General Information of the Protein
Protein ID
PT02718
Protein Name
Broad substrate specificity ATP-binding cassette transporter ABCG2
Secondarily
Protein Name
ATP-binding cassette sub-family G member 2
Breast cancer resistance protein
CDw338
Mitoxantrone resistance-associated protein
Placenta-specific ATP-binding cassette transporter
Urate exporter
Gene Name
ABCG2
Secondarily
Gene Name
ABCP
BCRP
BCRP1
MXR
Sequence
MSSSNVEVFIPVSQGNTNGFPATASNDLKAFTEGAVLSFHNICYRVKLKSGFLPCRKPVEKEILSNINGIMKPGLNAILGPTGGGKSSLLDVLAARKDPSGLSGDVLINGAPRPANFKCNSGYVVQDDVVMGTLTVRENLQFSAALRLATTMTNHEKNERINRVIQELGLDKVADSKVGTQFIRGVSGGERKRTSIGMELITDPSILFLDEPTTGLDSSTANAVLLLLKRMSKQGRTIIFSIHQPRYSIFKLFDSLTLLASGRLMFHGPAQEALGYFESAGYHCEAYNNPADFFLDIINGDSTAVALNREEDFKATEIIEPSKQDKPLIEKLAEIYVNSSFYKETKAELHQLSGGEKKKKITVFKEISYTTSFCHQLRWVSKRSFKNLLGNPQASIAQIIVTVVLGLVIGAIYFGLKNDSTGIQNRAGVLFFLTTNQCFSSVSAVELFVVEKKLFIHEYISGYYRVSSYFLGKLLSDLLPMRMLPSIIFTCIVYFMLGLKPKADAFFVMMFTLMMVAYSASSMALAIAAGQSVVSVATLLMTICFVFMMIFSGLLVNLTTIASWLSWLQYFSIPRYGFTALQHNEFLGQNFCPGLNATGNNPCNYATCTGEEYLVKQGIDLSPWGLWKNHVALACMIVIFLTIAYLKLLFLKKYS
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Primary active transporter
>
ATP-binding cassette
>
ABCG subfamily
Function
Broad substrate specificity ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes a wide variety of physiological compounds, dietary toxins and xenobiotics from cells (PubMed:11306452, PubMed:12958161, PubMed:19506252, PubMed:20705604, PubMed:28554189, PubMed:30405239, PubMed:31003562). Involved in porphyrin homeostasis, mediating the export of protoporphyrin IX (PPIX) from both mitochondria to cytosol and cytosol to extracellular space, it also functions in the cellular export of heme (PubMed:20705604, PubMed:23189181). Also mediates the efflux of sphingosine-1-P from cells (PubMed:20110355). Acts as a urate exporter functioning in both renal and extrarenal urate excretion (PubMed:19506252, PubMed:20368174, PubMed:22132962, PubMed:31003562, PubMed:36749388). In kidney, it also functions as a physiological exporter of the uremic toxin indoxyl sulfate (By similarity). Also involved in the excretion of steroids like estrone 3-sulfate/E1S, 3beta-sulfooxy-androst-5-en-17-one/DHEAS, and other sulfate conjugates (PubMed:12682043, PubMed:28554189, PubMed:30405239). Mediates the secretion of the riboflavin and biotin vitamins into milk (By similarity). Extrudes pheophorbide a, a phototoxic porphyrin catabolite of chlorophyll, reducing its bioavailability (By similarity). Plays an important role in the exclusion of xenobiotics from the brain (Probable). It confers to cells a resistance to multiple drugs and other xenobiotics including mitoxantrone, pheophorbide, camptothecin, methotrexate, azidothymidine, and the anthracyclines daunorubicin and doxorubicin, through the control of their efflux (PubMed:11306452, PubMed:12477054, PubMed:15670731, PubMed:18056989, PubMed:31254042). In placenta, it limits the penetration of drugs from the maternal plasma into the fetus (By similarity). May play a role in early stem cell self-renewal by blocking differentiation (By similarity).
