SLCO1B3

Summary

SLCO1B3 (solute carrier organic anion transporter family member 1B3, HGNC:10961) is a protein-coding gene on chromosome 12p12.2, encoding Solute carrier organic anion transporter family member 1B3 (Q9NPD5). Mediates the Na(+)-independent uptake of organic anions.

This gene encodes a liver-specific member of the organic anion transporter family. The encoded protein is a transmembrane receptor that mediates the sodium-independent uptake of endogenous and xenobiotic compounds and plays a critical role in bile acid and bilirubin transport. Mutations in this gene are a cause of Rotor type hyperbilirubinemia. Alternative splicing of this gene and the use of alternative promoters results in transcript variants encoding different isoforms that differ in their tissue specificity.

Source: NCBI Gene 28234 — RefSeq curated summary.

At a glance

• Gene–disease (curated): Rotor syndrome (Supportive, GenCC)
• GWAS associations: 24
• Clinical variants (ClinVar): 314 total — 5 pathogenic, 3 likely-pathogenic
• Phenotypes (HPO): 13
• Druggable target: yes — 50 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_019844

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10961
Approved symbol	SLCO1B3
Name	solute carrier organic anion transporter family member 1B3
Location	12p12.2
Locus type	gene with protein product
Status	Approved
Aliases	OATP8, OATP1B3
Ensembl gene	ENSG00000111700
Ensembl biotype	protein_coding
OMIM	605495
Entrez	28234

Gene structure

Transcript identifiers

Ensembl transcripts: 8 — 7 protein_coding, 1 protein_coding_CDS_not_defined

ENST00000261196, ENST00000381545, ENST00000540853, ENST00000544370, ENST00000545880, ENST00000901222, ENST00000901223, ENST00000901224

RefSeq mRNA: 2 — MANE Select: NM_019844 NM_001349920, NM_019844

CCDS: CCDS8684

Canonical transcript exons

ENST00000381545 — 16 exons

Exon	Start	End
ENSE00002239266	20810705	20810764
ENSE00002278641	20813524	20813638
ENSE00003458389	20883418	20883602
ENSE00003485207	20855028	20855169
ENSE00003508411	20875235	20875477
ENSE00003536743	20880855	20881020
ENSE00003578877	20858439	20858571
ENSE00003581259	20815674	20815822
ENSE00003604741	20862412	20862558
ENSE00003632432	20901350	20901467
ENSE00003644318	20861017	20861138
ENSE00003659378	20898436	20898500
ENSE00003660970	20862756	20862854
ENSE00003672431	20879436	20879631
ENSE00003679007	20877772	20877936
ENSE00003902745	20916004	20916911

Expression profiles

Bgee: expression breadth ubiquitous, 106 present calls, max score 96.13.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 1.1559 / max 414.3456, expressed in 75 samples.

FANTOM5 promoters (4 alternative TSS)

Promoter ID	TPM avg	Samples expressed
124652	0.4311	11
124653	0.3823	10
124654	0.1805	52
124655	0.1619	49

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	96.13	gold quality
liver	UBERON:0002107	95.50	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	86.60	gold quality
olfactory segment of nasal mucosa	UBERON:0005386	76.97	gold quality
choroid plexus epithelium	UBERON:0003911	74.97	gold quality
primordial germ cell in gonad	CL:0000670 ∩ UBERON:0000991	73.80	gold quality
nasal cavity mucosa	UBERON:0001826	72.54	gold quality
nasal cavity epithelium	UBERON:0005384	71.36	gold quality
buccal mucosa cell	CL:0002336	66.95	silver quality
tibial nerve	UBERON:0001323	63.93	gold quality
cervix squamous epithelium	UBERON:0006922	63.64	gold quality
endocervix	UBERON:0000458	58.93	gold quality
gall bladder	UBERON:0002110	58.59	gold quality
decidua	UBERON:0002450	56.55	gold quality
sural nerve	UBERON:0015488	55.16	gold quality
minor salivary gland	UBERON:0001830	53.67	gold quality
pancreatic ductal cell	CL:0002079	53.18	silver quality
visceral pleura	UBERON:0002401	52.67	gold quality
hair follicle	UBERON:0002073	52.43	gold quality
cervix epithelium	UBERON:0004801	52.30	gold quality
epithelial cell of pancreas	CL:0000083	52.26	gold quality
mouth mucosa	UBERON:0003729	51.92	gold quality
oviduct epithelium	UBERON:0004804	51.33	gold quality
lower esophagus mucosa	UBERON:0035834	51.10	gold quality
saliva-secreting gland	UBERON:0001044	50.20	gold quality
Brodmann (1909) area 46	UBERON:0006483	49.30	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
olfactory bulb	UBERON:0002264	48.92	gold quality
myocardium	UBERON:0002349	48.87	gold quality
type B pancreatic cell	CL:0000169	48.83	gold quality

Single-cell (SCXA)

Detected in 3 experiment(s), a significant marker in 2.

Experiment	Marker?	Max mean expression
E-CURD-6	yes	189.01
E-MTAB-8495	yes	118.98
E-ANND-3	no	1.95

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): CEBPG, FOXA2, HNF1A, IRF6, NR1H4, RARA, STAT5A

miRNA regulators (miRDB)

41 targeting SLCO1B3, 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-6833-3P	100.00	70.63	3197
HSA-MIR-4768-5P	100.00	69.49	2861
HSA-MIR-656-3P	100.00	72.15	2788
HSA-MIR-5011-5P	100.00	83.46	5820
HSA-MIR-186-5P	99.99	70.83	3707
HSA-MIR-607	99.97	73.62	5593
HSA-MIR-548AN	99.97	70.91	2817
HSA-MIR-3910	99.95	71.13	2227
HSA-MIR-6809-3P	99.91	71.45	3814
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-374A-5P	99.90	71.34	2923
HSA-MIR-374B-5P	99.90	69.98	2734
HSA-MIR-3671	99.90	73.04	3897
HSA-MIR-4697-3P	99.89	67.09	1123
HSA-MIR-153-5P	99.89	73.86	6317
HSA-MIR-6780A-5P	99.88	66.69	2776
HSA-MIR-4659A-3P	99.80	72.62	4248
HSA-MIR-4659B-3P	99.80	72.62	4248
HSA-MIR-1273H-5P	99.77	66.32	2471
HSA-MIR-377-5P	99.70	65.28	712
HSA-MIR-30B-3P	99.70	65.76	2325
HSA-MIR-3689A-3P	99.70	65.73	2306
HSA-MIR-3689B-3P	99.70	65.71	2311
HSA-MIR-3689C	99.70	65.71	2311
HSA-MIR-6779-5P	99.70	65.76	2363
HSA-MIR-6086	99.70	65.38	699
HSA-MIR-10394-5P	99.65	66.83	1852
HSA-MIR-1205	99.65	66.76	1826
HSA-MIR-513C-5P	99.50	68.42	1730
HSA-MIR-514B-5P	99.50	68.19	1766

Literature-anchored findings (GeneRIF, showing 40)

