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

Approval Year

Unknown
139594
Substance Class Protein
Created
by admin
on Sat Dec 16 09:06:26 GMT 2023
Edited
by admin
on Sat Dec 16 09:06:26 GMT 2023
Protein Type TRANSPORTER
Protein Sub Type
Sequence Origin HUMAN
Sequence Type COMPLETE
Record UNII
76UB6O122H
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
Common Name English
MGC102821
Common Name English
CD338
Common Name English
BMDP
Common Name English
ABC15
Common Name English
CDW338
Common Name English
BCRP
Common Name English
BREAST CANCER RESISTANT PROTEIN
Common Name English
URATE EXPORTER
Common Name English
MXR
Common Name English
PLACENTA-SPECIFIC ATP-BINDING CASSETTE TRANSPORTER
Common Name English
MRX
Common Name English
MITOXANTRONE RESISTANCE-ASSOCIATED PROTEIN
Common Name English
EST157481
Common Name English
MXR1
Common Name English
ABCG2
Common Name English
BCRP1
Common Name English
ABCP
Common Name English
Code System Code Type Description
UCSF-FDA TRANSPORTAL
ABCG2
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
PRIMARY
CAS
479876-41-0
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
PRIMARY
CAS
481134-43-4
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
ALTERNATIVE
UNIPROT
Q9UNQ0
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
PRIMARY
CAS
481133-43-1
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
ALTERNATIVE
FDA UNII
76UB6O122H
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
PRIMARY
CAS
658014-39-2
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
ALTERNATIVE
CAS
759386-70-4
Created by admin on Sat Dec 16 09:06:33 GMT 2023 , Edited by admin on Sat Dec 16 09:06:33 GMT 2023
ALTERNATIVE
From To
1_592 1_608
2_592 2_608
3_592 3_608
4_592 4_608
1_603 2_603
3_603 4_603
Glycosylation Type HUMAN
Glycosylation Link Type Site
N 1_596
N 2_596
N 3_596
N 4_596
Related Record Type Details
Structure of 7-ETHYL-10-HYDROXYCAMPTOTHECIN
INHIBITOR -> TRANSPORTER
Structure of PASIREOTIDE
NON-SUBSTRATE -> TRANSPORTER
Structure of Emidurdar
INHIBITOR -> TARGET
Structure of 1-(((4-((7-METHOXY-6-(SULFOOXY)-4-QUINOLINYL)OXY)PHENYL)AMINO)CARBONYL)CYCLOPROPANECARBOXYLIC ACID
SUBSTRATE -> TRANSPORTER
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
INHIBITOR -> TRANSPORTER
Structure of TRYPTOQUIVALINE
INHIBITOR -> TRANSPORTER
Structure of MOXIDECTIN
INHIBITOR -> TRANSPORTER
Structure of 25-HYDROXYVITAMIN D3 3.BETA.-SULFATE
SUBSTRATE -> TRANSPORTER
Structure of BT-070
INHIBITOR -> TRANSPORTER
Structure of BAFETINIB
INHIBITOR -> TRANSPORTER
Structure of ZIDOVUDINE
SUBSTRATE -> TRANSPORTER
Structure of TRILACICLIB
SUBSTRATE -> TRANSPORTER
Structure of DOXORUBICIN
SUBSTRATE -> TRANSPORTER
Structure of PACRITINIB
INHIBITOR -> TRANSPORTER
IC50
Structure of RIFAMYCIN
INHIBITOR -> TRANSPORTER
IC50
Structure of RELUGOLIX
INHIBITOR -> TRANSPORTER
Structure of GILTERITINIB
INHIBITOR -> TRANSPORTER
IC50
Structure of SCUTELLARIN
INHIBITOR -> TRANSPORTER
IC50
Structure of ALPELISIB
SUBSTRATE -> TRANSPORTER
Structure of TUCATINIB
SUBSTRATE -> TRANSPORTER
Structure of LOMITAPIDE
NON-INHIBITOR -> TRANSPORTER
HUMAN PLACENTAL TISSUE
TISSUE EXPRESSION->TRANSPORTER
APICAL
Structure of EDARAVONE SULFATE
SUBSTRATE -> TRANSPORTER
Structure of LORLATINIB
INHIBITOR -> TRANSPORTER
Structure of TECOVIRIMAT
INHIBITOR -> TRANSPORTER
Structure of ELACRIDAR
INDUCER -> TRANSPORTER
Structure of LUSUTROMBOPAG
SUBSTRATE -> TARGET
Structure of GLASDEGIB
SUBSTRATE -> TRANSPORTER
Structure of Zagociguat
INHIBITOR -> TRANSPORTER
IC50
Structure of BMS-986299
SUBSTRATE -> TRANSPORTER
Structure of ULIXERTINIB
INHIBITOR -> TRANSPORTER
In ABCG2-overexpressing cells, ulixertinib inhibited the efflux activity of ABCG2 and reversed resistance to sub-strate anticancer drugs. Mechanistic investigations revealed that ulixertinib stimulated the ATPase activity of both ABCB1 and ABCG2 in a concentration-dependent manner,
Structure of ENASIDENIB
NON-SUBSTRATE -> TRANSPORTER
Structure of PRASTERONE SULFATE
INHIBITOR -> TRANSPORTER
Structure of REGORAFENIB ANHYDROUS
INHIBITOR -> TRANSPORTER
Regorafenib inhibits BCRP in vitro.
