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
• GTEx eGene: eQTL in 16 tissues, sQTL in 16 (q < 0.05)
• ChEMBL bioactivity: 17 clinical-phase molecules tested; no curated mechanism-of-action drug
• Constraint (gnomAD): pLI 0.00 (LoF-tolerant), LOEUF 0.77 (unconstrained)
• MANE Select transcript: NM_007256
• Notable: 111 clinical variants but no curated precision-oncology (CIViC) evidence yet

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: 34 — 26 protein_coding, 6 retained_intron, 1 protein_coding_CDS_not_defined, 1 nonsense_mediated_decay

MANE Select: ENST00000289575

Transcript support level (Ensembl TSL; 1 = fully mRNA-supported): TSL 1: 5, TSL 2: 6, TSL 3: 4, TSL 4: 2, TSL 5: 1

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, ENST00001007978, ENST00001007979, ENST00001027345, ENST00001027346, ENST00001027347, ENST00001116352, ENST00001116709, ENST00001123071, ENST00001143567

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.

Highest expression (Bgee): lobe of liver, liver, sural nerve, upper lobe of left lung, C1 segment of cervical spinal cord.

Genetic regulation across tissues (GTEx eQTL / sQTL)

SLCO2B1 is an eGene in GTEx v10 — its expression is genetically regulated (eQTL) in 16 tissues and its splicing (sQTL) in 16 (q < 0.05). Strongest associations first; slope = normalized effect of the lead variant’s alternative allele.

showing 20 of 32 significant tissue × QTL associations:

Tissue	QTL	q-value	Slope	Lead variant
Testis	eqtl	4.3e-29	+0.45	11:75155062:G:A
Nerve Tibial	sqtl	9.7e-14	-1.42	11:75196376:G:T
Esophagus Mucosa	eqtl	1.3e-13	-0.38	11:75152238:T:A
Lung	sqtl	2.2e-11	+1.37	11:75196376:G:T
Adipose Subcutaneous	sqtl	2.4e-11	-1.15	11:75196376:G:T
Colon Transverse	sqtl	3.2e-09	-1.73	11:75196376:G:T
Pancreas	eqtl	1.1e-05	-0.31	11:75155998:C:G
Small Intestine Terminal Ileum	sqtl	1.7e-05	+2.04	11:75196376:G:T
Liver	eqtl	2.3e-05	+0.25	11:75155998:C:G
Liver	sqtl	4.8e-05	+0.71	11:75159374:T:C
Adrenal Gland	sqtl	9.7e-05	-1.45	11:75196376:G:T
Esophagus Muscularis	sqtl	1.9e-04	+0.90	11:75196537:C:T
Thyroid	eqtl	3.5e-04	-0.16	11:75156560:T:A
Breast Mammary Tissue	sqtl	3.5e-04	-1.24	11:75196376:G:T
Skin Sun Exposed Lower leg	sqtl	5.8e-04	-0.89	11:75196376:G:T
Colon Transverse	eqtl	2.2e-03	-0.11	11:75139268:A:G
Thyroid	sqtl	3.5e-03	+0.62	11:75208302:A:G
Brain Caudate basal ganglia	sqtl	6.9e-03	-1.16	11:75196159:A:C
Heart Left Ventricle	sqtl	8.9e-03	-1.13	11:75196376:G:T
Testis	sqtl	9.8e-03	-2.31	11:74455859:C:A