• Human organic anion transporting polypeptide 8 promoter is transactivated by the farnesoid X receptor/bile acid receptor. (PMID:12055601)
• HNF3beta represses transcription of the OATP8 but not the OATP-C gene, providing a mechanism for reduced expression of OATP8 in hepatocellular carcinoma (PMID:14739090)
• The functional consequences of three polymorphisms and one artificial mutation include differences in the localization and in hepatocellular transport of several OATP1B3 proteins. (PMID:15226676)
• OATP1B3 play important roles in CDCA uptake into the liver. (PMID:16534140)
• the transcription of the LST-2 gene is regulated by three transcription factors, FXR, HNF1alpha, and HNF3beta. (PMID:16741617)
• although both OATP-C/1B1 and OATP8/1B3 are highly expressed, and able to transport bile acids, their mechanisms of action are different (PMID:16877380)
• these results indicate that OATP1B3/OATP-8 and OATP1B1/OATP-C most likely function as bidirectional facilitated diffusion transporters and that GSH is not a substrate or activator of their transport activity. (PMID:17412826)
• Bosentan uptake into Chinese hamster ovary cells expressing human OATP1B1 or OATP1B3, and was efficiently inhibited by cyclosporin A, rifampicin, and to a lesser extent by sildenafil. (PMID:17496208)
• LST-2 overexpression is associated with a hormone-dependent growth mechanism of the breast cancer (PMID:17760952)
• Performed transport assays in OATP1B3-expressing cells as a method of indentifying novel antineoplastic agents. (PMID:18082941)
• A set of double transfectants expressing OATP1B3 combined with OAT1B1 can be used as a tool for rapid identification of hepatic uptake and efflux transporters of many organic anions that are substrates of OATP1B1 or OATP1B3. (PMID:18180273)
• SNPs in and SLCO1B3 may predict the risk of leukopenia/neutropenia induced by docetaxel chemotherapy. (PMID:18294295)
• Alterations of OATP1BB3 function by oral antidiabetic drugs have to be considered as potential mechanisms underlying drug-drug interactions. (PMID:18314419)
• Pregnane X receptor ligands, by inhibiting or stimulating OATP1B3-mediated uptake, can lead to drug-drug interactions at the transporter level. (PMID:18321482)
• The common SLCO1B3 GG/AA haplotype is associated with impaired testosterone transport and improved survival in patients with prostatic cancer. (PMID:18519758)
• A polymorphism in a transporter, in SLCO1B3, that increases testosterone import is associated with a shorter time to androgen independence in patients with prostate cancer who are treated with ADT. (PMID:18537956)
• identificaction of three amino acid residues (Y537, S545, and T550) in TM10 of organic anion transporting polypeptide 1B3 that are important for cholecystokinin octapeptide transport. (PMID:18690707)
• SLCO1B3 polymorphism significantly influences plasma mycophenolic acid glucuronide pharmacokinetics in Japanese renal transplant recipients. (PMID:18695635)
• OATP1B3 overexpression in colorectal cancer cells may provide a survival advantage by altering p53-dependent pathways. (PMID:19074900)
• The insert-variant allele of the SLCO1B3 gene may increase the concentration-to-dose ratio of digoxin in hemodialysis patients. (PMID:19122334)
• SLC01B3 variants contribute to mild unconjugated hyperbilirubinemia. (PMID:19419973)
• In this review, organic anion transporting polypeptide (OATP)1B3 is an uptake transporter specifically expressed in the liver, and is considered important for drugs, particularly as its pharmacological target organ is the liver. (PMID:19442037)
• Antiretroviral protease inhibitors, but not non-nucleoside reverse transcriptase inhibitors, are substrates for OATP1A2, OATP1B1 and OATP1B3. (PMID:20051929)
• DNA methylation-dependent gene silencing is at least partly involved in the regulation of OATP1B3 expression in cancer/immortalized cell lines. (PMID:20130966)
• Is present in high frequencies in the finnish population (PMID:20560925)
• OATP1B3 is one of the transporters contributing to the supply of the estrogen precursor estrone-3-sulfate to estrogen-dependent breast cancer cells. (PMID:20615467)
• data suggest that among the many known transporters common variations of PXR, SLCO1A2, SLCO1B1, SLCO1B3, and SLCO2B1 do not contribute to breast carcinogenesis (PMID:20635135)
• Genetic variations of SLCO1B3 and UGT1A1 is associated serum bilirubin levels in Korean population. (PMID:20639394)
• Forty one nucleotide sequence variants leading to nine major haplotypes in the SLCO1B3 were identified in caucasian Canadians. (PMID:20877131)
• These results suggested that the SLCO1B3 334T>G polymorphism could have a significant impact on the intracellular concentration of imatinib in leukocytes as a promising biomarker for personalized treatment of chronic myeloid leukemia patients. (PMID:21212528)
• Data indicate that hydroxyurea transport and cellular uptake by OATP1B3 is time- and temperature-dependent. (PMID:21256917)
• Six SLCO genes were highly expressed in castration resistane prostate cancer metastases versus untreated prostate cancer, including SLCO1B3 and SLCO2B. (PMID:21266523)
• OATP1B3 polymorphisms that result in altered expression, substrate specificity, and pH-dependent activity may be of potential relevance to hepatic clearance of substrate drugs in vivo. (PMID:21278621)
• Genetic variants of SLCO1B3 may function as pharmacogenomic determinants of resistance to androgen deprivation therapy in prostate cancer. (PMID:21606417)
• SLCO1B3 expression, rather than CTNNB1 mutation, is the critical determinant of intratumoral cholestasis. (PMID:21615622)
• immunohistochemical expression of OATP8 significantly decreases during multistep hepatocarcinogenesis (PMID:21626360)
• we studied a series of hepatocellular carcinomas from livers that underwent liver transplantation and correlated the expression of OATP 1B1/1B3 with morphological features (PMID:21691816)
• Data suggest OATP1B1 and OATP1B3 are high-affinity paclitaxel transporters expressed in ovarian cancer cell lines and tumor tissues (or when expressed as recombinant proteins in Xenopus laevis oocytes). (PMID:21719246)
• This study demonstrated that plated primary human hepatocytes are useful as an in vitro model for OATP1B1/1B3-mediated uptake studies, but the culture time may substantially change the uptake kinetics. (PMID:21787759)
• Digoxin inhibited the uptake of probe substrates of OATP1B1 (IC(50) of 47 muM), OATP1B3 (IC(50) > 8.1 muM), and OATP2B1 (IC(50) > 300 muM), but not OATP1A2 in transfected cell lines. (PMID:21849517)

Cross-species orthologs

3 orthologs

Organism	Symbol	Gene ID
mus_musculus	Slco1b2	ENSMUSG00000030236
rattus_norvegicus	Slco1b2	ENSRNOG00000030538
drosophila_melanogaster	Oatp30B	FBGN0032123

Paralogs (10): SLCO1A2 (ENSG00000084453), SLCO4A1 (ENSG00000101187), SLCO1B1 (ENSG00000134538), SLCO2B1 (ENSG00000137491), SLCO5A1 (ENSG00000137571), SLCO1C1 (ENSG00000139155), SLCO4C1 (ENSG00000173930), SLCO2A1 (ENSG00000174640), SLCO3A1 (ENSG00000176463), SLCO6A1 (ENSG00000205359)

Protein

Protein identifiers

Solute carrier organic anion transporter family member 1B3 — Q9NPD5 (reviewed: Q9NPD5)

Alternative names: Liver-specific organic anion transporter 2, OATP1B3, Organic anion transporter 8, Organic anion-transporting polypeptide 8, Solute carrier family 21 member 8

All UniProt accessions (3): Q9NPD5, F5H8K0, H0YGG9

UniProt curated annotations — full annotation on UniProt →

Function. Mediates the Na(+)-independent uptake of organic anions. Shows broad substrate specificity, can transport both organic anions such as bile acid taurocholate (cholyltaurine) and conjugated steroids (17-beta-glucuronosyl estradiol, dehydroepiandrosterone sulfate (DHEAS), and estrone 3-sulfate), as well as eicosanoid leukotriene C4, prostaglandin E2 and L-thyroxine (T4). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions. Shows a pH-sensitive substrate specificity towards sulfated steroids, taurocholate and T4 which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment. Involved in the clearance of bile acids and organic anions from the liver. Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop. Transports coproporphyrin I and III, by-products of heme synthesis, and may be involved in their hepatic disposition. May contribute to regulate the transport of organic compounds in testes across the blood-testis-barrier. Can transport HMG-CoA reductase inhibitors (also known as statins) such as pitavastatin, a clinically important class of hypolipidemic drugs. May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel. May also transport antihypertension agents, such as the angiotensin-converting enzyme (ACE) inhibitor prodrug enalapril, and the highly selective angiotensin II AT1-receptor antagonist valsartan, in the liver.

