SLCO1B1

Summary

SLCO1B1 (solute carrier organic anion transporter family member 1B1, HGNC:10959) is a protein-coding gene on chromosome 12p12.1, encoding Solute carrier organic anion transporter family member 1B1 (Q9Y6L6). Mediates the Na(+)-independent uptake of organic anions. In precision oncology, SLCO1B1 N130D confers sensitivity to Methotrexate in Cancer (CIViC Level B); 1 further curated variant–drug associations are listed below.

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 numerous endogenous compounds including bilirubin, 17-beta-glucuronosyl estradiol and leukotriene C4. This protein is also involved in the removal of drug compounds such as statins, bromosulfophthalein and rifampin from the blood into the hepatocytes. Polymorphisms in the gene encoding this protein are associated with impaired transporter function.

Source: NCBI Gene 10599 — RefSeq curated summary.

At a glance

• Gene–disease (curated): Rotor syndrome (Supportive, GenCC)
• GWAS associations: 101
• Clinical variants (ClinVar): 219 total — 5 pathogenic, 6 likely-pathogenic
• Phenotypes (HPO): 13
• Druggable target: yes — 57 molecules with ChEMBL bioactivity
• Precision-oncology evidence (CIViC): 2 curated variant–drug associations
• MANE Select transcript: NM_006446

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10959
Approved symbol	SLCO1B1
Name	solute carrier organic anion transporter family member 1B1
Location	12p12.1
Locus type	gene with protein product
Status	Approved
Aliases	OATP-C, LST-1, OATP1B1
Ensembl gene	ENSG00000134538
Ensembl biotype	protein_coding
OMIM	604843
Entrez	10599

Gene structure

Transcript identifiers

Ensembl transcripts: 13 — 13 protein_coding

ENST00000256958, ENST00000870178, ENST00000870179, ENST00000870180, ENST00000870181, ENST00000870182, ENST00000870183, ENST00000870184, ENST00000870185, ENST00000870186, ENST00000870187, ENST00000870188, ENST00000870189

RefSeq mRNA: 1 — MANE Select: NM_006446 NM_006446

CCDS: CCDS8685

Canonical transcript exons

ENST00000256958 — 15 exons

Exon	Start	End
ENSE00000725757	21202491	21202686
ENSE00000725819	21222300	21222364
ENSE00000822217	21217119	21217303
ENSE00000822219	21224722	21224839
ENSE00000994887	21131194	21131236
ENSE00001646157	21174577	21174709
ENSE00001663597	21172650	21172791
ENSE00001669501	21178576	21178722
ENSE00001674207	21178922	21179020
ENSE00001699552	21176776	21176897
ENSE00001721182	21205868	21206033
ENSE00001756615	21200508	21200672
ENSE00001799830	21196946	21197188
ENSE00002290238	21238979	21239796
ENSE00003625019	21141514	21141658

Expression profiles

Bgee: expression breadth broad, 29 present calls, max score 96.66.

FANTOM5 (CAGE): breadth tissue_specific, TPM avg 0.8773 / max 275.0224, expressed in 9 samples.

FANTOM5 promoters (2 alternative TSS)

Promoter ID	TPM avg	Samples expressed
124658	0.8468	8
124657	0.0304	6

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	96.66	gold quality
liver	UBERON:0002107	95.91	gold quality
male germ line stem cell (sensu Vertebrata) in testis	CL:0000089 ∩ UBERON:0000473	81.36	gold quality
buccal mucosa cell	CL:0002336	65.80	silver quality
endometrium epithelium	UBERON:0004811	55.79	gold quality
pancreatic ductal cell	CL:0002079	54.29	silver quality
cranial nerve II	UBERON:0000941	53.05	silver quality
frontal pole	UBERON:0002795	50.41	gold quality
middle frontal gyrus	UBERON:0002702	50.30	gold quality
paraflocculus	UBERON:0005351	50.18	gold quality
Brodmann (1909) area 10	UBERON:0013541	50.18	gold quality
quadriceps femoris	UBERON:0001377	50.05	gold quality
deltoid	UBERON:0001476	49.61	gold quality
Brodmann (1909) area 46	UBERON:0006483	49.30	gold quality
blood vessel layer	UBERON:0004797	49.29	gold quality
cerebellar vermis	UBERON:0004720	49.25	gold quality
cervix squamous epithelium	UBERON:0006922	49.20	gold quality
hair follicle	UBERON:0002073	49.18	gold quality
vastus lateralis	UBERON:0001379	49.11	gold quality
olfactory bulb	UBERON:0002264	48.92	gold quality
choroid plexus epithelium	UBERON:0003911	48.89	gold quality
myocardium	UBERON:0002349	48.87	gold quality
type B pancreatic cell	CL:0000169	48.83	gold quality
oviduct epithelium	UBERON:0004804	48.62	gold quality
cardiac muscle of right atrium	UBERON:0003379	48.55	gold quality
CA1 field of hippocampus	UBERON:0003881	48.50	gold quality
cervix epithelium	UBERON:0004801	48.38	gold quality
left ventricle myocardium	UBERON:0006566	48.24	gold quality
orbitofrontal cortex	UBERON:0004167	48.20	gold quality
upper arm skin	UBERON:0004263	48.06	gold quality

Single-cell (SCXA)

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

Experiment	Marker?	Max mean expression
E-ANND-3	yes	3.92

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, ESR1, FOXA2, HNF1A, NR1H3, NR1H4, NR1I2, NR1I3

miRNA regulators (miRDB)

28 targeting SLCO1B1, 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-1277-5P	100.00	73.95	5056
HSA-MIR-8068	99.98	73.85	2376
HSA-MIR-4650-5P	99.98	64.69	999
HSA-MIR-4775	99.98	75.00	6394
HSA-MIR-590-3P	99.96	74.34	6478
HSA-MIR-3658	99.96	73.87	4379
HSA-MIR-1-3P	99.93	72.35	1914
HSA-MIR-206	99.93	72.50	1893
HSA-MIR-613	99.91	71.50	1710
HSA-MIR-4753-3P	99.90	71.03	3786
HSA-MIR-4799-5P	99.82	70.60	2663
HSA-MIR-6875-3P	99.82	70.26	2983
HSA-MIR-4699-3P	99.71	70.15	3142
HSA-MIR-379-3P	99.69	69.60	1524
HSA-MIR-411-3P	99.69	69.63	1524
HSA-MIR-4261	99.59	70.30	3415
HSA-MIR-2053	99.57	69.15	1635
HSA-MIR-6833-5P	99.50	68.93	1161
HSA-MIR-4672	99.50	71.58	2893
HSA-MIR-302A-5P	99.39	68.21	1913
HSA-MIR-194-5P	99.01	69.65	1465
HSA-MIR-4477A	98.83	69.75	2952
HSA-MIR-6895-3P	98.79	65.69	996
HSA-MIR-12125	98.59	67.54	1044
HSA-MIR-374C-3P	98.47	67.93	451
HSA-MIR-10395-3P	98.10	66.70	1726
HSA-MIR-12116	97.94	68.91	595
HSA-MIR-630	97.50	66.38	921

