SLCO2B1

Summary

SLCO2B1 (solute carrier organic anion transporter family member 2B1, HGNC:10962) is a protein-coding gene on chromosome 11q13.4, encoding Solute carrier organic anion transporter family member 2B1 (O94956). Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions.

This locus encodes a member of the organic anion-transporting polypeptide family of membrane proteins. The protein encoded by this locus may function in regulation of placental uptake of sulfated steroids. Alternatively spliced transcript variants have been described.

Source: NCBI Gene 11309 — RefSeq curated summary.

At a glance

• Clinical variants (ClinVar): 111 total
• Druggable target: yes — 17 molecules with ChEMBL bioactivity
• MANE Select transcript: NM_007256

Identifiers

Gene identifiers

Field	Value
HGNC ID	HGNC:10962
Approved symbol	SLCO2B1
Name	solute carrier organic anion transporter family member 2B1
Location	11q13.4
Locus type	gene with protein product
Status	Approved
Aliases	OATP-B, OATP2B1
Ensembl gene	ENSG00000137491
Ensembl biotype	protein_coding
OMIM	604988
Entrez	11309

Gene structure

Transcript identifiers

Ensembl transcripts: 25 — 18 protein_coding, 6 retained_intron, 1 protein_coding_CDS_not_defined

ENST00000289575, ENST00000341411, ENST00000428359, ENST00000454962, ENST00000525650, ENST00000525845, ENST00000526660, ENST00000526839, ENST00000527180, ENST00000528108, ENST00000530012, ENST00000530015, ENST00000530556, ENST00000531457, ENST00000531713, ENST00000531756, ENST00000532236, ENST00000534004, ENST00000534186, ENST00000891031, ENST00000891032, ENST00000891033, ENST00000891034, ENST00000966603, ENST00000966604

RefSeq mRNA: 3 — MANE Select: NM_007256 NM_001145211, NM_001145212, NM_007256

CCDS: CCDS44683, CCDS53679, CCDS8235

Canonical transcript exons

ENST00000289575 — 14 exons

Exon	Start	End
ENSE00000927578	75169173	75169406
ENSE00000927579	75169666	75169764
ENSE00000927586	75203307	75203427
ENSE00002177299	75204400	75206549
ENSE00002177754	75151107	75151397
ENSE00003459017	75165787	75165949
ENSE00003465392	75202901	75202965
ENSE00003602013	75162655	75162785
ENSE00003629294	75200224	75200387
ENSE00003665558	75172379	75172569
ENSE00003672284	75163963	75164100
ENSE00003730334	75196514	75196679
ENSE00003741907	75193218	75193575
ENSE00003753466	75188136	75188238

Expression profiles

Bgee: expression breadth ubiquitous, 258 present calls, max score 97.68.

FANTOM5 (CAGE): breadth broad, TPM avg 15.4125 / max 995.7489, expressed in 568 samples.

FANTOM5 promoters (11 alternative TSS)

Promoter ID	TPM avg	Samples expressed
115881	7.6906	371
115880	3.4425	349
115871	2.3072	251
115883	0.8515	42
115872	0.4791	124
115879	0.1707	102
115870	0.1305	48
115884	0.1303	20
115882	0.1197	20
115869	0.0510	20

Top tissues by expression

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

Tissue	Anatomy ID	Expression score	Quality
right lobe of liver	UBERON:0001114	97.68	gold quality
liver	UBERON:0002107	96.27	gold quality
sural nerve	UBERON:0015488	94.87	gold quality
upper lobe of left lung	UBERON:0008952	93.92	gold quality
C1 segment of cervical spinal cord	UBERON:0006469	93.61	gold quality
lymph node	UBERON:0000029	93.53	gold quality
spleen	UBERON:0002106	93.46	gold quality
upper lobe of lung	UBERON:0008948	93.43	gold quality
ileal mucosa	UBERON:0000331	93.30	gold quality
gall bladder	UBERON:0002110	93.26	gold quality
small intestine Peyer’s patch	UBERON:0003454	93.25	gold quality
right adrenal gland cortex	UBERON:0035827	93.17	gold quality
vermiform appendix	UBERON:0001154	92.96	gold quality
left adrenal gland	UBERON:0001234	92.52	gold quality
right adrenal gland	UBERON:0001233	92.43	gold quality
left adrenal gland cortex	UBERON:0035825	92.41	gold quality
small intestine	UBERON:0002108	92.39	gold quality
spinal cord	UBERON:0002240	92.19	gold quality
rectum	UBERON:0001052	92.10	gold quality
right lung	UBERON:0002167	91.89	gold quality
colonic epithelium	UBERON:0000397	91.80	gold quality
right coronary artery	UBERON:0001625	91.74	gold quality
adrenal cortex	UBERON:0001235	91.24	gold quality
lung	UBERON:0002048	91.19	gold quality
adrenal gland	UBERON:0002369	91.07	gold quality
transverse colon	UBERON:0001157	90.46	gold quality
mucosa of transverse colon	UBERON:0004991	90.14	gold quality
nerve	UBERON:0001021	89.95	gold quality
tibial nerve	UBERON:0001323	89.95	gold quality
omental fat pad	UBERON:0010414	89.53	gold quality

Single-cell (SCXA)

Detected in 6 experiment(s), a significant marker in 6.