FANTOM5 promoters

showing 10 of 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

showing 100 of 290 tissues 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
peritoneum	UBERON:0002358	89.48	gold quality
duodenum	UBERON:0002114	89.47	gold quality
caecum	UBERON:0001153	89.29	gold quality
smooth muscle tissue	UBERON:0001135	88.96	gold quality
apex of heart	UBERON:0002098	88.63	gold quality
lower lobe of lung	UBERON:0008949	88.60	gold quality
substantia nigra	UBERON:0002038	88.54	gold quality
caudate nucleus	UBERON:0001873	88.48	gold quality
hypothalamus	UBERON:0001898	88.32	gold quality
decidua	UBERON:0002450	88.31	gold quality
left uterine tube	UBERON:0001303	88.30	gold quality
adipose tissue of abdominal region	UBERON:0007808	88.26	gold quality
intestine	UBERON:0000160	88.22	gold quality
descending thoracic aorta	UBERON:0002345	88.06	gold quality
right frontal lobe	UBERON:0002810	87.97	gold quality
amygdala	UBERON:0001876	87.88	gold quality
left coronary artery	UBERON:0001626	87.81	gold quality
putamen	UBERON:0001874	87.70	gold quality
prefrontal cortex	UBERON:0000451	87.40	gold quality
midbrain	UBERON:0001891	87.40	gold quality
coronary artery	UBERON:0001621	87.29	gold quality
colon	UBERON:0001155	87.27	gold quality
thoracic aorta	UBERON:0001515	87.26	gold quality
large intestine	UBERON:0000059	87.04	gold quality
mucosa of stomach	UBERON:0001199	86.97	gold quality
ascending aorta	UBERON:0001496	86.89	gold quality
visceral pleura	UBERON:0002401	86.36	gold quality
dorsal motor nucleus of vagus nerve	UBERON:0002870	86.26	gold quality
nucleus accumbens	UBERON:0001882	86.08	gold quality
subcutaneous adipose tissue	UBERON:0002190	86.04	gold quality
body of pancreas	UBERON:0001150	85.98	gold quality
lower esophagus muscularis layer	UBERON:0035833	85.91	gold quality
lower esophagus	UBERON:0013473	85.86	gold quality
cingulate cortex	UBERON:0003027	85.81	gold quality
corpus callosum	UBERON:0002336	85.75	gold quality
anterior cingulate cortex	UBERON:0009835	85.71	gold quality
Ammon’s horn	UBERON:0001954	85.47	gold quality
placenta	UBERON:0001987	85.32	gold quality
inferior vagus X ganglion	UBERON:0005363	85.11	gold quality
esophagogastric junction muscularis propria	UBERON:0035841	84.92	gold quality
frontal cortex	UBERON:0001870	84.74	gold quality
endocervix	UBERON:0000458	84.69	gold quality
muscle layer of sigmoid colon	UBERON:0035805	84.64	gold quality
adipose tissue	UBERON:0001013	84.55	gold quality
telencephalon	UBERON:0001893	84.39	gold quality
neocortex	UBERON:0001950	84.38	gold quality
layer of synovial tissue	UBERON:0007616	84.20	gold quality
sigmoid colon	UBERON:0001159	84.18	gold quality
Brodmann (1909) area 9	UBERON:0013540	84.12	gold quality
urinary bladder	UBERON:0001255	84.05	gold quality
temporal lobe	UBERON:0001871	83.87	gold quality
forebrain	UBERON:0001890	83.85	gold quality
heart left ventricle	UBERON:0002084	83.83	gold quality
esophagus	UBERON:0001043	83.81	gold quality
right lobe of thyroid gland	UBERON:0001119	83.77	gold quality
connective tissue	UBERON:0002384	83.74	gold quality
right ovary	UBERON:0002118	83.59	gold quality
cardiac ventricle	UBERON:0002082	83.55	gold quality
right atrium auricular region	UBERON:0006631	83.52	gold quality
cerebral cortex	UBERON:0000956	83.45	gold quality
dorsolateral prefrontal cortex	UBERON:0009834	83.39	gold quality
central nervous system	UBERON:0001017	83.30	gold quality
middle frontal gyrus	UBERON:0002702	83.30	gold quality
left lobe of thyroid gland	UBERON:0001120	83.11	gold quality
heart	UBERON:0000948	83.04	gold quality
body of uterus	UBERON:0009853	83.02	gold quality
brain	UBERON:0000955	83.01	gold quality
minor salivary gland	UBERON:0001830	83.00	gold quality
tonsil	UBERON:0002372	82.66	gold quality
thyroid gland	UBERON:0002046	82.64	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

HPA expression

RNA tissue specificity: Tissue enhanced

showing 60 of 77 HPA tissues / cells by nTPM:

Tissue / cell	Axis	nTPM	Protein (IHC)
Liver	tissue	214.5	low
Locus coeruleus	tissue	101.0
Hippocampus	tissue	94.7	medium
Choroid plexus	tissue	72.7
Nucleus accumbens	tissue	66.2
Lung	tissue	57.2	low
Lymph node	tissue	56.3	not detected
Small intestine	tissue	48.3	not detected
Spinal cord	tissue	45.8
Substantia nigra	tissue	45.7
Hypothalamus	tissue	44.9
Spleen	tissue	43.8	not detected
Placenta	tissue	41.2	not detected
Duodenum	tissue	39.6	not detected
Medulla oblongata	tissue	39.0
Pons	tissue	38.7
Septum	tissue	38.1
Adipose tissue	tissue	37.3	not detected
Midbrain	tissue	37.1
Putamen	tissue	36.8
Thalamus	tissue	35.8
Corpus callosum	tissue	35.4
Periaqueductal gray	tissue	35.0
Superior colliculi	tissue	34.0
Postcentral gyrus	tissue	32.9
Ventral forebrain	tissue	32.6
Appendix	tissue	32.0	not detected
Basal ganglia	tissue	30.3	not detected
Adrenal gland	tissue	29.7	medium
Amygdala	tissue	29.1
Colon	tissue	29.0	not detected
Cerebral cortex	tissue	28.1	not detected
Insular cortex	tissue	28.1
Motor cortex	tissue	27.5
Hippocampal formation	tissue	27.5
Tonsil	tissue	26.7	not detected
Gallbladder	tissue	26.6	not detected
Prefrontal cortex	tissue	25.2
Entorhinal cortex	tissue	25.2
Temporal cortex	tissue	25.2
Urinary bladder	tissue	24.6	not detected
Smooth muscle	tissue	24.5	not detected
Retrosplenial cortex	tissue	24.0
Occipital cortex	tissue	23.4
Somatosensory cortex	tissue	23.1
Retrosplenial and cingulate cortex	tissue	22.9
Rectum	tissue	22.2	not detected
Pancreas	tissue	20.8	medium
Olfactory bulb	tissue	19.8
Kidney	tissue	19.6	not detected
Esophagus	tissue	18.5	not detected
Cervix	tissue	17.0	not detected
Thymus	tissue	15.6
Heart muscle	tissue	14.6	medium
Stomach 1	tissue	14.1	medium
Caudate putamen	tissue	13.7
Ovary	tissue	13.4	low
Frontal cortex	tissue	12.6
Fallopian tube	tissue	12.4	not detected
Cerebellum	tissue	12.0	not detected

Brain sub-regions (HPA Brain Atlas): detected in 190; highest nTPM — Nucleus rhomboideus (198.7), Nucleus gracilis (188.6), Nucleus raphe pallidus (165.4), Anterior thalamic nucleus, ventral (163.7), Medial olivary nucleus (159.9).

Regulation

Is transcription factor: no

Upstream regulators (CollecTRI, top): AHR, HNF1A

miRNA regulators (miRDB)

Targeting SLCO2B1 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific).

showing 30 of 62 miRNAs:

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

Functional genomics

gnomAD constraint: pLI 1.68e-07, LOEUF 0.772, missense Z 1.37 — population loss-of-function intolerance (pLI ≥ 0.9 = LoF-intolerant; lower LOEUF = more constrained). gnomAD

Regional missense constraint (gnomAD RMC): no regional variation along ENST00000289575 — one region, missense o/e 0.91.

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
caenorhabditis_elegans		WBGENE00009023

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

Mouse-model phenotypes

Observed phenotypes of the mouse ortholog (MGI:1351872) from MGI (Alliance of Genome Resources) — knockout/mutant phenotypes, ranked by annotation count. 3 distinct phenotype terms.

Mouse phenotype (MP)	Records
increased body weight	1
increased blood urea nitrogen level	1
abnormal xenobiotic pharmacokinetics	1

Additional cross-species homologs

Sequence homologs in species beyond Ensembl Compara’s model organisms, by Diamond local protein alignment (% sequence identity; best hit per species). Lower-identity rows are more distant homologs. The matched accessions’ gene symbols aren’t in biobtree yet, so each row shows the UniProt accession.

Organism	UniProt	Identity	Method
Pongo abelii	Q5RFF0	97.9%	Diamond
Bos taurus	Q8HYW2	97.2%	Diamond

Genomic neighbors (locus context)

Genes flanking this one on the chromosome (NCBI/Entrez gene neighborhood). Positional context only — some neighbors share regulatory elements (bidirectional promoters, antisense/overlapping transcripts), but chromosomal adjacency is not itself a functional relationship (see Interactions for that).

