U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Created
by admin
on Sat Dec 16 10:43:03 GMT 2023
Edited
by admin
on Sat Dec 16 10:43:03 GMT 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 GMT 2023 , Edited by admin on Sat Dec 16 10:43:07 GMT 2023
Code System Code Type Description
FDA UNII
AIN96D6SGL
Created by admin on Sat Dec 16 10:43:07 GMT 2023 , Edited by admin on Sat Dec 16 10:43:07 GMT 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
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Based on in-vitro studies, eluxadoline appears to be a substrate for OAT3, OATP1B1, BSEP, and MRP2
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
TISSUE EXPRESSION->TRANSPORTER
INFLUX
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Inhibits at clinically relevant concentrations.
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IN VITRO
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
MINOR
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
IC50
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Clearance of glimepiridein OATP1B1*5 and *15 was significantly reduced compared to the wild-type.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
can potentially be used for in vivo (clinical) studies
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Coordination with OATP1B1 inhibitors (e.g. rifampicin, cyclosporine, etc.) could lead to an increase in systemic exposure of the active metabolite.
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Based on in vitro studies, lesinurad is a weak inhibitor of OATP1B1, OCT1, OAT1, and OAT3.
WEAK
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Km
INHIBITOR -> TRANSPORTER
Ki
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Compared with the OATP1B1*1a, mutants OATP1B1*5 and OATP1B1*15 showed significantly decreased transport capacity.
INHIBITOR -> TRANSPORTER
The results suggest that KLISYRI has no clinically meaningful effect on the PK of drugs mediated by OATP1B1
IC50
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IN VITRO
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
IC50
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL