SLCO4C1

Summary

SLCO4C1 (solute carrier organic anion transporter family member 4C1, HGNC:23612) is a protein-coding gene on chromosome 5q21.1, encoding Solute carrier organic anion transporter family member 4C1 (Q6ZQN7). Mediates the transport of organic anions such as steroids (estrone 3-sulfate, chenodeoxycholate, glycocholate) and thyroid hormones (3,3’,5-triiodo-L-thyronine (T3), L-thyroxine (T4)), in the kidney.

SLCO4C1 belongs to the organic anion transporter (OATP) family. OATPs are involved in the membrane transport of bile acids, conjugated steroids, thyroid hormone, eicosanoids, peptides, and numerous drugs in many tissues (Mikkaichi et al., 2004 [PubMed 14993604]).

Source: NCBI Gene 353189 — RefSeq curated summary.

At a glance

• GWAS associations: 2
• Clinical variants (ClinVar): 107 total
• Druggable target: yes — 2 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_180991

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:23612
Approved symbol	SLCO4C1
Name	solute carrier organic anion transporter family member 4C1
Location	5q21.1
Locus type	gene with protein product
Status	Approved
Aliases	SLC21A20, OATP4C1, OATPX, OATP-H
Ensembl gene	ENSG00000173930
Ensembl biotype	protein_coding
OMIM	609013
Entrez	353189

Gene structure

Transcript identifiers

Ensembl transcripts: 3 — 3 protein_coding

ENST00000310954, ENST00000893537, ENST00000893538

RefSeq mRNA: 1 — MANE Select: NM_180991 NM_180991

CCDS: CCDS34205

Canonical transcript exons

ENST00000310954 — 13 exons

Exon	Start	End
ENSE00001188943	102257943	102258087
ENSE00001188952	102270624	102270806
ENSE00001188957	102291343	102291606
ENSE00001188962	102239251	102239388
ENSE00001258422	102260213	102260319
ENSE00001258457	102295908	102296284
ENSE00001292745	102249638	102249788
ENSE00001292849	102247252	102247442
ENSE00001311328	102257115	102257310
ENSE00001313877	102240718	102240782
ENSE00001376896	102233986	102237018
ENSE00001504700	102261912	102262033
ENSE00001504701	102263684	102263780

Expression profiles

Bgee: expression breadth ubiquitous, 165 present calls, max score 94.00.

FANTOM5 (CAGE): breadth broad, TPM avg 2.2602 / max 148.7481, expressed in 614 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
62781	1.3555	427
62783	0.5169	216
62784	0.2440	117
62782	0.1438	57

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
nephron tubule	UBERON:0001231	94.00	gold quality
palpebral conjunctiva	UBERON:0001812	91.96	gold quality
renal medulla	UBERON:0000362	90.63	gold quality
kidney epithelium	UBERON:0004819	89.15	gold quality
lower lobe of lung	UBERON:0008949	88.57	gold quality
renal glomerulus	UBERON:0000074	88.06	gold quality
mucosa of paranasal sinus	UBERON:0005030	87.88	gold quality
metanephric glomerulus	UBERON:0004736	86.85	gold quality
metanephros cortex	UBERON:0010533	85.31	gold quality
cortex of kidney	UBERON:0001225	84.64	gold quality
kidney	UBERON:0002113	84.50	gold quality
adult mammalian kidney	UBERON:0000082	83.31	gold quality
bronchial epithelial cell	CL:0002328	82.62	gold quality
bone marrow	UBERON:0002371	81.81	gold quality
trabecular bone tissue	UBERON:0002483	81.56	gold quality
metanephros	UBERON:0000081	81.50	gold quality
nasal cavity mucosa	UBERON:0001826	79.09	gold quality
granulocyte	CL:0000094	78.04	gold quality
blood	UBERON:0000178	77.45	gold quality
epithelium of bronchus	UBERON:0002031	77.31	gold quality
bone marrow cell	CL:0002092	77.09	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	77.08	gold quality
bronchus	UBERON:0002185	76.00	gold quality
leukocyte	CL:0000738	75.70	gold quality
monocyte	CL:0000576	75.24	gold quality
mononuclear cell	CL:0000842	75.16	gold quality
nasal cavity epithelium	UBERON:0005384	74.37	gold quality
right lung	UBERON:0002167	73.49	gold quality
epithelium of nasopharynx	UBERON:0001951	73.11	gold quality
upper lobe of lung	UBERON:0008948	72.56	gold quality

Single-cell (SCXA)

Detected in 2 experiment(s), a significant marker in 1.

