Proteins > ATP-dependent translocase ABCB1
Page last updated: 2024-08-07 15:45:38
ATP-dependent translocase ABCB1
An ATP-dependent translocase ABCB1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P08183]
Synonyms
ATP-binding cassette sub-family B member 1;
Multidrug resistance protein 1;
7.6.2.2;
P-glycoprotein 1;
Phospholipid transporter ABCB1;
7.6.2.1
Research
Bioassay Publications (174)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 23 (13.22) | 18.2507 |
| 2000's | 71 (40.80) | 29.6817 |
| 2010's | 61 (35.06) | 24.3611 |
| 2020's | 19 (10.92) | 2.80 |
Compounds (222)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gallopamil | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| amiodarone | Homo sapiens (human) | IC50 | 34.0500 | 2 | 2 |
| amiodarone | Homo sapiens (human) | Ki | 4.4900 | 2 | 2 |
| amlodipine | Homo sapiens (human) | IC50 | 22.0000 | 1 | 1 |
| astemizole | Homo sapiens (human) | IC50 | 0.9667 | 3 | 3 |
| azelastine | Homo sapiens (human) | IC50 | 23.0000 | 2 | 2 |
| verapamil | Homo sapiens (human) | IC50 | 18.7117 | 93 | 94 |
| verapamil | Homo sapiens (human) | Ki | 3.6114 | 7 | 7 |
| carvedilol | Homo sapiens (human) | IC50 | 5.7333 | 3 | 3 |
| celiprolol | Homo sapiens (human) | Ki | 313.0000 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | Ki | 6.4000 | 2 | 2 |
| cimetidine | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| clofazimine | Homo sapiens (human) | IC50 | 0.9000 | 3 | 3 |
| clotrimazole | Homo sapiens (human) | IC50 | 4.9000 | 3 | 3 |
| clotrimazole | Homo sapiens (human) | Ki | 36.9600 | 2 | 2 |
| dipyridamole | Homo sapiens (human) | IC50 | 26.9000 | 3 | 3 |
| donepezil | Homo sapiens (human) | IC50 | 34.8500 | 1 | 1 |
| ebastine | Homo sapiens (human) | IC50 | 1.5000 | 1 | 1 |
| felodipine | Homo sapiens (human) | IC50 | 39.5333 | 3 | 3 |
| fentanyl | Homo sapiens (human) | IC50 | 6.5000 | 1 | 1 |
| fluconazole | Homo sapiens (human) | Ki | 700.0000 | 2 | 2 |
| fluphenazine | Homo sapiens (human) | IC50 | 7.5333 | 3 | 3 |
| fluoxetine | Homo sapiens (human) | IC50 | 115.5000 | 1 | 1 |
| haloperidol | Homo sapiens (human) | IC50 | 5.3000 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Ki | 0.2000 | 1 | 1 |
| indomethacin | Homo sapiens (human) | IC50 | 30.0000 | 1 | 2 |
| itraconazole | Homo sapiens (human) | IC50 | 1.6660 | 5 | 5 |
| ketoconazole | Homo sapiens (human) | IC50 | 12.2540 | 10 | 10 |
| ketoconazole | Homo sapiens (human) | Ki | 10.4567 | 3 | 3 |
| lansoprazole | Homo sapiens (human) | IC50 | 62.8000 | 1 | 1 |
| loperamide | Homo sapiens (human) | IC50 | 2.5000 | 1 | 1 |
| loratadine | Homo sapiens (human) | IC50 | 11.4000 | 1 | 1 |
| manidipine | Homo sapiens (human) | IC50 | 4.6250 | 2 | 2 |
| methadone | Homo sapiens (human) | IC50 | 7.5000 | 1 | 1 |
| metoprolol | Homo sapiens (human) | IC50 | 1,300.0000 | 1 | 1 |
| metoprolol | Homo sapiens (human) | Ki | 200.0000 | 1 | 1 |
| miconazole | Homo sapiens (human) | IC50 | 3.0000 | 3 | 3 |
| miconazole | Homo sapiens (human) | Ki | 40.9300 | 2 | 2 |
| midazolam | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| mitoxantrone | Homo sapiens (human) | IC50 | 1.5010 | 1 | 1 |
| nefazodone | Homo sapiens (human) | IC50 | 4.7000 | 1 | 1 |
| nicardipine | Homo sapiens (human) | IC50 | 7.7927 | 15 | 15 |
| nifedipine | Homo sapiens (human) | IC50 | 292.5000 | 2 | 2 |
| nilvadipine | Homo sapiens (human) | IC50 | 18.0000 | 1 | 1 |
| nisoldipine | Homo sapiens (human) | IC50 | 44.1000 | 1 | 1 |
| nitrendipine | Homo sapiens (human) | IC50 | 68.2000 | 1 | 1 |
| omeprazole | Homo sapiens (human) | IC50 | 73.7750 | 2 | 4 |
| pantoprazole | Homo sapiens (human) | IC50 | 17.9000 | 1 | 1 |
| propafenone | Homo sapiens (human) | IC50 | 0.3311 | 1 | 1 |
| propafenone | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| propranolol | Homo sapiens (human) | IC50 | 573.0000 | 1 | 1 |
| propranolol | Homo sapiens (human) | Ki | 48.0000 | 1 | 1 |
| ranitidine | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| imatinib | Homo sapiens (human) | IC50 | 6.9145 | 4 | 4 |
| terfenadine | Homo sapiens (human) | IC50 | 1.8167 | 6 | 6 |
| trifluoperazine | Homo sapiens (human) | IC50 | 8.1333 | 3 | 3 |
| trifluoperazine | Homo sapiens (human) | Ki | 6.5000 | 1 | 1 |
| triflupromazine | Homo sapiens (human) | Ki | 15.7000 | 1 | 1 |
| reserpine | Homo sapiens (human) | IC50 | 3.2092 | 10 | 10 |
| reserpine | Homo sapiens (human) | Ki | 5.4160 | 5 | 5 |
| spironolactone | Homo sapiens (human) | IC50 | 23.6000 | 1 | 1 |
| vincristine | Homo sapiens (human) | Ki | 213.0000 | 1 | 1 |
| colchicine | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| ergotamine | Homo sapiens (human) | Ki | 56.5750 | 2 | 2 |
| emetine | Homo sapiens (human) | IC50 | 72.7571 | 7 | 7 |