Symbol	Type	Entrez
TPBGL	protein-coding	100507050
TPBGL-AS1	ncRNA	105369388
OR2AT4	protein-coding	341152

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)

• 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

Predicted structure (AlphaFold)

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

Human Protein Atlas

Protein class: Metabolic proteins, Transporters, Electrochemical Potential-driven transporters, Predicted membrane proteins, Predicted intracellular proteins

Protein evidence: Evidence at protein level

Antibody reliability (HPA): IH uncertain

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)

Position	Role
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)

Type	Positions
Phosphoserine	34, 320
Phosphothreonine	318

Disulfide bonds (3)

Type	Positions
Disulfide bond	489–520, 495–516, 504–541

Glycosylation sites (2)

Type	Positions
N-linked (glcnac…) asparagine	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-affinity and no …
607	loss of e1s transport; small decrease in cell surface expression. strong decrease in low-affinity transport of e1s and loss of …
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 and higher vmax/km …
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 transport.
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 taurocholate …
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 transport activity …
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 transport activity …

Function

Pathways and Gene Ontology

Reactome pathways

4 curated (TAS) of 7; 0 disease pathways. Curated-first; evidence = TAS (manually curated) vs IEA (electronic inference).

7 pathways:

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

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 (8): xenobiotic metabolic process (GO:0006805), monoatomic ion transport (GO:0006811), 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 (5): bile acid transmembrane transporter activity (GO:0015125), prostaglandin transmembrane transporter activity (GO:0015132), secondary active transmembrane transporter activity (GO:0015291), 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

5 top-level categories:

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

29 GO namespaces:

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
active 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

Experimentally-supported GO annotations

GO terms backed by direct experimental evidence (ECO experimental codes) — 7 of 19 annotations. The rest are phylogenetic / computational / electronic (IEA).

7 experimentally-supported GO terms:

GO term	NS	Evidence
transmembrane transport	BP	direct assay
apical plasma membrane	CC	direct assay
basal plasma membrane	CC	direct assay
plasma membrane	CC	direct assay
prostaglandin transmembrane transporter activity	MF	direct assay
secondary active transmembrane transporter activity	MF	direct assay
transmembrane transporter activity	MF	direct assay

Protein interactions and networks

STRING

showing 15 of 836 interactions by confidence (×1000):

Protein A	Protein B	Partner UniProt	Score
SLCO2B1	ABCG2	Q9UNQ0	746
SLCO2B1	SLC22A7	Q9Y694	742
SLCO2B1	SLC22A8	Q8TCC7	737
SLCO2B1	SLC10A1	Q14973	719
SLCO2B1	ABCC2	Q92887	715
SLCO2B1	SLC22A9	Q8IVM8	702
SLCO2B1	ABCC3	O15438	702
SLCO2B1	ABCC4	O15439	702
SLCO2B1	SLC15A1	P46059	700
SLCO2B1	SLC22A1	O15245	688
SLCO2B1	SLC47A1	Q96FL8	662
SLCO2B1	ABCB1	P08183	655
SLCO2B1	SLC22A11	Q9NSA0	655
SLCO2B1	ABCB11	O95342	653
SLCO2B1	CYP3A4	P05184	622

IntAct

Human interaction partners of SLCO2B1 in IntAct, one row per partner (best MIscore; records = supporting IntAct interaction records).

showing 30 of 77 partners by confidence:

Partner	Interaction type	MIscore	Records
PATJ	direct interaction	0.440	9
GRIP1	direct interaction	0.440	5
GRIP2	direct interaction	0.440	4
MAGI2	direct interaction	0.440	4
DLG3	direct interaction	0.440	3
FRMPD2	direct interaction	0.440	3
LNX1	direct interaction	0.440	3
MPDZ	direct interaction	0.440	3
NHERF4	direct interaction	0.440	3
SCRIB	direct interaction	0.440	3
APBA1	direct interaction	0.440	2
APBA2	direct interaction	0.440	2
DLG4	direct interaction	0.440	2
GRID2IP	direct interaction	0.440	2
IL16	direct interaction	0.440	2
LNX2	direct interaction	0.440	2
MAGI1	direct interaction	0.440	2
PDZK1	direct interaction	0.440	2
TJP1	direct interaction	0.440	2
WHRN	direct interaction	0.440	2
AHNAK	direct interaction	0.440	1
APBA3	direct interaction	0.440	1
ARHGEF12	direct interaction	0.440	1
CARD11	direct interaction	0.440	1
CASK	direct interaction	0.440	1
DLG1	direct interaction	0.440	1
DLG2	direct interaction	0.440	1
DLG5	direct interaction	0.440	1
DVL3	direct interaction	0.440	1
FRMPD1	direct interaction	0.440	1