Experiment	Marker?	Max mean expression
E-MTAB-6678	yes	1711.75
E-MTAB-7381	yes	627.58
E-GEOD-84465	yes	38.68
E-HCAD-35	yes	32.26
E-ANND-3	yes	26.59
E-HCAD-25	yes	15.93

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, HNF1A

miRNA regulators (miRDB)

62 targeting SLCO2B1, 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-9-5P	100.00	72.28	2361
HSA-MIR-1252-5P	100.00	69.80	2774
HSA-MIR-3148	99.97	75.06	6478
HSA-MIR-6825-5P	99.96	69.81	3431
HSA-MIR-1468-3P	99.96	72.74	3797
HSA-MIR-4267	99.96	66.53	2368
HSA-MIR-545-3P	99.95	70.74	2783
HSA-MIR-381-3P	99.93	71.87	2854
HSA-MIR-300	99.92	71.76	2856
HSA-MIR-6768-5P	99.92	67.36	1942
HSA-MIR-4648	99.91	67.00	710
HSA-MIR-380-3P	99.89	70.18	1978
HSA-MIR-6124	99.87	69.78	3551
HSA-MIR-659-3P	99.85	70.69	1620
HSA-MIR-765	99.84	68.24	2442
HSA-MIR-6764-5P	99.75	67.89	2304
HSA-MIR-11181-3P	99.75	66.38	2205
HSA-MIR-1200	99.71	70.42	1838
HSA-MIR-5093	99.67	69.26	2291
HSA-MIR-6762-3P	99.66	66.94	1188
HSA-MIR-1915-3P	99.58	66.79	1988
HSA-MIR-12122	99.56	69.33	1672
HSA-MIR-3153	99.55	67.59	2337
HSA-MIR-6733-3P	99.54	67.80	1281
HSA-MIR-5009-3P	99.45	69.43	1341
HSA-MIR-4505	99.27	67.81	2678
HSA-MIR-3978	99.24	68.39	2201
HSA-MIR-5787	99.22	67.86	2628
HSA-MIR-2054	99.20	68.89	1699
HSA-MIR-6852-5P	99.17	66.69	2073

Literature-anchored findings (GeneRIF, showing 40)

• Genetic polymorphisms: allele frequencies in the Japanese population and functional analysis (PMID:12130747)
• uptake of steroid sulfates by isolated trophoblasts is mediated by OATP-B and OAT-4 suggesting a physiological role of both carrier proteins in placental uptake of fetal-derived steroid sulfates. (PMID:12409283)
• The trafficking and function of OATP2B1 is vulnerable to changes in the cysteine residues of extracellular loop IX-X. (PMID:16754786)
• The results indicate functional modification of OATP2B1-mediated estrone-3-sulfate and dehydroepiandrosterone-sulfate as well as pregnenolone sulfate transport through steroid hormones such as progesterone. (PMID:16908597)
• Functional differences in steroid uptake of SLC22A9 and SLC02B1 in human placenta are reported. (PMID:18501590)
• OATP2B1 is an uptake transporter expressed in platelets and is involved in statin-mediated alteration of platelet aggregation (PMID:19237515)
• Results describe the transcription of the OATP2B1 gene (SLCO2B1) in 14 different human tissues by means of 5’-RACE analysis. (PMID:19383542)
• OATP2B1 -282G > A is a major factor affecting expression, suggesting a contribution to inter-individual differences in the expression level of OATP2B1 in human liver (PMID:19620935)
• Results identify key membrane transporters OATP2B1, MRP1, MRP4, and MRP5 as modulators of skeletal muscle statin exposure and toxicity. (PMID:19940267)
• OATP2B1/SLCO2B1 function is modulated by protein kinase C-mediated internalization (PMID:20159975)
• Is present in high frequencies in the finnish population (PMID:20560925)
• 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)
• SLCO2B1 is a major transporter for montelukast and pharmacokinetics were affected by SLCO2B1 genotype and not fruit juice. (PMID:20974993)
• Six SLCO genes were highly expressed in castration resistane prostate cancer metastases versus untreated prostate cancer, including SLCO1B3 and SLCO2B. (PMID:21266523)
• tissue-specific localization of OATP2B1, OATP3A1 and OATP5A1 has been analyzed in normal mammary tissue and corresponding breast cancer tissues. (PMID:21278488)
• The biologic function of a SLCO2B1 coding SNP in transporting androgen was examined. 3 SNPs in SLCO2B1 were associated with time to progression in androgen-deprived prostatic cancer patients. (PMID:21606417)
• investigation of vectorial transport across enterocytes: Data from Caco-2 cells, models of intestinal absorption, suggest that OATP2B1 mediates apical fexofenadine/zwitterion uptake. Recombinant OATP2B1 mediates fexofenadine uptake in MDCKII cells. (PMID:21780830)
• 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)
• OATP2B1 represents a low-affinity transport route for antifolates at low pH. In contrast, the high affinity of this transporter for sulfobromophthalein seems to be intrinsic to its binding site and independent of pH. (PMID:22021325)
• Data suggest the OATP2B1 has multiple binding sites for endogenous steroids, dietary flavones, and drugs; the binding sites vary in affinity for ligands. (PMID:22201122)
• The selective hepatic uptake of scutellarin mediated by OATP2B1 is likely a key determinant of its unique pharmacokinetic characteristics. (PMID:22822035)
• Report flavonoid components in grapefruit, orange, and apple juices responsible for OATP2B1-mediated drug interactions. (PMID:23132664)
• SLCO2B1 c.935G>A single nucleotide polymorphism has no effect on the pharmacokinetics of montelukast and aliskiren. (PMID:23151832)
• in end-stage renal failure patients, some uremic toxins are related to the downregulation of intestinal MRP2 and hepatic OATP1B1 and/or OATP2B1 (PMID:23190519)
• the major OATP2B1 protein form in liver is transport competent and its hepatic expression is regulated by HNF4alpha. (PMID:23531488)
• SLCO2B1 rs12422149 variants could provide prognostic value for prostate cancer patients treated with androgen deprivation therapy (ADT) and influence ethnic differences in response to ADT. (PMID:23896625)
• SLCO2B1 polymorphisms do not affect the pharmacokinetics of montelukast and SLCO2B1 polymorphisms appear to be a minor determinant of inter-individual variability of montelukast. (PMID:23970434)
• The genotypes of the two other SLCOs,SLCO1B3 and SLCO2B1, did not show any association with bladder cancer susceptibility (PMID:24762081)
• These results suggest that OATP2B1 plays an important role in the stereoselective pharmacokinetics of fexofenadine and that one-time apple juice ingestion probably inhibits intestinal OATP2B1-mediated transport of both enantiomers (PMID:24903351)
• Suggest that OATP2B1 is involved in cell proliferation by increasing the amount of estrogen in ER1-positive breast cancer cells. (PMID:25857231)
• OATP2B1 as a determinant of pharmacokinetics in the coronary artery. (PMID:26091578)
• Results identified interethnic differences of genetic variations of the SLCO1B1, SLCO1B3, and SLCO2B1 genes in Korean population compared with other ethnic groups. (PMID:26409184)
• OATP2B1 contributes to the uptake of SN-38 by intestinal tissues, triggering gastrointestinal toxicity. (PMID:26526067)
• The association of SNP rs1077858 with OS may be a result of differential SLCO2B1 expression and the consequent increased uptake of DHEAS and subsequent resistance to ADT, which, in turn, may contribute to decreased OS. (PMID:26668348)
• Data show that prostaglandin E3 (PGE3) uptake by prostaglandin transporter OATP2A1-expressing HEK293 cells (HEK/2A1) was the highest and followed by SLCO2B1 (HEK/1B1). (PMID:26692285)
• Data suggest that OATP1B1, OATP1B3, and OATP2B1 participate in transport of perfluoroalkyl acids in hepatocytes; environmental pollutants transported include PFBS (perfluorobutane sulfonate), PFHxS (perfluorohexane sulfonate), and PFOS (perfluorooctane sulfonate). (PMID:28013215)
• results indicate that insulin acts on the small intestine to increase OATP2B1-mediated absorption (PMID:28318878)
• The OATP2B1 was primarily found in beta cells, suggesting a distinct expression pattern for OATP1B3 and OATP2B1 in islets. (PMID:28493059)
• OATP1A2, OATP1B1, and OATP2B1 can mediate cellular uptake of ochratoxin A, which could aggravate OTA toxicity. (PMID:28532671)
• genetic association studies in population in South Korea: Data suggest that an SNP in SLCO2B1 (c.935G>A, rs12422149) is associated with lipid-lowering response to rosuvastatin (an HMG-CoA reductase inhibitor) in subjects with hypercholesterolemia. (PMID:28627804)