| dihydroergotamine | Homo sapiens (human) | Ki | 559.9700 | 2 | 2 |
| alpha-naphthoflavone | Homo sapiens (human) | IC50 | 24.6000 | 1 | 1 |
| erythromycin | Homo sapiens (human) | IC50 | 47.6667 | 3 | 3 |
| erythromycin | Homo sapiens (human) | Ki | 518.8950 | 2 | 2 |
| vinblastine | Homo sapiens (human) | IC50 | 25.2571 | 10 | 10 |
| vinblastine | Homo sapiens (human) | Ki | 32.5000 | 6 | 6 |
| pimozide | Homo sapiens (human) | IC50 | 2.2000 | 3 | 3 |
| dexpropranolol | Homo sapiens (human) | IC50 | 583.0000 | 1 | 1 |
| daunorubicin | Homo sapiens (human) | Ki | 56.7500 | 2 | 2 |
| bromocriptine | Homo sapiens (human) | Ki | 3.3850 | 2 | 2 |
| ergocristine | Homo sapiens (human) | Ki | 28.0650 | 2 | 2 |
| paclitaxel | Homo sapiens (human) | IC50 | 36.6592 | 5 | 5 |
| etoposide | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| etoposide | Homo sapiens (human) | Ki | 522.0000 | 2 | 2 |
| diltiazem | Homo sapiens (human) | IC50 | 54.7351 | 5 | 5 |
| sufentanil | Homo sapiens (human) | IC50 | 4.5000 | 1 | 1 |
| paroxetine | Homo sapiens (human) | IC50 | 29.8000 | 1 | 1 |
| colforsin | Homo sapiens (human) | IC50 | 134.2000 | 2 | 2 |
| alfentanil | Homo sapiens (human) | IC50 | 112.0000 | 1 | 1 |
| lovastatin | Homo sapiens (human) | IC50 | 50.0200 | 5 | 5 |
| simvastatin | Homo sapiens (human) | IC50 | 29.5800 | 5 | 5 |
| sertindole | Homo sapiens (human) | IC50 | 6.5000 | 1 | 1 |
| niguldipine | Homo sapiens (human) | IC50 | 0.7080 | 1 | 1 |
| mibefradil | Homo sapiens (human) | IC50 | 1.5800 | 5 | 5 |
| aripiprazole | Homo sapiens (human) | IC50 | 0.7800 | 1 | 1 |
| atorvastatin | Homo sapiens (human) | IC50 | 289.0000 | 2 | 2 |
| nelfinavir | Homo sapiens (human) | IC50 | 5.2278 | 9 | 9 |
| amprenavir | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| oseltamivir | Homo sapiens (human) | IC50 | 1,300.0000 | 1 | 1 |
| epigallocatechin gallate | Homo sapiens (human) | IC50 | 0.1234 | 2 | 2 |
| dexverapamil | Homo sapiens (human) | IC50 | 3.4900 | 3 | 3 |
| dexverapamil | Homo sapiens (human) | Ki | 1.6000 | 1 | 1 |
| tangeretin | Homo sapiens (human) | IC50 | 39.0000 | 1 | 1 |
| sertraline | Homo sapiens (human) | IC50 | 31.8000 | 1 | 1 |
| pafenolol | Homo sapiens (human) | Ki | 5.5000 | 1 | 1 |
| hernandezine | Homo sapiens (human) | IC50 | 0.6129 | 29 | 29 |
| hernandezine | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| nobiletin | Homo sapiens (human) | IC50 | 11.5000 | 1 | 1 |
| ergocornine | Homo sapiens (human) | Ki | 64.8500 | 2 | 2 |
| 5,7,4'-trimethylapigenin | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
| clarithromycin | Homo sapiens (human) | IC50 | 34.7000 | 7 | 7 |
| tebufenozide | Homo sapiens (human) | IC50 | 21.5000 | 1 | 1 |
| lekoptin | Homo sapiens (human) | IC50 | 3.2867 | 3 | 3 |
| lopinavir | Homo sapiens (human) | IC50 | 6.0000 | 2 | 2 |
| 3,5,7,3',4'-pentamethoxyflavone | Homo sapiens (human) | IC50 | 23.4000 | 1 | 1 |
| 6-methoxyflavanone | Homo sapiens (human) | IC50 | 64.0000 | 1 | 1 |
| desethylamiodarone | Homo sapiens (human) | IC50 | 20.3000 | 2 | 2 |
| norverapamil | Homo sapiens (human) | IC50 | 1.8133 | 3 | 3 |
| methoxyfenozide | Homo sapiens (human) | IC50 | 44.3000 | 1 | 1 |
| dihydroergocristine | Homo sapiens (human) | Ki | 263.5000 | 2 | 2 |
| dihydroergocryptine | Homo sapiens (human) | Ki | 190.1600 | 2 | 2 |
| efonidipine | Homo sapiens (human) | IC50 | 16.9667 | 3 | 3 |
| elacridar | Homo sapiens (human) | IC50 | 0.4427 | 6 | 6 |
| gefitinib | Homo sapiens (human) | IC50 | 19.9700 | 1 | 1 |
| desloratadine | Homo sapiens (human) | IC50 | 43.0000 | 1 | 1 |
| norgallopamil | Homo sapiens (human) | IC50 | 5.7000 | 3 | 3 |
| hapalosin | Homo sapiens (human) | IC50 | 9.8000 | 2 | 2 |
| 5'-(sulfonylbenzoyl)adenosine | Homo sapiens (human) | IC50 | 0.3533 | 3 | 3 |
| alpha-ergocryptine | Homo sapiens (human) | Ki | 9.3150 | 2 | 2 |
| sinensetin | Homo sapiens (human) | IC50 | 16.1000 | 2 | 2 |
| 6-methoxyflavone | Homo sapiens (human) | IC50 | 15.0000 | 1 | 1 |
| atazanavir | Homo sapiens (human) | IC50 | 67.8000 | 1 | 1 |
| lonafarnib | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| tariquidar | Homo sapiens (human) | IC50 | 1.4278 | 38 | 39 |
| 3,3',4',5,6,7,8-heptamethoxyflavone | Homo sapiens (human) | IC50 | 31.0000 | 1 | 1 |
| zosuquidar trihydrochloride | Homo sapiens (human) | IC50 | 2.3006 | 6 | 7 |
| 3',4',7-trimethoxyflavone | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| desmethylazelastine | Homo sapiens (human) | IC50 | 26.8000 | 2 | 2 |
| tetraphenylphosphonium | Homo sapiens (human) | IC50 | 458.3000 | 2 | 2 |
| erlotinib | Homo sapiens (human) | IC50 | 26.0000 | 1 | 1 |
| limonin | Homo sapiens (human) | IC50 | 19.1400 | 1 | 1 |
| etravirine | Homo sapiens (human) | IC50 | 7.6000 | 1 | 1 |
| troleandomycin | Homo sapiens (human) | IC50 | 77.6000 | 3 | 3 |