BioGRID (17 interactions; top human partners by supporting records): APP (Reconstituted Complex), ATP5H (Affinity Capture-MS), ATP5I (Affinity Capture-MS), ATP5J (Affinity Capture-MS), CANX (Affinity Capture-MS), CLGN (Affinity Capture-MS), HSP90B1 (Cross-Linking-MS (XL-MS)), JPH1 (Affinity Capture-MS), KRAS (Proximity Label-MS), NUCKS1 (Cross-Linking-MS (XL-MS)), PDIA3 (Affinity Capture-MS), PGRMC2 (Affinity Capture-MS), PLD3 (Affinity Capture-MS), SEC61B (Affinity Capture-MS), SLC28A2 (Affinity Capture-MS)

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

Genetic variants

Variant evidence for SLCO2B1: 111 ClinVar records (0 pathogenic / likely pathogenic); 4 PharmGKB clinical annotations.

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

SpliceAI

Top 10 splice-impact sites by Δscore (adjacent positions with the same effect merged into one range; 45 predictions of 1,347):

Position(s)	Effect	Δscore	Sites
11:75164101–75164102	donor_loss	1.0000	4
11:75165785–75165786	acceptor_loss	1.0000	3
11:75165950–75165951	donor_loss	1.0000	5
11:75172377–75172378	acceptor_loss	1.0000	4
11:75172570–75172571	donor_loss	1.0000	5
11:75188239–75188240	donor_loss	1.0000	4
11:75162786–75162787	donor_loss	0.9900	6
11:75165785–75165786	acceptor_loss	0.9900	2
11:75169171–75169172	acceptor_loss	0.9900	6
11:75169407–75169408	donor_loss	0.9900	6

AlphaMissense

1,298 missense substitutions predicted likely pathogenic (of 4,609 scored), across 371 residues. Top 20 hotspot residues, ranked by the number of likely-pathogenic substitutions (of those reachable by a single-nucleotide change), then by mean score:

Residue	Likely-pathogenic substitutions	Mean am_pathogenicity	Max am_pathogenicity
D623	8	0.970	0.991
D215	8	0.943	0.979
F51	8	0.938	0.990
D216	8	0.903	0.960
D269	8	0.898	0.961
F297	8	0.879	0.967
F360	8	0.820	0.933
C639	7	0.993	0.997
C626	7	0.992	0.996
F402	7	0.990	0.996
F393	7	0.983	0.995
C520	7	0.978	0.993
W272	7	0.975	0.995
W276	7	0.971	0.997
C539	7	0.967	0.985
W277	7	0.963	0.997
C465	7	0.959	0.980
C504	7	0.957	0.982
E77	7	0.954	0.994
F80	7	0.950	0.985

HPA cancer prognostics

RNA cancer specificity: Low cancer specificity

Human Protein Atlas survival analysis — favorable = higher expression predicts better survival.

1 prognostic cancer types:

Cancer	Prognostic	p-value
Kidney Renal Clear Cell Carcinoma (TCGA)	favorable	8.52e-05

Disease associations

OMIM: gene MIM:604988 | disease phenotypes:

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (1): CHEMBL1743124 (SINGLE PROTEIN)

Molecules with ChEMBL bioactivity

Phase ≥1, by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 738,029 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

17 molecules by phase:

Molecule	Name	Phase	Patents
CHEMBL1163	ATAZANAVIR	4	22,353
CHEMBL160	CYCLOSPORINE	4	169,776
CHEMBL461101	ELTROMBOPAG	4	625
CHEMBL553	ERLOTINIB	4	109,860
CHEMBL374478	RIFAMPIN	4	94,660
CHEMBL437765	RIFAMYCIN	4	2,833
CHEMBL163	RITONAVIR	4	54,258
CHEMBL421	SULFASALAZINE	4	74,280
CHEMBL297453	EPIGALOCATECHIN GALLATE	3	23,201
CHEMBL50	QUERCETIN	3	75,572
CHEMBL431701	SILYBIN A	3	6,362
CHEMBL31574	FISETIN	2	7,874
CHEMBL44	GENISTEIN	2	44,589
CHEMBL250450	ISOQUERCETIN	2	1,676
CHEMBL151	LUTEOLIN	2	23,845
CHEMBL4802105	SILICRISTIN	2	19
CHEMBL150	KAEMPFEROL	1	26,246

