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Approval Year

Unknown
139594
Substance Class Protein
Created
by admin
on Sat Dec 16 10:43:03 UTC 2023
Edited
by admin
on Sat Dec 16 10:43:03 UTC 2023
Protein Sub Type
Sequence Type COMPLETE
Record UNII
AIN96D6SGL
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
OATP1B1
Common Name English
SLCO1B1
Common Name English
SOLUTE CARRIER ORGANIC ANION TRANSPORTER FAMILY MEMBER 1B1
Common Name English
OATPC
Common Name English
OATP-C
Common Name English
OATP-2
Common Name English
OATP-1B1
Common Name English
LST1
Common Name English
OATP2
Common Name English
LST-1
Common Name English
SOLUTE CARRIER FAMILY 21 MEMBER 6
Common Name English
SODIUM-INDEPENDENT ORGANIC ANION-TRANSPORTING POLYPEPTIDE 2
Common Name English
SLC21A6
Common Name English
MGC133282
Common Name English
Classification Tree Code System Code
UCSF-FDA TRANSPORTAL SLCO1B1
Created by admin on Sat Dec 16 10:43:07 UTC 2023 , Edited by admin on Sat Dec 16 10:43:07 UTC 2023
Code System Code Type Description
FDA UNII
AIN96D6SGL
Created by admin on Sat Dec 16 10:43:07 UTC 2023 , Edited by admin on Sat Dec 16 10:43:07 UTC 2023
PRIMARY
From To
1_459 1_485
1_463 1_474
1_465 1_489
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_130
N 1_134
N 1_432
N 1_503
N 1_516
N 1_617
Related Record Type Details
Structure of ATAZANAVIR
INHIBITOR -> TRANSPORTER
Structure of SELEXIPAG
SUBSTRATE -> TRANSPORTER
Structure of ROSIGLITAZONE
INHIBITOR -> TRANSPORTER
Structure of PACLITAXEL
INHIBITOR -> TRANSPORTER
Structure of REMDESIVIR
INHIBITOR -> TRANSPORTER
Structure of INDINAVIR
INHIBITOR -> TRANSPORTER
Structure of ELIMUSERTIB
INHIBITOR -> TRANSPORTER
Structure of ELUXADOLINE
SUBSTRATE -> TRANSPORTER
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
Structure of DUVELISIB
INHIBITOR -> TRANSPORTER
Structure of ELAGOLIX
SUBSTRATE -> TRANSPORTER
Structure of CLOTRIMAZOLE
INHIBITOR -> TRANSPORTER
SILIBININ DIHEMISUCCINATE
INHIBITOR -> TRANSPORTER
Structure of PF-04991532
SUBSTRATE -> TRANSPORTER
Structure of OPICAPONE
INHIBITOR -> TRANSPORTER
IC50
HUMAN LIVER
TISSUE EXPRESSION->TRANSPORTER
INFLUX
Structure of GLECAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of LURBINECTEDIN
INHIBITOR -> TRANSPORTER
Structure of Belumosudil
INHIBITOR -> TRANSPORTER
Inhibits at clinically relevant concentrations.