| troleandomycin | Homo sapiens (human) | Ki | 285.4700 | 2 | 2 |
| darunavir | Homo sapiens (human) | IC50 | 43.0400 | 5 | 5 |
| 3',4'-dimethoxy-alpha-naphthoflavone | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| ritonavir | Homo sapiens (human) | IC50 | 14.1000 | 6 | 6 |
| tryptoquivaline | Homo sapiens (human) | IC50 | 1.8080 | 1 | 1 |
| quinidine | Homo sapiens (human) | IC50 | 49.2333 | 9 | 9 |
| quinidine | Homo sapiens (human) | Ki | 3.6240 | 5 | 5 |
| saquinavir | Homo sapiens (human) | IC50 | 26.4200 | 5 | 5 |
| abacavir | Homo sapiens (human) | IC50 | 500.0000 | 3 | 3 |
| mepirodipine | Homo sapiens (human) | IC50 | 10.6000 | 2 | 2 |
| ergonovine | Homo sapiens (human) | Ki | 107.7500 | 2 | 2 |
| doxorubicin hydrochloride | Homo sapiens (human) | IC50 | 96.9100 | 1 | 1 |
| resveratrol | Homo sapiens (human) | IC50 | 60.0000 | 1 | 1 |
| ketoconazole | Homo sapiens (human) | IC50 | 1.0580 | 1 | 1 |
| 5,7,3',4',5'-pentamethoxyflavone | Homo sapiens (human) | IC50 | 0.4000 | 1 | 1 |
| piperine | Homo sapiens (human) | IC50 | 44.8000 | 2 | 2 |
| 2-amino-5,6,7,8-tetrahydro-[1]benzothiolo[2,3-d][1,3]thiazin-4-one | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| 3',4'-dimethoxyflavone | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| reversan | Homo sapiens (human) | IC50 | 6.8000 | 1 | 1 |
| digoxin | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| tamoxifen | Homo sapiens (human) | IC50 | 19.7250 | 4 | 4 |
| tamoxifen | Homo sapiens (human) | Ki | 0.1000 | 1 | 1 |
| polysulfide rubber | Homo sapiens (human) | IC50 | 0.6026 | 1 | 1 |
| valinomycin | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| quinine | Homo sapiens (human) | IC50 | 137.8556 | 9 | 9 |
| quinine | Homo sapiens (human) | Ki | 12.0000 | 1 | 1 |
| ly335979 | Homo sapiens (human) | IC50 | 0.0589 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 52.5000 | 1 | 1 |
| luteolin | Homo sapiens (human) | IC50 | 19.6000 | 1 | 1 |
| ayanin | Homo sapiens (human) | IC50 | 13.0000 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 41.0000 | 1 | 1 |
| pterostilbene | Homo sapiens (human) | IC50 | 42.0000 | 1 | 1 |
| sdz psc 833 | Homo sapiens (human) | IC50 | 0.3969 | 5 | 5 |
| sdz psc 833 | Homo sapiens (human) | Ki | 0.7170 | 2 | 2 |
| cyclosporine | Homo sapiens (human) | IC50 | 3.0464 | 41 | 42 |
| cyclosporine | Homo sapiens (human) | Ki | 1.7183 | 6 | 6 |
| sirolimus | Homo sapiens (human) | IC50 | 1.2500 | 1 | 1 |
| morphine | Homo sapiens (human) | IC50 | 50.0000 | 3 | 3 |
| licochalcone a | Homo sapiens (human) | IC50 | 109.0850 | 4 | 4 |
| 5,4'-dihydroxy-3,6,7-trimethoxyflavone | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
| fosbretabulin | Homo sapiens (human) | IC50 | 0.0090 | 2 | 2 |
| 5-hydroxy-3,3',4',7-tetramethoxyflavone | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| indinavir sulfate | Homo sapiens (human) | IC50 | 72.0000 | 2 | 2 |
| 3,4',5-trimethoxystilbene | Homo sapiens (human) | IC50 | 8.0000 | 1 | 1 |
| brecanavir | Homo sapiens (human) | IC50 | 24.1000 | 1 | 1 |
| oc 144-093 | Homo sapiens (human) | IC50 | 0.0316 | 1 | 1 |
| dexniguldipine | Homo sapiens (human) | Ki | 2.3000 | 1 | 1 |
| ly 295337 | Homo sapiens (human) | IC50 | 2.2700 | 1 | 1 |
| reversin 121 | Homo sapiens (human) | IC50 | 1.4100 | 1 | 1 |
| ko 143 | Homo sapiens (human) | IC50 | 37.5270 | 3 | 3 |
| 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone | Homo sapiens (human) | IC50 | 24.7300 | 1 | 1 |
| alisporivir | Homo sapiens (human) | IC50 | 0.5900 | 1 | 1 |
| wk-x-34 | Homo sapiens (human) | IC50 | 0.3342 | 5 | 5 |
| xr 9577 | Homo sapiens (human) | IC50 | 0.4002 | 5 | 5 |
| bms 754807 | Homo sapiens (human) | IC50 | 17.7000 | 1 | 1 |
| dolutegravir | Homo sapiens (human) | IC50 | 95.0000 | 2 | 2 |
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 5-methoxypsoralen | Homo sapiens (human) | EC200 | 0.0500 | 1 | 1 |
| verapamil | Homo sapiens (human) | Activity | 1.6000 | 2 | 2 |
| verapamil | Homo sapiens (human) | ED50 | 3.0000 | 1 | 1 |
| verapamil | Homo sapiens (human) | I0.5 | 1.6000 | 1 | 1 |
| verapamil | Homo sapiens (human) | INH | 1.6000 | 1 | 1 |
| verapamil | Homo sapiens (human) | Km | 13.3433 | 6 | 6 |
| verapamil | Homo sapiens (human) | MIC | 8.0000 | 1 | 1 |
| verapamil | Homo sapiens (human) | Vmax | 65.0000 | 1 | 1 |
| chlorpromazine | Homo sapiens (human) | Km | 27.4000 | 1 | 1 |
| diazepam | Homo sapiens (human) | Km | 72.4000 | 1 | 1 |
| haloperidol | Homo sapiens (human) | Km | 33.0000 | 1 | 1 |
| loperamide | Homo sapiens (human) | Km | 13.8000 | 1 | 1 |
| losartan | Homo sapiens (human) | Km | 245.0667 | 3 | 3 |
| metoprolol | Homo sapiens (human) | Ki1 | 200.0000 | 1 | 1 |
| metoprolol | Homo sapiens (human) | Ki2 | 1,750.0000 | 1 | 1 |