Experiment	Marker?	Max mean expression
E-ANND-3	yes	17.19
E-MTAB-8060	no	159.37

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): GATA3

miRNA regulators (miRDB)

133 targeting SLCO4C1, 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-6867-5P	100.00	82.21	3464
HSA-MIR-190A-3P	100.00	80.35	5520
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-3163	100.00	77.23	8605
HSA-MIR-340-5P	100.00	72.50	4437
HSA-MIR-1277-5P	100.00	73.95	5056
HSA-MIR-511-3P	99.99	68.85	1467
HSA-MIR-548C-3P	99.99	74.01	7587
HSA-MIR-568	99.98	69.86	2084
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-8075	99.97	67.20	962
HSA-MIR-3065-5P	99.97	71.56	3281
HSA-MIR-548AJ-3P	99.96	73.38	5345
HSA-MIR-548X-3P	99.96	73.38	5345
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-3912-5P	99.95	66.11	925
HSA-MIR-548AB	99.95	71.31	3488
HSA-MIR-559	99.95	72.28	3609
HSA-MIR-548A-5P	99.94	71.27	3482
HSA-MIR-548AD-5P	99.94	71.23	3502
HSA-MIR-548AE-5P	99.94	71.23	3502
HSA-MIR-548AK	99.94	71.24	3488
HSA-MIR-548AM-5P	99.94	71.24	3488
HSA-MIR-548AP-5P	99.94	71.14	3489
HSA-MIR-548AQ-5P	99.94	71.34	3426
HSA-MIR-548AR-5P	99.94	71.28	3515
HSA-MIR-548AS-5P	99.94	71.22	3482
HSA-MIR-548AU-5P	99.94	71.24	3488
HSA-MIR-548AY-5P	99.94	71.23	3502

Literature-anchored findings (GeneRIF, showing 7)

• isolation, cloning, and activity in the transport pathway of digoxin in the kidney (PMID:14993604)
• overexpression of human kidney-specific organic anion transporter SLCO4C1 in rat kidney reduced hypertension, cardiomegaly, and inflammation in the setting of renal failure (PMID:19875811)
• In conclusion, we found that estrone 3-sulfate is a novel substrate for OATP4C1. Moreover, our results indicate that estrone 3-sulfate does not bind to the recognition site for digoxin in OATP4C1. (PMID:20610891)
• single-nucleotide polymorphisms and haplotypes in SLCO4C1 in blacks are significantly associated with preeclampsia. (PMID:20691413)
• SLCO4C1 promoter methylation, including that at three CpG sites, namely, cg06480736, cg19774478 and cg22149516, is a potential biomarker for risk stratification and might offer significantly relevant prognostic information for prostate cancer patients after radical prostatectomy. (PMID:31288850)
• Knockdown of SLCO4C1 inhibits cell proliferation and metastasis in endometrial cancer through inactivating the PI3K/Akt signaling pathway. (PMID:32020231)
• Role of OATP4C1 in Renal Handling of Remdesivir and its Nucleoside Analog GS-441524: The First Approved Drug for Patients with COVID-19. (PMID:34048668)

Cross-species orthologs

5 orthologs

Organism	Symbol	Gene ID
mus_musculus	Slco4c1	ENSMUSG00000040693
rattus_norvegicus	Slco4c1	ENSRNOG00000022711
caenorhabditis_elegans		WBGENE00013499
caenorhabditis_elegans		WBGENE00018739
caenorhabditis_elegans		WBGENE00019346

Paralogs (10): SLCO1A2 (ENSG00000084453), SLCO4A1 (ENSG00000101187), SLCO1B3 (ENSG00000111700), SLCO1B1 (ENSG00000134538), SLCO2B1 (ENSG00000137491), SLCO5A1 (ENSG00000137571), SLCO1C1 (ENSG00000139155), SLCO2A1 (ENSG00000174640), SLCO3A1 (ENSG00000176463), SLCO6A1 (ENSG00000205359)

Protein

Protein identifiers

Solute carrier organic anion transporter family member 4C1 — Q6ZQN7 (reviewed: Q6ZQN7)

Alternative names: OATP-H, Organic anion transporter M1, Organic anion transporting polypeptide 4C1, Solute carrier family 21 member 20