Literature-anchored findings (GeneRIF, showing 40)

• The promoter of SLC21A6 gene was characterized and regulated by HNF 1alpha. (PMID:11483603)
• Genetic polymorphisms: allele frequencies in the Japanese population and functional analysis (PMID:12130747)
• A naturally occurring mutation in the gene causes impaired membrane localization of the hepatocyte uptake transporter (PMID:12196548)
• human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation (PMID:12490595)
• a role for OATP2 in hepatocyte bilirubin transport is unlikely (PMID:12670950)
• commonly occurring single-nucleotide polymorphisms in OATP-C, such as T521C (Val174Ala), are likely to be associated with altered pharmacokinetics of pravastatin (PMID:12811365)
• In heterozygous carriers the pharmacokinetics of pravastatin were higher compared to non-carriers. (PMID:15226675)
• neonates who carry the 211 and 388 variants in the UGT1A1 and OATP 2 genes, respectively, as well as feed with breast milk are at high risk to develop severe hyperbilirubinemia. (PMID:15319464)
• Inhibition of OATP1B1 is an important mechanism for drug-induced unconjugated hyperbilirubinemia. (PMID:15535988)
• UGT1A1, OATP2 and G6PD genes have roles in genetic predisposition to unconjugated hyperbilirubinemia (PMID:15864125)
• Increased exposures of OATP1B1 substrates might be expected in individuals who have the poor transporter phenotype or are treated with an OATP1B1 inhibitor (PMID:16513443)
• single nucleotide polymorphisms has been proposed to cause functional alternations in OATP1B1 with shown consequences for the pharmacokinetics of drugs that are OATP1B1 substrates (PMID:16515396)
• OATP1B1 play an important roles in CDCA uptake into the liver. (PMID:16534140)
• SLCO1B1 haplotypes seem to play a role in basal cholesterol homeostasis. (PMID:16568260)
• Sequence variations of SLCO1B1 occur at high frequencies in the Caucasian population. (PMID:16758257)
• SLCO1B1 polymorphism does not affect the extent of induction of hepatic CYP3A4 by rifampicin. (PMID:16847425)
• SLCO1B1 polymorphism markedly affects the pharmacokinetics of active simvastatin acid, but has no significant effect on parent simvastatin. (PMID:17108811)
• 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)
• We found eight polymorphic variants that differed in genotypic and allelic frequencies between the Chinese, Malay and Indian populations. (PMID:17415554)
• The 521T–>C polymorphism of SLCO1B1 appears to modulate significantly the total cholesterol-lowering efficacy of pravastatin in Chinese patients with CHD. (PMID:17439540)
• Although the SLCO1B1 polymorphism was found to have a significant effect on the pharmacokinetics of pitavastatin, a nonsynonymous ABCG2 variant, 421C>A, did not appear to be associated with the altered pharmacokinetics of pitavastatin. (PMID:17460607)
• 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)
• Suggest a potential association between the OATP1B1 genetic polymorphisms and altered rosuvastatin pharmacokinetics in Korean populations. (PMID:17568401)
• cAMP-PKA regulation of OATPC membrane expression involves the Golgi complex. (PMID:17641954)
• HNF1alpha is an essential regulator of OATP1B1 mRNA expression and thus the level of HNF1alpha expression is one of the major determinants of interindividual variability in OATP1B1 mRNA expression. (PMID:17932728)
• Genetic polymorphism in SLCO1B1 is a major determinant of interindividual variability in the serum bilirubin level. (PMID:17973861)
• Data demonstrated that the frequent SLCO1B1 SNP c.1929A>C had no effect on the hepatic OATP1B1 protein expression and on the transport properties. (PMID:17989996)
• most common allele was SLCO1B1*1b, while SLCO1B1*5 was rare or abse (PMID:17996736)
• selective pressure may have acted on SLCO1B1 during human dispersal favoring low-activity variants in the north (PMID:18154446)
• Indicated genetic variation in SLCO1B1 in Japanese population. (PMID:18159134)
• 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)
• results demonstrate a high sequence variability of OATP1B1 within different popuations (PMID:18185926)
• SLCO1B1 polymorphism had no significant effect on the plasma pharmacokinetics or pharmacodynamics of nateglinide or its M7 metabolite. (PMID:18187595)
• Alterations of OATP1BB1 function by oral antidiabetic drugs have to be considered as potential mechanisms underlying drug-drug interactions. (PMID:18314419)
• Pregnane X receptor ligands, by inhibiting OATP1B1-mediated uptake, can lead to drug-drug interactions at the transporter level. (PMID:18321482)
• Substrate dependency in the consequences of the SLCO1B1*15 variant could modulate the effect of SLCO1B1 polymorphism on the disposition of pitavastatin and pravastatin. (PMID:18408565)
• OATP1B1-Ala174 displays decreased transport activity and thereby gives rise to higher bilirubin, estrone sulfate, and T4 sulfate levels in carriers of this polymorphism. (PMID:18499754)
• Pharmacokinetics of ezetimibe is influenced by OATP1B1 polymorphisms in healthy participants after single dose administration. (PMID:18551036)
• Eight nonsynonymous OATP1B1 gene variants were detected in children with hereditary hyperbilirubinemia; degree of genetic heterogeneity and variant coexpression across OATP1B1 gene points to polygenic nature of this disease. (PMID:18558634)
• SLCO1B1 polymorphism is associated with Pharmacokinetic interaction between pravastatin and olmesartan. (PMID:18641915)

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), SLCO1B3 (ENSG00000111700), SLCO2B1 (ENSG00000137491), SLCO5A1 (ENSG00000137571), SLCO1C1 (ENSG00000139155), SLCO4C1 (ENSG00000173930), SLCO2A1 (ENSG00000174640), SLCO3A1 (ENSG00000176463), SLCO6A1 (ENSG00000205359)

Protein

Protein identifiers

Solute carrier organic anion transporter family member 1B1 — Q9Y6L6 (reviewed: Q9Y6L6)

Alternative names: Liver-specific organic anion transporter 1, OATP-C, Organic anion transporter SLC21A6, Sodium-independent organic anion-transporting polypeptide 2, Solute carrier family 21 member 6

All UniProt accessions (1): Q9Y6L6

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 (dehydroepiandrosterone 3-sulfate, 17-beta-glucuronosyl estradiol, and estrone 3-sulfate), as well as eicosanoids (prostaglandin E2, thromboxane B2, leukotriene C4, and leukotriene E4), and thyroid hormones (T4/L-thyroxine, and T3/3,3’,5’-triiodo-L-thyronine). Can take up bilirubin glucuronides from plasma into the liver, contributing to the detoxification-enhancing liver-blood shuttling loop. Involved in the clearance of endogenous and exogenous substrates from the liver. 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 pravastatin and pitavastatin, a clinically important class of hypolipidemic drugs. May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drug methotrexate. 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. Shows a pH-sensitive substrate specificity towards prostaglandin E2 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. Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions.

Subcellular location. Basolateral cell membrane. Basal cell membrane.

Tissue specificity. Highly expressed in liver, at the basolateral membranes of centrilobular hepatocytes. Expressed in liver (at protein level). Expressed in fetal liver. Not detected in heart, brain, placenta, lung, skeletal muscle, kidney, pancreas, spleen, thymus, prostate, testis, ovary, small intestine, colon and leukocyte. In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed in Leydig cells and within the tubules.

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 SLCO1B1/OATP1B1-mediated substrate transport.

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

RefSeq proteins (1): NP_006437* (*=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), 12 shown:

• prostaglandin E2(out) = prostaglandin E2(in) (RHEA:50984)
• thromboxane B2(out) = thromboxane B2(in) (RHEA:50992)
• taurocholate(out) = taurocholate(in) (RHEA:71703)
• 3,3’,5’-triiodo-L-thyronine(out) = 3,3’,5’-triiodo-L-thyronine(in) (RHEA:71815)
• 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)
• leukotriene E4(out) = leukotriene E4(in) (RHEA:72747)
• (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)

UniProt features (108 total): helix 27, sequence variant 18, topological domain 13, transmembrane region 12, strand 12, turn 8, glycosylation site 6, modified residue 4, disulfide bond 3, mutagenesis site 3, chain 1, domain 1

Structure

Experimental structures (PDB)

9 structures.

PDB	Method	Resolution (Å)
8K6L	ELECTRON MICROSCOPY	2.92
9CY1	ELECTRON MICROSCOPY	3.15
8HND	ELECTRON MICROSCOPY	3.19
9CY3	ELECTRON MICROSCOPY	3.2
9CY4	ELECTRON MICROSCOPY	3.41
8HNB	ELECTRON MICROSCOPY	3.53
8PHW	ELECTRON MICROSCOPY	3.6
8HNC	ELECTRON MICROSCOPY	3.73
8HNH	ELECTRON MICROSCOPY	3.73

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-Q9Y6L6-F1	80.40	0.49

Antibody-complex structures (SAbDab): 4 — 8PHW, 9CY1, 9CY3, 9CY4

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 (4): 293, 295, 672, 682

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

Glycosylation sites (6): 130, 134, 432, 503, 516, 617

Mutagenesis-validated functional residues (3):

Position	Phenotype
367	decreased estradiol-17beta-d-glucuronide uptake.
625	decreased estradiol-17beta-d-glucuronide uptake.
645	decreased estradiol-17beta-d-glucuronide uptake.

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-5619110	Defective SLCO1B1 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: 126 (showing top): GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, REACTOME_METABOLISM_OF_PORPHYRINS, GOBP_REGULATION_OF_HORMONE_LEVELS, GOBP_HORMONE_TRANSPORT, HNF1_Q6, GOBP_ORGANIC_ACID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_PORPHYRIN_CONTAINING_COMPOUND_METABOLIC_PROCESS, CAIRO_HEPATOBLASTOMA_CLASSES_DN, GOBP_TETRAPYRROLE_METABOLIC_PROCESS, GOBP_ORGANIC_ANION_TRANSPORT, GOBP_PIGMENT_METABOLIC_PROCESS, GOBP_BILE_ACID_AND_BILE_SALT_TRANSPORT, MORF_EPHA7, GOBP_MONOCARBOXYLIC_ACID_TRANSPORT

GO Biological Process (10): 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), prostaglandin transport (GO:0015732), transmembrane transport (GO:0055085), thyroid hormone transport (GO:0070327)

GO Molecular Function (7): obsolete organic anion transmembrane transporter activity (GO:0008514), bile acid transmembrane transporter activity (GO:0015125), prostaglandin transmembrane transporter activity (GO:0015132), obsolete sodium-independent organic anion transmembrane transporter activity (GO:0015347), thyroid hormone transmembrane transporter activity (GO:0015349), protein binding (GO:0005515), transmembrane transporter activity (GO:0022857)

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

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
fatty acid transport	1
icosanoid transport	1
cellular process	1
hormone transport	1
bile acid and bile salt transport	1
carboxylic acid transmembrane transporter activity	1
lipid transmembrane transporter activity	1
prostaglandin transport	1
icosanoid transmembrane transporter activity	1
secondary active transmembrane transporter activity	1
thyroid hormone transport	1
binding	1
transporter activity	1
membrane	1
cell periphery	1
basal part of cell	1
cellular anatomical structure	1
basal plasma membrane	1

Protein interactions and networks

STRING

1216 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO1B1	SLC22A7	Q9Y694	958
SLCO1B1	CYP2C8	P10632	932
SLCO1B1	CYP3A4	P05184	924
SLCO1B1	UGT1A1	P22309	924
SLCO1B1	CYP2C9	P11712	911
SLCO1B1	ABCG2	Q9UNQ0	886
SLCO1B1	ABCB1	P08183	877
SLCO1B1	CYP2D6	P10635	853
SLCO1B1	NR1I2	O75469	840
SLCO1B1	SLC10A1	Q14973	831
SLCO1B1	ABCC2	Q92887	828
SLCO1B1	SLC22A8	Q8TCC7	827
SLCO1B1	ABCB11	O95342	800
SLCO1B1	UGT1A6	P19224	792
SLCO1B1	UGT1A4	P22310	792

IntAct

122 interactions, top by confidence:

A	B	Type	Score
SLCO1B1	SYNGR2	psi-mi:“MI:0914”(association)	0.530
SLCO1B3	LGALS3	psi-mi:“MI:0914”(association)	0.530
SLCO1B1	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	ARHGAP21	psi-mi:“MI:0407”(direct interaction)	0.440
PTPN3	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	APBA3	psi-mi:“MI:0407”(direct interaction)	0.440
MPP2	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	PDZRN4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	DLG1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	LNX1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	PATJ	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
PCLO	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	MPDZ	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	MAGI3	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	LNX2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
APBA2	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	HTRA2	psi-mi:“MI:0407”(direct interaction)	0.440
DLG3	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
PDZD7	SLCO1B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	GRID2IP	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	LRRC7	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO1B1	MPP7	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (42): USO1 (Affinity Capture-MS), VAMP3 (Affinity Capture-MS), MZT2B (Affinity Capture-MS), SYNGR2 (Affinity Capture-MS), ORMDL2 (Affinity Capture-MS), TUBB3 (Affinity Capture-MS), WAPAL (Affinity Capture-MS), DYM (Affinity Capture-MS), C20orf24 (Affinity Capture-MS), SLCO1B1 (Synthetic Lethality), METTL15 (Affinity Capture-MS), MPC2 (Affinity Capture-MS), ORMDL2 (Affinity Capture-MS), DNAAF5 (Affinity Capture-MS), VAMP3 (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

0 interactions.