Structure of SAQUINAVIR
INHIBITOR -> TRANSPORTER
Structure of NELFINAVIR
INHIBITOR -> TRANSPORTER
Structure of MONTELUKAST
INHIBITOR -> TRANSPORTER
Structure of PIBRENTASVIR
INHIBITOR -> TRANSPORTER
Structure of Digoxin
INHIBITOR -> TRANSPORTER
Structure of OLACAFTOR
INHIBITOR -> TRANSPORTER
Structure of ESTRADIOL
INHIBITOR -> TRANSPORTER
Structure of Olaparib
INHIBITOR -> TRANSPORTER
INHIBITOR
IC50
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
SUBSTRATE -> TRANSPORTER
Structure of GRAZOPREVIR ANHYDROUS
SUBSTRATE -> TRANSPORTER
Structure of GS-563117
INHIBITOR -> TRANSPORTER
IN VITRO
Structure of CYCLOSPORINE
SUBSTRATE -> TRANSPORTER
Structure of RHINACANTHIN C
INHIBITOR -> TRANSPORTER
IC50
Structure of IDELALISIB
INHIBITOR -> TRANSPORTER
Structure of Crizotinib
SUBSTRATE -> TRANSPORTER
Structure of MIFEPRISTONE
INHIBITOR -> TRANSPORTER
Structure of HYPERFORIN
INHIBITOR -> TRANSPORTER
Structure of CENOBAMATE
INHIBITOR -> TRANSPORTER
WEAK
Structure of 25OHD3-3-O-GLUCURONIDE
SUBSTRATE -> TRANSPORTER
Structure of DEOXYCHOLIC ACID
NON-INHIBITOR -> TRANSPORTER
Structure of BRANEBRUTINIB
INHIBITOR -> TRANSPORTER
Structure of BILIRUBIN
SUBSTRATE -> TRANSPORTER
MINOR
Structure of BMS-962212
SUBSTRATE -> TRANSPORTER
Structure of GW-4064
INHIBITOR -> TRANSPORTER
Structure of LOPINAVIR
INHIBITOR -> TRANSPORTER
Structure of ESTRONE SULFATE
INHIBITOR -> TRANSPORTER
Structure of Nirmatrelvir
INHIBITOR -> TRANSPORTER
Structure of ARTESUNATE
INHIBITOR -> TRANSPORTER
WEAK
IC50
Structure of LETERMOVIR
INHIBITOR -> TRANSPORTER
Structure of SILDENAFIL
INHIBITOR -> TRANSPORTER
Structure of CHENODIOL
INHIBITOR -> TRANSPORTER
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
INHIBITOR -> TRANSPORTER
IC50
Structure of FEXOFENADINE
INHIBITOR -> TRANSPORTER
Structure of DABRAFENIB
INHIBITOR -> TRANSPORTER
Structure of ACT-333679
INHIBITOR -> TRANSPORTER
IC50
Structure of LEVOTHYROXINE
SUBSTRATE -> TRANSPORTER
Structure of GLYBURIDE
INHIBITOR -> TRANSPORTER
Structure of ENCORAFENIB
INHIBITOR -> TRANSPORTER
IC50
Structure of PRALSETINIB
INHIBITOR -> TRANSPORTER
Structure of PAZOPANIB
SUBSTRATE -> TRANSPORTER
Structure of VALSARTAN
INHIBITOR -> TRANSPORTER
Structure of FEXOFENADINE
SUBSTRATE -> TRANSPORTER
Structure of TENOFOVIR ALAFENAMIDE
SUBSTRATE -> TRANSPORTER
Structure of GEFITINIB
SUBSTRATE -> TRANSPORTER
Structure of FENOFIBRATE
INHIBITOR -> TRANSPORTER
Structure of ATORVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of PRAVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of TELMISARTAN
INHIBITOR -> TRANSPORTER
Structure of AMPRENAVIR
INHIBITOR -> TRANSPORTER
Structure of DARUNAVIR
INHIBITOR -> TRANSPORTER
Structure of TERIFLUNOMIDE
INHIBITOR -> TRANSPORTER
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
Structure of GEMFIBROZIL
INHIBITOR -> TRANSPORTER
Structure of PASIREOTIDE
NON-SUBSTRATE -> TRANSPORTER
Structure of LOVASTATIN
INHIBITOR -> TRANSPORTER
Structure of LETERMOVIR
SUBSTRATE -> TRANSPORTER
Structure of LONAFARNIB
INHIBITOR -> TRANSPORTER
Structure of CASPOFUNGIN
SUBSTRATE -> TRANSPORTER
Structure of GLIMEPIRIDE
SUBSTRATE -> TRANSPORTER
Clearance of glimepiridein OATP1B1*5 and *15 was significantly reduced compared to the wild-type.
Structure of OLACAFTOR
SUBSTRATE -> TRANSPORTER
Structure of DEHYDROCHOLIC ACID
INHIBITOR -> TRANSPORTER
Structure of METHOTREXATE
SUBSTRATE -> TRANSPORTER
Structure of TACROLIMUS
INHIBITOR -> TRANSPORTER
Structure of CYCLOSPORINE
INHIBITOR -> TRANSPORTER
can potentially be used for in vivo (clinical) studies
Structure of NILOTINIB
SUBSTRATE -> TRANSPORTER
Structure of MK-571
INHIBITOR -> TRANSPORTER
TROGLITAZONE
INHIBITOR -> TRANSPORTER
Structure of TEMSAVIR
INHIBITOR -> TRANSPORTER
Structure of GW-1929
INHIBITOR -> TRANSPORTER
Structure of BEZAFIBRATE
INHIBITOR -> TRANSPORTER
Structure of VELPATASVIR
INHIBITOR -> TRANSPORTER
IC50
Structure of ESTRONE SULFATE
SUBSTRATE -> TRANSPORTER
Structure of THRX-195518
SUBSTRATE -> TRANSPORTER
Coordination with OATP1B1 inhibitors (e.g. rifampicin, cyclosporine, etc.) could lead to an increase in systemic exposure of the active metabolite.
