General Information of the Protein
Protein ID
PT01546
Protein Name
ATP-dependent translocase ABCB1
Secondarily
Protein Name
ATP-binding cassette sub-family B member 1
Multidrug resistance protein 1
P-glycoprotein 1
Phospholipid transporter ABCB1
Gene Name
ABCB1
Secondarily
Gene Name
MDR1
PGY1
Sequence
MDLEGDRNGGAKKKNFFKLNNKSEKDKKEKKPTVSVFSMFRYSNWLDKLYMVVGTLAAIIHGAGLPLMMLVFGEMTDIFANAGNLEDLMSNITNRSDINDTGFFMNLEEDMTRYAYYYSGIGAGVLVAAYIQVSFWCLAAGRQIHKIRKQFFHAIMRQEIGWFDVHDVGELNTRLTDDVSKINEGIGDKIGMFFQSMATFFTGFIVGFTRGWKLTLVILAISPVLGLSAAVWAKILSSFTDKELLAYAKAGAVAEEVLAAIRTVIAFGGQKKELERYNKNLEEAKRIGIKKAITANISIGAAFLLIYASYALAFWYGTTLVLSGEYSIGQVLTVFFSVLIGAFSVGQASPSIEAFANARGAAYEIFKIIDNKPSIDSYSKSGHKPDNIKGNLEFRNVHFSYPSRKEVKILKGLNLKVQSGQTVALVGNSGCGKSTTVQLMQRLYDPTEGMVSVDGQDIRTINVRFLREIIGVVSQEPVLFATTIAENIRYGRENVTMDEIEKAVKEANAYDFIMKLPHKFDTLVGERGAQLSGGQKQRIAIARALVRNPKILLLDEATSALDTESEAVVQVALDKARKGRTTIVIAHRLSTVRNADVIAGFDDGVIVEKGNHDELMKEKGIYFKLVTMQTAGNEVELENAADESKSEIDALEMSSNDSRSSLIRKRSTRRSVRGSQAQDRKLSTKEALDESIPPVSFWRIMKLNLTEWPYFVVGVFCAIINGGLQPAFAIIFSKIIGVFTRIDDPETKRQNSNLFSLLFLALGIISFITFFLQGFTFGKAGEILTKRLRYMVFRSMLRQDVSWFDDPKNTTGALTTRLANDAAQVKGAIGSRLAVITQNIANLGTGIIISFIYGWQLTLLLLAIVPIIAIAGVVEMKMLSGQALKDKKELEGSGKIATEAIENFRTVVSLTQEQKFEHMYAQSLQVPYRNSLRKAHIFGITFSFTQAMMYFSYAGCFRFGAYLVAHKLMSFEDVLLVFSAVVFGAMAVGQVSSFAPDYAKAKISAAHIIMIIEKTPLIDSYSTEGLMPNTLEGNVTFGEVVFNYPTRPDIPVLQGLSLEVKKGQTLALVGSSGCGKSTVVQLLERFYDPLAGKVLLDGKEIKRLNVQWLRAHLGIVSQEPILFDCSIAENIAYGDNSRVVSQEEIVRAAKEANIHAFIESLPNKYSTKVGDKGTQLSGGQKQRIAIARALVRQPHILLLDEATSALDTESEKVVQEALDKAREGRTCIVIAHRLSTIQNADLIVVFQNGRVKEHGTHQQLLAQKGIYFSMVSVQAGTKRQ
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Organism
Homo sapiens, Human
Protein Classification
Transporter
>
Primary active transporter
>
ATP-binding cassette
>
ABCB subfamily
Function
Translocates drugs and phospholipids across the membrane (PubMed:8898203, PubMed:2897240, PubMed:9038218, PubMed:35970996). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:9038218, PubMed:35970996).