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 78 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

Pathway	Partners	Fold	FDR
Ras activation upon Ca2+ influx through NMDA receptor	5	54.9×	1e-06
Unblocking of NMDA receptors, glutamate binding and activation	5	52.3×	1e-06
Negative regulation of NMDA receptor-mediated neuronal transmission	5	52.3×	1e-06
Long-term potentiation	5	45.8×	2e-06
Assembly and cell surface presentation of NMDA receptors	9	43.9×	4e-11
Neurexins and neuroligins	10	37.9×	2e-11
Protein-protein interactions at synapses	6	30.6×	1e-06
RHOB GTPase cycle	6	17.8×	3e-05

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	11	84.1×	1e-16
protein localization to synapse	6	60.5×	6e-08
receptor clustering	7	57.5×	6e-09
regulation of postsynaptic membrane neurotransmitter receptor levels	7	45.6×	2e-08
cell-cell adhesion	10	13.4×	3e-07
protein-containing complex assembly	8	12.0×	2e-05
chemical synaptic transmission	7	7.1×	2e-03
protein transport	8	4.6×	6e-03

Disease & clinical

Cancer significance

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	5
Likely pathogenic	6
Uncertain significance	120
Likely benign	20
Benign	52

Top pathogenic / likely-pathogenic (11)

Variant ID	HGVS	Classification
30437	NM_006446.5(SLCO1B1):c.1738C>T (p.Arg580Ter)	Pathogenic
30439	NM_006446.5(SLCO1B1):c.757C>T (p.Arg253Ter)	Pathogenic
4076017	GRCh37/hg19 12p12.2-12.1(chr12:21007732-21415496)x1	Pathogenic
4279252	GRCh37/hg19 12p12.2-12.1(chr12:21000551-21415634)x1	Pathogenic
915961	GRCh37/hg19 12p12.2-12.1(chr12:21017576-21404166)	Pathogenic
2506538	GRCh37/hg19 12p12.2-12.1(chr12:21007963-21392123)	Likely pathogenic
2572603	NM_006446.5(SLCO1B1):c.1865+1G>A	Likely pathogenic
3780636	NM_006446.5(SLCO1B1):c.1497+2T>A	Likely pathogenic
3780639	NM_006446.5(SLCO1B1):c.226+1G>A	Likely pathogenic
3892500	NM_006446.5(SLCO1B1):c.1634T>G (p.Leu545Ter)	Likely pathogenic
4685640	NM_006446.5(SLCO1B1):c.1009_1010dup (p.Tyr338fs)	Likely pathogenic

SpliceAI

2345 predictions. Top by Δscore:

Variant	Effect	Δscore
12:21141508:TAATA:T	acceptor_loss	1.0000
12:21141511:TAGGT:T	acceptor_loss	1.0000
12:21141512:A:AG	acceptor_gain	1.0000
12:21141512:A:C	acceptor_loss	1.0000
12:21141513:G:GA	acceptor_loss	1.0000
12:21141513:G:GG	acceptor_gain	1.0000
12:21141513:GGT:G	acceptor_gain	1.0000
12:21141654:TGAAG:T	donor_loss	1.0000
12:21141656:AAG:A	donor_loss	1.0000
12:21141657:AG:A	donor_loss	1.0000
12:21141658:GGTA:G	donor_loss	1.0000
12:21141659:GTA:G	donor_loss	1.0000
12:21141660:T:G	donor_loss	1.0000
12:21141664:A:AG	donor_gain	1.0000
12:21200568:T:TA	acceptor_gain	1.0000
12:21224840:G:GG	donor_gain	1.0000
12:21141509:A:AG	acceptor_gain	0.9900
12:21141509:AATAG:A	acceptor_gain	0.9900
12:21141510:A:G	acceptor_gain	0.9900
12:21141512:AG:A	acceptor_gain	0.9900
12:21141512:AGGT:A	acceptor_gain	0.9900
12:21141513:GG:G	acceptor_gain	0.9900
12:21141513:GGTG:G	acceptor_gain	0.9900
12:21141513:GGTGA:G	acceptor_gain	0.9900
12:21179021:G:GG	donor_gain	0.9900
12:21200562:T:TA	acceptor_gain	0.9900
12:21200571:C:CA	acceptor_gain	0.9900
12:21202490:GGA:G	acceptor_gain	0.9900
12:21202604:A:AG	donor_gain	0.9900
12:21222299:GA:G	acceptor_gain	0.9900

AlphaMissense

4504 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
12:21196990:T:A	W258R	0.995
12:21196990:T:C	W258R	0.995
12:21172779:A:C	S72R	0.994
12:21172781:C:A	S72R	0.994
12:21172781:C:G	S72R	0.994
12:21196993:T:A	W259R	0.994
12:21196993:T:C	W259R	0.994
12:21200585:A:C	S350R	0.994
12:21200587:C:A	S350R	0.994
12:21200587:C:G	S350R	0.994
12:21205946:G:C	W470C	0.994
12:21205946:G:T	W470C	0.994
12:21206001:T:A	C489S	0.993
12:21206002:G:C	C489S	0.993
12:21174603:A:C	S85R	0.992
12:21174605:T:A	S85R	0.992
12:21174605:T:G	S85R	0.992
12:21196980:G:C	W254C	0.991
12:21196980:G:T	W254C	0.991
12:21178623:G:C	G177R	0.990
12:21224780:G:C	W602C	0.990
12:21224780:G:T	W602C	0.990
12:21174663:G:A	G105R	0.989
12:21174663:G:C	G105R	0.989
12:21178636:G:C	R181P	0.989
12:21178638:G:A	G182R	0.989
12:21178638:G:C	G182R	0.989
12:21196978:T:A	W254R	0.988
12:21196978:T:C	W254R	0.988
12:21178624:G:A	G177D	0.987

dbSNP variants (sampled 300 via entrez): RS1000105428 (12:21217416 T>G), RS1000107729 (12:21210579 T>C,G), RS1000137355 (12:21161828 T>C), RS1000142412 (12:21159383 G>T), RS1000154926 (12:21228208 C>G,T), RS1000212008 (12:21143561 G>T), RS1000217906 (12:21217606 T>C), RS1000219688 (12:21138212 C>G,T), RS1000246621 (12:21215907 G>A), RS1000248015 (12:21212583 C>T), RS1000268564 (12:21134737 A>T), RS1000270361 (12:21138425 A>C), RS1000293386 (12:21205204 A>C,G), RS1000303072 (12:21207031 A>G), RS1000339671 (12:21130828 T>C)

Disease associations

OMIM: gene MIM:604843 | 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

101 associations (top):