| prazosin | Homo sapiens (human) | Km | 20.0000 | 1 | 1 |
| quetiapine | Homo sapiens (human) | Km | 12.3000 | 1 | 1 |
| risperidone | Homo sapiens (human) | Km | 12.4000 | 1 | 1 |
| vincristine | Homo sapiens (human) | Ki1 | 0.4700 | 1 | 1 |
| vincristine | Homo sapiens (human) | Ki2 | 148.0000 | 1 | 1 |
| colchicine | Homo sapiens (human) | Km | 23.1650 | 2 | 2 |
| emetine | Homo sapiens (human) | Km | 6.0000 | 1 | 1 |
| vinblastine | Homo sapiens (human) | Activity | 15.9000 | 3 | 3 |
| vinblastine | Homo sapiens (human) | Km | 75.5400 | 5 | 5 |
| daunorubicin | Homo sapiens (human) | Km | 1.7400 | 1 | 1 |
| paclitaxel | Homo sapiens (human) | Km | 5.7380 | 3 | 3 |
| paclitaxel | Homo sapiens (human) | Vmax | 35.0000 | 1 | 1 |
| etoposide | Homo sapiens (human) | Km | 254.9600 | 1 | 1 |
| oseltamivir | Homo sapiens (human) | Km | 4,200.0000 | 1 | 1 |
| talinolol | Homo sapiens (human) | Ki1 | 72.0000 | 1 | 1 |
| talinolol | Homo sapiens (human) | Ki2 | 1,570.0000 | 1 | 1 |
| pafenolol | Homo sapiens (human) | Ki1 | 5.5000 | 1 | 1 |
| pafenolol | Homo sapiens (human) | Ki2 | 3,200.0000 | 1 | 1 |
| hernandezine | Homo sapiens (human) | Activity | 0.0200 | 1 | 1 |
| grepafloxacin | Homo sapiens (human) | Km | 580.0000 | 1 | 1 |
| formylmethionyl-leucyl-phenylalanine methyl ester | Homo sapiens (human) | Km | 100.0000 | 1 | 1 |
| levofloxacin | Homo sapiens (human) | Km | 4,300.0000 | 2 | 2 |
| quinidine | Homo sapiens (human) | Km | 11.8100 | 2 | 2 |
| acetylleucyl-leucyl-norleucinal | Homo sapiens (human) | Km | 100.0000 | 1 | 1 |
| resveratrol | Homo sapiens (human) | AC50 | 100.0000 | 1 | 1 |
| 3'-deamino-3'-hydroxydoxorubicin | Homo sapiens (human) | Km | 2.0000 | 1 | 1 |
| dactinomycin | Homo sapiens (human) | Km | 10.0000 | 1 | 1 |
| digoxin | Homo sapiens (human) | Km | 25.9000 | 1 | 1 |
| valinomycin | Homo sapiens (human) | Km | 1.0000 | 1 | 1 |
| quinine | Homo sapiens (human) | Km | 10.0000 | 1 | 1 |
| bergaptol | Homo sapiens (human) | EC200 | 0.3000 | 1 | 1 |
| pterostilbene | Homo sapiens (human) | AC50 | 85.0000 | 1 | 1 |
| estradiol-17 beta-glucuronide | Homo sapiens (human) | Km | 62.0000 | 1 | 1 |
| cyclosporine | Homo sapiens (human) | Activity | 9.0333 | 3 | 3 |
| cyclosporine | Homo sapiens (human) | Km | 4.1233 | 3 | 3 |
| 3,4',5-trimethoxystilbene | Homo sapiens (human) | AC50 | 50.0000 | 1 | 1 |
| enkephalin, ala(2)-mephe(4)-gly(5)- | Homo sapiens (human) | Km | 43.0000 | 1 | 1 |
| bergamottin | Homo sapiens (human) | EC200 | 0.0350 | 1 | 1 |
| oc 144-093 | Homo sapiens (human) | ED50 | 0.0500 | 1 | 1 |
| dolastatin 10 | Homo sapiens (human) | Km | 0.9000 | 1 | 1 |
| (2s,3s)-2-phenyl-3-((5-trifluoromethoxy-2-methoxy)benzylamino)piperidine | Homo sapiens (human) | Km | 34.4000 | 1 | 1 |
| rhodamine 123 | Homo sapiens (human) | Ki1 | 0.1100 | 1 | 1 |
| rhodamine 123 | Homo sapiens (human) | Ki2 | 3.4000 | 1 | 1 |
| (R)-(+)-6',7'-dihydroxybergamottin | Homo sapiens (human) | EC200 | 0.0400 | 1 | 1 |
| clozapine | Homo sapiens (human) | Km | 58.0000 | 1 | 1 |
| olanzapine | Homo sapiens (human) | Km | 8.3000 | 1 | 1 |
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Interaction of cytochrome P450 3A inhibitors with P-glycoprotein.The Journal of pharmacology and experimental therapeutics, , Volume: 303, Issue:1, 2002
Inhibitory effects of CYP3A4 substrates and their metabolites on P-glycoprotein-mediated transport.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 12, Issue:4, 2001
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.Anti-cancer drugs, , Volume: 7, Issue:5, 1996
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.European journal of medicinal chemistry, , Apr-05, Volume: 233, 2022
Glenthenamines A-F: Enamine Pyranonaphthoquinones from the Australian Pasture Plant Derived Journal of natural products, , 02-25, Volume: 85, Issue:2, 2022
Neochrysosporazines: Precursor-Directed Biosynthesis Defines a Marine-Derived Fungal Natural Product P-Glycoprotein Inhibitory Pharmacophore.Journal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Synthesis and evaluation of stereoisomers of methylated catechin and epigallocatechin derivatives on modulating P-glycoprotein-mediated multidrug resistance in cancers.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
[no title available]Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Discovery of Potent Inhibitors against P-Glycoprotein-Mediated Multidrug Resistance Aided by Late-Stage Functionalization of a 2-(4-(Pyridin-2-yl)phenoxy)pyridine Analogue.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
[no title available]Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Chrysosporazines F-M: P-Glycoprotein Inhibitory Phenylpropanoid Piperazines from an Australian Marine Fish Derived Fungus, Journal of natural products, , 02-28, Volume: 83, Issue:2, 2020