IC50
Structure of NELFINAVIR
INHIBITOR -> TRANSPORTER
Structure of VELPATASVIR
INHIBITOR -> TRANSPORTER
IC50
Structure of ELAGOLIX
INHIBITOR -> TRANSPORTER
Structure of ACT-777991
SUBSTRATE -> TRANSPORTER
Structure of PIBRENTASVIR
INHIBITOR -> TRANSPORTER
Structure of PRUCALOPRIDE
SUBSTRATE -> TRANSPORTER
Structure of BICTEGRAVIR
SUBSTRATE -> TRANSPORTER
Structure of DAROLUTAMIDE
SUBSTRATE -> TRANSPORTER
MINOR
Structure of PIBRENTASVIR
SUBSTRATE -> TRANSPORTER
Structure of DUVELISIB
INHIBITOR -> TRANSPORTER
Structure of GLECAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of ABEMACICLIB
INHIBITOR -> TRANSPORTER
IC50
Structure of COPANLISIB
SUBSTRATE -> TRANSPORTER
Structure of RHINACANTHIN C
INHIBITOR -> TRANSPORTER
IC50
Structure of RIBOCICLIB
INHIBITOR -> TRANSPORTER
Structure of AGI-16903
SUBSTRATE -> TRANSPORTER
Structure of NINGETINIB
SUBSTRATE -> TRANSPORTER
Structure of ATORVASTATIN
INHIBITOR -> TRANSPORTER
Structure of LONAFARNIB
INHIBITOR -> TRANSPORTER
Structure of UBROGEPANT
SUBSTRATE -> TRANSPORTER
Structure of RIVAROXABAN
SUBSTRATE -> TRANSPORTER
Structure of TEMSAVIR
SUBSTRATE -> TRANSPORTER
Drugs that induce or inhibit CYP3A, P-gp, and BCRP may affect temsavir plasma concentrations.
Structure of DACOMITINIB ANHYDROUS
INHIBITOR -> TRANSPORTER
Structure of GLASDEGIB
INHIBITOR -> TRANSPORTER
Structure of PITAVASTATIN
INHIBITOR -> TRANSPORTER
Structure of ELBASVIR
INHIBITOR -> TRANSPORTER
IC50
Structure of SAQUINAVIR
INHIBITOR -> TRANSPORTER
Structure of NETUPITANT
INHIBITOR -> TRANSPORTER
Netupitnat: Cmax/IC50= (1-1.5μM)/6 μM = (0.167-0.25)>0.1
Structure of 4-AMINO-N-(3-BROMO-4-FLUOROPHENYL)-1,2,5-OXADIAZOLE-3-CARBOXIMIDAMIDE
SUBSTRATE -> TRANSPORTER
Structure of GLECAPREVIR
INHIBITOR -> TRANSPORTER
Structure of Binimetinib
SUBSTRATE -> TRANSPORTER
Structure of PALBOCICLIB
SUBSTRATE -> TRANSPORTER
Structure of ABACAVIR
INHIBITOR -> TRANSPORTER
Structure of DAUNORUBICIN
INHIBITOR -> TRANSPORTER
Structure of EDARAVONE
INHIBITOR -> TRANSPORTER
Edaravone inhib it e d CYP2C9, BCRP, OAT3, and induced CYP1A2 in vitro.
Structure of IMATINIB
INHIBITOR -> TRANSPORTER
Gao et al. reported that in vitro, imatinib (1 μM) increases the intracellular concentration of vincristine and mitoxantrone in cells overexpressing ABCB1 and ABCG2, respectively (Gao et al., 2006).