Cross-species orthologs

4 orthologs

Organism	Symbol	Gene ID
danio_rerio	slco2b1	ENSDARG00000054609
mus_musculus	Slco2b1	ENSMUSG00000030737
rattus_norvegicus	Slco2b1	ENSRNOG00000017976
drosophila_melanogaster	Oatp30B	FBGN0032123

Paralogs (10): SLCO1A2 (ENSG00000084453), SLCO4A1 (ENSG00000101187), SLCO1B3 (ENSG00000111700), SLCO1B1 (ENSG00000134538), SLCO5A1 (ENSG00000137571), SLCO1C1 (ENSG00000139155), SLCO4C1 (ENSG00000173930), SLCO2A1 (ENSG00000174640), SLCO3A1 (ENSG00000176463), SLCO6A1 (ENSG00000205359)

Protein

Protein identifiers

Solute carrier organic anion transporter family member 2B1 — O94956 (reviewed: O94956)

Alternative names: Organic anion transporter B, Organic anion transporter polypeptide-related protein 2, Organic anion transporting polypeptide 2B1, Solute carrier family 21 member 9

All UniProt accessions (8): O94956, A0A0A0MTF1, A0A1B0GX35, E9PI53, E9PIU9, E9PN87, E9PRW4, H0YE11

UniProt curated annotations — full annotation on UniProt →

Function. Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions. Responsible for the transport of estrone 3-sulfate (E1S) through the basal membrane of syncytiotrophoblast, highlighting a potential role in the placental absorption of fetal-derived sulfated steroids including the steroid hormone precursor dehydroepiandrosterone sulfate (DHEA-S). Also facilitates the uptake of sulfated steroids at the basal/sinusoidal membrane of hepatocytes, therefore accounting for the major part of organic anions clearance of liver. Mediates the intestinal uptake of sulfated steroids. Mediates the uptake of the neurosteroids DHEA-S and pregnenolone sulfate (PregS) into the endothelial cells of the blood-brain barrier as the first step to enter the brain. Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons. May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC. Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition. Mediates the uptake of other substrates such as prostaglandins D2 (PGD2), E1 (PGE1) and E2 (PGE2), taurocholate, L-thyroxine, leukotriene C4 and thromboxane B2 (PubMed:10873595, PubMed:14610227, PubMed:19129463, PubMed:29871943, Ref.25). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier. Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment. The exact transport mechanism has not been yet deciphered but most likely involves an anion exchange, coupling the cellular uptake of organic substrate with the efflux of an anionic compound. Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions. Cytoplasmic glutamate may also act as counteranion in the placenta. An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1). Has estrone 3-sulfate (E1S) transport activity comparable with the full-length isoform 1.