All UniProt accessions (1): Q6ZQN7

UniProt curated annotations — full annotation on UniProt →

Function. Mediates the transport of organic anions such as steroids (estrone 3-sulfate, chenodeoxycholate, glycocholate) and thyroid hormones (3,3’,5-triiodo-L-thyronine (T3), L-thyroxine (T4)), in the kidney. Capable of transporting cAMP and pharmacological substances such as digoxin, ouabain and methotrexate. Transport is independent of sodium, chloride ion, and ATP. Transport activity is stimulated by an acidic extracellular environment due to increased substrate affinity to the transporter. The driving force for this transport activity is currently not known. The role of hydrogencarbonate (HCO3(-), bicarbonate) as the probable counteranion that exchanges for organic anions is still not well defined. Functions as an uptake transporter at the apical membrane, suggesting a role in renal reabsorption. Involved in the renal secretion of the uremic toxin ADMA (N(omega),N(omega)-dimethyl-L-arginine or asymmetrical dimethylarginine), which is associated to cardiovascular events and mortality, and the structurally related amino acids L-arginine and L-homoarginine (a cardioprotective biomarker). Can act bidirectionally, suggesting a dual protective role of this transport protein; exporting L-homoarginine after being synthesized in proximal tubule cells, and mediating uptake of ADMA from the blood into proximal tubule cells where it is degraded by the enzyme dimethylarginine dimethylaminohydrolase 1 (DDAH1). May be involved in sperm maturation by enabling directed movement of organic anions and compounds within or between cells. This ion-transporting process is important to maintain the strict epididymal homeostasis necessary for sperm maturation. May have a role in secretory functions since seminal vesicle epithelial cells are assumed to secrete proteins involved in decapacitation by modifying surface proteins to facilitate the acquisition of the ability to fertilize the egg.

Subcellular location. Basolateral cell membrane.

Tissue specificity. Predominantly expressed in kidney but also weakly expressed in both fetal liver and kidney.

Miscellaneous. SLCO4C1-mediated digoxin uptake is inhibited by digoxin itself and related compounds such as ouabain, digitoxin and digoxigenin.

Similarity. Belongs to the organo anion transporter (TC 2.A.60) family.

RefSeq proteins (1): NP_851322* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002350	Kazal_dom	Domain
IPR004156	OATP	Family
IPR020846	MFS_dom	Domain
IPR036058	Kazal_dom_sf	Homologous_superfamily
IPR036259	MFS_trans_sf	Homologous_superfamily

Pfam: PF03137, PF07648

Catalyzed reactions (Rhea), 8 shown:

• L-arginine(in) = L-arginine(out) (RHEA:32143)
• L-homoarginine(in) = L-homoarginine(out) (RHEA:71203)
• 3,3’,5-triiodo-L-thyronine(out) = 3,3’,5-triiodo-L-thyronine(in) (RHEA:71811)
• L-thyroxine(out) = L-thyroxine(in) (RHEA:71819)
• estrone 3-sulfate(out) = estrone 3-sulfate(in) (RHEA:71835)
• glycocholate(out) = glycocholate(in) (RHEA:71851)
• N(omega),N(omega)-dimethyl-L-arginine(out) = N(omega),N(omega)-dimethyl-L-arginine(in) (RHEA:75047)
• chenodeoxycholate(out) = chenodeoxycholate(in) (RHEA:75051)

UniProt features (38 total): topological domain 13, transmembrane region 12, modified residue 5, disulfide bond 3, chain 1, domain 1, region of interest 1, compositionally biased region 1, sequence conflict 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q6ZQN7-F1	78.71	0.46

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 (5): 15, 16, 24, 26, 28

Disulfide bonds (3): 501–530, 507–526, 516–547

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-6798695	Neutrophil degranulation
R-HSA-879518	Organic anion transport by SLCO transporters
R-HSA-168249	Innate Immune System
R-HSA-168256	Immune System
R-HSA-382551	Transport of small molecules
R-HSA-425397	Transport of vitamins, nucleosides, and related molecules
R-HSA-425407	SLC-mediated transmembrane transport

MSigDB gene sets: 116 (showing top): GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, REACTOME_INNATE_IMMUNE_SYSTEM, GOCC_VACUOLAR_MEMBRANE, GOCC_SECRETORY_GRANULE, GCANCTGNY_MYOD_Q6, LUCAS_HNF4A_TARGETS_UP, GOBP_MALE_GAMETE_GENERATION, HERNANDEZ_ABERRANT_MITOSIS_BY_DOCETACEL_2NM_UP, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_UP, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_DEVELOPMENTAL_PROCESS_INVOLVED_IN_REPRODUCTION, chr5q21, GOBP_TRANSMEMBRANE_TRANSPORT, GOCC_SECRETORY_VESICLE, GOCC_SPECIFIC_GRANULE