Synthesis and biological evaluation of thiophenylbenzofuran derivatives as potential P-glycoprotein inhibitors.European journal of medicinal chemistry, , Sep-01, Volume: 201, 2020
Potential Tools for Eradicating HIV Reservoirs in the Brain: Development of Trojan Horse Prodrugs for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Design, synthesis and biological evaluation of chalcones as reversers of P-glycoprotein-mediated multidrug resistance.European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Jatrophane Diterpenoids from Euphorbia glomerulans.Journal of natural products, , 04-26, Volume: 82, Issue:4, 2019
Discovery and synthesis of 3- and 21-substituted fusidic acid derivatives as reversal agents of P-glycoprotein-mediated multidrug resistance.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Modulation of the spacer in N,N-bis(alkanol)amine aryl ester heterodimers led to the discovery of a series of highly potent P-glycoprotein-based multidrug resistance (MDR) modulators.European journal of medicinal chemistry, , Jun-15, Volume: 172, 2019
Design, synthesis, and discovery of ocotillol-type amide derivatives as orally available modulators of P-glycoprotein-mediated multidrug resistance.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
1,2,3,4-Tetrahydroisoquinoline/2H-chromen-2-one conjugates as nanomolar P-glycoprotein inhibitors: Molecular determinants for affinity and selectivity over multidrug resistance associated protein 1.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Novel virosecurinine bivalent mimetics as potent reversal agents against P-glycoprotein-mediated multidrug resistance.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Halogenated naphthochalcones and structurally related naphthopyrazolines with antitumor activity.Bioorganic & medicinal chemistry letters, , 11-01, Volume: 26, Issue:21, 2016
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness.Chemical biology & drug design, , Volume: 88, Issue:6, 2016
Optimization of permethyl ningalin B analogs as P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Multidrug resistance (MDR) reversers: High activity and efficacy in a series of asymmetrical N,N-bis(alkanol)amine aryl esters.European journal of medicinal chemistry, , Nov-24, Volume: 87, 2014
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
20(S)-Protopanaxadiol (PPD) analogues chemosensitize multidrug-resistant cancer cells to clinical anticancer drugs.Bioorganic & medicinal chemistry, , Jul-15, Volume: 21, Issue:14, 2013
New structure-activity relationship studies in a series of N,N-bis(cyclohexanol)amine aryl esters as potent reversers of P-glycoprotein-mediated multidrug resistance (MDR).Bioorganic & medicinal chemistry, , Jan-15, Volume: 21, Issue:2, 2013
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.Journal of medicinal chemistry, , Jan-12, Volume: 55, Issue:1, 2012
Thiorhodamines containing amide and thioamide functionality as inhibitors of the ATP-binding cassette drug transporter P-glycoprotein (ABCB1).Bioorganic & medicinal chemistry, , Jul-15, Volume: 20, Issue:14, 2012
Design and synthesis of indomethacin analogues that inhibit P-glycoprotein and/or multidrug resistant protein without COX inhibitory activity.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Chalcogenopyrylium compounds as modulators of the ATP-binding cassette transporters P-glycoprotein (P-gp/ABCB1) and multidrug resistance protein 1 (MRP1/ABCC1).Journal of medicinal chemistry, , May-24, Volume: 55, Issue:10, 2012
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Amine linked flavonoid dimers as modulators for P-glycoprotein-based multidrug resistance: structure-activity relationship and mechanism of modulation.Journal of medicinal chemistry, , Mar-08, Volume: 55, Issue:5, 2012
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Structure-activity relationships studies in a series of N,N-bis(alkanol)amine aryl esters as P-glycoprotein (Pgp) dependent multidrug resistance (MDR) inhibitors.Journal of medicinal chemistry, , Feb-25, Volume: 53, Issue:4, 2010
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Rhodamine inhibitors of P-glycoprotein: an amide/thioamide "switch" for ATPase activity.Journal of medicinal chemistry, , May-28, Volume: 52, Issue:10, 2009
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 18, Issue:17, 2008
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Isomeric N,N-bis(cyclohexanol)amine aryl esters: the discovery of a new class of highly potent P-glycoprotein (Pgp)-dependent multidrug resistance (MDR) inhibitors.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Exploratory chemistry toward the identification of a new class of multidrug resistance reverters inspired by pervilleine and verapamil models.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.Biochemical and biophysical research communications, , Jul-30, Volume: 320, Issue:3, 2004
