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 Mon Oct 21 20:18:58 UTC 2019
Edited
by admin
on Mon Oct 21 20:18:58 UTC 2019
Protein Sub Type
Sequence Type COMPLETE
Record UNII
22ES734693
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MULTIDRUG RESISTANCE PROTEIN 1
Common Name English
MDR1
Common Name English
PGY1
Common Name English
ATP-BINDING CASSETTE SUB-FAMILY B MEMBER 1
Common Name English
MULTIDRUG RESISTANCE PROTEIN 1 (HUMAN)
Common Name English
P-GP
Common Name English
GP170
Common Name English
MGC163296
Common Name English
CD-243
Code English
CLCS
Common Name English
P-GLYCOPROTEIN 1
Common Name English
MDR-1
Common Name English
ATP-BINDING CASSETTE B1
Common Name English
ABC20
Common Name English
ABCB1
Common Name English
P-GLYCOPROTEIN
Common Name English
CD243
Common Name English
Classification Tree Code System Code
UCSF-FDA TRANSPORTAL ABCB1
Created by admin on Mon Oct 21 20:18:59 UTC 2019 , Edited by admin on Mon Oct 21 20:18:59 UTC 2019
EC (ENZYME CLASS) EC 3.6.3.44
Created by admin on Mon Oct 21 20:18:59 UTC 2019 , Edited by admin on Mon Oct 21 20:18:59 UTC 2019
Code System Code Type Description
CAS
1646537-23-6
Created by admin on Mon Oct 21 20:18:59 UTC 2019 , Edited by admin on Mon Oct 21 20:18:59 UTC 2019
PRIMARY
UNIPROT
P08183
Created by admin on Mon Oct 21 20:18:59 UTC 2019 , Edited by admin on Mon Oct 21 20:18:59 UTC 2019
PRIMARY
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_91
N 1_94
N 1_99
Related Record Type Details
INHIBITOR -> TRANSPORTER
Regorafenib inhibits Pgp and BCRP in vitro.
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
In vitro investigations indicated that indacaterol is a low affinity substrate for the efflux pump P-gp.
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Niraparib is a substrate of P-gp and BCRP in vitro.
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
COADMINSTERED WITH RITONAVIR TO INCREASE BIOAVAILABILITY
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
a high-fat meal increased bosutinib AUC 1.7-fold and Cmax 1.8-fold compared with bosutinib administration under fasting conditions
MAJOR
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
The in vitro study result indicated that alpelisib is a weak P-gp inhibitor with a Ki of 98.6 ?M (R0900459).
Ki
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Co-administration of talazoparib with certain P-gp inhibitors including amiodarone, carvedilol, clarithromycin, itraconazole, and verapamil in the clinical studies (PRP-001, PRP-002, ABRAZO and EMBRACA) increased talazoparib exposure by 44.7%, in conjunction with an increased rate of Talzenna dose reductions (41%).
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TARGET
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
The sponsor evaluated ospemifene as a potential substrate for transporters in a P-gp in vitro study. No in vivo transporter studies were conducted.
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
IC50
INHIBITOR -> TRANSPORTER
Simeprevir inhibited P-gp-dependent transport of paclitaxel in Caco-2 cells with an IC50 value of 64.4 ug/mL (Study NC113).
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Crizotinib is a substrate for P-glycoprotein in vitro.
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
Abiraterone acetate inhibits Pgp significantly, with an IC50 of 10.8 ?M in vitro.
IC50
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
In overexpressing BCRP and P-gp cell line, the estimate Km for both transporters is >300 ?M. Coadministration of larotrectinib with a single dose of a P-gp inhibitor (rifampin), increased the AUCinf of larotrectinib by 1.7-fold and the Cmax by 1.8-fold as compared to larotrectinib administered alone.
SUBSTRATE -> TRANSPORTER
INHIBITOR -> METABOLIC ENZYME
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
LDV is a substrate for P-gp and BCRP in vitro (AD-256-2144 and AD-256-2150).
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TARGET
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
WEAK
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
MINOR
INHIBITOR -> TRANSPORTER
Gao et al. reported that in vitro, imatinib (1 M) increases the intracellular concentration of vincristine and mitoxantrone in cells overexpressing ABCB1 and ABCG2, respectively.
INHIBITOR
CLINICALLY SIGNIFICANT
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
INDUCER -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
MAJOR
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-INHIBITOR -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
NON-SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
[I]/IC50 value for p-gp inhibition was estimated to be 0.23. Based on [I]/IC50 > 0.1 a potential in-vivo drug interaction via inhibition of p-gp cannot be ruled out.
INHIBITOR
IC50
TRANSPORTER -> SUBSTRATE
INHIBITOR -> TARGET
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
PARENT->INNOVATOR
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
IC50
INDUCER -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
WEAK
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
INHIBITOR -> TRANSPORTER
SUBSTRATE -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER(CALCULATED) CHEMICAL