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Uniprot ID
Primary ID:
Q9UNQ0

Secondarily ID:
A0A1W3
A8K1T5
O95374
Q4W5I3
Q53ZQ1
Q569L4
Q5YLG4
Q86V64
Q8IX16
Q96LD6
Q96TA8
Q9BY73
Q9NUS0
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Ensembl ID
ENSG00000118777
HGNC ID
HGNC:74
Subcellular Location
Cell membrane
Apical cell membrane
Mitochondrion membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000023 , BTI-Tn-5B1-4
Compound ID Compound Name Compound Formula
CP0389588
N-(3,4-dimethoxyphenyl)-6-nitro-2-[3-(trifluoromethyl)phenyl]quinazolin-4-amine
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C23H17F3N4O4
 1
1
Activity = 35 nM
   TI
   LI
   LO
   TS
CP0389586
4-N-(3-methoxyphenyl)-2-pyridin-3-ylquinazoline-4,6-diamine
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C20H17N5O
 1
1
Activity = 250 nM
   TI
   LI
   LO
   TS
CP0389585
6-nitro-2-phenyl-N-[3-(trifluoromethyl)phenyl]quinazolin-4-amine
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C21H13F3N4O2
 1
1
Activity = 1000 nM
   TI
   LI
   LO
   TS
CP0440751
N-(4-methoxyphenyl)-6-nitro-2-pyridin-3-ylquinazolin-4-amine
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C20H15N5O3
 1
1
Activity = 1000 nM
   TI
   LI
   LO
   TS
CP0409100
4-[[2-(3-methoxyphenyl)-6-nitroquinazolin-4-yl]amino]benzonitrile
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C22H15N5O3
 1
1
EC50 = 10 nM
   TI
   LI
   LO
   TS
CP0435285
4-[(6-nitro-2-phenylquinazolin-4-yl)amino]benzonitrile
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C21H13N5O2
 1
1
EC50 = 29 nM
   TI
   LI
   LO
   TS
CP0409037
6-nitro-N-phenyl-2-[3-(trifluoromethyl)phenyl]quinazolin-4-amine
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C21H13F3N4O2
 1
1
EC50 = 48 nM
   TI
   LI
   LO
   TS
CP0389672
N-(3,4-dimethoxyphenyl)-6-nitro-2-phenylquinazolin-4-amine
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C22H18N4O4
 1
1
EC50 = 63 nM
   TI
   LI
   LO
   TS
CP0389584
N-(4-methoxyphenyl)-6-nitro-2-pyridin-4-ylquinazolin-4-amine
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C20H15N5O3
 1
1
EC50 = 112 nM
   TI
   LI
   LO
   TS
CP0389668
3-[(6-nitro-2-phenylquinazolin-4-yl)amino]benzonitrile
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C21H13N5O2
 1
1
EC50 = 326 nM
   TI
   LI
   LO
   TS
CP0435284
N-(3-methoxyphenyl)-6-nitro-2-pyridin-3-ylquinazolin-4-amine
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C20H15N5O3
 1
1
EC50 = 690 nM
   TI
   LI
   LO
   TS
CP0435283
4-N-(3-methoxyphenyl)-2-[3-(trifluoromethyl)phenyl]quinazoline-4,6-diamine
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C22H17F3N4O
 1
1
EC50 = 1230 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0141589
3-((3S,6S)-6-Isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,6,7,12,12a-octahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indol-3-yl)-propionic acid tert-butyl ester
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C26H35N3O5
 1
1 EC50 = 10 nM
CP0116921
1N-{4-[2-(6,7-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolinyl)ethyl]phenyl}-4,5-dimethoxy-2-(3-quinolylcarboxamido)benzamide
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C38H38N4O6
 2
1 EC50 = 100 nM
2 IC50 = 183.3 nM
CP0036082
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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C22H24ClFN4O3
 1
1 EC50 = 300 nM
CP0046870
FTC
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C22H25N3O3
 1
1 EC50 = 1000 nM
CP0528032
5-[(2,4-dibromophenyl)methoxy]-N-[2-(5-methoxy-1H-indol-3-yl)ethyl]-4-oxochromene-2-carboxamide
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C28H22Br2N2O5
 1
1 IC50 = 46 nM
CP0254388
5-Methoxy-9-oxo-9,10-dihydro-acridine-4-carboxylic acid {4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-amide
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C34H33N3O5
 1
1 IC50 = 252.2 nM
CP0197212
N-[(3,4-dimethoxyphenyl)methyl]-2-[2-(3-methoxyphenyl)ethyl]aniline
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C24H27NO3
 1
1 IC50 = 500 nM
CP0064543
N-[(2,3-dimethoxyphenyl)methyl]-2-[2-(3-methoxyphenyl)ethyl]aniline
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C24H27NO3
 1
1 IC50 = 1500 nM
CP0197181
(E)-1,3-bis(3,4-dimethoxyphenyl)prop-2-en-1-one
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C19H20O5
 1
1 IC50 = 5120 nM
CP0035720
(-)-reserpine
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C33H40N2O9
 1
1 IC50 = 12600 nM
CP0071795
CHEBI:76010
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C20H19F2N3O5
 1
1 IC50 = 67000 nM
CP0036222
(3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-30-ethyl-33-[(1R,2R,4E)-1-hydroxy-2-methylhex-4-en-1-yl]-1,4,7,10,12,15,19,25,28-nonamethyl-6,9,18,24-tetrakis(2-methylpropyl)-3,21-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecone
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C62H111N11O12
 1
1 IC50 > 6568 nM
Clinical Information about the Protein
Target 1 ( ATP-binding cassette transporter G2 (ABCG2) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Rheumatoid arthritis [ICD-11: FA20]
Approved Drug(s) 1 Approved Drug  1
1 Sulfasalazine Approved
Rheumatoid arthritis