Transport characteristics of fexofenadine in the Caco-2 cell model.Pharmaceutical research, , Volume: 21, Issue:8, 2004
Differential effects of the optical isomers of KR30031 on cardiotoxicity and on multidrug resistance reversal activity.Anti-cancer drugs, , Volume: 14, Issue:2, 2003
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.Pharmaceutical research, , Volume: 20, Issue:2, 2003
Inhibition of P-glycoprotein by newer antidepressants.The Journal of pharmacology and experimental therapeutics, , Volume: 305, Issue:1, 2003
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.Pharmaceutical research, , Volume: 18, Issue:2, 2001
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 29, Issue:8, 2001
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:10, 2000
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.Bioorganic & medicinal chemistry letters, , Jun-07, Volume: 9, Issue:11, 1999
Two pimarane diterpenoids from Ephemerantha lonchophylla and their evaluation as modulators of the multidrug resistance phenotype.Journal of natural products, , Volume: 61, Issue:1, 1998
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
In vitro P-glycoprotein affinity for atypical and conventional antipsychotics.Life sciences, , May-31, Volume: 71, Issue:2, 2002
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
In vitro P-glycoprotein affinity for atypical and conventional antipsychotics.Life sciences, , May-31, Volume: 71, Issue:2, 2002
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Interaction of common azole antifungals with P glycoprotein.Antimicrobial agents and chemotherapy, , Volume: 46, Issue:1, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Investigating the binding interactions of the anti-Alzheimer's drug donepezil with CYP3A4 and P-glycoprotein.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 25, Issue:2, 2015
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.Molecular pharmacology, , Volume: 61, Issue:5, 2002
Interaction of common azole antifungals with P glycoprotein.Antimicrobial agents and chemotherapy, , Volume: 46, Issue:1, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Interaction of morphine, fentanyl, sufentanil, alfentanil, and loperamide with the efflux drug transporter P-glycoprotein.Anesthesiology, , Volume: 96, Issue:4, 2002
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco-2 cell monolayers.British journal of pharmacology, , Volume: 129, Issue:6, 2000
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 16, Issue:3, 2002
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.Pharmaceutical research, , Volume: 17, Issue:10, 2000
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 16, Issue:3, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.Pharmaceutical research, , Volume: 17, Issue:10, 2000
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Interaction of omeprazole, lansoprazole and pantoprazole with P-glycoprotein.Naunyn-Schmiedeberg's archives of pharmacology, , Volume: 364, Issue:6, 2001
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Self-organizing maps for identification of new inhibitors of P-glycoprotein.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
[no title available],
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.Pharmaceutical research, , Volume: 20, Issue:2, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.Molecular pharmacology, , Volume: 61, Issue:5, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
A continuous fluorescence assay for the study of P-glycoprotein-mediated drug efflux using inside-out membrane vesicles.Analytical biochemistry, , Mar-15, Volume: 268, Issue:2, 1999
Partial purification and reconstitution of the human multidrug-resistance pump: characterization of the drug-stimulatable ATP hydrolysis.Proceedings of the National Academy of Sciences of the United States of America, , Sep-15, Volume: 89, Issue:18, 1992
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.The Journal of biological chemistry, , Nov-02, Volume: 282, Issue:44, 2007
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 33, Issue:4, 2005
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.Pharmaceutical research, , Volume: 20, Issue:2, 2003
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.Pharmaceutical research, , Volume: 18, Issue:2, 2001
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein.Molecular pharmacology, , Volume: 57, Issue:1, 2000
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.The Journal of pharmacology and experimental therapeutics, , Volume: 290, Issue:2, 1999