Subcellular location. Basolateral cell membrane. Basal cell membrane.

Tissue specificity. Highly expressed in liver, in particular at the basolateral membrane of hepatocytes near the central vein. Expressed in the placenta. In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and within the tubules.

Post-translational modifications. N-glycosylated.

Disease relevance. Hyperbilirubinemia, Rotor type (HBLRR) [MIM:237450] An autosomal recessive form of primary conjugated hyperbilirubinemia. Affected individuals develop mild jaundice not associated with hemolysis shortly after birth or in childhood. They have delayed plasma clearance of the unconjugated anionic dye bromsulphthalein and prominent urinary excretion of coproporphyrin I. Hepatic pigmentation is normal. The disease is caused by variants affecting the gene represented in this entry.

Domain organisation. A conserved histidine residue in the third TMD (His-115) may play an essential role in the pH sensitivity of SLCO1B3/OATP1B3-mediated substrate transport.

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

Isoforms (3)

UniProt ID	Names	Canonical?
Q9NPD5-1	SLCO1B3-1	yes
Q9NPD5-2	SLCO1B3-2
F5H094-1	SLCO1B3-SLCO1B7-1

RefSeq proteins (2): NP_001336849, NP_062818* (*=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), 10 shown:

• prostaglandin E2(out) = prostaglandin E2(in) (RHEA:50984)
• taurocholate(out) = taurocholate(in) (RHEA:71703)
• L-thyroxine(out) = L-thyroxine(in) (RHEA:71819)
• estrone 3-sulfate(out) = estrone 3-sulfate(in) (RHEA:71835)
• dehydroepiandrosterone 3-sulfate(out) = dehydroepiandrosterone 3-sulfate(in) (RHEA:71839)
• 17beta-estradiol 17-O-(beta-D-glucuronate)(out) = 17beta-estradiol 17-O-(beta-D-glucuronate)(in) (RHEA:72691)
• leukotriene C4(out) = leukotriene C4(in) (RHEA:72743)
• (4E,15E)-bilirubin IXalpha C8-beta-D-glucuronoside(out) = (4E,15E)-bilirubin IXalpha C8-beta-D-glucuronoside(in) (RHEA:72791)
• bilirubin IXalpha bis-beta-D-glucuronoside(out) = bilirubin IXalpha bis-beta-D-glucuronoside(in) (RHEA:72795)
• estrone 3-sulfate(out) + hydrogencarbonate(in) = estrone 3-sulfate(in) + hydrogencarbonate(out) (RHEA:73055)

UniProt features (81 total): helix 24, topological domain 13, transmembrane region 12, strand 7, glycosylation site 6, sequence variant 6, modified residue 3, disulfide bond 3, splice variant 3, turn 2, chain 1, domain 1

Structure

Experimental structures (PDB)

1 structures.

PDB	Method	Resolution (Å)
8PG0	ELECTRON MICROSCOPY	2.97

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9NPD5-F1	79.20	0.48

Antibody-complex structures (SAbDab): 1 — 8PG0

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 (3): 293, 295, 683

Disulfide bonds (3): 459–489, 465–485, 474–506

Glycosylation sites (6): 134, 145, 151, 445, 503, 516

Function

Pathways and Gene Ontology

Reactome pathways

17 pathways

ID	Pathway
R-HSA-159418	Recycling of bile acids and salts
R-HSA-189483	Heme degradation
R-HSA-5619058	Defective SLCO1B3 causes hyperbilirubinemia, Rotor type (HBLRR)
R-HSA-879518	Organic anion transport by SLCO transporters
R-HSA-9754706	Atorvastatin ADME
R-HSA-1430728	Metabolism
R-HSA-1643685	Disease
R-HSA-189445	Metabolism of porphyrins
R-HSA-194068	Bile acid and bile salt metabolism
R-HSA-382551	Transport of small molecules
R-HSA-425397	Transport of vitamins, nucleosides, and related molecules
R-HSA-425407	SLC-mediated transmembrane transport
R-HSA-556833	Metabolism of lipids
R-HSA-5619102	SLC transporter disorders
R-HSA-5619115	Disorders of transmembrane transporters
R-HSA-8957322	Metabolism of steroids
R-HSA-9748784	Drug ADME

MSigDB gene sets: 129 (showing top): GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, REACTOME_METABOLISM_OF_PORPHYRINS, GOBP_ORGANIC_ACID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_PORPHYRIN_CONTAINING_COMPOUND_METABOLIC_PROCESS, CAIRO_HEPATOBLASTOMA_CLASSES_DN, FISCHER_G2_M_CELL_CYCLE, GOBP_TETRAPYRROLE_METABOLIC_PROCESS, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_PIGMENT_METABOLIC_PROCESS, GOBP_BILE_ACID_AND_BILE_SALT_TRANSPORT, NAKAMURA_TUMOR_ZONE_PERIPHERAL_VS_CENTRAL_DN, GOBP_MONOCARBOXYLIC_ACID_TRANSPORT, HAN_SATB1_TARGETS_DN, GOBP_LIPID_LOCALIZATION

GO Biological Process (8): xenobiotic metabolic process (GO:0006805), monoatomic ion transport (GO:0006811), obsolete organic anion transport (GO:0015711), bile acid and bile salt transport (GO:0015721), heme catabolic process (GO:0042167), sodium-independent organic anion transport (GO:0043252), lipid transport (GO:0006869), transmembrane transport (GO:0055085)

GO Molecular Function (7): serine-type endopeptidase inhibitor activity (GO:0004867), obsolete organic anion transmembrane transporter activity (GO:0008514), bile acid transmembrane transporter activity (GO:0015125), obsolete sodium-independent organic anion transmembrane transporter activity (GO:0015347), protein binding (GO:0005515), transmembrane transporter activity (GO:0022857), peptidase inhibitor activity (GO:0030414)

GO Cellular Component (4): plasma membrane (GO:0005886), basal plasma membrane (GO:0009925), basolateral plasma membrane (GO:0016323), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-12 pathways:

Category	Pathways
Metabolism	2
Bile acid and bile salt metabolism	1
Metabolism of porphyrins	1
SLC transporter disorders	1
SLC-mediated transport of organic anions	1
Drug ADME	1
Metabolism of steroids	1
SLC-mediated transmembrane transport	1
Transport of small molecules	1
Disorders of transmembrane transporters	1
Disease	1
Metabolism of lipids	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
transport	3
transmembrane transport	2
plasma membrane region	2
metabolic process	1
cellular response to xenobiotic stimulus	1
lipid transport	1
monocarboxylic acid transport	1
organic hydroxy compound transport	1
porphyrin-containing compound catabolic process	1
heme metabolic process	1
pigment catabolic process	1
lipid localization	1
cellular process	1
serine-type endopeptidase activity	1
endopeptidase inhibitor activity	1
bile acid and bile salt transport	1
carboxylic acid transmembrane transporter activity	1
lipid transmembrane transporter activity	1
binding	1
transporter activity	1
enzyme inhibitor activity	1
peptidase activity	1
peptidase regulator activity	1
membrane	1
cell periphery	1
basal part of cell	1
basal plasma membrane	1
cellular anatomical structure	1