PharmGKB: 1 entry (CPIC guideline: no)

PharmGKB clinical annotations

4 annotations by evidence level (1 strongest → 4):

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

PharmGKB variants

3 variants:

Variant	Genes	Level	Score	#Clin annots	Drugs
rs2306168	SLCO2B1	3	1.00	1	fexofenadine
rs12422149	SLCO2B1	3	1.62	2	montelukast;rosuvastatin
rs3781727	SLCO2B1	3	0.12	1	voriconazole

PharmGKB variant annotations

Per-publication pharmacogenomic findings for this gene (significant associations).

15 published findings:

Variant	Drug(s)	Category	Finding	PMID
rs12422149	chloroquine, primaquine	Efficacy	Genotype GG is associated with increased severity of Parasitemia when treated with chloroquine and primaquine in people with Malaria as compared to genotypes AA + AG.	PMID:28975866
rs12422149	rosuvastatin	Efficacy	Genotypes AA + AG are associated with decreased response to rosuvastatin in healthy individuals as compared to genotype GG.	PMID:28627804
rs2306168	rosuvastatin	Metabolism/PK	Allele T is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele C.	PMID:34594217
rs142693902	rosuvastatin	Metabolism/PK	Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G.	PMID:34594217
rs35199625	rosuvastatin	Metabolism/PK	Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G.	PMID:34594217
rs12422149	tamoxifen	Metabolism/PK	Genotypes AA + AG is associated with increased concentrations of tamoxifen in women with Breast Neoplasms as compared to genotype GG.	PMID:36373739
rs1077858	abiraterone	Metabolism/PK	Genotypes AA + AG is associated with increased concentrations of abiraterone in healthy individuals as compared to genotype GG.	PMID:37574850
rs12422149	4-hydroxyatorvastatin, 4-hydroxyatorvastatin lactone	Metabolism/PK	Genotype AG is associated with increased concentrations of 4-hydroxyatorvastatin and 4-hydroxyatorvastatin lactone in people with Coronary Disease as compared to genotype GG.	PMID:38293288
rs1009122956	estrone sulfate, rosuvastatin	Metabolism/PK	Allele C is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele G.	PMID:40154787
rs1621378	estrone sulfate, rosuvastatin	Metabolism/PK	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.	PMID:40154787
rs199654337	estrone sulfate, rosuvastatin	Metabolism/PK	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate or rosuvastatin HEK293 cells expressing OATP2B1 variants as compared to allele C.	PMID:40154787
rs2306168	estrone sulfate	Metabolism/PK	Allele T is associated with decreased transport of SLCO2B1 when assayed with estrone sulfate HEK293 cells expressing OATP2B1 variants as compared to allele C.	PMID:40154787
rs2306168	pitavastatin	Metabolism/PK	Genotype CT is associated with increased concentrations of pitavastatin in healthy individuals as compared to genotype CC.	PMID:42212460
rs12422149	montelukast	Efficacy, Metabolism/PK	Genotype AG is associated with decreased response to montelukast in people with Asthma as compared to genotype GG.	PMID:19151602
rs2306168	fexofenadine	Metabolism/PK	Allele T is associated with decreased area under the plasma concentration-time curve when treated with fexofenadine in healthy individuals as compared to genotype CC.	PMID:21280267

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

Binding affinities (BindingDB)

40 measured of 44 human assays (52 total across all organisms); most potent 40 below. Values come from heterogeneous assays and are not directly comparable.

