General Information of the Protein
Protein ID
PT04616
Protein Name
Solute carrier organic anion transporter family member 2B1
Secondarily
Protein Name
Organic anion transporter B
Organic anion transporter polypeptide-related protein 2
Organic anion transporting polypeptide 2B1
Solute carrier family 21 member 9
Gene Name
SLCO2B1
Secondarily
Gene Name
KIAA0880
OATP2B1
OATPB
SLC21A9
Sequence
MGPRIGPAGEVPQVPDKETKATMGTENTPGGKASPDPQDVRPSVFHNIKLFVLCHSLLQLAQLMISGYLKSSISTVEKRFGLSSQTSGLLASFNEVGNTALIVFVSYFGSRVHRPRMIGYGAILVALAGLLMTLPHFISEPYRYDNTSPEDMPQDFKASLCLPTTSAPASAPSNGNCSSYTETQHLSVVGIMFVAQTLLGVGGVPIQPFGISYIDDFAHNSNSPLYLGILFAVTMMGPGLAFGLGSLMLRLYVDINQMPEGGISLTIKDPRWVGAWWLGFLIAAGAVALAAIPYFFFPKEMPKEKRELQFRRKVLAVTDSPARKGKDSPSKQSPGESTKKQDGLVQIAPNLTVIQFIKVFPRVLLQTLRHPIFLLVVLSQVCLSSMAAGMATFLPKFLERQFSITASYANLLIGCLSFPSVIVGIVVGGVLVKRLHLGPVGCGALCLLGMLLCLFFSLPLFFIGCSSHQIAGITHQTSAHPGLELSPSCMEACSCPLDGFNPVCDPSTRVEYITPCHAGCSSWVVQDALDNSQVFYTNCSCVVEGNPVLAGSCDSTCSHLVVPFLLLVSLGSALACLTHTPSFMLILRGVKKEDKTLAVGIQFMFLRILAWMPSPVIHGSAIDTTCVHWALSCGRRAVCRYYNNDLLRNRFIGLQFFFKTGSVICFALVLAVLRQQDKEARTKESRSSPAVEQQLLVSGPGKKPEDSRV
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Electrochemical transporter
>
SLC superfamily of solute carriers
>
SLC21/SLCO family of organic anion transporting polypeptides
Function
Mediates the Na(+)-independent transport of steroid sulfate conjugates and other specific organic anions (PubMed:10873595, PubMed:11159893, PubMed:11932330, PubMed:12724351, PubMed:14610227, PubMed:16908597, PubMed:18501590, PubMed:20507927, PubMed:22201122, PubMed:23531488, PubMed:25132355, PubMed:27576593, PubMed:26383540, PubMed:28408210, PubMed:29871943, PubMed:34628357). 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) (PubMed:11932330, PubMed:12409283). 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 (PubMed:11159893). Mediates the intestinal uptake of sulfated steroids (PubMed:12724351, PubMed:28408210). 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 (PubMed:16908597, PubMed:25132355). Also plays a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May act as a heme transporter that promotes cellular iron availability via heme oxygenase/HMOX2 and independently of TFRC (PubMed:35714613). Also transports heme by-product coproporphyrin III (CPIII), and may be involved in their hepatic disposition (PubMed:26383540). 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, Ref.25, PubMed:29871943). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable). 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 (PubMed:14610227, PubMed:19129463, PubMed:22201122). 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 (PubMed:19129463, PubMed:20507927, PubMed:26277985). Hydrogencarbonate/HCO3(-) acts as a probable counteranion that exchanges for organic anions (PubMed:19129463). Cytoplasmic glutamate may also act as counteranion in the placenta (PubMed:26277985). An inwardly directed proton gradient has also been proposed as the driving force of E1S uptake with a (H(+):E1S) stoichiometry of (1:1) (PubMed:20507927).
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Uniprot ID
Primary ID:
O94956

Secondarily ID:
A0A024R5I4
A8K2G9
B4DGA9
B4DTB0
E7ERN5
E9PPU8
Q9H2Z0
Q9UFU1
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Ensembl ID
ENSG00000137491
HGNC ID
HGNC:10962
Subcellular Location
Cell membrane
Basal cell membrane
Basolateral cell membrane
Apical cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000088 , Flp-In-293
Compound ID Compound Name Compound Formula
CP0037987
N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine
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C22H23N3O4
 2
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
2
Ki = 530 nM
   TI
   LI
   LO
   TS
CP0078757
(E)-3-((3-(2-(7-chloroquinolin-2-yl)vinyl)phenyl)(3-(dimethylamino)-3-oxopropylthio)methylthio)propanoic acid
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C26H27ClN2O3S2
 2
1
IC50 = 2900 nM
   TI
   LI
   LO
   TS
2
Ki = 2800 nM
   TI
   LI
   LO
   TS
CP0047485
(E)-2-hydroxy-5-((4-(N-pyridin-2-ylsulfamoyl)-phenyl)diazenyl) benzoic acid (A8)
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C18H14N4O5S
 2
1
IC50 = 3000 nM
   TI
   LI
   LO
   TS
2
Ki = 3000 nM
   TI
   LI
   LO
   TS
CP0086074
Atazanavir
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C38H52N6O7
 2
1
IC50 = 5200 nM
   TI
   LI
   LO
   TS
2
Ki = 5100 nM
   TI
   LI
   LO
   TS
CP0036175
1,3-thiazol-5-ylmethyl N-[(2S,3S,5S)-3-hydroxy-5-[(2S)-3-methyl-2-{[methyl({[2-(propan-2-yl)-1,3-thiazol-4-yl]methyl})carbamoyl]amino}butanamido]-1,6-diphenylhexan-2-yl]carbamate
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C37H48N6O5S2
 2
1
IC50 = 6100 nM
   TI
   LI
   LO
   TS
2
Ki = 5900 nM
   TI
   LI
   LO
   TS
CP0036222
(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
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C62H111N11O12
 2
1
IC50 = 37000 nM
   TI
   LI
   LO
   TS
2
Ki = 36000 nM
   TI
   LI
   LO
   TS
CP0095997
2-(4-ethoxyphenyl)-6-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-benzimidazole
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C27H28N6O
 2
1
IC50 = 51000 nM
   TI
   LI
   LO
   TS
2
Ki = 20000 nM
   TI
   LI
   LO
   TS
CP0071702
BA-41166E
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C43H58N4O12
 2
1
IC50 = 65000 nM
   TI
   LI
   LO
   TS
2
Ki = 63000 nM
   TI
   LI
   LO
   TS
CP0071076
(3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
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C33H35FN2O5
 1
1
Km = 2840 nM
   TI
   LI
   LO
   TS
CP0127632
ESTRONE
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C18H22O5S
 1
1
Km = 38240 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0127632
ESTRONE
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C18H22O5S
 2
1 Km = 100 nM
2 Km = 29900 nM
CP0047485
(E)-2-hydroxy-5-((4-(N-pyridin-2-ylsulfamoyl)-phenyl)diazenyl) benzoic acid (A8)
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C18H14N4O5S
 1
1 Km = 1730 nM
CP0071701
(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
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C23H36O7
 2
1 Km = 6250 nM
2 Km = 225000 nM
Clinical Information about the Protein
Target 1 ( Organic anion transporter B (SLCO2B1) )
Target Type Literature-reported Target