CLINICALLY SIGNIFICANT
Structure of LETERMOVIR
INHIBITOR -> TRANSPORTER
Structure of TERIFLUNOMIDE
INHIBITOR -> TRANSPORTER
Terifluniomide is an inhibitor of BCRP, OAT3, OATP1B1, OCT2 in vitro
Structure of ARTESUNATE
SUBSTRATE -> TRANSPORTER
Structure of TEZACAFTOR
SUBSTRATE -> TRANSPORTER
Structure of ELACRIDAR
INHIBITOR -> TARGET
Structure of UPADACITINIB
SUBSTRATE -> TRANSPORTER
Structure of GRAZOPREVIR ANHYDROUS
INHIBITOR -> TRANSPORTER
IC50
Structure of CABOTEGRAVIR
SUBSTRATE -> TRANSPORTER
Cabotegravir is a substrate of P-gp and BCRP in vitro; however, because of its high permeability, no alteration in cabotegravir absorption is expected with coadministration of P-gp or BCRP inhibitors.
Structure of ENCORAFENIB
INHIBITOR -> TRANSPORTER
IC50
Structure of TOPOTECAN
SUBSTRATE -> TRANSPORTER
Structure of RIMEGEPANT
SUBSTRATE -> TRANSPORTER
Structure of VOXILAPREVIR
SUBSTRATE -> TRANSPORTER
Structure of AVATROMBOPAG
INHIBITOR -> TRANSPORTER
IC50
Structure of SULFASALAZINE
INHIBITOR -> TRANSPORTER
Structure of Ertugliflozin
SUBSTRATE -> TRANSPORTER
Structure of LENVATINIB
SUBSTRATE -> TRANSPORTER
Structure of NIRAPARIB
SUBSTRATE -> TRANSPORTER
Niraparib is a substrate of P-gp and BCRP in vitro.
Structure of LAROTRECTINIB
SUBSTRATE -> TRANSPORTER
In overexpressing BCRP and P-gp cell line, the estimate Km for both transporters is >300 μM.
Structure of VENETOCLAX
INHIBITOR -> TRANSPORTER
Structure of ROSUVASTATIN
INHIBITOR -> TRANSPORTER
Structure of BEROTRALSTAT
SUBSTRATE -> TRANSPORTER
Structure of TAFAMIDIS
INHIBITOR -> TRANSPORTER
Tafamidis inhibits BCRP in-vitro.
IC50
Structure of RIOCIGUAT
SUBSTRATE -> TRANSPORTER
Structure of DABRAFENIB
INHIBITOR -> TRANSPORTER
Structure of DOLUTEGRAVIR
SUBSTRATE -> TRANSPORTER
Structure of CERIVASTATIN
INHIBITOR -> TRANSPORTER
Structure of TERIFLUNOMIDE
SUBSTRATE -> TRANSPORTER
Teriflunomide is a substrate of BCRP in vitro
Structure of ERVOGASTAT
INHIBITOR -> TRANSPORTER
Structure of Tildacerfont
INHIBITOR -> TRANSPORTER
Structure of ESAXERENONE
SUBSTRATE -> TRANSPORTER
Structure of Selpercatinib
INHIBITOR -> TRANSPORTER
Structure of VERICIGUAT
SUBSTRATE -> TRANSPORTER
Structure of TOZASERTIB
SUBSTRATE -> TRANSPORTER
Structure of EPACADOSTAT
SUBSTRATE -> TRANSPORTER
Structure of FEDRATINIB
INHIBITOR -> TRANSPORTER
IC50
Structure of ACYCLOVIR
SUBSTRATE -> TRANSPORTER
Structure of STIRIPENTOL
INHIBITOR -> TARGET
IC50
Structure of OLACAFTOR
INHIBITOR -> TRANSPORTER
Structure of IDELALISIB
SUBSTRATE -> TRANSPORTER
Structure of RUCAPARIB
SUBSTRATE -> TRANSPORTER
Structure of EFAVIRENZ
INHIBITOR -> TRANSPORTER
Structure of ATAZANAVIR
INHIBITOR -> TRANSPORTER
Structure of VOXILAPREVIR
INHIBITOR -> TRANSPORTER
inhibit 6.7% at 10 μM
IC50
Structure of GS-563117
SUBSTRATE -> TRANSPORTER
IN VITRO
Structure of PRALSETINIB
SUBSTRATE -> TRANSPORTER
Structure of TALAZOPARIB
SUBSTRATE -> TRANSPORTER
Co-administration with BCRP inhibitors may increase talazoparib exposure.