Subcellular location. Cell membrane. Basal cell membrane. Basolateral cell membrane. Apical cell membrane.

Tissue specificity. Strongly expressed in the liver, at the sinusoidal membrane of the hepatocytes. Expressed in the kidney. Expressed in placental trophoblasts and syncytiotrophoblast. Expressed in the small intestine. Expressed in the blood-brain barrier, in endothelial cells of brain capillaries. Expressed in the retina, in the inner nuclear layer and the inner plexiform layer. Expressed in skelettal muscles. In testis, primarily localized to the basal membrane of Sertoli cells and weakly expressed within the tubules. Also expressed in pancreas, lung, heart, colon, ovary and spleen. Expressed in fetal brain, heart, kidney, liver, lung, skeletal muscle, spleen and pancreas. Highest expression in brain. Predominant isoform compared to isoform 3 in small intestine duodenum, kidney, placenta, and skeletal muscle. Predominant isoform compared to isoform 1 in liver. Also expressed in small intestine duodenum, kidney, brain, placenta, and skeletal muscle.

Activity regulation. E1S, DHEA-S and PregS transports are regulated by steroid hormones. In the case of testosterone, transport of E1S and DHEA-S was inhibited, whereas progesterone stimulated E1S, DHEA-S and PregS uptake. Progesterone stimulates high-affinity uptake of E1S whereas it inhibits low-affinity uptake of E1S (Ref.25). Progesterone doesn’t affect the uptake of PGE2 (Ref.25).

Domain organisation. A conserved histidine residue in the third transmembrane domain (His-136) might play an essential role in the pH sensitivity of SLCO2B1/OATP2B1-mediated substrate transport. Transmembrane domain 1 (TM1) may be localized within the substrate binding pocket.

Induction. Its expression is regulated by HNF4A.

Miscellaneous. Most likely contributes to the oral absorption and the disposition of a wide range of drugs in the intestine and the liver (PubMed:10873595, PubMed:11159893, PubMed:12724351, PubMed:14610227, PubMed:23531488, PubMed:26277985, PubMed:27576593, Ref.25).

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

Isoforms (4)

UniProt ID	Names	Canonical?
O94956-1	1, 1b, FL	yes
O94956-2	2
O94956-3	3, 1e, Short
O94956-4	4

RefSeq proteins (3): NP_001138683, NP_001138684, NP_009187* (*=MANE)

Domains & families (InterPro)

ID	Name	Type
IPR002350	Kazal_dom	Domain
IPR004156	OATP	Family
IPR036259	MFS_trans_sf	Homologous_superfamily

Pfam: PF03137

Catalyzed reactions (Rhea), 10 shown:

• prostaglandin D2(out) = prostaglandin D2(in) (RHEA:50976)
• 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)
• pregnenolone sulfate(out) = pregnenolone sulfate(in) (RHEA:73023)
• estrone 3-sulfate(out) + hydrogencarbonate(in) = estrone 3-sulfate(in) + hydrogencarbonate(out) (RHEA:73055)
• coproporphyrin III(out) = coproporphyrin III(in) (RHEA:74363)
• substance P(out) = substance P(in) (RHEA:74367)

UniProt features (112 total): mutagenesis site 58, topological domain 13, transmembrane region 12, sequence variant 5, region of interest 4, site 4, splice variant 4, modified residue 3, disulfide bond 3, sequence conflict 2, glycosylation site 2, chain 1, domain 1

Structure

Experimental structures (PDB)

0 structures.

Predicted structure (AlphaFold)

Model	pLDDT	Fraction very-high
AF-O94956-F1	78.65	0.43

Functional residue map

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

Catalytic / active sites (4): 579 (implicated in low-affinity site for e1s transport); 607 (essential for e1s and pge2 transport activity and may interact with these substrates); 611 (essential for e1s transport activity and may interact with this substrate); 618 (implicated in high-affinity site for e1s transport)

Post-translational modifications (3): 34, 318, 320

Disulfide bonds (3): 489–520, 495–516, 504–541

Glycosylation sites (2): 176, 538

Mutagenesis-validated functional residues (58):

Position	Phenotype
579	strong decrease in low-affinity and decreased in high-affinity transport of e1s; undetectable kinetic parameter for low-
607	loss of e1s transport; small decrease in cell surface expression. strong decrease in low-affinity transport of e1s and l
611	decreased e1s transport; decreased cell surface expression.
618	strong decrease in high-affinity transport of e1s and lower vmax/km value; no change in low-affinity transport of e1s an
628	decreased low- and high-affinity transport of e1s.
629	no change in e1s transport; decreased cell surface expression.
46	no change in low- and high-affinity transport of e1s.
49	decreased e1s transport, no change in cell surface expression.
50	no change in e1s transport.
51	decreased e1s transport; decreased cell surface expression; no change in km and vmax values. decreased taurocholate tran
51	decreased e1s transport; decreased cell surface expression.
52	decreased e1s transport, decreased cell surface expression; no change in km value and decreased vmax value. decreased ta
52	decreased e1s transport.
53	no change in e1s transport.
54	no change in e1s transport.
55	decreased e1s transport, decreased cell surface expression; no change in km value and decreased vmax value for e1s trans
55	decreased e1s transport; decreased cell surface expression.
55	decreased low- and high-affinity transport of e1s.
56	decreased e1s transport.
57	decreased e1s transport.
58	decreased e1s transport, no change in cell surface expression; increased km value and decreased vmax value for e1s trans

