# SLCO2B1

> Gene · canonical: https://sugi.bio/atlas/gene/SLCO2B1/
> Atlas v1.12.2 · generated 2026-10-13T13:32:47+00:00

## 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](https://www.ncbi.nlm.nih.gov/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](https://www.ebi.ac.uk/gxa/sc/experiments/E-MTAB-6678) | yes | 1711.75 |
| [E-MTAB-7381](https://www.ebi.ac.uk/gxa/sc/experiments/E-MTAB-7381) | yes | 627.58 |
| [E-GEOD-84465](https://www.ebi.ac.uk/gxa/sc/experiments/E-GEOD-84465) | yes | 38.68 |
| [E-HCAD-35](https://www.ebi.ac.uk/gxa/sc/experiments/E-HCAD-35) | yes | 32.26 |
| [E-ANND-3](https://www.ebi.ac.uk/gxa/sc/experiments/E-ANND-3) | yes | 26.59 |
| [E-HCAD-25](https://www.ebi.ac.uk/gxa/sc/experiments/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](https://gnomad.broadinstitute.org/)

**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](https://www.informatics.jax.org/marker/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](https://www.uniprot.org/uniprotkb/Q5RFF0/entry) | 97.9% | Diamond |
| Bos taurus | [Q8HYW2](https://www.uniprot.org/uniprotkb/Q8HYW2/entry) | 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](/atlas/gene/TPBGL/) | protein-coding | 100507050 |
| [TPBGL-AS1](/atlas/gene/TPBGL-AS1/) | ncRNA | 105369388 |
| [OR2AT4](/atlas/gene/OR2AT4/) | protein-coding | 341152 |

<a id="protein-O94956"></a>

## 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 →](https://www.uniprot.org/uniprotkb/O94956/entry)

**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](https://amigo.geneontology.org/amigo/term/GO:0055085) | BP | direct assay |
| [apical plasma membrane](https://amigo.geneontology.org/amigo/term/GO:0016324) | CC | direct assay |
| [basal plasma membrane](https://amigo.geneontology.org/amigo/term/GO:0009925) | CC | direct assay |
| [plasma membrane](https://amigo.geneontology.org/amigo/term/GO:0005886) | CC | direct assay |
| [prostaglandin transmembrane transporter activity](https://amigo.geneontology.org/amigo/term/GO:0015132) | MF | direct assay |
| [secondary active transmembrane transporter activity](https://amigo.geneontology.org/amigo/term/GO:0015291) | MF | direct assay |
| [transmembrane transporter activity](https://amigo.geneontology.org/amigo/term/GO:0022857) | 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](#clinvar) (0 pathogenic / likely pathogenic); [4 PharmGKB clinical annotations](#pharmgkb-clinical).

#### 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](/atlas/drug/atazanavir/) | 4 | 22,353 |
| CHEMBL160 | [CYCLOSPORINE](/atlas/drug/cyclosporine/) | 4 | 169,776 |
| CHEMBL461101 | [ELTROMBOPAG](/atlas/drug/eltrombopag/) | 4 | 625 |
| CHEMBL553 | [ERLOTINIB](/atlas/drug/erlotinib/) | 4 | 109,860 |
| CHEMBL374478 | [RIFAMPIN](/atlas/drug/rifampin/) | 4 | 94,660 |
| CHEMBL437765 | [RIFAMYCIN](/atlas/drug/rifamycin/) | 4 | 2,833 |
| CHEMBL163 | [RITONAVIR](/atlas/drug/ritonavir/) | 4 | 54,258 |
| CHEMBL421 | [SULFASALAZINE](/atlas/drug/sulfasalazine/) | 4 | 74,280 |
| CHEMBL297453 | [EPIGALOCATECHIN GALLATE](/atlas/drug/epigalocatechin-gallate/) | 3 | 23,201 |
| CHEMBL50 | [QUERCETIN](/atlas/drug/quercetin/) | 3 | 75,572 |
| CHEMBL431701 | [SILYBIN A](/atlas/drug/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](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | Efficacy | 3 | [montelukast](/atlas/drug/montelukast/) | Asthma |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | Efficacy | 3 | [rosuvastatin](/atlas/drug/rosuvastatin/) |  |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | Metabolism/PK | 3 | [fexofenadine](/atlas/drug/fexofenadine/) |  |
| [rs3781727](https://www.ncbi.nlm.nih.gov/snp/rs3781727) | Metabolism/PK | 3 | [voriconazole](/atlas/drug/voriconazole/) |  |