Study	Trait	p-value
GCST000213_1	Response to statin therapy	2.000000e-09
GCST000386_4	Bilirubin levels	7.000000e-13
GCST000523_5	Methotrexate pharmacokinetics (acute lymphoblastic leukemia)	7.000000e-07
GCST000523_6	Methotrexate pharmacokinetics (acute lymphoblastic leukemia)	7.000000e-06
GCST000523_7	Methotrexate pharmacokinetics (acute lymphoblastic leukemia)	8.000000e-11
GCST001091_4	Bilirubin levels	5.000000e-08
GCST001217_5	Metabolic traits	3.000000e-22
GCST001612_22	Sex hormone-binding globulin levels	2.000000e-08
GCST001770_1	Methotrexate clearance (acute lymphoblastic leukemia)	6.000000e-21
GCST001882_2	Metabolite levels	5.000000e-15
GCST002285_16	Chagas cardiomyopathy in Tripanosoma cruzi seropositivity	1.000000e-07
GCST002875_10	Diisocyanate-induced asthma	7.000000e-06
GCST002883_2	AR-C124910XX levels in individuals with acute coronary syndromes treated with ticagrelor	4.000000e-13
GCST003322_1	Ischemic stroke (large artery atherosclerosis)	3.000000e-08
GCST003540_2	Clinical laboratory measurements	4.000000e-22
GCST004359_1	Plasma estrone conjugates levels in resected early stage estrogen-receptor positive breast cancer	4.000000e-11
GCST004359_2	Plasma estrone conjugates levels in resected early stage estrogen-receptor positive breast cancer	7.000000e-10
GCST004360_1	Estrone conjugates/estrone ratio in resected early stage estrogen-receptor positive breast cancer	3.000000e-12
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
GCST006249_105	Serum metabolite levels	2.000000e-13
GCST006249_106	Serum metabolite levels	1.000000e-37
GCST006249_54	Serum metabolite levels	8.000000e-17
GCST006249_57	Serum metabolite levels	3.000000e-81

EFO canonical traits (28, from GWAS)

EFO ID	Trait name
EFO:0004570	bilirubin measurement
EFO:0004725	metabolite measurement
EFO:0004696	sex hormone-binding globulin measurement
EFO:0006995	response to diisocyanate
EFO:0007020	AR-C124910XX measurement
EFO:0004297	clinical laboratory measurement
EFO:0007971	estrone conjugate measurement
EFO:0007970	estrone measurement
EFO:0006336	diastolic blood pressure
EFO:0006527	smoking status measurement
EFO:0006335	systolic blood pressure
EFO:0004530	triglyceride measurement
EFO:0009270	heel bone mineral density
EFO:0009603	stroke outcome severity measurement
EFO:0010225	lysophosphatidylethanolamine measurement
EFO:0004531	urate measurement
EFO:0010370	lysophosphatidylethanolamine 20:4 measurement
EFO:0005059	acylcarnitine measurement
EFO:0005116	urinary metabolite measurement
EFO:0011010	glycodeoxycholate 3-O-glucuronide measurement
EFO:0011009	glycochenodeoxycholate 3-O-glucuronide measurement
EFO:0007986	reticulocyte count
EFO:0004527	mean corpuscular hemoglobin
EFO:0007989	monocyte percentage of leukocytes
EFO:0010701	mean reticulocyte volume
EFO:0007990	neutrophil percentage of leukocytes
EFO:0007985	platelet crit
EFO:0004309	platelet count

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 (2): CHEMBL1697668 (SINGLE PROTEIN), CHEMBL3885536 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

57 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 1,317,927 (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
CHEMBL1064	SIMVASTATIN	4	123,163
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
CHEMBL1487	ATORVASTATIN	4	68,788
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
CHEMBL2218877	ERYTHROMYCIN ESTOLATE	4
CHEMBL269732	TACROLIMUS ANHYDROUS	4
CHEMBL374478	RIFAMPIN	4
CHEMBL393220	ATORVASTATIN CALCIUM	4
CHEMBL413	SIROLIMUS	4
CHEMBL421	SULFASALAZINE	4
CHEMBL428647	PACLITAXEL	4
CHEMBL437765	RIFAMYCIN	4
CHEMBL457	GEMFIBROZIL	4

Clinical evidence (CIViC)

Drug × variant × indication: 2 predictive associations from 2 curated evidence items.

Variant	Therapy	Indication	Effect	Level	CIViC
SLCO1B1 N130D	Methotrexate	Cancer	Adverse Response	CIViC B	EID1842
SLCO1B1 RS4149056	Methotrexate	Cancer	Adverse Response	CIViC B	EID1841

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

PharmGKB clinical annotations

96 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs10841753	Metabolism/PK	4	methotrexate	Acute lymphoblastic leukemia
rs11045819	Efficacy	3	fluvastatin	Hypercholesterolemia
rs11045819	Metabolism/PK	3	rifampin
rs11045819	Efficacy	3	HMG-CoA reductase inhibitors
rs11045821	Metabolism/PK	3	methotrexate	Acute lymphoblastic leukemia
rs11045872	Metabolism/PK	3	methotrexate	Acute lymphoblastic leukemia
rs11045879	Metabolism/PK	3	methotrexate	Neoplasms
rs11045879	Toxicity	3	mercaptopurine	Acute lymphoblastic leukemia;Gastrointestinal toxicity
rs11045879	Toxicity	4	methotrexate	Acute lymphoblastic leukemia;Lymphoma;Osteosarcoma
rs113681054	Metabolism/PK	3	ticagrelor	Acute coronary syndrome
rs2291073	Efficacy	3	lovastatin
rs2291075	Efficacy	3	cytarabine;daunorubicin;etoposide;mitoxantrone	Leukemia;Myeloid;Acute
rs2306283	Other	3	repaglinide
rs2306283	Metabolism/PK	3	pravastatin
rs2306283	Efficacy	3	HMG-CoA reductase inhibitors
rs2306283	Toxicity	4	irinotecan	Neoplasms
rs2306283	Efficacy	4	atorvastatin	Hypercholesterolemia
rs2306283	Efficacy	4	pravastatin	Dyslipidaemia
rs2306283	Efficacy	4	simvastatin	Coronary Disease;Dyslipidaemia;Hypercholesterolemia;Hyperlipidemias
rs2306283	Other	3	pitavastatin
rs2306283	Efficacy	3	irinotecan	Colorectal Neoplasms
rs2306283	Efficacy	3	rocuronium
rs2306283	Metabolism/PK	3	rifampin
rs2306283	Metabolism/PK	3	mycophenolic acid	Kidney Transplantation
rs2306283	Toxicity	3	sorafenib	Diarrhea
rs2306283	Toxicity	3	HMG-CoA reductase inhibitors	Coronary Artery Disease;Diabetes Mellitus;Hypercholesterolemia
rs2306283	Metabolism/PK	3	methotrexate	Acute lymphoblastic leukemia
rs2900478	Efficacy	3	HMG-CoA reductase inhibitors
rs4149015	Toxicity	3	irinotecan	Non-Small Cell Lung Carcinoma
rs4149015	Metabolism/PK	3	pravastatin
rs4149032	Metabolism/PK	3	rifampin	Tuberculosis
rs4149032	Metabolism/PK	3	letermovir
rs4149036	Efficacy	3	atorvastatin
rs4149056	Metabolism/PK	1A	simvastatin;simvastatin acid
rs4149056	Toxicity	1A	simvastatin	statin-related myopathy
rs4149056	Toxicity	1A	fluvastatin	statin-related myopathy
rs4149056	Metabolism/PK	1A	fluvastatin
rs4149056	Metabolism/PK	1A	atorvastatin
rs4149056	Toxicity	2A	HMG-CoA reductase inhibitors	statin-related myopathy