Function

Pathways and Gene Ontology

Reactome pathways

7 pathways

ID	Pathway
R-HSA-879518	Organic anion transport by SLCO transporters
R-HSA-189483	Heme degradation
R-HSA-9749641	Aspirin ADME
R-HSA-9754706	Atorvastatin ADME
R-HSA-382551	Transport of small molecules
R-HSA-425397	Transport of vitamins, nucleosides, and related molecules
R-HSA-425407	SLC-mediated transmembrane transport

MSigDB gene sets: 207 (showing top): GOBP_SODIUM_INDEPENDENT_ORGANIC_ANION_TRANSPORT, GOBP_CIRCULATORY_SYSTEM_PROCESS, BHATI_G2M_ARREST_BY_2METHOXYESTRADIOL_DN, REACTOME_METABOLISM_OF_PORPHYRINS, RIZKI_TUMOR_INVASIVENESS_3D_DN, GGGTGGRR_PAX4_03, chr11q13, GOBP_ORGANIC_ACID_TRANSPORT, GOBP_ORGANIC_HYDROXY_COMPOUND_TRANSPORT, GOBP_PORPHYRIN_CONTAINING_COMPOUND_METABOLIC_PROCESS, PICCALUGA_ANGIOIMMUNOBLASTIC_LYMPHOMA_UP, OSWALD_HEMATOPOIETIC_STEM_CELL_IN_COLLAGEN_GEL_UP, TGCTGAY_UNKNOWN, SCHAEFFER_PROSTATE_DEVELOPMENT_48HR_DN, GOBP_TETRAPYRROLE_METABOLIC_PROCESS

GO Biological Process (9): 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), transmembrane transport (GO:0055085), transport across blood-brain barrier (GO:0150104), prostaglandin transport (GO:0015732)

GO Molecular Function (6): 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), transmembrane transporter activity (GO:0022857), protein binding (GO:0005515)

GO Cellular Component (5): plasma membrane (GO:0005886), basal plasma membrane (GO:0009925), basolateral plasma membrane (GO:0016323), apical plasma membrane (GO:0016324), membrane (GO:0016020)

Reactome top-level categories

Rollup of top-5 pathways:

Category	Pathways
Drug ADME	2
SLC-mediated transport of organic anions	1
Metabolism of porphyrins	1
SLC-mediated transmembrane transport	1
Transport of small molecules	1

GO top-level categories

Rollup of top GO terms by namespace:

Category	Terms
plasma membrane region	3
transport	2
transmembrane transport	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
cellular process	1
vascular transport	1
fatty acid transport	1
icosanoid 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
transporter activity	1
binding	1
membrane	1
cell periphery	1
basal part of cell	1
basal plasma membrane	1
apical part of cell	1
cellular anatomical structure	1

Protein interactions and networks

STRING

1022 interactions, top by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO2B1	SLC22A8	Q8TCC7	769
SLCO2B1	ABCG2	Q9UNQ0	767
SLCO2B1	SLC22A7	Q9Y694	767
SLCO2B1	SLC47A1	Q96FL8	741
SLCO2B1	SLC10A1	Q14973	726
SLCO2B1	ABCC2	Q92887	719
SLCO2B1	ABCC3	O15438	713
SLCO2B1	ABCC4	O15439	713
SLCO2B1	SLC22A9	Q8IVM8	702
SLCO2B1	SLC22A1	O15245	701
SLCO2B1	SLC15A1	P46059	696
SLCO2B1	SLC22A11	Q9NSA0	669
SLCO2B1	ABCB11	O95342	665
SLCO2B1	ABCB1	P08183	663
SLCO2B1	SLC22A5	O76082	611

IntAct

118 interactions, top by confidence:

A	B	Type	Score
SLCO2B1	PDZD2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	SNX27	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MAST2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	SYNJ2BP	psi-mi:“MI:0407”(direct interaction)	0.440
SNTA1	SLCO2B1	psi-mi:“MI:0407”(direct interaction)	0.440
SNTB1	SLCO2B1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	DLG4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	APBA3	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MAST1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	FRMPD2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	LDB3	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	GRIP1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	APBA2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	GIPC2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	HTRA4	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	IL16	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	WHRN	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MPP2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MAGI1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	LIN7B	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	PALS2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	PICK1	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	DLG5	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MAGI2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	PATJ	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	TIAM2	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	LIN7C	psi-mi:“MI:0407”(direct interaction)	0.440
SLCO2B1	MPDZ	psi-mi:“MI:0407”(direct interaction)	0.440
GRIP2	SLCO2B1	psi-mi:“MI:0407”(direct interaction)	0.440

BioGRID (17): SLCO2B1 (Proximity Label-MS), HSP90B1 (Cross-Linking-MS (XL-MS)), NUCKS1 (Cross-Linking-MS (XL-MS)), ATP5I (Affinity Capture-MS), ATP5H (Affinity Capture-MS), ATP5J (Affinity Capture-MS), CANX (Affinity Capture-MS), CLGN (Affinity Capture-MS), JPH1 (Affinity Capture-MS), PDIA3 (Affinity Capture-MS), PGRMC2 (Affinity Capture-MS), PLD3 (Affinity Capture-MS), SEC61B (Affinity Capture-MS), SLC28A2 (Affinity Capture-MS), TMX1 (Affinity Capture-MS)

