetic acid	496844: Inhibition of human OAT1	ic50	3.0000	uM
Indomethacin	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	3.0000	uM
Cefotaxime	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	3.1300	uM
bis(4-hydroxy-3-methoxyphenyl)methanone	1639437: Inhibition of OAT1 (unknown origin) expressed in HEK293 cells assessed as reduction in 6-CF uptake measured after 5 mins by fluorescence assay	ic50	3.5000	uM
Diclofenac	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	4.0000	uM
Probenecid	679393: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing CHO cells	ki	4.3000	uM
4-ethenyl-7-hydroxy-8-methyl-9,10-dihydrophenanthrene-2-carboxylic acid	1639437: Inhibition of OAT1 (unknown origin) expressed in HEK293 cells assessed as reduction in 6-CF uptake measured after 5 mins by fluorescence assay	ic50	4.4000	uM
pentanedioic acid	681331: TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells	ic50	4.9000	uM
caprylic acid	678821: TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT1-expressing S2 cells	ki	5.4100	uM
Naproxen	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	5.8000	uM
3-benzamidopropanoic acid	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	6.0000	uM
aminohippuric acid	598877: Inhibition of human Oat1 expressed in Drosophila S2 cells	ki	6.0200	uM
Cefadroxil	681377: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	6.1400	uM
N-[[(2S)-1-(6-bromoquinoline-4-carbonyl)pyrrolidin-2-yl]methyl]-1,1,1-trifluoromethanesulfonamide	2075651: Inhibition of human OAT1 expressed in MDCK-II cells using 6-carboxyfluorescein as substrate	ic50	6.1900	uM
(3,5-dibromo-4-hydroxyphenyl)-(2,3-dihydropyrido[4,3-b][1,4]oxazin-4-yl)methanone	1649929: Inhibition of human OAT1	ki	7.2000	uM
1,3-dipropyl-8-(3-tricyclo[3.3.1.03,7]nonanyl)-7H-purine-2,6-dione	678999: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells	ki	7.8200	uM
2-[4-(2-methylpropyl)phenyl]propanoic acid	681160: TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells	ic50	8.0000	uM
3-ethenyl-7-hydroxy-8-methyl-9,10-dihydrophenanthrene-2-carboxylic acid	1639437: Inhibition of OAT1 (unknown origin) expressed in HEK293 cells assessed as reduction in 6-CF uptake measured after 5 mins by fluorescence assay	ic50	8.4000	uM
N-[[(2S)-1-(6-cyclopropylquinoline-4-carbonyl)pyrrolidin-2-yl]methyl]-1,1,1-trifluoromethanesulfonamide	2075651: Inhibition of human OAT1 expressed in MDCK-II cells using 6-carboxyfluorescein as substrate	ic50	9.1700	uM
(2R)-2-amino-3-(1,3-benzothiazol-2-ylsulfanyl)propanoic acid	679392: TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing CHO cells	ic50	9.9000	uM
(2S)-2-amino-3-(1,3-benzothiazol-2-ylsulfanyl)propanoic acid	679384: TP_TRANSPORTER: trans-stimulation in OAT1-COS7 cells	ic50	9.9000	uM

CTD chemical–gene interactions

116 total (human), top 30 by PubMed support.

Chemical	Actions (top 5)	PubMed papers
p-Aminohippuric Acid	increases import, increases uptake, increases reaction, affects transport, increases transport (+6 more)	22
Probenecid	increases import, increases response to substance, affects cotreatment, increases uptake, increases chemical synthesis (+3 more)	16
adefovir	decreases reaction, increases uptake, increases response to substance, affects response to substance	5
Glutarates	increases uptake, affects activity, affects binding, decreases reaction, increases transport (+2 more)	4
6-carboxyfluorescein	increases uptake, increases reaction, decreases reaction, increases import	3
glutaric acid	increases reaction, increases export, increases activity, decreases reaction, increases transport (+1 more)	3
Tenofovir	increases import, increases uptake, decreases reaction, increases response to substance	3
Cidofovir	increases import, increases response to substance, increases uptake	3
Cimetidine	decreases reaction, increases uptake, affects transport	3
Mercury	affects abundance, affects response to substance, affects cotreatment, increases transport	3
Methotrexate	decreases reaction, increases uptake, increases response to substance	3
Quercetin	decreases reaction, increases response to substance, increases uptake, decreases activity	3
aristolochic acid I	decreases activity, increases activity, increases response to substance, decreases reaction, increases uptake (+2 more)	2
ochratoxin A	increases uptake, increases reaction	2
adipic acid	decreases reaction, increases response to substance, increases transport, affects cotreatment	2
methylmercury cysteine	increases transport	2
2-amino-3-(2-amino-2-carboxyethylsulfanyl-mercuricsulfanyl)-propionic acid	decreases reaction, increases transport	2
Resveratrol	affects cotreatment, decreases expression, decreases reaction, increases uptake	2
Acetaminophen	decreases activity, decreases expression	2
Acetylcysteine	affects cotreatment, decreases reaction, increases response to substance, increases uptake, increases transport	2
Benzo(a)pyrene	affects methylation, decreases activity, increases methylation	2
Cisplatin	decreases expression	2
Ketoglutaric Acids	affects transport, decreases reaction, affects cotreatment, increases response to substance	2
Unithiol	increases uptake, increases reaction, increases secretion, decreases reaction	2
2,4-Dichlorophenoxyacetic Acid	decreases reaction, increases uptake	2
aurantio-obtusin	decreases activity	1
bisphenol F	increases reaction, increases uptake	1
pyrazinoic acid	affects transport, decreases reaction	1
baicalein	decreases activity	1
bisphenol A	increases reaction, increases uptake	1

ChEMBL screening assays

157 unique, capped per target: 94 functional, 39 binding, 22 admet, 2 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1217025	Binding	Inhibition of human OAT1	alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside. — J Med Chem
CHEMBL1743147	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OAT1	Membrane transporters in drug development. — Nat Rev Drug Discov
CHEMBL2075808	Functional	TP_TRANSPORTER: uptake in OAT1-expressing S2 cells	Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. — J Pharmacol Exp Ther

Cellosaurus cell lines

3 cell lines: 1 conditionally immortalized cell line, 1 telomerase immortalized cell line, 1 transformed cell line

First 10 cell lines (id-ordered, not curated):

Cellosaurus	Name	Category	Sex
CVCL_LI01	ciPTEC-OAT1	Conditionally immortalized cell line	Female
CVCL_RM67	RPTEC/TERT1 OAT1	Telomerase immortalized cell line	Male
CVCL_UE07	OAT1 HEK 293T/17	Transformed cell line	Female

Clinical trials (associated diseases)

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