PharmGKB variants

56 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2291073	SLCO1B1	3	2.75	1	lovastatin
rs2291075	SLCO1B1	3	2.50	2	cytarabine;daunorubicin;etoposide;mitoxantrone
rs2306282	SLCO1B1		0.00	0
rs2306283	SLCO1B1	3	3.00	33	repaglinide;methotrexate;irinotecan;pitavastatin;HMG-CoA reductase inhibitors;rocuronium;sorafenib;rifampin;mycophenolic acid;pravastatin
rs2900478	SLCO1B1	3	1.25	1	HMG-CoA reductase inhibitors
rs3829306	SLCO1B1		0.00	0
rs4149015	SLCO1B1	3	0.50	2	pravastatin;irinotecan
rs4149032	SLCO1B1	3	2.25	2	rifampin;letermovir
rs4149036	SLCO1B1	3	3.00	1	atorvastatin
rs4149044	SLCO1B1		0.00	0
rs4149045	SLCO1B1		0.00	0
rs4149056	SLCO1B1	1A	211.75	56	methotrexate;atorvastatin;rifampin;mercaptopurine;methotrexate;lovastatin acid;fluvastatin;pravastatin;atorvastatin;simvastatin;rosuvastatin;lovastatin
rs4149057	SLCO1B1		0.00	0
rs4149081	SLCO1B1	3	4.00	4	methotrexate;rosuvastatin;simvastatin
rs4149087	SLCO1B1		0.00	0
rs4363657	SLCO1B1	4	-4.00	1	simvastatin
rs11045818	SLCO1B1		0.00	0
rs11045819	SLCO1B1	3	3.00	6	fluvastatin;rifampin;HMG-CoA reductase inhibitors
rs11045821	SLCO1B1	3	1.50	1	methotrexate
rs11045872	SLCO1B1	3	0.00	1	methotrexate
rs11045879	SLCO1B1	3	2.50	3	methotrexate;mercaptopurine
rs34671512	SLCO1B1		0.00	0
rs55901008	SLCO1B1		0.00	0
rs56101265	SLCO1B1		0.00	0
rs59502379	SLCO1B1		0.00	2
rs113681054	SLCO1B1	3	0.00	1	ticagrelor
rs373327528	SLCO1B1		0.00	0
rs4149014	SLCO1B1		0.00	0
rs10841753	SLCO1B1	4	-1.75	1	methotrexate
rs11045854	SLCO1B1		0.00	0
rs12305884	SLCO1B1		0.00	0
rs11045873	SLCO1B1		0.00	0
rs11045874	SLCO1B1		0.00	0
rs4149034	SLCO1B1		0.00	0
rs2900476	SLCO1B1		0.00	0
rs1463565	SLCO1B1		0.00	0
rs4149026	SLCO1B1		0.00	0
rs2417955	SLCO1B1		0.00	0
rs4149035	SLCO1B1		0.00	0
rs10444413	SLCO1B1		0.00	0

PharmGKB dosing guidelines

14 guidelines.

Source	Drug	Guideline	Dosing?	Recommendation?
CPIC	atorvastatin	Annotation of CPIC Guideline for atorvastatin and SLCO1B1	yes	yes
CPIC	fluvastatin	Annotation of CPIC Guideline for fluvastatin and CYP2C9, SLCO1B1	yes	yes
CPIC	lovastatin	Annotation of CPIC Guideline for lovastatin and SLCO1B1	yes	yes
CPIC	pitavastatin	Annotation of CPIC Guideline for pitavastatin and SLCO1B1	yes	yes
CPIC	pravastatin	Annotation of CPIC Guideline for pravastatin and SLCO1B1	yes	yes
CPIC	rosuvastatin	Annotation of CPIC Guideline for rosuvastatin and ABCG2, SLCO1B1	yes	yes
CPIC	simvastatin	Annotation of CPIC Guideline for simvastatin and SLCO1B1	yes	yes
DPWG	atorvastatin	Annotation of DPWG Guideline for atorvastatin and SLCO1B1	yes	yes
DPWG	fluvastatin	Annotation of DPWG Guideline for fluvastatin and SLCO1B1
DPWG	pravastatin	Annotation of DPWG Guideline for pravastatin and SLCO1B1
DPWG	rosuvastatin	Annotation of DPWG Guideline for rosuvastatin and SLCO1B1	yes	yes
DPWG	simvastatin	Annotation of DPWG Guideline for simvastatin and SLCO1B1	yes	yes
RNPGx	HMG-CoA reductase inhibitors;simvastatin	Annotation of RNPGx Guideline for hmg coa reductase inhibitors, simvastatin and SLCO1B1	yes	yes
RNPGx	methotrexate	Annotation of RNPGx Guideline for methotrexate and ABCB1, MTHFR, SLC19A1, SLCO1B1

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 (5 total), top 5:

Ligand	Action	Affinity	Parameter
cyclosporin A	Inhibition	7.29	pKi
estrone-3-sulphate	Inhibition	7.22	pIC50
sarsagenin	Inhibition	6.89	pKi
rifampicin	Inhibition	5.96	pKi
rifamycin	Inhibition	5.7	pKi

Binding affinities (BindingDB)

6 measured of 8 human assays (8 total across all organisms); most potent 6 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value	Patent
5-Chloro-3-(4-methanesulfonyl-phenyl)-6’’-methyl-[2,3’’]bipyridinyl	KI	79 nM
CHEMBL3138660	IC50	933 nM
CHEMBL1314749	IC50	1150 nM
CHEMBL3137741	IC50	2000 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
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