Protein interactions and networks

STRING

876 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO1B3	SLC22A7	Q9Y694	958
SLCO1B3	UGT1A1	P22309	870
SLCO1B3	SLC22A8	Q8TCC7	845
SLCO1B3	ABCB1	P08183	836
SLCO1B3	SLC10A1	Q14973	812
SLCO1B3	ABCC2	Q92887	801
SLCO1B3	NR1I2	O75469	798
SLCO1B3	ABCG2	Q9UNQ0	790
SLCO1B3	ABCB11	O95342	779
SLCO1B3	SLC47A2	Q86VL8	764
SLCO1B3	SLC47A1	Q96FL8	763
SLCO1B3	BLVRA	P53004	735
SLCO1B3	CYP3A4	P05184	728
SLCO1B3	SLC22A1	O15245	727
SLCO1B3	ABCC3	O15438	724

IntAct

4 interactions, top by confidence:

A	B	Type	Score
SLCO1B3	LGALS3	psi-mi:“MI:0914”(association)	0.530
SLCO1B1	CLGN	psi-mi:“MI:0914”(association)	0.350
SLCO1B3	SNAP23	psi-mi:“MI:0914”(association)	0.350

BioGRID (116): SLCO1B3 (Affinity Capture-MS), SLCO1B3 (Reconstituted Complex), DYM (Affinity Capture-MS), ACTA2 (Affinity Capture-MS), SLCO1B1 (Affinity Capture-MS), ADCK1 (Affinity Capture-MS), GK (Affinity Capture-MS), FNDC3B (Affinity Capture-MS), LGALS3 (Affinity Capture-MS), SLCO1B3 (Affinity Capture-MS), ABCB1 (Affinity Capture-MS), ACBD3 (Affinity Capture-MS), ARFGAP1 (Affinity Capture-MS), ATP11B (Affinity Capture-MS), ATP11C (Affinity Capture-MS)

ESM2 similar proteins: A0A084AFH0, A0A125YQS6, A0A286LF00, A1Z7R6, A2AJQ3, A4IHK6, A9JTG4, B2RYH9, B8NCQ3, B8NM75, C8V3Y8, F5H094, G4SDH4, O60706, O74901, O74902, O74921, O75387, P0DPB1, P34711, P38318, P46996, P47159, P59845, P70170, P81721, P82451, P9WEL1, P9WEL2, Q08C75, Q12519, Q3EAQ5, Q5BIZ0, Q5F4B8, Q5ZJZ4, Q63563, Q7SXB7, Q8BSM7, Q8CA03, Q8CF82

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

5 interactions.

A	Effect	B	Mechanism
FOXA2	“down-regulates quantity by repression”	SLCO1B3	“transcriptional regulation”
CEBPG	“up-regulates quantity by expression”	SLCO1B3	“transcriptional regulation”
HNF1A	“up-regulates quantity by expression”	SLCO1B3	“transcriptional regulation”
RARA	“up-regulates quantity by expression”	SLCO1B3	“transcriptional regulation”
STAT5A	“up-regulates quantity by expression”	SLCO1B3	“transcriptional regulation”

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	3
Uncertain significance	180
Likely benign	44
Benign	52

Top pathogenic / likely-pathogenic (8)

Variant ID	HGVS	Classification
1330928	NM_019844.4(SLCO1B3):c.1637dup (p.Leu546fs)	Pathogenic
30487	SLCO1B3, 7.2-KB DEL	Pathogenic
30488	NM_019844.4(SLCO1B3):c.1747+1G>A	Pathogenic
632183	NM_019844.4(SLCO1B3):c.971-2A>G	Pathogenic
977762	NC_000012.11:g.21014093_21014094insLINE1	Pathogenic
1330934	NM_019844.4(SLCO1B3):c.1135+1G>A	Likely pathogenic
3374929	NM_019844.4(SLCO1B3):c.481+1G>C	Likely pathogenic
3766697	NM_019844.4(SLCO1B3):c.727+1_727+2delinsA	Likely pathogenic

SpliceAI

2706 predictions. Top by Δscore:

Variant	Effect	Δscore
12:20815670:ACAGG:A	acceptor_loss	1.0000
12:20815671:CAGG:C	acceptor_loss	1.0000
12:20815672:A:AG	acceptor_gain	1.0000
12:20815672:A:T	acceptor_loss	1.0000
12:20815672:AGGT:A	acceptor_gain	1.0000
12:20815673:G:A	acceptor_loss	1.0000
12:20815673:G:GA	acceptor_gain	1.0000
12:20815673:GGT:G	acceptor_gain	1.0000
12:20815673:GGTG:G	acceptor_gain	1.0000
12:20815818:TCAAG:T	donor_loss	1.0000
12:20815819:CAAG:C	donor_loss	1.0000
12:20815820:AAG:A	donor_loss	1.0000
12:20815821:AGGTA:A	donor_loss	1.0000
12:20815824:T:G	donor_loss	1.0000
12:20855155:G:GT	donor_gain	1.0000
12:20858532:G:GT	donor_gain	1.0000
12:20858532:G:T	donor_gain	1.0000
12:20858567:GGATA:G	donor_gain	1.0000
12:20858568:GATA:G	donor_gain	1.0000
12:20858568:GATAG:G	donor_gain	1.0000
12:20858572:G:GG	donor_gain	1.0000
12:20859273:G:GT	donor_gain	1.0000
12:20859273:G:T	donor_gain	1.0000
12:20859281:T:G	donor_gain	1.0000
12:20862853:GA:G	donor_gain	1.0000
12:20862855:G:GG	donor_gain	1.0000
12:20901344:TTGCA:T	acceptor_loss	1.0000
12:20901345:TGCA:T	acceptor_loss	1.0000
12:20901346:GCAG:G	acceptor_loss	1.0000
12:20901346:GCAGG:G	acceptor_loss	1.0000

AlphaMissense

4604 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:20875279:T:A	W258R	0.996
12:20875279:T:C	W258R	0.996
12:20875269:G:C	W254C	0.995
12:20875269:G:T	W254C	0.995
12:20875282:T:A	W259R	0.995
12:20875282:T:C	W259R	0.995
12:20877849:A:C	S350R	0.994
12:20877851:C:A	S350R	0.994
12:20877851:C:G	S350R	0.994
12:20880933:G:C	W470C	0.994
12:20880933:G:T	W470C	0.994
12:20880988:T:A	C489S	0.994
12:20880989:G:C	C489S	0.994
12:20855157:A:C	S72R	0.993
12:20855159:C:A	S72R	0.993
12:20855159:C:G	S72R	0.993
12:20875267:T:A	W254R	0.993
12:20875267:T:C	W254R	0.993
12:20901399:T:G	C599W	0.993
12:20858465:A:C	S85R	0.992
12:20858467:T:A	S85R	0.992
12:20858467:T:G	S85R	0.992
12:20862472:G:C	R181P	0.992
12:20901397:T:A	C599S	0.992
12:20901398:G:C	C599S	0.992
12:20862459:G:A	G177R	0.991
12:20862459:G:C	G177R	0.991
12:20862474:G:C	G182R	0.991
12:20880943:T:A	C474S	0.991
12:20880944:G:C	C474S	0.991

dbSNP variants (sampled 300 via entrez): RS1000005745 (12:20887145 G>T), RS1000025675 (12:20839891 T>C), RS1000034198 (12:20829282 T>G), RS1000045148 (12:20839672 A>G), RS1000103472 (12:20813099 T>C,G), RS1000108213 (12:20818504 G>A), RS1000126086 (12:20870321 G>A), RS1000175728 (12:20836594 G>A), RS1000260974 (12:20903911 C>A), RS1000276139 (12:20844537 C>T), RS1000281708 (12:20831608 T>C), RS1000352890 (12:20826241 T>A,C), RS1000367092 (12:20902506 T>A), RS1000389188 (12:20892787 A>C), RS1000391239 (12:20830642 C>T)

