ABCB1 | ABCB subfamily | IUPHAR Guide to IMMUNOPHARMACOLOGY

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ABCB1

Target not currently curated in GtoImmuPdb

Target id: 768

Nomenclature: ABCB1

Abbreviated Name: MDR1, PGP1

Systematic Nomenclature: ABCB1

Family: ABCB subfamily

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ABCB1 ATP binding cassette subfamily B member 1
Mouse - - Abcb1a ATP-binding cassette, sub-family B (MDR/TAP), member 1A
Rat - - Abcb1a ATP binding cassette subfamily B member 1A
Previous and Unofficial Names
P-glycoprotein 1 | ABC20 | CD243 | CLCS | GP170 | MDR1 | PGY1 | colchicin sensitivity | multidrug resistance protein 1 | multiple drug resistant 1a | Abcb1 | ATP-binding cassette, sub-family B (MDR/TAP), member 1 | ATP-binding cassette, subfamily B (MDR/TAP), member 1A | Mdr1a | Evi32 | MDR3 | mdr-3 | Pgp | Pgy3 | Pgy-3 | P-gp | Abcb1a | ATP binding cassette subfamily B member 1 | ATP-binding cassette
Database Links
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Molecular structure of human P-glycoprotein (ABCB1) in the ATP-bound, outward-facing conformation
PDB Id:  6C0V
Ligand:  ATP   This ligand is endogenous
Resolution:  3.4Å
Species:  Human
References:  1

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 14 [PMID: 30925062] Hs Competitive 5.8 – 6.2 pIC50 2
pIC50 6.2 (IC50 6.76x10-7 M) [2]
Description: Measuring inhibition of cyclosporine A transport in A2780/ADR cells expressing hABCB1.
pIC50 5.8 (IC50 1.73x10-6 M) [2]
Description: Measuring inhibition of calcein AM transport in A2780/ADR cells expressing hABCB1.

References

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1. Kim Y, Chen J. (2018) Molecular structure of human P-glycoprotein in the ATP-bound, outward-facing conformation. Science, 359 (6378): 915-919. [PMID:29371429]

2. Silbermann K, Stefan SM, Elshawadfy R, Namasivayam V, Wiese M. (2019) Identification of Thienopyrimidine Scaffold as an Inhibitor of the ABC Transport Protein ABCC1 (MRP1) and Related Transporters Using a Combined Virtual Screening Approach. J. Med. Chem., 62 (9): 4383-4400. [PMID:30925062]

Contributors

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