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Uniprot ID
Primary ID:
P08183

Secondarily ID:
A8K294
B5AK60
Q12755
Q14812
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Ensembl ID
ENSG00000085563
HGNC ID
HGNC:40
Subcellular Location
Cell membrane
Apical cell membrane
Cytoplasm
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: CL000924 , 12D7-MDR1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0473348
 Compound Info 
[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl 4-[[4-[(2R,3S)-3-[[(3aS,4R,6aR)-2,3,3a,4,5,6a-hexahydrofuro[2,3-b]furan-4-yl]oxycarbonylamino]-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-4-phenylbutan-2-yl]oxy-4-oxobutyl]disulfanyl]butanoate
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C49H65N9O10S3
  2
1
IC50 = 500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 510 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0479821
 Compound Info 
[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl 4-[[4-[3-[[(2R,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinolin-2-yl]-3-hydroxy-1-phenylsulfanylbutan-2-yl]carbamoyl]-2-methylphenoxy]-4-oxobutyl]disulfanyl]butanoate
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C54H73N9O7S3
  2
1
IC50 = 650 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 770 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0036382
 Compound Info 
CAS_52-53-9
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C27H38N2O4
  1
1
IC50 = 1200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0422359
 Compound Info 
bis[[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl] dodecanedioate
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C40H54N12O4
  2
1
IC50 = 1400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 1800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0381640
 Compound Info 
bis[[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl] decanedioate
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C38H50N12O4
  2
1
IC50 = 2100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 2300 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0403732
 Compound Info 
bis[[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl] nonanedioate
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C37H48N12O4
  1
1
IC50 = 2600 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0010655
 Compound Info 
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylphenyl)formamido]-4-(phenylsulfanyl)butyl]-decahydroisoquinoline-3-carboxamide
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C32H45N3O4S
  2
1
IC50 = 5800 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 9100 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0381641
 Compound Info 
bis[[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl] heptanedioate
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C35H44N12O4
  2
1
IC50 = 7700 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 10500 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0013112
 Compound Info 
(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl N-[(2S,3R)-4-[(4-aminobenzene)(2-methylpropyl)sulfonamido]-3-hydroxy-1-phenylbutan-2-yl]carbamate
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C27H37N3O7S
  2
1
IC50 = 33200 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
2
IC50 = 60000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0411668
 Compound Info 
bis[[(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methyl] butanedioate
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C32H38N12O4
  1
1
IC50 = 50000 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000072 , A2780
 Cell Line Info 
Cell Line ID: CL000135 , A2780ADR
 Cell Line Info 
Cell Line ID: CL000051 , BHK-21
 Cell Line Info 
Cell Line ID: CL000023 , BTI-Tn-5B1-4
 Cell Line Info 
Cell Line ID: CL000034 , Caco-2
 Cell Line Info 
Cell Line ID: CL000108 , CCRF-CEM
 Cell Line Info 
Cell Line ID: CL000253 , CCRF/VCR1000
 Cell Line Info 
Cell Line ID: CL000345 , CEM/VLB100
 Cell Line Info 
Cell Line ID: CL000357 , CEM/VLB500
 Cell Line Info 
Cell Line ID: CL000946 , DU145-TxR
 Cell Line Info 
Cell Line ID: CL000088 , Flp-In-293
 Cell Line Info 
Cell Line ID: CL000598 , hCMEC/D3
 Cell Line Info 
Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000017 , HeLa