Structure of RITONAVIR
INHIBITOR -> TRANSPORTER
Structure of Guretolimod
SUBSTRATE -> TRANSPORTER
Structure of LESINURAD
INHIBITOR -> TRANSPORTER
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
Structure of RIFAMPIN
SUBSTRATE -> TRANSPORTER
Structure of PRASTERONE SULFATE
SUBSTRATE -> TRANSPORTER
Structure of ABAMETAPIR CARBOXYL
INHIBITOR -> TRANSPORTER
Structure of ROSUVASTATIN
SUBSTRATE -> TRANSPORTER
Km
Structure of BRILANESTRANT
INHIBITOR -> TRANSPORTER
Ki
Structure of SIMEPREVIR
SUBSTRATE -> TRANSPORTER
Structure of LEVOTHYROXINE
INHIBITOR -> TRANSPORTER
Structure of (2S,3S,4S,5R,6S)-6-((E)-((3-BROMO-4-FLUORO-ANILINO)-(4-(2-(SULFAMOYLAMINO)ETHYLAMINO)-1,2,5-OXADIAZOL-3-YL)METHYLENE)AMINO)OXY-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
SUBSTRATE -> TRANSPORTER
Structure of VOXILAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of TAUROCHOLIC ACID
INHIBITOR -> TRANSPORTER
Structure of TAUROCHOLIC ACID
SUBSTRATE -> TRANSPORTER
Structure of PRAVASTATIN
INHIBITOR -> TRANSPORTER
Structure of RIFAMPIN
INHIBITOR -> TRANSPORTER
Structure of SULFOBROMOPHTHALEIN SODIUM
INHIBITOR -> TRANSPORTER
Structure of PENICILLIN G
SUBSTRATE -> TRANSPORTER
Structure of REPAGLINIDE
INHIBITOR -> TRANSPORTER
Structure of SELEXIPAG
INHIBITOR -> TRANSPORTER
IC50
Structure of GLECAPREVIR
INHIBITOR -> TRANSPORTER
Structure of PANOBINOSTAT
INHIBITOR -> TRANSPORTER
Structure of GLICLAZIDE
SUBSTRATE -> TRANSPORTER
Compared with the OATP1B1*1a, mutants OATP1B1*5 and OATP1B1*15 showed significantly decreased transport capacity.
Structure of TIRBANIBULIN
INHIBITOR -> TRANSPORTER
The results suggest that KLISYRI has no clinically meaningful effect on the PK of drugs mediated by OATP1B1
IC50
Structure of TEZACAFTOR
SUBSTRATE -> TRANSPORTER
Structure of VOCLOSPORIN
INHIBITOR -> TRANSPORTER
IN VITRO
Structure of ELAGOLIX
INHIBITOR -> TRANSPORTER
Structure of ELUXADOLINE
INHIBITOR -> TRANSPORTER
WEAK
Structure of GRAZOPREVIR ANHYDROUS
INHIBITOR -> TRANSPORTER
IC50
Structure of IMATINIB
SUBSTRATE -> TRANSPORTER
Structure of GILTERITINIB
INHIBITOR -> TRANSPORTER
WEAK
IC50
Structure of GLYCOCHOLIC ACID
INHIBITOR -> TRANSPORTER
Structure of ELISMETREP
NON-SUBSTRATE -> TRANSPORTER
Structure of CHOLIC ACID
INHIBITOR -> TRANSPORTER
Structure of SIMVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of ELISMETREP
INHIBITOR -> TRANSPORTER
Structure of PIRINIXIC ACID
INHIBITOR -> TRANSPORTER
Structure of PRAVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of LITHOCHOLIC ACID
INHIBITOR -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL
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