Effect of modulators on the ATPase activity and vanadate nucleotide trapping of human P-glycoprotein.Biochemical pharmacology, , Sep-15, Volume: 56, Issue:6, 1998
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.Anti-cancer drugs, , Volume: 7, Issue:5, 1996
Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers.Pharmaceutical research, , Volume: 10, Issue:5, 1993
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.Pharmaceutical research, , Volume: 18, Issue:2, 2001
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.Bioorganic & medicinal chemistry, , Feb-15, Volume: 21, Issue:4, 2013
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.Bioorganic & medicinal chemistry letters, , May-16, Volume: 15, Issue:10, 2005
Kinetics of P-glycoprotein-mediated efflux of paclitaxel.The Journal of pharmacology and experimental therapeutics, , Volume: 298, Issue:3, 2001
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Taxol transport by human intestinal epithelial Caco-2 cells.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 26, Issue:4, 1998
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
Delineating the contribution of secretory transporters in the efflux of etoposide using Madin-Darby canine kidney (MDCK) cells overexpressing P-glycoprotein (Pgp), multidrug resistance-associated protein (MRP1), and canalicular multispecific organic anionDrug metabolism and disposition: the biological fate of chemicals, , Volume: 30, Issue:4, 2002
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.Pharmaceutical research, , Volume: 18, Issue:2, 2001
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 16, Issue:3, 2002
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 33, Issue:4, 2005
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:6, 2001
Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 33, Issue:4, 2005
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:6, 2001
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.Molecular pharmacology, , Volume: 61, Issue:5, 2002
Mibefradil is a P-glycoprotein substrate and a potent inhibitor of both P-glycoprotein and CYP3A in vitro.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:8, 2000
Potential Tools for Eradicating HIV Reservoirs in the Brain: Development of Trojan Horse Prodrugs for the Inhibition of P-Glycoprotein with Anti-HIV-1 Activity.Journal of medicinal chemistry, , 03-12, Volume: 63, Issue:5, 2020
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:10, 2007
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:10, 2007
Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein.AIDS (London, England), , May-02, Volume: 17, Issue:7, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.Chemical research in toxicology, , Volume: 14, Issue:12, 2001
Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein.The Journal of pharmacology and experimental therapeutics, , Volume: 293, Issue:2, 2000
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 16, Issue:3, 2002
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.Pharmaceutical research, , Volume: 17, Issue:10, 2000
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Benzanilide-Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-Type ABCG2 Modulators.ACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
2-[(3-Methoxyphenylethyl)phenoxy]-based ABCB1 inhibitors: effect of different basic side-chains on their biological properties.Journal of medicinal chemistry, , Dec-11, Volume: 51, Issue:23, 2008
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.Journal of medicinal chemistry, , Nov-02, Volume: 49, Issue:22, 2006
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.Biochemical and biophysical research communications, , Jul-30, Volume: 320, Issue:3, 2004
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Design, synthesis, and biological evaluation of hederagenin derivatives with improved aqueous solubility and tumor resistance reversal activity.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.Journal of natural products, , 05-22, Volume: 83, Issue:5, 2020
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Synthesis and biological evaluation of JL-A7 derivatives as potent ABCB1 inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Flavonoid derivatives as selective ABCC1 modulators: Synthesis and functional characterization.European journal of medicinal chemistry, , Feb-15, Volume: 109, 2016
Hernandezine, a Bisbenzylisoquinoline Alkaloid with Selective Inhibitory Activity against Multidrug-Resistance-Linked ATP-Binding Cassette Drug Transporter ABCB1.Journal of natural products, , 08-26, Volume: 79, Issue:8, 2016
SAR study on arylmethyloxyphenyl scaffold: looking for a P-gp nanomolar affinity.European journal of medicinal chemistry, , Apr-09, Volume: 76, 2014
Benzanilide-Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-Type ABCG2 Modulators.ACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 23, Issue:5, 2013