GO Biological Process (5): monoatomic ion transport (GO:0006811), spermatogenesis (GO:0007283), cell differentiation (GO:0030154), sodium-independent organic anion transport (GO:0043252), transmembrane transport (GO:0055085)

GO Molecular Function (4): obsolete organic anion transmembrane transporter activity (GO:0008514), obsolete sodium-independent organic anion transmembrane transporter activity (GO:0015347), protein binding (GO:0005515), transmembrane transporter activity (GO:0022857)

GO Cellular Component (6): plasma membrane (GO:0005886), basolateral plasma membrane (GO:0016323), azurophil granule membrane (GO:0035577), specific granule membrane (GO:0035579), extracellular exosome (GO:0070062), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Innate Immune System	1
SLC-mediated transport of organic anions	1
Immune System	1
SLC-mediated transmembrane transport	1
Transport of small molecules	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	2
transmembrane transport	2
secretory granule membrane	2
developmental process involved in reproduction	1
male gamete generation	1
cellular developmental process	1
cellular process	1
binding	1
transporter activity	1
membrane	1
cell periphery	1
basal plasma membrane	1
plasma membrane region	1
lysosomal membrane	1
azurophil granule	1
specific granule	1
extracellular vesicle	1
cellular anatomical structure	1

Protein interactions and networks

STRING

634 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO4C1	SLC22A8	Q8TCC7	722
SLCO4C1	SLC47A1	Q96FL8	703
SLCO4C1	SLC47A2	Q86VL8	687
SLCO4C1	SLC22A9	Q8IVM8	682
SLCO4C1	SLC22A7	Q9Y694	667
SLCO4C1	SLC22A11	Q9NSA0	666
SLCO4C1	SLC22A5	O76082	649
SLCO4C1	SLC22A4	Q9H015	640
SLCO4C1	SLC22A6	Q4U2R8	619
SLCO4C1	SLC22A2	O15244	588
SLCO4C1	SLC15A1	P46059	544
SLCO4C1	SLC22A12	Q96S37	538
SLCO4C1	ABCC4	O15439	531
SLCO4C1	SLC15A2	Q16348	531
SLCO4C1	SLC22A10	Q63ZE4	508

IntAct

8 interactions, top by confidence:

A	B	Type	Score
CLGN	NPC1	psi-mi:“MI:0914”(association)	0.530
SLCO4C1	CLGN	psi-mi:“MI:0914”(association)	0.530
CANX	HLA-A	psi-mi:“MI:0914”(association)	0.350
DSC1	TBC1D4	psi-mi:“MI:0914”(association)	0.350
SLC45A1	TBC1D4	psi-mi:“MI:0914”(association)	0.350
SLCO4C1	SLC9A1	psi-mi:“MI:0914”(association)	0.350
TMEM17	ESYT2	psi-mi:“MI:2364”(proximity)	0.270

BioGRID (48): SLCO4C1 (Proximity Label-MS), SLCO4C1 (Affinity Capture-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Proximity Label-MS), SLCO4C1 (Affinity Capture-MS), MTX1 (Affinity Capture-MS), SLCO4C1 (Affinity Capture-MS), ATP11C (Affinity Capture-MS), PDK1 (Affinity Capture-MS)

ESM2 similar proteins: A0A0G2KQY6, A1A5V7, A4II98, A8I499, A8NX72, B3TP03, B5D5N9, F4I8Q7, G5ECB2, O01840, O62126, O64759, P18581, P30823, P30825, P52569, P91679, P92942, Q10046, Q10320, Q17320, Q25479, Q2UVJ5, Q41745, Q42093, Q4QQU5, Q502G2, Q5BJD5, Q5FVN2, Q5N808, Q5PR34, Q5RBZ8, Q5REV9, Q5RFF0, Q5U4K5, Q5ZIL6, Q6IWY1, Q6NV38, Q6ZQN7, Q759P7

Diamond homologs: F5H094, G3V0H7, O35913, O88397, O94956, P46720, P46721, P70502, Q00910, Q5RFF0, Q6ZQN7, Q71MB6, Q8BGD4, Q8BXB6, Q8HYW2, Q8R3L5, Q91YY5, Q92959, Q96BD0, Q99J94, Q99N01, Q99N02, Q9EP96, Q9EPT5, Q9EPZ7, Q9ERB5, Q9GMU6, Q9H2Y9, Q9JHI3, Q9JJL3, Q9NPD5, Q9NYB5, Q9QXZ6, Q9QYE2, Q9QZX8, Q9UIG8, Q9Y6L6, Q8K078, Q86UG4, Q8C0X7

SIGNOR signaling

0 interactions.