Disease associations

OMIM: gene MIM:605495 | disease phenotypes: MIM:237450, MIM:143500

GenCC curated gene-disease

Disease	Classification	Inheritance
Rotor syndrome	Supportive	Autosomal recessive

Mondo (2): Rotor syndrome (MONDO:0009379), Gilbert syndrome (MONDO:0007745)

Orphanet (2): Rotor syndrome (Orphanet:3111), NON RARE IN EUROPE: Gilbert syndrome (Orphanet:357)

HPO phenotypes

13 total (13 of 13 shown, HPO-id order):

HPO	Term
HP:0000924	Abnormality of the skeletal system
HP:0000952	Jaundice
HP:0000989	Pruritus
HP:0001000	Abnormality of skin pigmentation
HP:0001046	Intermittent jaundice
HP:0002904	Hyperbilirubinemia
HP:0002908	Conjugated hyperbilirubinemia
HP:0010473	Porphyrinuria
HP:0010984	Digenic inheritance
HP:0012379	Abnormal circulating enzyme concentration or activity
HP:0031137	Storage in hepatocytes
HP:0031811	Bilirubinuria
HP:0032106	Conjunctival icterus

GWAS associations

24 associations (top):

Study	Trait	p-value
GCST000175_11	Height	2.000000e-06
GCST000388_3	Bilirubin levels	3.000000e-14
GCST000730_4	Bilirubin levels	2.000000e-17
GCST001846_7	Bilirubin levels	7.000000e-19
GCST001846_8	Bilirubin levels	2.000000e-16
GCST001846_9	Bilirubin levels	5.000000e-13
GCST003628_1	Clozapine-induced agranulocytosis/granulocytopenia in treatment-resistant schizophrenia	2.000000e-08
GCST005980_5	Total bilirubin levels	8.000000e-106
GCST006190_49	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	2.000000e-18
GCST006190_72	Diastolic blood pressure x smoking status (ever vs never) interaction (2df test)	2.000000e-17
GCST006192_59	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	3.000000e-14
GCST006192_70	Systolic blood pressure x smoking status (ever vs never) interaction (2df test)	2.000000e-14
GCST006193_32	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	1.000000e-17
GCST006193_71	Diastolic blood pressure x smoking status (current vs non-current) interaction (2df test)	1.000000e-16
GCST006195_14	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	4.000000e-14
GCST006195_63	Systolic blood pressure x smoking status (current vs non-current) interaction (2df test)	7.000000e-14
GCST008817_5	Bilirubin levels	1.000000e-65
GCST010117_7	Bilirubin levels	5.000000e-08
GCST011037_2	Parkinson’s disease progression (cognitive)	7.000000e-07
GCST90011898_13	Alanine aminotransferase levels	7.000000e-13
GCST90013405_105	Liver enzyme levels (alanine transaminase)	3.000000e-20
GCST90013407_126	Liver enzyme levels (gamma-glutamyl transferase)	2.000000e-60
GCST90013663_6	Alanine aminotransferase levels	1.000000e-21
GCST90013664_32	Aspartate aminotransferase levels	2.000000e-12

EFO canonical traits (7, from GWAS)

EFO ID	Trait name
EFO:0004570	bilirubin measurement
EFO:0006336	diastolic blood pressure
EFO:0006527	smoking status measurement
EFO:0006335	systolic blood pressure
EFO:0008336	disease progression measurement
EFO:0004532	serum gamma-glutamyl transferase measurement
EFO:0004736	aspartate aminotransferase measurement

MeSH disease descriptors (1)

Descriptor	Name	Tree numbers
D005878	Gilbert Disease	C16.320.565.300.528; C18.452.648.300.528

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1743121 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

50 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,223,089 (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
CHEMBL1014	CANDESARTAN CILEXETIL	4	11,194
CHEMBL1017	TELMISARTAN	4	27,457
CHEMBL1136	TELITHROMYCIN	4	15,927
CHEMBL1144	PRAVASTATIN	4	70,953
CHEMBL1161	MOMETASONE FUROATE	4	25,884
CHEMBL1163	ATAZANAVIR	4	22,094
CHEMBL1200467	HYDROXYZINE PAMOATE	4	7,357
CHEMBL1200688	ERYTHROMYCIN ETHYLSUCCINATE	4	51,700
CHEMBL1200692	OLMESARTAN MEDOXOMIL	4	17,268
CHEMBL1200701	DICLOXACILLIN SODIUM	4	2,653
CHEMBL1293	BETA CAROTENE	4	94,544
CHEMBL1410	NONOXYNOL 9	4	14,701
CHEMBL159	VINBLASTINE	4	412,636
CHEMBL160	CYCLOSPORINE	4	168,247
CHEMBL163	RITONAVIR	4	53,773
CHEMBL1697717	CARBENOXOLONE SODIUM	4	4,870
CHEMBL1741	CLARITHROMYCIN	4	57,376
CHEMBL1751	DIGOXIN	4	67,342
CHEMBL191	LOSARTAN	4	88,932
CHEMBL2218877	ERYTHROMYCIN ESTOLATE	4	8,181
CHEMBL374478	RIFAMPIN	4
CHEMBL393220	ATORVASTATIN CALCIUM	4
CHEMBL421	SULFASALAZINE	4
CHEMBL428647	PACLITAXEL	4
CHEMBL437765	RIFAMYCIN	4
CHEMBL44657	ETOPOSIDE	4
CHEMBL457	GEMFIBROZIL	4
CHEMBL461101	ELTROMBOPAG	4
CHEMBL506247	TANNIC ACID	4
CHEMBL515	CHLORAMBUCIL	4

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

PharmGKB clinical annotations

14 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs11045585	Toxicity	3	docetaxel	Neoplasms
rs4149117	Toxicity	3	carboplatin;paclitaxel	Lung Neoplasms
rs4149117	Dosage,Toxicity	3	mycophenolate mofetil	Kidney Transplantation
rs4149117	Efficacy	3	sunitinib	Gastrointestinal Stromal Tumors
rs4149117	Efficacy	3	mycophenolic acid	Lung transplantation;Overall survival
rs4149117	Efficacy	3	mycophenolic acid	Chronic lung allograft dysfunction;Lung transplantation
rs4149117	Efficacy	3	mycophenolic acid	Lung transplantation;Transplant rejection
rs60140950	Metabolism/PK	3	telmisartan
rs7311358	Other	3	mycophenolate mofetil	Kidney Transplantation
rs7311358	Other	3	docetaxel
rs7311358	Toxicity	3	carboplatin;paclitaxel	Non-Small Cell Lung Carcinoma
rs7311358	Efficacy	3	mycophenolic acid	Lung transplantation;Overall survival
rs7311358	Efficacy	3	mycophenolic acid	Lung transplantation;Transplant rejection
rs7311358	Efficacy	3	mycophenolic acid	Chronic lung allograft dysfunction;Lung transplantation