ESM2 similar proteins: A0A075B734, A1L272, A2IBY8, A8W649, A9Y006, D4A7H1, E7EXX2, F7B113, O14520, O35454, O54794, O62735, O94956, P34080, P35525, P41181, P47862, P47863, P47864, P51789, P51797, P56402, P56403, P79099, Q06495, Q06496, Q08DE6, Q4R691, Q5PQL3, Q62052, Q866S3, Q8BLV3, Q8BXB6, Q8BZ00, Q8IVB4, Q8K078, Q8MIQ9, Q8R2N1, Q8TCT8, Q921R8

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 77 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	58.3×	7e-07
Unblocking of NMDA receptors, glutamate binding and activation	5	55.5×	7e-07
Negative regulation of NMDA receptor-mediated neuronal transmission	5	55.5×	7e-07
Assembly and cell surface presentation of NMDA receptors	10	51.8×	2e-13
Dopamine Neurotransmitter Release Cycle	5	50.7×	1e-06
Long-term potentiation	5	48.5×	1e-06
Neurexins and neuroligins	11	44.2×	1e-13
Protein-protein interactions at synapses	7	37.9×	3e-08

GO biological processes:

GO term	Partners	Fold	FDR
establishment or maintenance of epithelial cell apical/basal polarity	10	78.5×	1e-14
protein localization to synapse	6	62.1×	7e-08
receptor clustering	7	59.0×	5e-09
regulation of postsynaptic membrane neurotransmitter receptor levels	6	40.2×	6e-07
protein-containing complex assembly	9	13.8×	1e-06
cell-cell adhesion	10	13.7×	3e-07
chemical synaptic transmission	7	7.3×	1e-03
protein transport	8	4.7×	5e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

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

Classification	Count (floor)
Pathogenic	0
Likely pathogenic	0
Uncertain significance	80
Likely benign	8
Benign	4

Top pathogenic / likely-pathogenic (0)

SpliceAI

2623 predictions. Top by Δscore:

Variant	Effect	Δscore
11:75164097:CGAGG:C	donor_loss	1.0000
11:75164098:GAG:G	donor_gain	1.0000
11:75164098:GAGG:G	donor_loss	1.0000
11:75164099:AGG:A	donor_loss	1.0000
11:75164100:GGTAC:G	donor_loss	1.0000
11:75164101:G:C	donor_loss	1.0000
11:75164101:G:GG	donor_gain	1.0000
11:75164102:T:A	donor_loss	1.0000
11:75165784:CA:C	acceptor_loss	1.0000
11:75165785:AGG:A	acceptor_loss	1.0000
11:75165785:AGGT:A	acceptor_gain	1.0000
11:75165785:AGGTG:A	acceptor_gain	1.0000
11:75165786:GGT:G	acceptor_gain	1.0000
11:75165786:GGTG:G	acceptor_gain	1.0000
11:75165786:GGTGG:G	acceptor_gain	1.0000
11:75165946:CCTGG:C	donor_loss	1.0000
11:75165947:CTGG:C	donor_loss	1.0000
11:75165948:TGG:T	donor_loss	1.0000
11:75165950:G:GC	donor_loss	1.0000
11:75165950:G:GG	donor_gain	1.0000
11:75165951:T:G	donor_loss	1.0000
11:75169171:A:AG	acceptor_gain	1.0000
11:75169171:AGAG:A	acceptor_gain	1.0000
11:75169172:G:GG	acceptor_gain	1.0000
11:75169172:GA:G	acceptor_gain	1.0000
11:75169172:GAGG:G	acceptor_gain	1.0000
11:75172374:TCCA:T	acceptor_loss	1.0000
11:75172375:CCA:C	acceptor_loss	1.0000
11:75172376:CAGGT:C	acceptor_loss	1.0000
11:75172377:A:T	acceptor_loss	1.0000

AlphaMissense

4609 scored. Top likely-pathogenic:

Variant	Protein change	am_pathogenicity
11:75172423:T:A	W276R	0.997
11:75172423:T:C	W276R	0.997
11:75172426:T:A	W277R	0.997
11:75172426:T:C	W277R	0.997
11:75203393:T:A	C639S	0.997
11:75203394:G:C	C639S	0.997
11:75165817:A:C	S106R	0.996
11:75165819:C:A	S106R	0.996
11:75165819:C:G	S106R	0.996
11:75193346:T:C	F402L	0.996
11:75193348:T:A	F402L	0.996
11:75193348:T:G	F402L	0.996
11:75203354:T:A	C626S	0.996
11:75203355:G:A	C626Y	0.996
11:75203355:G:C	C626S	0.996
11:75203356:T:G	C626W	0.996
11:75203394:G:A	C639Y	0.996
11:75203395:T:G	C639W	0.996
11:75172413:G:C	W272C	0.995
11:75172413:G:T	W272C	0.995
11:75193319:T:C	F393L	0.995
11:75193321:C:A	F393L	0.995
11:75193321:C:G	F393L	0.995
11:75203365:G:C	W629C	0.995
11:75203365:G:T	W629C	0.995
11:75203393:T:C	C639R	0.995
11:75163981:A:C	S56R	0.994
11:75163983:C:A	S56R	0.994
11:75163983:C:G	S56R	0.994
11:75164046:G:C	E77D	0.994

dbSNP variants (sampled 300 via entrez): RS1000000178 (11:75189846 A>C), RS1000002586 (11:75190438 C>G), RS1000065032 (11:75163493 A>G), RS1000070990 (11:75158123 G>A), RS1000192752 (11:75177561 T>C), RS1000194805 (11:75195353 C>A), RS1000206200 (11:75195019 G>A,C), RS1000283708 (11:75162288 G>A,C,T), RS1000361626 (11:75162002 T>C), RS1000364679 (11:75152117 T>C), RS1000403436 (11:75200594 G>C), RS1000541854 (11:75167458 G>A), RS1000612710 (11:75201189 AC>A), RS1000614183 (11:75173811 T>A), RS1000614884 (11:75173571 C>G,T)