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	85
Likely benign	8
Benign	1

Top pathogenic / likely-pathogenic (0)

SpliceAI

2033 predictions. Top by Δscore:

Variant	Effect	Δscore
5:102239249:A:AC	donor_gain	1.0000
5:102239250:C:CC	donor_gain	1.0000
5:102249646:T:TA	donor_gain	1.0000
5:102257185:G:C	donor_gain	1.0000
5:102257941:A:C	donor_loss	1.0000
5:102257942:C:CT	donor_loss	1.0000
5:102257944:T:TA	donor_gain	1.0000
5:102258054:C:CC	acceptor_gain	1.0000
5:102260207:TTTTA:T	donor_loss	1.0000
5:102260208:TTTA:T	donor_loss	1.0000
5:102260209:TTAC:T	donor_loss	1.0000
5:102260210:TAC:T	donor_loss	1.0000
5:102260211:A:AC	donor_gain	1.0000
5:102260211:A:AT	donor_loss	1.0000
5:102260212:C:CA	donor_loss	1.0000
5:102260212:C:CC	donor_gain	1.0000
5:102260320:C:CC	acceptor_gain	1.0000
5:102260320:C:CG	acceptor_loss	1.0000
5:102291512:G:C	donor_gain	1.0000
5:102247369:G:C	donor_gain	0.9900
5:102247372:TCAAA:T	donor_gain	0.9900
5:102249789:C:CC	acceptor_gain	0.9900
5:102257941:ACCT:A	donor_gain	0.9900
5:102257942:CCTC:C	donor_gain	0.9900
5:102258086:TT:T	acceptor_gain	0.9900
5:102258088:C:CC	acceptor_gain	0.9900
5:102260315:TGTAC:T	acceptor_gain	0.9900
5:102260316:GTAC:G	acceptor_gain	0.9900
5:102260317:TAC:T	acceptor_gain	0.9900
5:102260318:AC:A	acceptor_gain	0.9900

AlphaMissense

4698 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
5:102258004:A:C	F404L	0.997
5:102258004:A:T	F404L	0.997
5:102258006:A:G	F404L	0.997
5:102291555:C:G	R136P	0.997
5:102261993:A:G	W314R	0.996
5:102261993:A:T	W314R	0.996
5:102291512:G:C	S150R	0.996
5:102291512:G:T	S150R	0.996
5:102291514:T:G	S150R	0.996
5:102263747:G:T	A279D	0.995
5:102291539:A:C	S141R	0.995
5:102291539:A:T	S141R	0.995
5:102291541:T:G	S141R	0.995
5:102291560:C:A	E134D	0.995
5:102291560:C:G	E134D	0.995
5:102239339:A:C	C642W	0.994
5:102263741:C:T	G281D	0.994
5:102291496:A:G	C156R	0.994
5:102291575:G:C	S129R	0.994
5:102291575:G:T	S129R	0.994
5:102291577:T:G	S129R	0.994
5:102291591:C:T	G124D	0.994
5:102291592:C:G	G124R	0.994
5:102239297:G:C	C656W	0.993
5:102239298:C:G	C656S	0.993
5:102239299:A:T	C656S	0.993
5:102239361:C:T	G635D	0.993
5:102270708:C:A	G240W	0.993
5:102291508:C:G	D152H	0.993
5:102239298:C:T	C656Y	0.992

dbSNP variants (sampled 300 via entrez): RS1000000499 (5:102290977 G>A,T), RS1000034686 (5:102247022 G>GCACA), RS1000105382 (5:102245445 G>A,C), RS1000116594 (5:102245671 T>A), RS1000159456 (5:102288596 T>C), RS1000214490 (5:102294878 T>G), RS1000279729 (5:102251943 T>C), RS1000298357 (5:102258031 G>A), RS1000309239 (5:102294561 T>C), RS1000314928 (5:102252143 G>A), RS1000329155 (5:102258343 G>A,C), RS1000388979 (5:102240119 C>T), RS1000547155 (5:102252218 A>G), RS1000555936 (5:102246766 T>G), RS1000628024 (5:102296870 T>C)