PharmGKB variants

11 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs3834935	SLCO1B3		0.00	0
rs4149117	SLCO1B3	3	5.00	6	mycophenolate mofetil;sunitinib;carboplatin;paclitaxel;mycophenolic acid
rs4149118	SLCO1B3		0.00	0
rs7311358	SLCO1B3	3	2.50	6	mycophenolate mofetil;docetaxel;carboplatin;paclitaxel;mycophenolic acid
rs7977213	SLCO1B3		0.00	0
rs10841661	SLCO1B3		0.00	0
rs11045585	SLCO1B3	3	4.25	1	docetaxel
rs60140950	SLCO1B3	3	1.50	1	telmisartan
rs2053098	SLCO1B3		0.00	0
rs3764006	SLCO1B3		0.00	0
rs2417940	SLCO1B3		0.00	0

GtoPdb / IUPHAR curated pharmacology

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

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

Most potent curated ligand interactions (4 total), top 4:

Ligand	Action	Affinity	Parameter
sarsagenin	Inhibition	7.1	pKi
cyclosporin A	Inhibition	6.1	pIC50
sildenafil	Inhibition	6.1	pIC50
rifampicin	Inhibition	5.8	pIC50

Binding affinities (BindingDB)

8 measured of 9 human assays (9 total across all organisms); most potent 8 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
CHEMBL3138642	KI	680 nM
CHEMBL3039411	IC50	692 nM
CHEMBL3039293	IC50	724 nM
NSC_2909	KI	1200 nM
30-ethyl-33-[(E)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone	IC50	3100 nM	US-9090657: Compound and methods for its production
CHEMBL1436860	IC50	5130 nM
NSC_60719	KI	8500 nM
25,30-diethyl-33-[(E)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,27,28-nonamethyl-6,9,18-tris(2-methylpropyl)-3,21,24-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone	IC50	16000 nM	US-9090657: Compound and methods for its production

ChEMBL bioactivities

174 potent at pChembl≥5 of 208 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.85	EC50	1.4	nM	CHEMBL4636474
8.62	EC50	2.4	nM	CHEMBL4637446
8.52	EC50	3	nM	CHEMBL4633668
7.10	Ki	80	nM	SARSASAPOGENIN
6.98	IC50	104.7	nM	SARSASAPOGENIN
6.89	IC50	130	nM	CYCLOSPORINE
6.72	IC50	190	nM	CHEMBL3704745
6.66	IC50	220	nM	ALISPORIVIR
6.58	IC50	260	nM	PACLITAXEL
6.43	Ki	370	nM	ATAZANAVIR
6.40	IC50	400	nM	ATAZANAVIR
6.38	Ki	420	nM	NORSTICTIC ACID
6.38	Ki	420	nM	ENOXOLONE
6.36	Ki	440	nM	OLIGOMYCIN
6.28	Ki	530	nM	BUSSEIN
6.26	IC50	549.5	nM	NORSTICTIC ACID
6.26	IC50	549.5	nM	ENOXOLONE
6.25	Ki	560	nM	CHUKRASIN METHYL ETHER
6.25	Ki	560	nM	SCANDENIN
6.24	IC50	570	nM	BMS-986020
6.23	Ki	590	nM	LASALOCID A SODIUM
6.22	Ki	600	nM	UTILIN
6.20	IC50	631	nM	BMS-986020
6.17	Ki	680	nM	HEDERAGENIN
6.16	IC50	691.8	nM	BUSSEIN
6.14	IC50	724.4	nM	CHUKRASIN METHYL ETHER
6.13	IC50	741.3	nM	SCANDENIN
6.12	Ki	750	nM	OLMESARTAN MEDOXOMIL
6.11	IC50	776.2	nM	UTILIN
6.11	IC50	776.2	nM	LASALOCID A SODIUM
6.10	IC50	788	nM	CHEMBL6150561
6.09	Ki	820	nM	ARACHIDONIC ACID
6.06	Ki	870	nM	MOMETASONE FUROATE
6.06	IC50	880	nM	CHEMBL3344501
6.05	IC50	891.2	nM	HEDERAGENIN
6.05	Ki	890	nM	LOSARTAN
6.03	Ki	940	nM	HYDROXYZINE PAMOATE
6.02	Ki	960	nM	TELMISARTAN
6.01	IC50	977.2	nM	OLMESARTAN MEDOXOMIL
5.99	Ki	1030	nM	DIOSCIN
5.97	IC50	1072	nM	ARACHIDONIC ACID
5.97	Ki	1080	nM	CHEMBL3138689
5.94	IC50	1148	nM	LOSARTAN
5.94	IC50	1148	nM	MOMETASONE FUROATE
5.92	Ki	1200	nM	CYCLOSPORINE
5.91	IC50	1230	nM	HYDROXYZINE PAMOATE
5.90	IC50	1259	nM	TELMISARTAN
5.90	Ki	1250	nM	LOBARIC ACID
5.89	IC50	1300	nM	CYCLOSPORINE
5.85	Ki	1400	nM	RIFAMPIN