238 potent at pChembl≥5 of 283 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
8.96	EC50	1.1	nM	CHEMBL4637446
8.77	EC50	1.7	nM	CHEMBL4636474
8.35	EC50	4.5	nM	CHEMBL4633668
7.36	Ki	44	nM	SULFOBROMOPHTHALEIN SODIUM
7.34	Ki	45.8	nM	ESTRONE SULFURIC ACID
7.30	IC50	50	nM	SULFOBROMOPHTHALEIN SODIUM
7.22	Ki	60	nM	GANGALEOIDIN
7.18	IC50	66	nM	CHEMBL4209316
7.10	Ki	80	nM	LEOIDIN
7.00	IC50	100	nM	CHEMBL5077187
6.99	IC50	102.3	nM	GANGALEOIDIN
6.89	Ki	130	nM	SARSASAPOGENIN
6.89	EC50	130	nM	CHEMBL5091040
6.84	IC50	144.5	nM	LEOIDIN
6.80	Ki	160	nM	LOSARTAN
6.80	IC50	158.5	nM	BMS-986020
6.77	IC50	170	nM	BMS-986020
6.75	IC50	180	nM	ALISPORIVIR
6.70	Ki	200	nM	CYCLOSPORINE
6.64	IC50	230	nM	RIFAMYCIN
6.62	Ki	238	nM	CYCLOSPORINE
6.61	IC50	245.5	nM	SARSASAPOGENIN
6.60	Ki	250	nM	OLIGOMYCIN
6.58	Ki	260	nM	LASALOCID A SODIUM
6.55	IC50	280	nM	PACLITAXEL
6.54	IC50	288.4	nM	LOSARTAN
6.54	Ki	290	nM	ENOXOLONE
6.52	IC50	300	nM	RIFAMPIN
6.48	Ki	330	nM	ARACHIDONIC ACID
6.47	Ki	340	nM	BETA CAROTENE
6.43	Ki	370	nM	DICLOXACILLIN SODIUM
6.42	Ki	380	nM	UTILIN
6.42	Ki	380	nM	BUSSEIN
6.40	IC50	398.1	nM	CHEMBL2018969
6.40	Ki	400	nM	CANDESARTAN CILEXETIL
6.40	Ki	400	nM	LOBARIC ACID
6.39	Ki	410	nM	3-DEOXO-3beta-ACETOXYDEOXYDIHYDROGEDUNIN
6.38	Ki	420	nM	CHUKRASIN METHYL ETHER
6.36	Ki	440	nM	CHEMBL3138689
6.35	Ki	450	nM	ATORVASTATIN CALCIUM
6.35	Ki	450	nM	HYDROXYZINE PAMOATE
6.35	IC50	450	nM	CHEMBL3704745
6.32	IC50	478.6	nM	LASALOCID A SODIUM
6.32	Ki	480	nM	CHEMBL3138678
6.29	Ki	510	nM	CHEMBL3138660
6.28	Ki	530	nM	SULFASALAZINE
6.28	IC50	524.8	nM	ENOXOLONE
6.27	Ki	540	nM	OLMESARTAN MEDOXOMIL
6.27	Ki	540	nM	CHEMBL3138712
6.25	IC50	560	nM	SULFASALAZINE