Ligand	Measure	Value
HOE-33342	KI	0.9 nM
(3R,5R)-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-{[(2S)-2-methylbutanoyl]oxy}-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid	IC50	30 nM
CHEMBL6163420	EC50	89 nM
Naringenin, 18	IC50	710 nM
CHEMBL5277249	IC50	910 nM
cid_5280863	IC50	1050 nM
CHEMBL6161472	IC50	1060 nM
2-(3,4-Dihydroxy-phenyl)-5,7-dihydroxy-3-((2S,4R,5R)-3,4,5-trihydroxy-6-hydroxymethyl-tetrahydro-pyran-2-yloxy)-chromen-4-one	IC50	1320 nM
(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecone	IC50	1400 nM
OROXYLIN A	IC50	1480 nM
CHEMBL6146403	EC50	2010 nM
Prunetol	IC50	2210 nM
Salazosulfapyridine	IC50	3040 nM
ELTROMBOPAG	IC50	3100 nM
CHEMBL6162249	EC50	3340 nM
CHEMBL6161464	EC50	3830 nM
CHEMBL6150561	EC50	3890 nM
CHEMBL6151074	EC50	4390 nM
Quercetin 3-O-beta-D-glucoside	IC50	4500 nM
CHEMBL6171119	EC50	4670 nM
CHEMBL6172851	EC50	4750 nM
(2S)-5,7-dihydroxy-2-(4-hydroxyphenyl)-3,4-dihydro-2H-1-benzopyran-4-one	IC50	4960 nM
Adriamycin	IC50	10000 nM
3-[(R)-{3-[(E)-2-(7-Chloro-quinolin-2-yl)-vinyl]-phenyl}-(2-dimethylcarbamoyl-ethylsulfanyl)-methylsulfanyl]-propionic acid	IC50	10000 nM
ABT-538	IC50	12000 nM
CHEMBL6161092	IC50	12100 nM
5,6,7-trihydroxy-2-(4-hydroxyphenyl)-4H-chromen-4-one	IC50	12500 nM
CHEBI:17558	IC50	18000 nM
SILYBIN A	IC50	18000 nM
CHEMBL3542370	IC50	50000 nM
(-)-Epigallocatechin-3-o-gallate	IC50	58000 nM
CHEMBL509624	IC50	61500 nM
scutellarin	IC50	63400 nM
CGP 73547	IC50	67800 nM
2-(3,4-dihydroxyphenyl)-3,5,7,8-tetrahydroxy-4H-chromen-4-one	IC50	82000 nM
NSC-407303	IC50	100000 nM
indometacin	IC50	235000 nM
CB-01-11	KD	1e+06 nM
Silybin B	IC50	1.64e+06 nM
eriodicryol	IC50	1.66e+06 nM

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

39 with measured affinity, of 511 total; 27 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
1-[2-(2-methoxyanilino)-2-oxoethyl]-N-(3-methoxyphenyl)indazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.1240	uM
1-[2-(4-chloroanilino)-2-oxoethyl]-N-pyridin-3-ylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.1550	uM
1-[2-(2,5-dichloroanilino)-2-oxoethyl]-N-pyridin-2-ylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.1670	uM
1-[1-(2-methylanilino)-1-oxopropan-2-yl]-N-phenylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.1700	uM
1-[1-(4-fluoroanilino)-1-oxopropan-2-yl]-N-phenylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.2650	uM
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
1-[1-(4-methoxyanilino)-1-oxopropan-2-yl]-N-phenylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.3870	uM
1-(1-anilino-1-oxopropan-2-yl)-N-(4-chlorophenyl)indazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.4020	uM
1-(1-anilino-1-oxopropan-2-yl)-N-phenylindazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.4200	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
1-[2-(3-methoxyanilino)-2-oxoethyl]-N-(3-methoxyphenyl)indazole-3-carboxamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.5830	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
N-(3,4-dichlorophenyl)-2-[3-(4-methylsulfonylphenyl)indazol-1-yl]acetamide	2236920: Inhibition of OATP2B1 (unknown origin) transfected in human A-431 cells assessed as inhibition of pyranine uptake preincubated for 5 mins followed by pyranine addition and measured after 15 mins by fluorescence based analysis	ic50	0.8260	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 import, decreases activity, affects reaction, increases transport (+3 more)	9
Sulfobromophthalein	decreases reaction, increases uptake, affects reaction, affects import, increases import (+1 more)	6
Cyclosporine	affects expression, decreases reaction, increases uptake, decreases expression, increases expression	6
Benzo(a)pyrene	affects methylation, decreases expression, decreases methylation	5
Tetrachlorodibenzodioxin	decreases expression	5
sodium arsenite	decreases expression, increases expression, affects methylation	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	affects binding, affects cotreatment, increases expression	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

3 cell lines: 3 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
CVCL_F6GR	EDITGENE SLCO2B1 Knockout HuH-7 Cell Line	Cancer cell line	Male

Clinical trials (associated diseases)

Via MONDO — disease-level, not drug-specific.

Predicted chemistry — Sugi Predict

The predicted patent-compound landscape for SLCO2B1 across ~30M SureChEMBL compounds — explore on Sugi Predict.