 Cell Line Info 
Cell Line ID: CL000162 , HeLa S3
 Cell Line Info 
Cell Line ID: CL000885 , HeLa-T5
 Cell Line Info 
Cell Line ID: CL000828 , HL60/MDR
 Cell Line Info 
Cell Line ID: CL000002 , K-562
 Cell Line Info 
Cell Line ID: CL000137 , K562/A02
 Cell Line Info 
Cell Line ID: CL000353 , K562/Adr
 Cell Line Info 
Cell Line ID: CL000356 , KB-V1
 Cell Line Info 
Cell Line ID: CL000346 , L-5178-Y
 Cell Line Info 
Cell Line ID: CL000089 , LLC-GA5-CoL150
 Cell Line Info 
Cell Line ID: CL000009 , LLC-PK1
 Cell Line Info 
Cell Line ID: CL000105 , LS180
 Cell Line Info 
Cell Line ID: CL000083 , MCF-7
 Cell Line Info 
Cell Line ID: CL000920 , MCF-7/DX1
 Cell Line Info 
Cell Line ID: CL000350 , MDA435/LCC6MDR1
 Cell Line Info 
Cell Line ID: CL000031 , MDCK
 Cell Line Info 
Cell Line ID: CL000036 , MDCK-II
 Cell Line Info 
Cell Line ID: CL000359 , MDCK-MDR1
 Cell Line Info 
Cell Line ID: CL001024 , MDR CCRF vcr1000
 Cell Line Info 
Cell Line ID: CL000838 , MDR-KB-VCR
 Cell Line Info 
Cell Line ID: CL000840 , MDR-KB-VIN
 Cell Line Info 
Cell Line ID: CL000355 , MES-SA/Dx5
 Cell Line Info 
Cell Line ID: CL000349 , NCI-ADR-RES
 Cell Line Info 
Cell Line ID: CL000035 , NIH 3T3
 Cell Line Info 
Cell Line ID: CL000167 , NIH-3T3-G185
 Cell Line Info 
Cell Line ID: CL000248 , OCI-AML-2
 Cell Line Info 
Cell Line ID: CL001059 , P388/VMDRC.04
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Cell Line ID: CL000084 , SK-OV-3
 Cell Line Info 
Cell Line ID: CL000113 , SW620/AD300
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0212865
 Compound Info 
CHEBI:5677
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C39H44N2O7
  2
1 Activity = 20 nM
2 Ki = 20 nM
CP0036082
 Compound Info 
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
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C22H24ClFN4O3
  1
1 EC50 > 1000 nM
CP0317641
 Compound Info 
Encequidar
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C38H36N6O7
  1
1 IC50 = 0.6 nM
CP0254388
 Compound Info 
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 = 4.9 nM
CP0116921
 Compound Info 
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
  1
1 IC50 = 32.7 nM
CP0064543
 Compound Info 
N-[(2,3-dimethoxyphenyl)methyl]-2-[2-(3-methoxyphenyl)ethyl]aniline
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C24H27NO3
  1
1 IC50 = 85 nM
CP0036222
 Compound Info 
(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
  2
1 IC50 = 141.3 nM
2 IC50 = 1412.54 nM
CP0197212
 Compound Info 
N-[(3,4-dimethoxyphenyl)methyl]-2-[2-(3-methoxyphenyl)ethyl]aniline
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C24H27NO3
  1
1 IC50 = 180 nM
CP0170006
 Compound Info 
1,2-dimethoxy-3-((2-(3-methoxyphenethyl)phenoxy)methyl)benzene
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C24H26O4
  1
1 IC50 = 250 nM
CP0136582
 Compound Info 
N-[2-[[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]phenyl]-3,4-dimethoxybenzamide
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C35H37N3O6
  1
1 IC50 = 331.13 nM
CP0307451
 Compound Info 
N-[2-[[4-[2-(3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]carbamoyl]phenyl]quinoline-3-carboxamide
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C34H30N4O2
  1
1 IC50 = 354.81 nM
CP0250552
 Compound Info 
CHEMBL2087786
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C32H31Cl2N3O2
  1
1 IC50 = 400 nM
CP0109403
 Compound Info 
2-benzamido-N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]benzamide
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C33H33N3O4
  1
1 IC50 = 512.86 nM
CP0139168
 Compound Info 
1,2-dimethoxy-4-((2-(3-methoxyphenethyl)phenoxy)methyl)benzene
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C24H26O4
  1
1 IC50 = 650 nM
CP0036382
 Compound Info 
CAS_52-53-9
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C27H38N2O4
  7
1 IC50 = 1480 nM
2 IC50 = 2110 nM
3 IC50 = 6606.93 nM
4 IC50 = 12000 nM
5 IC50 = 18000 nM
6 Ki = 300 nM
7 Ki = 2500 nM
CP0087258
 Compound Info 
ethyl 2-[(1S)-2-methyl-1-[[2-[(1S)-2-methyl-1-[[2-[(1S)-2-methyl-1-[(2-methylpropan-2-yl)oxycarbonylamino]propyl]-1,3-thiazole-4-carbonyl]amino]propyl]-1,3-thiazole-4-carbonyl]amino]propyl]-1,3-thiazole-4-carboxylate