Disease associations

OMIM: gene MIM:604988 | disease phenotypes:

GenCC curated gene-disease

Mondo (0):

Orphanet (0):

HPO phenotypes

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

GWAS associations

0 associations (top):

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1743124 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

17 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 730,002 (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
CHEMBL1163	ATAZANAVIR	4	22,094
CHEMBL160	CYCLOSPORINE	4	168,247
CHEMBL163	RITONAVIR	4	53,773
CHEMBL374478	RIFAMPIN	4	93,834
CHEMBL421	SULFASALAZINE	4	73,629
CHEMBL437765	RIFAMYCIN	4	2,798
CHEMBL461101	ELTROMBOPAG	4	602
CHEMBL553	ERLOTINIB	4	108,300
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	22,804
CHEMBL431701	SILYBIN A	3	6,297
CHEMBL50	QUERCETIN	3	74,559
CHEMBL151	LUTEOLIN	2	23,523
CHEMBL250450	ISOQUERCETIN	2	1,626
CHEMBL31574	FISETIN	2	7,745
CHEMBL44	GENISTEIN	2	44,212
CHEMBL4802105	SILICRISTIN	2	19
CHEMBL150	KAEMPFEROL	1	25,940

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

PharmGKB clinical annotations

4 annotations.

Variant	Type	Level	Drugs	Phenotypes
rs12422149	Efficacy	3	montelukast	Asthma
rs12422149	Efficacy	3	rosuvastatin
rs2306168	Metabolism/PK	3	fexofenadine
rs3781727	Metabolism/PK	3	voriconazole

PharmGKB variants

11 variants.

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2306168	SLCO2B1	3	1.00	1	fexofenadine
rs2712807	SLCO2B1		0.00	0
rs12422149	SLCO2B1	3	1.62	2	montelukast;rosuvastatin
rs35199625	SLCO2B1		0.00	0
rs3781727	SLCO2B1	3	0.12	1	voriconazole
rs142693902	SLCO2B1		0.00	0
rs1077858	SLCO2B1		0.00	0
rs1009122956	SLCO2B1		0.00	0
rs1621378	SLCO2B1		0.00	0
rs199654337	SLCO2B1		0.00	0
rs61555831	SLCO2B1		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 (2 total), top 2:

Ligand	Action	Affinity	Parameter
erlotinib	Inhibition	6.28	pKi
verlukast	Inhibition	5.55	pKi

ChEMBL bioactivities

39 potent at pChembl≥5 of 77 total, top 39 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChembl	Type	Value	Unit	Molecule
6.91	IC50	124	nM	CHEMBL6162249
6.81	IC50	155	nM	CHEMBL6171119
6.78	IC50	167	nM	CHEMBL6163420
6.77	IC50	170	nM	CHEMBL6150561
6.58	IC50	265	nM	CHEMBL6151074
6.46	IC50	350	nM	SCUTELLAREIN
6.46	IC50	346.7	nM	SCUTELLAREIN
6.41	IC50	387	nM	CHEMBL6172851
6.40	IC50	402	nM	CHEMBL6161092
6.38	IC50	420	nM	CHEMBL6161464
6.28	Ki	530	nM	ERLOTINIB
6.26	IC50	550	nM	ERLOTINIB
6.23	IC50	583	nM	CHEMBL6146403
6.10	IC50	800	nM	SILYBIN B
6.08	IC50	826	nM	CHEMBL6161472
6.04	IC50	910	nM	CHEMBL5277249
6.04	IC50	912	nM	CHEMBL5277249
5.55	Ki	2800	nM	MK-571
5.54	IC50	2900	nM	MK-571
5.52	Ki	3000	nM	RIFAMYCIN
5.52	Ki	3000	nM	SULFASALAZINE
5.52	IC50	3000	nM	SULFASALAZINE
5.44	IC50	3600	nM	SILICRISTIN
5.41	IC50	3900	nM	LUTEOLIN
5.41	IC50	3890	nM	LUTEOLIN
5.35	IC50	4500	nM	SILYBIN A
5.29	Ki	5100	nM	ATAZANAVIR
5.28	IC50	5200	nM	ATAZANAVIR
5.28	IC50	5300	nM	GENISTEIN
5.28	IC50	5248	nM	GENISTEIN
5.23	Ki	5900	nM	RITONAVIR
5.21	IC50	6100	nM	RITONAVIR
5.17	IC50	6700	nM	FISETIN
5.17	IC50	6761	nM	FISETIN
5.15	IC50	7100	nM	OROXYLIN A
5.15	IC50	7079	nM	OROXYLIN A
5.14	IC50	7300	nM	QUERCETIN
5.14	IC50	7244	nM	QUERCETIN
5.07	Ki	8480	nM	ELTROMBOPAG