#### PharmGKB variants

3 variants:

| Variant | Genes | Level | Score | #Clin annots | Drugs |
| --- | --- | --- | --- | --- | --- |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | [SLCO2B1](/atlas/gene/SLCO2B1/) | 3 | 1.00 | 1 | [fexofenadine](/atlas/drug/fexofenadine/) |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | [SLCO2B1](/atlas/gene/SLCO2B1/) | 3 | 1.62 | 2 | montelukast;rosuvastatin |
| [rs3781727](https://www.ncbi.nlm.nih.gov/snp/rs3781727) | [SLCO2B1](/atlas/gene/SLCO2B1/) | 3 | 0.12 | 1 | [voriconazole](/atlas/drug/voriconazole/) |

#### PharmGKB variant annotations

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

15 published findings:

| Variant | Drug(s) | Category | Finding | PMID |
| --- | --- | --- | --- | --- |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | [chloroquine](/atlas/drug/chloroquine/), [primaquine](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/28975866/) |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | [rosuvastatin](/atlas/drug/rosuvastatin/) | Efficacy | Genotypes AA + AG are associated with decreased response to rosuvastatin in healthy individuals as compared to genotype GG. | [PMID:28627804](https://pubmed.ncbi.nlm.nih.gov/28627804/) |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | [rosuvastatin](/atlas/drug/rosuvastatin/) | Metabolism/PK | Allele T is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele C. | [PMID:34594217](https://pubmed.ncbi.nlm.nih.gov/34594217/) |
| [rs142693902](https://www.ncbi.nlm.nih.gov/snp/rs142693902) | [rosuvastatin](/atlas/drug/rosuvastatin/) | Metabolism/PK | Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G. | [PMID:34594217](https://pubmed.ncbi.nlm.nih.gov/34594217/) |
| [rs35199625](https://www.ncbi.nlm.nih.gov/snp/rs35199625) | [rosuvastatin](/atlas/drug/rosuvastatin/) | Metabolism/PK | Allele A is associated with decreased uptake of rosuvastatin in transfected HEK293T cells as compared to allele G. | [PMID:34594217](https://pubmed.ncbi.nlm.nih.gov/34594217/) |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | [tamoxifen](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/36373739/) |
| [rs1077858](https://www.ncbi.nlm.nih.gov/snp/rs1077858) | [abiraterone](/atlas/drug/abiraterone/) | Metabolism/PK | Genotypes AA + AG is associated with increased concentrations of abiraterone in healthy individuals as compared to genotype GG. | [PMID:37574850](https://pubmed.ncbi.nlm.nih.gov/37574850/) |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/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](https://pubmed.ncbi.nlm.nih.gov/38293288/) |
| [rs1009122956](https://www.ncbi.nlm.nih.gov/snp/rs1009122956) | [estrone sulfate](/atlas/drug/estrone-sulfuric-acid/), [rosuvastatin](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/40154787/) |
| [rs1621378](https://www.ncbi.nlm.nih.gov/snp/rs1621378) | [estrone sulfate](/atlas/drug/estrone-sulfuric-acid/), [rosuvastatin](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/40154787/) |
| [rs199654337](https://www.ncbi.nlm.nih.gov/snp/rs199654337) | [estrone sulfate](/atlas/drug/estrone-sulfuric-acid/), [rosuvastatin](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/40154787/) |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | [estrone sulfate](/atlas/drug/estrone-sulfuric-acid/) | 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](https://pubmed.ncbi.nlm.nih.gov/40154787/) |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | [pitavastatin](/atlas/drug/pitavastatin/) | Metabolism/PK | Genotype CT is associated with increased concentrations of pitavastatin in healthy individuals as compared to genotype CC. | [PMID:42212460](https://pubmed.ncbi.nlm.nih.gov/42212460/) |
| [rs12422149](https://www.ncbi.nlm.nih.gov/snp/rs12422149) | [montelukast](/atlas/drug/montelukast/) | Efficacy, Metabolism/PK | Genotype AG is associated with decreased response to montelukast in people with Asthma as compared to genotype GG. | [PMID:19151602](https://pubmed.ncbi.nlm.nih.gov/19151602/) |
| [rs2306168](https://www.ncbi.nlm.nih.gov/snp/rs2306168) | [fexofenadine](/atlas/drug/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](https://pubmed.ncbi.nlm.nih.gov/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](/atlas/drug/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](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6162249/) |
| 6.81 | IC50 | 155 | nM | [CHEMBL6171119](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6171119/) |
| 6.78 | IC50 | 167 | nM | [CHEMBL6163420](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6163420/) |
| 6.77 | IC50 | 170 | nM | [CHEMBL6150561](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6150561/) |