PubChem BioAssay actives

162 with measured affinity, of 2500 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
(5R,8S,11R,12S,15S,18S,19S,22R)-15-[3-(diaminomethylideneamino)propyl]-8-[[4-[[1-(7-hydroxy-2-oxochromen-3-yl)triazol-4-yl]methoxy]phenyl]methyl]-18-[(1E,3E,5S,6S)-6-methoxy-3,5-dimethyl-7-phenylhepta-1,3-dienyl]-1,5,12,19-tetramethyl-2-methylidene-3,6,9,13,16,20,25-heptaoxo-1,4,7,10,14,17,21-heptazacyclopentacosane-11,22-dicarboxylic acid	1660550: Substrate activity at OATP1B3 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0014	uM
(5R,8S,11R,12S,15S,18S,19S,22R)-15-[3-(diaminomethylideneamino)propyl]-18-[(1E,3E,5S,6S)-6-methoxy-3,5-dimethyl-7-phenylhepta-1,3-dienyl]-1,5,12,19-tetramethyl-2-methylidene-3,6,9,13,16,20,25-heptaoxo-8-[(4-prop-2-ynoxyphenyl)methyl]-1,4,7,10,14,17,21-heptazacyclopentacosane-11,22-dicarboxylic acid	1660550: Substrate activity at OATP1B3 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0024	uM
(5R,8S,11R,12S,15S,18S,19S,22R)-15-[3-(diaminomethylideneamino)propyl]-8-[(4-hydroxyphenyl)methyl]-18-[(1E,3E,5S,6S)-6-methoxy-3,5-dimethyl-7-phenylhepta-1,3-dienyl]-1,5,12,19-tetramethyl-2-methylidene-3,6,9,13,16,20,25-heptaoxo-1,4,7,10,14,17,21-heptazacyclopentacosane-11,22-dicarboxylic acid	1660550: Substrate activity at OATP1B3 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0030	uM
(1R,2S,4S,5’S,6R,7S,8R,9S,12S,13S,16S,18R)-5’,7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icosane-6,2’-oxane]-16-ol	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.0800	uM
(3S,6S,9S,12R,15S,18S,21S,24S,27R,30S,33S)-25,30-diethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-1,4,7,10,12,15,19,27,28-nonamethyl-6,9,18-tris(2-methylpropyl)-3,21,24-tri(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone	1168842: Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	ic50	0.2200	uM
Paclitaxel	1197747: Inhibition of human OATP1B3-mediated [3H]CCK-8 after 5 mins by Dixon plot method	ic50	0.2600	uM
Atazanavir	699543: Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	ki	0.3700	uM
(2S,4aS,6aR,6aS,6bR,8aR,10S,12aS,14bR)-10-hydroxy-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-3,4,5,6,6a,7,8,8a,10,11,12,14b-dodecahydro-1H-picene-2-carboxylic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.4200	uM
5,13,17-trihydroxy-7,12-dimethyl-9,15-dioxo-2,10,16-trioxatetracyclo[9.7.0.03,8.014,18]octadeca-1(11),3(8),4,6,12,14(18)-hexaene-4-carbaldehyde	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.4200	uM
(1R,4E,5’S,6S,6’S,7R,8S,10R,11R,12S,14R,15S,16R,18E,20E,22R,25S,27R,28S,29R)-22-ethyl-7,11,14,15-tetrahydroxy-6’-[(2R)-2-hydroxypropyl]-5’,6,8,10,12,14,16,28,29-nonamethylspiro[2,26-dioxabicyclo[23.3.1]nonacosa-4,18,20-triene-27,2’-oxane]-3,9,13-trione	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.4400	uM
[(1R,3Z,6S,7R,9R,10R,15R,16S,19S,20R)-8,9,20-triacetyloxy-6-(furan-3-yl)-19-hydroxy-3-(1-hydroxy-2-methylpropylidene)-16-(2-methoxy-2-oxoethyl)-7,12,15,17-tetramethyl-4-oxo-5,11,13,21-tetraoxaheptacyclo[10.8.1.114,17.01,10.02,7.010,15.014,19]docosan-18-yl] 2-methylpropanoate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.5300	uM
4-hydroxy-3-(4-hydroxyphenyl)-5-methoxy-8,8-dimethyl-6-(3-methylbut-2-enyl)pyrano[2,3-h]chromen-2-one	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.5600	uM
[(1R,3Z,6S,7R,9R,10R,15R,16S,19S,20S)-18-acetyloxy-6-(furan-3-yl)-9,19,20-trimethoxy-3-(1-methoxy-2-methylpropylidene)-16-(2-methoxy-2-oxoethyl)-7,12,15,17-tetramethyl-4-oxo-5,11,13,21-tetraoxaheptacyclo[10.8.1.114,17.01,10.02,7.010,15.014,19]docosan-8-yl] 2-methylpropanoate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.5600	uM
1-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	1813452: Inhibition of OATP1B3 (unknown origin)	ic50	0.5700	uM
Lasalocid Sodium	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.5900	uM
[(1R,2R,7S,8R,9S,17S,18S,20R,22S)-8-acetyloxy-17-(furan-3-yl)-3,7-dihydroxy-22-(2-methoxy-2-oxoethyl)-2,5,11,18-tetramethyl-20-(2-methylbutanoyloxy)-15-oxo-10,12,16,21-tetraoxaheptacyclo[9.9.1.12,5.01,9.03,7.09,13.013,18]docosan-6-yl] 2,3-dimethyloxirane-2-carboxylate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.6000	uM
(4aS,6aR,6aS,6bR,8aR,9R,10S,12aR,14bS)-10-hydroxy-9-(hydroxymethyl)-2,2,6a,6b,9,12a-hexamethyl-1,3,4,5,6,6a,7,8,8a,10,11,12,13,14b-tetradecahydropicene-4a-carboxylic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.6800	uM
Olmesartan Medoxomil	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.7500	uM
(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.8200	uM
Mometasone Furoate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.8700	uM
(3S,6S,9S,12R,15S,18S,21S,24S,27R,30S,33S)-30-ethyl-33-[(E,1R,2R)-1-hydroxy-2-methylhex-4-enyl]-24-[(2S)-1-[4-(2-methoxyethyl)piperazin-1-yl]propan-2-yl]-1,4,7,10,12,15,19,25,27,28-decamethyl-6,9,18-tris(2-methylpropyl)-3,21-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,32-undecone	1168842: Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	ic50	0.8800	uM
Losartan	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.8900	uM
Hydroxyzine Pamoate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.9400	uM
Telmisartan	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	0.9600	uM
(2S,3R,4R,5R,6S)-2-[(2R,3S,4S,5R,6R)-4-hydroxy-2-(hydroxymethyl)-6-[(1S,2S,4S,5’R,6R,7S,8R,9S,12S,13R,16S)-5’,7,9,13-tetramethylspiro[5-oxapentacyclo[10.8.0.02,9.04,8.013,18]icos-18-ene-6,2’-oxane]-16-yl]oxy-5-[(2S,3R,4R,5R,6S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxyoxan-3-yl]oxy-6-methyloxane-3,4,5-triol	1215886: Cellular uptake in HEK293 cells expressing OATP1B3 (unknown origin) assessed as inhibition of telmisartan-mediated drug transport	ki	1.0300	uM
[(1S,4bS,5R,6aS,8R,10aR,10bS,12aS)-5-acetyloxy-1-(furan-3-yl)-4b,7,7,10a,12a-pentamethyl-3-oxo-1,5,6,6a,8,9,10,10b,11,12-decahydronaphtho[2,1-f]isochromen-8-yl] acetate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.0800	uM
cyclosporine	699543: Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	ki	1.2000	uM
3-hydroxy-9-methoxy-6-oxo-7-pentanoyl-1-pentylbenzo[b][1,4]benzodioxepine-2-carboxylic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.2500	uM
rifampin	699543: Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	ki	1.4000	uM
disodium;(2S,4aS,6aR,6aS,6bR,8aR,10S,12aS,14bR)-10-(3-carboxylatopropanoyloxy)-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-3,4,5,6,6a,7,8,8a,10,11,12,14b-dodecahydro-1H-picene-2-carboxylate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.4800	uM
sodium;(2S,5R,6R)-6-[[3-(2,6-dichlorophenyl)-5-methyl-1,2-oxazole-4-carbonyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate;hydrate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.5500	uM
erythromycin ethylsuccinate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.6100	uM
(4R)-4-[(E)-3-carboxybut-2-enyl]-14-hydroxy-6,6,18-trimethyl-21-(3-methylbut-2-enyl)-18-(4-methylpent-3-enyl)-12-oxo-2,5,19-trioxapentacyclo[11.8.0.03,7.03,11.015,20]henicosa-1(13),10,14,16,20-pentaene-4-carboxylic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.7300	uM
4-[12,18-dihydroxy-8,21,21-trimethyl-5-(3-methylbutyl)-8-(4-methylpentyl)-14-oxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11-tetraen-19-yl]-2-methylbutanoic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.7700	uM
