Gene and Protein Information
Species	TM	AA	Chromosomal Location	Gene Symbol	Gene Name	Reference
Human	12	1280	7q21.12	ABCB1	ATP binding cassette subfamily B member 1
Mouse	12	1276	5 3.43 cM	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 | Abcb1 | ATP-binding cassette, sub-family B (MDR/TAP), member 1 | ATP-binding cassette, subfamily B (MDR/TAP), member 1A | Mdr1a | multiple drug resistant 1a | 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	CHEMBL4302 (Hs), CHEMBL2573 (Mm)
DrugBank Target	P08183 (Hs)
Ensembl Gene	ENSG00000085563 (Hs), ENSMUSG00000040584 (Mm), ENSRNOG00000008012 (Rn)
Entrez Gene	5243 (Hs), 18671 (Mm), 170913 (Rn)
Human Protein Atlas	ENSG00000085563 (Hs)
KEGG Gene	hsa:5243 (Hs), mmu:18671 (Mm), rno:170913 (Rn)
OMIM	171050 (Hs)
Pharos	P08183 (Hs)
UniProtKB	P08183 (Hs), P21447 (Mm)
Wikipedia	ABCB1 (Hs)

Selected 3D Structures
	Description:  Molecular structure of human P-glycoprotein (ABCB1) in the ATP-bound, outward-facing conformation PDB Id:  6C0V Ligand:  ATP    Resolution:  3.4Å Species:  Human References:  2

Download all structure-activity data for this target as a CSV file

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 5 ⤷ pIC50 6.2 (IC50 6.76x10-7 M) [5] Description: Measuring inhibition of cyclosporine A transport in A2780/ADR cells expressing hABCB1. pIC50 5.8 (IC50 1.73x10-6 M) [5] Description: Measuring inhibition of calcein AM transport in A2780/ADR cells expressing hABCB1.

Biologically Significant Variant Comments

Nonsense mutation in ABCB1 has been described in collie dogs [3-4] and when these animals are treated with ivermectin they develop potentially fatal neurologic disorders, due to a toxic accumulation of ivermectin in the central nervous system. Similar ivermectin-induced pathology has been noted in humans. In 2020 mutated human ABCB1 alleles were identified in a patient who developed serious ivermectin toxicity following a single oral dose of the drug. Genetic analysis revealed that this patient harboured a different nonsense alteration in each copy of their ABCB1 genes. Both mutations generated premature stop codons and truncated transporter proteins that lacked the C-terminal nucleotide-binding domain, rendering the proteins incapable of drug-transport [1].