| 6.58 | IC50 | 265 | nM | [CHEMBL6151074](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6151074/) |
| 6.46 | IC50 | 350 | nM | [SCUTELLAREIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL55415/) |
| 6.46 | IC50 | 346.7 | nM | [SCUTELLAREIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL55415/) |
| 6.41 | IC50 | 387 | nM | [CHEMBL6172851](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6172851/) |
| 6.40 | IC50 | 402 | nM | [CHEMBL6161092](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6161092/) |
| 6.38 | IC50 | 420 | nM | [CHEMBL6161464](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6161464/) |
| 6.28 | Ki | 530 | nM | [ERLOTINIB](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL553/) |
| 6.26 | IC50 | 550 | nM | [ERLOTINIB](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL553/) |
| 6.23 | IC50 | 583 | nM | [CHEMBL6146403](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6146403/) |
| 6.10 | IC50 | 800 | nM | [SILYBIN B](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL592675/) |
| 6.08 | IC50 | 826 | nM | [CHEMBL6161472](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL6161472/) |
| 6.04 | IC50 | 910 | nM | [CHEMBL5277249](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL5277249/) |
| 6.04 | IC50 | 912 | nM | [CHEMBL5277249](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL5277249/) |
| 5.55 | Ki | 2800 | nM | [MK-571](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL15177/) |
| 5.54 | IC50 | 2900 | nM | [MK-571](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL15177/) |
| 5.52 | Ki | 3000 | nM | [RIFAMYCIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL437765/) |
| 5.52 | Ki | 3000 | nM | [SULFASALAZINE](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL421/) |
| 5.52 | IC50 | 3000 | nM | [SULFASALAZINE](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL421/) |
| 5.44 | IC50 | 3600 | nM | [SILICRISTIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL4802105/) |
| 5.41 | IC50 | 3900 | nM | [LUTEOLIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL151/) |
| 5.41 | IC50 | 3890 | nM | [LUTEOLIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL151/) |
| 5.35 | IC50 | 4500 | nM | [SILYBIN A](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL431701/) |
| 5.29 | Ki | 5100 | nM | [ATAZANAVIR](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1163/) |
| 5.28 | IC50 | 5200 | nM | [ATAZANAVIR](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL1163/) |
| 5.28 | IC50 | 5300 | nM | [GENISTEIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL44/) |
| 5.28 | IC50 | 5248 | nM | [GENISTEIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL44/) |
| 5.23 | Ki | 5900 | nM | [RITONAVIR](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL163/) |
| 5.21 | IC50 | 6100 | nM | [RITONAVIR](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL163/) |
| 5.17 | IC50 | 6700 | nM | [FISETIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL31574/) |
| 5.17 | IC50 | 6761 | nM | [FISETIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL31574/) |
| 5.15 | IC50 | 7100 | nM | [OROXYLIN A](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL183513/) |
| 5.15 | IC50 | 7079 | nM | [OROXYLIN A](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL183513/) |
| 5.14 | IC50 | 7300 | nM | [QUERCETIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL50/) |
| 5.14 | IC50 | 7244 | nM | [QUERCETIN](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL50/) |
| 5.07 | Ki | 8480 | nM | [ELTROMBOPAG](https://www.ebi.ac.uk/chembl/compound_report_card/CHEMBL461101/) |

#### 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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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](https://pubchem.ncbi.nlm.nih.gov/bioassay/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 <i>in vitro</i> and <i>in vivo</i>. — \*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](https://sugi.bio/predict/target/SLCO2B1/).

## Related Atlas pages

- **Targeted by drugs:** [Erlotinib](/atlas/drug/erlotinib/), [Estrone Sulfuric Acid](/atlas/drug/estrone-sulfuric-acid/), [Gemfibrozil](/atlas/drug/gemfibrozil/), [Glyburide](/atlas/drug/glyburide/), [Rifamycin](/atlas/drug/rifamycin/), [Sildenafil](/atlas/drug/sildenafil/)
- **Pharmacogenomically associated drugs** *(drugs whose metabolism/response is associated with variants in this gene (PharmGKB) — not drugs that target it)*: [Abiraterone](/atlas/drug/abiraterone/), [Chloroquine](/atlas/drug/chloroquine/), [Fexofenadine](/atlas/drug/fexofenadine/), [Montelukast](/atlas/drug/montelukast/), [Primaquine](/atlas/drug/primaquine/), [Tamoxifen](/atlas/drug/tamoxifen/), [Voriconazole](/atlas/drug/voriconazole/)