Disease associations

OMIM: gene MIM:609013 | 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
GCST010420_2	Pulse pressure x educational attainment (some college) interaction (2df)	2.000000e-08
GCST010420_3	Pulse pressure x educational attainment (some college) interaction (2df)	1.000000e-07

EFO canonical traits (2, from GWAS)

EFO ID	Trait name
EFO:0004784	self reported educational attainment
EFO:0005763	pulse pressure measurement

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL2073690 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

2 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 98,400 (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
CHEMBL1624	LEVOTHYROXINE	4	81,643
CHEMBL254219	DIGITOXIN	4	16,757

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

PharmGKB variants

1 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2600834	SLCO4C1		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

Target class: transporter — SLCO family of organic anion transporting polypeptides

ChEMBL bioactivities

3 potent at pChembl≥5 of 3 total, top 3 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.92	IC50	120	nM	DIGITOXIN
6.31	IC50	490	nM	DIGOXIGENIN
5.10	IC50	8000	nM	LEVOTHYROXINE

PubChem BioAssay actives

3 with measured affinity, of 7 total; 3 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
3-[(3S,5R,8R,9S,10S,13R,14S,17R)-3-[(2R,4S,5S,6R)-5-[(2S,4S,5S,6R)-5-[(2S,4S,5S,6R)-4,5-dihydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-4-hydroxy-6-methyloxan-2-yl]oxy-14-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one	679785: TP_TRANSPORTER: inhibition of Digoxin uptake in OATP4C1-expressing MDCK cells	ic50	0.1200	uM
3-[(3S,5R,8R,9S,10S,12R,13S,14S,17R)-3,12,14-trihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]-2H-furan-5-one	679785: TP_TRANSPORTER: inhibition of Digoxin uptake in OATP4C1-expressing MDCK cells	ic50	0.4900	uM
(2S)-2-amino-3-[4-(4-hydroxy-3,5-diiodophenoxy)-3,5-diiodophenyl]propanoic acid	679784: TP_TRANSPORTER: inhibition of Triiodothyronine uptake in OATP4C1-expressing MDCK cells	ic50	8.0000	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Valproic Acid	affects cotreatment, increases expression, affects expression	8
Benzo(a)pyrene	increases methylation, affects methylation, decreases expression	7
Aflatoxin B1	affects expression, decreases expression, increases methylation	5
trichostatin A	affects cotreatment, increases expression	3
Tetrachlorodibenzodioxin	decreases expression	3
Cyclosporine	decreases expression	3
triphenyl phosphate	affects expression, increases expression	2
perfluorooctane sulfonic acid	decreases expression	2
entinostat	increases expression, affects cotreatment	2
belinostat	increases expression, affects cotreatment	2
Vorinostat	affects cotreatment, increases expression	2
Panobinostat	increases expression, affects cotreatment	2
Nickel	decreases expression	2
Phenylmercuric Acetate	affects cotreatment, increases expression	2
Tobacco Smoke Pollution	decreases expression	2
Tretinoin	increases expression	2
p-Chloromercuribenzoic Acid	affects cotreatment, increases expression	2
aristolochic acid I	decreases expression	1
dicrotophos	decreases expression	1
methylmercuric chloride	decreases expression	1
dodecyldimethylamine oxide	increases expression	1
sulforaphane	increases expression	1
tris(1,3-dichloro-2-propyl)phosphate	affects expression	1
sodium arsenite	increases expression	1
butyraldehyde	increases expression	1
N,N-dimethylarginine	increases uptake	1
potassium chromate(VI)	increases expression	1
S-(1,2-dichlorovinyl)cysteine	affects response to substance, increases expression	1
mercuric bromide	affects cotreatment, increases expression	1
di-n-butylphosphoric acid	affects expression	1

ChEMBL screening assays

3 unique, capped per target: 3 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL2075763	Functional	TP_TRANSPORTER: inhibition of Triiodothyronine uptake in OATP4C1-expressing MDCK cells	Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. — Proc Natl Acad Sci U S A

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D4UU	HuH7-SLCO4C1-KO-c1	Cancer cell line	Male
CVCL_D4UV	HuH7-SLCO4C1-KO-c7	Cancer cell line	Male

Clinical trials (associated diseases)

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