PubChem BioAssay actives

232 with measured affinity, of 2666 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]-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	1660551: Substrate activity at OATP1B1 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0011	uM
(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	1660551: Substrate activity at OATP1B1 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0017	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	1660551: Substrate activity at OATP1B1 (unknown origin) expressed in HEK293 cells assessed as cytotoxicity incubated for 48 hrs by sulforhodamine B assay	ec50	0.0045	uM
disodium;2-hydroxy-5-[4,5,6,7-tetrabromo-1-(4-hydroxy-3-sulfonatophenyl)-3-oxo-2-benzofuran-1-yl]benzenesulfonate	680730: TP_TRANSPORTER: inhibition of E217betaG uptake in OATP-C-expressing HEK293 cells	ki	0.0440	uM
[(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate	679506: TP_TRANSPORTER: inhibition of E217betaG uptake in OATP-C-expressing HEK293 cells	ki	0.0458	uM
methyl 8,10-dichloro-9-hydroxy-3-methoxy-1,7-dimethyl-6-oxobenzo[b][1,4]benzodioxepine-2-carboxylate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.0600	uM
(7S)-7-(4-fluorophenyl)-2-N-[3-methoxy-4-(3-methyl-1,2,4-triazol-1-yl)phenyl]-4-N-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidine-2,4-diamine	1695957: Inhibition of OATP1B1 (unknown origin)	ic50	0.0660	uM
methyl 8,10-dichloro-3,9-dihydroxy-1,4,7-trimethyl-6-oxobenzo[b][1,4]benzodioxepine-2-carboxylate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.0800	uM
(2S)-2-[5-[4-[2-(4-cyanophenyl)ethoxy]phenyl]-4-(4,4-dimethylpiperidin-1-yl)-2,6-dimethyl-3-pyridinyl]-2-[(2-methylpropan-2-yl)oxy]acetic acid	1826539: Inhibition of OATP1B1 (unknown origin)	ic50	0.1000	uM
(2S,5S,8S,14S,32S,35R,38S,46E,50S,54S)-54-[(5-fluoro-1H-indol-3-yl)methyl]-5-[(1R)-1-methoxyethyl]-8-[(4-methoxyphenyl)methyl]-14,32,35-trimethyl-49-oxa-19,27-dithia-1,4,7,10,16,31,34,37,55-nonazahexacyclo[36.14.4.121,25.140,44.02,50.010,14]octapentaconta-21,23,25(58),40,42,44(57),46-heptaene-3,6,9,15,30,33,36,53,56-nonone	1813399: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction in OATP 1B1-mediated [3H]-pitavastatin uptake preincubated for 30 mins followed by [3H]-pitavastatin addition and measured after 2 mins by liquid scintillation analysis	ec50	0.1300	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.1300	uM
Losartan	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.1600	uM
1-[4-[4-[3-methyl-4-[[(1R)-1-phenylethoxy]carbonylamino]-1,2-oxazol-5-yl]phenyl]phenyl]cyclopropane-1-carboxylic acid	1813451: Inhibition of OATP1B1 (unknown origin)	ic50	0.1700	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	1168841: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using [3H]estradiol-17beta-glucuronide substrate	ic50	0.1800	uM
cyclosporine	1218867: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake	ki	0.2000	uM
Rifamycin	681366: TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells	ic50	0.2300	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.2500	uM
Lasalocid Sodium	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.2600	uM
Paclitaxel	1197744: Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at after 5 mins by Dixon plot method	ic50	0.2800	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.2900	uM
rifampin	1218864: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	ic50	0.3000	uM
(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoic acid	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.3300	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.3400	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.3700	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.3800	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.3800	uM
N-[[3-[[3-[(5-chlorothiophen-2-yl)sulfonylamino]-4-methoxyindazol-1-yl]methyl]phenyl]methyl]-2-hydroxy-2-methylpropanamide	728750: Antagonist activity at OATP1B1 (unknown origin) by [35S]GTPgammaS binding assay	ic50	0.3981	uM
Candesartan Cilexetil	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4000	uM
3-hydroxy-9-methoxy-6-oxo-7-pentanoyl-1-pentylbenzo[b][1,4]benzodioxepine-2-carboxylic acid	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4000	uM
[(1S,4bS,5R,8S,10aR,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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4100	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4200	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4400	uM
Hydroxyzine Pamoate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4500	uM
atorvastatin calcium anhydrous	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4500	uM
[(1S,2R,4S,7S,8S,10R,11R,12S,13S,15R,17S,19R)-10,13,15-triacetyloxy-7-(furan-3-yl)-1,8,12,16,16-pentamethyl-5-oxo-3,6-dioxapentacyclo[9.8.0.02,4.02,8.012,17]nonadecan-19-yl] acetate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.4800	uM
methyl 2-[(1S,3S,5S,7S,8S,9R,12S,13S)-5-acetyloxy-13-(furan-3-yl)-6,6,8,12-tetramethyl-17-methylidene-15-oxo-2,14-dioxatetracyclo[7.7.1.01,12.03,8]heptadecan-7-yl]acetate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.5100	uM
2-hydroxy-5-[[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl]benzoic acid	699542: Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	ki	0.5300	uM
Olmesartan Medoxomil	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.5400	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.5400	uM
4-hydroxy-3-(4-hydroxyphenyl)-5-methoxy-8,8-dimethyl-6-(3-methylbut-2-enyl)pyrano[2,3-h]chromen-2-one	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.5900	uM
trans-(1S,3S)-3-[4-[4-[[cyclopentyl(methyl)carbamoyl]oxymethyl]-3-methyl-1,2-oxazol-5-yl]phenoxy]cyclohexane-1-carboxylic acid	1813451: Inhibition of OATP1B1 (unknown origin)	ic50	0.6000	uM
(1S,9E,13S,17S,20S,23S,29S,55S,60R,63S)-63-(aminomethyl)-50-fluoro-20-[(1R)-1-hydroxyethyl]-23-[(4-methoxyphenyl)methyl]-29,60-dimethyl-12-oxa-34,68-dithia-16,19,22,25,31,41,42,43,46,56,58,61,64-tridecazadecacyclo[36.19.12.13,7.116,55.136,40.141,44.146,53.013,17.025,29.047,52]tetraheptaconta-3,5,7(74),9,36(73),37,39,42,44(72),47(52),48,50,53(71)-tridecaene-18,21,24,30,57,59,62,65,70-nonone	1813399: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction in OATP 1B1-mediated [3H]-pitavastatin uptake preincubated for 30 mins followed by [3H]-pitavastatin addition and measured after 2 mins by liquid scintillation analysis	ec50	0.6000	uM
Atorvastatin	1218864: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	ic50	0.6000	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.6200	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.6300	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.6500	uM
methyl 2-[(1S,3S,5S,7S,8S,9R,12S,13S)-13-(furan-3-yl)-5-hydroxy-6,6,8,12-tetramethyl-17-methylidene-15-oxo-2,14-dioxatetracyclo[7.7.1.01,12.03,8]heptadecan-7-yl]acetate	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.6800	uM
(7S)-2-N-[4-(4-chloroimidazol-1-yl)-3-methoxyphenyl]-4-N-methyl-7-phenyl-6,7-dihydro-5H-cyclopenta[d]pyrimidine-2,4-diamine	1695957: Inhibition of OATP1B1 (unknown origin)	ic50	0.6900	uM
Ritonavir	1218864: Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	ic50	0.7000	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	977601: Ki values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells	ki	0.7200	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
estradiol-17 beta-glucuronide	increases transport, affects transport, affects uptake, decreases transport, decreases reaction (+3 more)	15
Rifampin	increases uptake, decreases activity, decreases uptake, increases expression, affects uptake (+3 more)	13
Sulfobromophthalein	increases response to substance, decreases activity, decreases reaction, increases import, increases uptake (+2 more)	12
estrone sulfate	decreases reaction, increases import, increases reaction, affects binding, decreases degradation (+5 more)	10
Cyclosporine	decreases activity, affects cotreatment, decreases expression, decreases reaction, increases uptake	9
Taurocholic Acid	increases uptake, decreases reaction, increases import, increases transport, increases abundance (+3 more)	7
Simvastatin	decreases reaction, increases transport, decreases activity, affects response to substance, increases response to substance (+1 more)	7
Atorvastatin	increases import, increases transport, decreases activity, increases uptake, decreases transport (+1 more)	6
Pravastatin	decreases reaction, increases uptake, decreases activity, increases response to substance, decreases transport (+1 more)	6
cyanoginosin LR	decreases reaction, increases response to substance, increases uptake	4
pitavastatin	increases uptake, affects transport, decreases reaction, increases import, increases response to substance	4
Chenodeoxycholic Acid	decreases expression, increases transport, affects cotreatment	4
Valproic Acid	increases expression, decreases activity, decreases expression, decreases methylation, affects cotreatment	4
perfluorooctane sulfonic acid	increases transport, decreases expression, increases expression	3
Rosuvastatin Calcium	decreases reaction, increases uptake, increases response to substance	3
Fluvastatin	affects import, decreases activity, decreases uptake, decreases reaction, increases response to substance (+1 more)	3
Acetaminophen	decreases expression, affects cotreatment	3
Bile Acids and Salts	increases uptake, affects transport, affects uptake, increases transport, decreases reaction	3
Deoxycholic Acid	decreases expression, increases uptake, affects cotreatment	3
Glycochenodeoxycholic Acid	increases transport, affects cotreatment, decreases expression	3
Glycocholic Acid	affects cotreatment, decreases expression, increases abundance	3
Methotrexate	affects abundance, affects response to substance, increases response to substance	3
Triclosan	affects cotreatment, decreases expression, affects expression	3
Okadaic Acid	decreases reaction, increases response to substance, decreases expression	3
kaempferol	decreases reaction, increases import, decreases activity, decreases uptake	2
perfluorooctanoic acid	decreases expression, increases expression	2
2’,7’-dichlorofluorescein	affects binding, decreases reaction, increases uptake, decreases activity, decreases uptake (+1 more)	2
nefazodone	decreases expression, affects cotreatment	2
perfluorooctanesulfonamide	increases expression	2
repaglinide	decreases reaction, increases uptake, affects metabolic processing	2

ChEMBL screening assays

242 unique, capped per target: 106 functional, 82 admet, 53 binding, 1 toxicity

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1692729	Binding	Induction of SLCO1B1 activity	Interaction potential of etravirine with drug transporters assessed in vitro. — Antimicrob Agents Chemother
CHEMBL1743145	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1B1	Membrane transporters in drug development. — Nat Rev Drug Discov
CHEMBL2076052	Functional	TP_TRANSPORTER: uptake in Xenopus laevis oocytes	Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. — J Biol Chem

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_B6AL	HepaRG OATP1B1 KO	Cancer cell line	Female
CVCL_B6AM	HepaRG OATP1B1/OATP1B3 KO	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