PubChem BioAssay actives

29 with measured affinity, of 497 total; 17 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
5,6,7-trihydroxy-2-(4-hydroxyphenyl)chromen-4-one	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	0.3467	uM
Erlotinib	699544: Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	ki	0.5300	uM
(2R,3R)-3,5,7-trihydroxy-2-[(2S,3S)-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-yl]-2,3-dihydrochromen-4-one	1214763: Inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells assessed as reduction of [3H]estrone-3-sulfate uptake after 3 mins by beta-counting	ic50	0.8000	uM
(2S,3S,4S,5R,6S)-6-[[5,6-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-2,3-dihydrochromen-7-yl]oxy]-3,4,5-trihydroxyoxane-2-carboxylic acid	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	0.9100	uM
3-[[3-[(E)-2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-[3-(dimethylamino)-3-oxopropyl]sulfanylmethyl]sulfanylpropanoic acid	699544: Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	ki	2.8000	uM
2-hydroxy-5-[[4-(pyridin-2-ylsulfamoyl)phenyl]diazenyl]benzoic acid	699544: Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	ki	3.0000	uM
Rifamycin	679448: TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes	ki	3.0000	uM
(2R,3R)-3,5,7-trihydroxy-2-[7-hydroxy-2-(4-hydroxy-3-methoxyphenyl)-3-(hydroxymethyl)-2,3-dihydro-1-benzofuran-5-yl]-2,3-dihydrochromen-4-one	1214763: Inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells assessed as reduction of [3H]estrone-3-sulfate uptake after 3 mins by beta-counting	ic50	3.6000	uM
2-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-4-one	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	3.8904	uM
(2R,3R)-3,5,7-trihydroxy-2-[(2R,3R)-3-(4-hydroxy-3-methoxyphenyl)-2-(hydroxymethyl)-2,3-dihydro-1,4-benzodioxin-6-yl]-2,3-dihydrochromen-4-one	1214763: Inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells assessed as reduction of [3H]estrone-3-sulfate uptake after 3 mins by beta-counting	ic50	4.5000	uM
Atazanavir	699544: Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	ki	5.1000	uM
Genistein	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	5.2481	uM
Ritonavir	699544: Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	ki	5.9000	uM
2-(3,4-dihydroxyphenyl)-3,7-dihydroxychromen-4-one	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	6.7000	uM
5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	7.0795	uM
Quercetin	1956628: Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay	ic50	7.2444	uM
3-[3-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]diazenyl]-2-hydroxyphenyl]benzoic acid	1217113: Inhibition of OATP2B1-mediated [3H]estrone-3-sulfate uptake in human OATP2B1 expressing HEK293/PDZK1 cells by scintillation counting	ki	8.4800	uM

CTD chemical–gene interactions

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

Chemical	Actions (top 5)	PubMed papers
estrone sulfate	decreases reaction, increases transport, increases uptake, decreases uptake, increases reaction (+3 more)	9
Sulfobromophthalein	affects import, increases import, decreases activity, decreases reaction, increases uptake (+1 more)	6
Cyclosporine	decreases reaction, increases uptake, decreases expression, increases expression, affects expression	6
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation	5
Tetrachlorodibenzodioxin	decreases expression	5
sodium arsenite	affects methylation, decreases expression, increases expression	4
Phenobarbital	affects expression, decreases expression, increases expression	3
Rifampin	decreases reaction, increases expression, increases uptake, decreases expression	3
Aflatoxin B1	affects expression, decreases expression, increases methylation	3
Atorvastatin	decreases reaction, increases uptake	2
Rosiglitazone	decreases reaction, increases uptake, decreases expression	2
Zoledronic Acid	increases expression	2
Arsenic Trioxide	increases expression	2
Lipopolysaccharides	decreases expression, increases expression, decreases reaction, affects response to substance	2
Tobacco Smoke Pollution	decreases reaction, increases import, decreases expression, increases expression	2
Okadaic Acid	decreases expression	2
Mesalamine	decreases reaction, increases uptake, affects uptake	2
5-(N-(4-((4-ethylbenzyl)thio)phenyl)sulfamoyl)-2-methylbenzoic acid	decreases activity	1
daidzein	decreases reaction, increases transport	1
methyleugenol	decreases expression	1
bisphenol A	affects expression	1
senkirkine	decreases expression	1
heliotrine	decreases expression	1
ascorbate-2-phosphate	increases expression, affects binding, affects cotreatment	1
sodium bichromate	decreases expression	1
tris(1,3-dichloro-2-propyl)phosphate	decreases expression	1
cobaltous chloride	increases expression	1
9,10-dihydro-9,10-dihydroxybenzo(a)pyrene	decreases expression	1
ochratoxin A	increases uptake	1
zearalenol	decreases activity	1

ChEMBL screening assays

150 unique, capped per target: 94 admet, 50 functional, 6 binding

Representative assays (with source publication via chembl_document):

Assay ID	Type	Description	Source paper
CHEMBL1743151	ADMET	Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP2B1	Membrane transporters in drug development. — Nat Rev Drug Discov
CHEMBL2075389	Functional	TP_TRANSPORTER: uptake of Salicylic acid at a concentration of 1.43uM in OATP2B1-expressing HEK293 cells	Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. — Drug Metab Dispos
CHEMBL4257832	Binding	Inhibition of human OATP2B1 expressed in HEK293 cells assessed as DBF uptake after 5 mins by fluorescence assay	Deciphering the origins of molecular toxicity of combretastatin A4 and its glycoconjugates: interactions with major drug transporters and their safety profiles in vitro and in vivo. — Medchemcomm

Cellosaurus cell lines

2 cell lines: 2 cancer cell line

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

Cellosaurus	Name	Category	Sex
CVCL_D4US	HuH7-SLCO2B1-KO-c2	Cancer cell line	Male
CVCL_D4UT	HuH7-SLCO2B1-KO-c3	Cancer cell line	Male

Clinical trials (associated diseases)

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