Structure of RIPRETINIB
SUBSTRATE -> TRANSPORTER
Structure of AMISULPRIDE
SUBSTRATE -> TRANSPORTER
Structure of VENETOCLAX
SUBSTRATE -> TRANSPORTER
Structure of ELISMETREP
NON-SUBSTRATE -> TRANSPORTER
Structure of ERLOTINIB
INHIBITOR -> TRANSPORTER
Structure of OPICAPONE
SUBSTRATE -> TRANSPORTER
Structure of PROPANAMIDE, N-(5-(2-(2-METHOXY-3-PYRIDINYL)-7-METHYLIMIDAZO(1,2-A)PYRIDIN-3-YL)-6-(2-(1-METHYL-6-ISOQUINOLINYL)ETHYNYL)-2-PYRIDINYL)-2-(METHYLAMINO)-, (2S)-
NON-SUBSTRATE -> TRANSPORTER
Structure of GEFITINIB
INDUCER -> TRANSPORTER
Structure of LEDIPASVIR
SUBSTRATE -> TRANSPORTER
LDV is a substrate for P-gp and BCRP in vitro (AD-256-2144 and AD-256-2150).
Structure of MIVEBRESIB
SUBSTRATE -> TRANSPORTER
Structure of BMS-962212
NON-SUBSTRATE -> TRANSPORTER
Structure of FLUVASTATIN
INHIBITOR -> TRANSPORTER
Structure of Selpercatinib
SUBSTRATE -> TRANSPORTER
Structure of Tildacerfont
NON-SUBSTRATE -> TRANSPORTER
Structure of RISDIPLAM
SUBSTRATE -> TRANSPORTER
IN VITRO
WEAK
Structure of REVEFENACIN
SUBSTRATE -> TRANSPORTER
Structure of ROSUVASTATIN
SUBSTRATE -> TRANSPORTER
Structure of LOPINAVIR
INHIBITOR -> TRANSPORTER
Structure of SCUTELLARIN
SUBSTRATE -> TRANSPORTER
Structure of BARICITINIB
SUBSTRATE -> TRANSPORTER
Structure of BRIGATINIB
SUBSTRATE -> TRANSPORTER
Structure of DOTINURAD
INHIBITOR -> TRANSPORTER
IC50
Structure of DAUNORUBICIN
SUBSTRATE -> TRANSPORTER
Structure of SELUMETINIB
SUBSTRATE -> TRANSPORTER
Structure of ACT-333679
SUBSTRATE -> TRANSPORTER
Structure of BRANEBRUTINIB
INHIBITOR -> TRANSPORTER
Structure of DUVELISIB
SUBSTRATE -> TRANSPORTER
Structure of Belumosudil
INHIBITOR -> TRANSPORTER
Inhibits at clinically relevant concentrations.
Structure of DELAFLOXACIN
SUBSTRATE -> TRANSPORTER
Structure of SULFASALAZINE
SUBSTRATE -> TRANSPORTER
Structure of OTESECONAZOLE
INHIBITOR -> TRANSPORTER
Clinically relevant in DDI study resulted in a clinically significant increase in rosuvastatin exposure.
IC50
Structure of TENOFOVIR ALAFENAMIDE
SUBSTRATE -> TRANSPORTER
Structure of ACALABRUTINIB
SUBSTRATE -> TRANSPORTER
Structure of ABEMACICLIB
SUBSTRATE -> TRANSPORTER
Structure of Olaparib
INHIBITOR -> TRANSPORTER
The clinical relevance of these findings is unknown.
Structure of NILOTINIB
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 TAMATINIB
INHIBITOR -> METABOLIC ENZYME
Structure of AMPRENAVIR
INHIBITOR -> TRANSPORTER
Structure of VELPATASVIR
SUBSTRATE -> TRANSPORTER
Structure of LASMIDITAN
INHIBITOR -> TRANSPORTER
Lasmiditan is an in-vitro inhibitor of P-gp and BCRP.
Structure of DELAVIRDINE
INHIBITOR -> TRANSPORTER
Structure of PRALSETINIB
INHIBITOR -> TRANSPORTER
Structure of ACT-333679
INHIBITOR -> TRANSPORTER
IC50
Structure of PONATINIB
NON-SUBSTRATE -> TRANSPORTER
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT:NUMBER AVERAGE(CALCULATED) CHEMICAL
NIH
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