methyl 8,10-dichloro-3,9-dihydroxy-1,4,7-trimethyl-6-oxobenzo[b][1,4]benzodioxepine-2-carboxylate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.8400	uM
Candesartan Cilexetil	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	1.9000	uM
methyl 8,10-dichloro-9-hydroxy-3-methoxy-1,7-dimethyl-6-oxobenzo[b][1,4]benzodioxepine-2-carboxylate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.0200	uM
(Z)-4-[(1S,2S,8R,17S,19S)-12,18-dihydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14-oxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11-tetraen-19-yl]-2-methylbut-2-enoic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.1600	uM
(Z)-4-[12,18-dihydroxy-8,21,21-trimethyl-5-(3-methylbut-2-enyl)-8-(4-methylpent-3-enyl)-14-oxo-3,7,20-trioxahexacyclo[15.4.1.02,15.02,19.04,13.06,11]docosa-4(13),5,9,11,15-pentaen-19-yl]-2-methylbut-2-enoic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.2400	uM
1,3,3-trimethyl-2-[(1E,3E,5E,7E,9E,11E,13E,15E,17E)-3,7,12,16-tetramethyl-18-(2,6,6-trimethylcyclohexen-1-yl)octadeca-1,3,5,7,9,11,13,15,17-nonaenyl]cyclohexene	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.2600	uM
[(1R,2R,4S,7R,8R,11R,12S,13S,15R,17S,19R)-13-acetyloxy-7-(furan-3-yl)-19-hydroxy-1,8,12,16,16-pentamethyl-5-oxo-3,6-dioxapentacyclo[9.8.0.02,4.02,8.012,17]nonadecan-15-yl] acetate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.2700	uM
[(2S,3R,4S,6R)-4-(dimethylamino)-2-[[(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-oxacyclotetradec-6-yl]oxy]-6-methyloxan-3-yl] propanoate;dodecyl hydrogen sulfate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.3500	uM
[(1R,4bR,5R,6aR,8S,10aS,10bR,12aR)-1-(furan-3-yl)-8-hydroxy-4b,7,7,10a,12a-pentamethyl-3-oxo-1,5,6,6a,8,9,10,10b,11,12-decahydronaphtho[2,1-f]isochromen-5-yl] acetate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.3900	uM
(1S,4bS,5R,6aS,10aS,10bS,12aS)-1-(furan-3-yl)-5-hydroxy-4b,7,7,10a,12a-pentamethyl-5,6,6a,9,10,10b,11,12-octahydro-1H-naphtho[2,1-f]isochromene-3,8-dione	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.5500	uM
atorvastatin calcium anhydrous	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.5800	uM
trans-(1S,3S)-3-[[6-[5-[[cyclobutylmethyl(methyl)carbamoyl]oxymethyl]-1-methyltriazol-4-yl]-2-methyl-3-pyridinyl]oxy]cyclohexane-1-carboxylic acid	1813452: Inhibition of OATP1B3 (unknown origin)	ic50	2.6000	uM
(2S,3S,4S,5R,6R)-6-[[(3S,4S,6aR,6bR,8R,8aR,9R,10R,14aR,14bS)-9-acetyloxy-8-hydroxy-4,8a-bis(hydroxymethyl)-6a,6b,11,11,14b-pentamethyl-10-[(E)-2-methylbut-2-enoyl]oxy-2,3,4,4a,5,6,7,8,9,10,12,12a,14,14a-tetradecahydro-1H-picen-3-yl]oxy]-4-hydroxy-3,5-bis[[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy]oxane-2-carboxylic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.6100	uM
3-[2-[[3-(2-carboxyethyl)-5-[(Z)-(3-ethenyl-4-methyl-5-oxopyrrol-2-ylidene)methyl]-4-methyl-1H-pyrrol-2-yl]methyl]-5-[(Z)-(4-ethenyl-3-methyl-5-oxopyrrol-2-ylidene)methyl]-4-methyl-1H-pyrrol-3-yl]propanoic acid	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.6300	uM
methyl (2S,3R,4R,5S)-4-[(1S,3aS,5R,6R,7R,7aR)-6-formyloxy-1-(furan-3-yl)-3a-hydroxy-7-[(2R,3R)-2-hydroxy-3-methylpentanoyl]oxy-7a-methyl-4-methylidene-3-oxo-2,5,6,7-tetrahydro-1H-inden-5-yl]-5-acetyloxy-2-(acetyloxymethyl)-2,4-dimethyl-7-oxooxepane-3-carboxylate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.6300	uM
[(1R,2R,4R,6S,7S,9R,11R)-6-(furan-3-yl)-17-hydroxy-1,7,11,15,15-pentamethyl-14,18-dioxo-3-oxapentacyclo[8.8.0.02,4.02,7.011,16]octadeca-12,16-dien-9-yl] acetate	977604: Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells	ki	2.6400	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
Rifampin	increases uptake, decreases activity, decreases expression, decreases reaction, increases import (+1 more)	11
Sulfobromophthalein	increases uptake, affects reaction, affects import, increases response to substance, decreases reaction (+1 more)	9
estradiol-17 beta-glucuronide	decreases reaction, increases import, increases uptake, affects cotreatment	6
Cyclosporine	increases uptake, decreases expression, increases expression, decreases reaction, increases import	6
cyanoginosin LR	decreases reaction, increases import, increases response to substance, increases uptake	4
Chenodeoxycholic Acid	increases expression, affects cotreatment, decreases expression, increases transport	4
Deoxycholic Acid	increases transport, increases uptake, increases expression, affects cotreatment, decreases expression	4
rifamycin SV	decreases reaction, increases import, increases uptake, decreases activity	3
Acetaminophen	decreases activity, decreases expression, affects cotreatment	3
Lithocholic Acid	increases expression, increases transport, increases uptake	3
Sincalide	decreases activity, decreases uptake, affects import, affects uptake	3
Taurocholic Acid	increases uptake, decreases reaction, increases response to substance	3
Tetrachlorodibenzodioxin	affects expression, affects cotreatment, increases expression, decreases expression	3
bisphenol F	increases reaction, increases uptake, decreases methylation	2
naringin	decreases reaction, increases import, increases uptake	2
estrone sulfate	decreases reaction, increases uptake	2
fexofenadine	increases uptake, affects cotreatment, decreases reaction	2
TAK-875	decreases activity, decreases reaction, increases transport	2
Rosuvastatin Calcium	decreases reaction, increases uptake	2
Atorvastatin	affects reaction, increases uptake, decreases reaction	2
Rosiglitazone	decreases reaction, increases uptake, decreases activity	2
Pioglitazone	increases uptake, decreases activity, affects reaction	2
Bile Acids and Salts	decreases reaction, increases transport, affects transport, affects uptake	2
Fusidic Acid	decreases reaction, increases uptake, decreases activity	2
Phalloidine	increases uptake	2
Quercetin	decreases reaction, increases import, increases uptake	2
Tobacco Smoke Pollution	decreases expression, decreases reaction, increases import	2
Ursodeoxycholic Acid	decreases reaction, increases uptake	2
Valproic Acid	decreases activity, decreases expression	2
Aflatoxin B1	affects expression, decreases expression, decreases methylation	2

ChEMBL screening assays

136 unique, capped per target: 79 admet, 30 binding, 27 functional

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1743146	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1B3	Membrane transporters in drug development. — Nat Rev Drug Discov
CHEMBL2075310	Functional	TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes	Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. — Hepatology
CHEMBL2154255	Binding	Transport mediated by human OATP1B3 stably transfected in butyrate treated dog MDCK2 cells at 10 uM after 3 hrs by scintillation counting	Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia. — J Med Chem

Cellosaurus cell lines

4 cell lines: 4 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B6AM	HepaRG OATP1B1/OATP1B3 KO	Cancer cell line	Female
CVCL_B6AN	HepaRG OATP1B3 KO	Cancer cell line	Female
CVCL_D4WF	LS180-SLCO1B3-KO-c10	Cancer cell line	Female
CVCL_D4WG	LS180-SLCO1B3-KO-c7	Cancer cell line	Female

Clinical trials (associated diseases)

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

Trial	Phase	Status	Title
NCT06336369	Not specified	RECRUITING	Brown Adipose Tissue Activity in Gilbert’s Syndrome