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C31H44N6O6S3
  1
1 IC50 = 1500 nM
CP0069095
 Compound Info 
(S) Verapamil
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C27H38N2O4
  1
1 IC50 = 2090 nM
CP0067890
 Compound Info 
(R)-5-((3,4-dimethoxyphenethyl)(methyl)amino)-2-(3,4-dimethoxyphenyl)-2-isopropylpentanenitrile
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C27H38N2O4
  2
1 IC50 = 2370 nM
2 Ki = 1600 nM
CP0035720
 Compound Info 
(-)-reserpine
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C33H40N2O9
  2
1 IC50 = 3019.95 nM
2 Ki = 100 nM
CP0206932
 Compound Info 
2-(3,4-Dimethoxy-phenyl)-5-[2-(3,4-dimethoxy-phenyl)-ethylamino]-2-isopropyl-pentanenitrile
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C26H36N2O4
  1
1 IC50 = 4240 nM
CP0471245
 Compound Info 
4-[3-[4-[1-[(2-bromophenyl)methyl]-2-phenylindol-3-yl]-7-methoxyquinazolin-6-yl]oxypropyl]morpholine
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C37H35BrN4O3
  1
1 IC50 = 5100 nM
CP0055461
 Compound Info 
CHEBI:7550
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C26H29N3O6
  1
1 IC50 = 5128.61 nM
CP0075209
 Compound Info 
(2ALPHA,2''BETA,3BETA,4ALPHA,5BETA)-VINCALEUKOBLASTINE
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C46H58N4O9
  4
1 IC50 = 10000 nM
2 IC50 = 34000 nM
3 Ki = 100 nM
4 Ki = 1300 nM
CP0002778
 Compound Info 
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
  1
1 IC50 = 12589.25 nM
CP0005212
 Compound Info 
US8987315, Ketoconazole
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C26H28Cl2N4O4
  2
1 IC50 = 13000 nM
2 Ki = 1200 nM
CP0720909
 Compound Info 
(2S,3R,4R)-5-(3,4-dimethylbenzamido)pentane-1,2,3,4-tetrayl tetraacetate
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C22H29NO9
  1
1 IC50 = 28000 nM
CP0768756
 Compound Info 
2-(acetoxymethyl)-6-(phenylthio)tetrahydro-2H-pyran-3,4,5-triyl triacetate
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C20H24O9S
  1
1 IC50 = 37000 nM
CP0038813
 Compound Info 
(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
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C21H30O2
  1
1 IC50 = 48977.88 nM
CP0077731
 Compound Info 
(+)-cis-Diltiazem
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C22H26N2O4S
  1
1 IC50 = 61659.5 nM
CP0071795
 Compound Info 
CHEBI:76010
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C20H19F2N3O5
  1
1 IC50 > 90000 nM
CP0020849
 Compound Info 
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chromen-4-one
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C15H10O7
  1
1 Kd = 7079.46 nM
CP0003923
 Compound Info 
(2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}ethyl)dimethylamine
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C26H29NO
  1
1 Ki = 100 nM
CP0034615
 Compound Info 
(6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol
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C20H24N2O2
  2
1 Ki = 2600 nM
2 Ki = 5000 nM
CP0068493
 Compound Info 
(2-{4-[(2-butyl-1-benzofuran-3-yl)carbonyl]-2,6-diiodophenoxy}ethyl)diethylamine
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C25H29I2NO3
  1
1 Ki = 3200 nM
CP0011846
 Compound Info 
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenylpropan-1-one
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C21H27NO3
  1
1 Ki = 4200 nM
CP0031625
 Compound Info 
10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)phenothiazine;hydrochloride
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C21H24F3N3S
  1
1 Ki = 6500 nM
CP0078400
 Compound Info 
QUININE
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C20H24N2O2
  1
1 Ki = 12000 nM
Clinical Information about the Protein
Target 1 ( Multidrug resistance protein 1 (ABCB1) )
Target Type Clinical trial Target
Disease 3 Target-related Diseases  3
1 Ovarian cancer [ICD-11: 2C73]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Adrenocortical carcinoma [ICD-11: 2D11.Z]
Discontinued Drug(s) 5 Discontinued Drugs  5
1 Biricodar
 Drug Info 
Discontinued in Phase 2
Ovarian cancer
2 S-9788
 Drug Info 
Discontinued in Phase 2
Solid tumour/cancer
3 Tariquidar
 Drug Info 
Discontinued in Phase 2
Adrenocortical carcinoma
4 Elacridar
 Drug Info 
Discontinued in Phase 1
Solid tumour/cancer
5 ONT-093
 Drug Info 
Discontinued in Phase 1
Solid tumour/cancer