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Structure-activity relationships of flavonoids as inhibitors of breast cancer resistance protein (BCRP).Bioorganic & medicinal chemistry, , Mar-15, Volume: 19, Issue:6, 2011
Solid phase synthesis of tariquidar-related modulators of ABC transporters preferring breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 21, Issue:12, 2011
Potent and selective inhibitors of breast cancer resistance protein (ABCG2) derived from the p-glycoprotein (ABCB1) modulator tariquidar.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
In vitro activity of novel dual action MDR anthranilamide modulators with inhibitory activity on CYP-450 (Part 2).Bioorganic & medicinal chemistry, , Jun-01, Volume: 15, Issue:11, 2007
Synthesis and biological evaluation of novel H6 analogues as drug resistance reversal agents.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Inhibition of P-glycoprotein by newer antidepressants.The Journal of pharmacology and experimental therapeutics, , Volume: 305, Issue:1, 2003
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.The Journal of pharmacology and experimental therapeutics, , Volume: 290, Issue:2, 1999
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:10, 2007
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein.The Journal of pharmacology and experimental therapeutics, , Volume: 304, Issue:3, 2003
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.Pharmaceutical research, , Volume: 20, Issue:2, 2003
Inhibition of P-glycoprotein by newer antidepressants.The Journal of pharmacology and experimental therapeutics, , Volume: 305, Issue:1, 2003
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.Pharmaceutical research, , Volume: 18, Issue:2, 2001
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
P-glycoprotein efflux at the blood-brain barrier mediates differences in brain disposition and pharmacodynamics between two structurally related neurokinin-1 receptor antagonists.The Journal of pharmacology and experimental therapeutics, , Volume: 298, Issue:3, 2001
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:10, 2007
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Effects of 12 Ca2+ antagonists on multidrug resistance, MDR1-mediated transport and MDR1 mRNA expression.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, , Volume: 16, Issue:3, 2002
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.Pharmaceutical research, , Volume: 17, Issue:10, 2000
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A.Biopharmaceutics & drug disposition, , Volume: 25, Issue:7, 2004
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Self-organizing maps for identification of new inhibitors of P-glycoprotein.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Quantitative distinctions of active site molecular recognition by P-glycoprotein and cytochrome P450 3A4.Chemical research in toxicology, , Volume: 14, Issue:12, 2001
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
Natural products as multidrug resistance modulators in cancer.European journal of medicinal chemistry, , Aug-15, Volume: 176, 2019
Pharmacophore model of drugs involved in P-glycoprotein multidrug resistance: explanation of structural variety (hypothesis).Journal of medicinal chemistry, , Dec-19, Volume: 45, Issue:26, 2002
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity.The Journal of biological chemistry, , Feb-09, Volume: 271, Issue:6, 1996
Docking and 3D-QSAR (quantitative structure activity relationship) studies of flavones, the potent inhibitors of p-glycoprotein targeting the nucleotide binding domain.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Reversal of P-glycoprotein-mediated MDR by 5,7,3',4',5'-pentamethoxyflavone and SAR.Biochemical and biophysical research communications, , Jul-30, Volume: 320, Issue:3, 2004
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Selective inhibition of human cytochrome P450 3A4 by N-[2(R)-hydroxy-1(S)-indanyl]-5-[2(S)-(1, 1-dimethylethylaminocarbonyl)-4-[(furo[2, 3-b]pyridin-5-yl)methyl]piperazin-1-yl]-4(S)-hydroxy-2(R)-phenylmethy lpentanamide and P-glycoprotein by valspodar in Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:10, 2000
PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.Biochemical and biophysical research communications, , Apr-13, Volume: 257, Issue:2, 1999
Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein.Japanese journal of cancer research : Gann, , Volume: 89, Issue:11, 1998
Interaction of cyclosporin derivatives with the ATPase activity of human P-glycoprotein.British journal of pharmacology, , Volume: 122, Issue:2, 1997
Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay.Anti-cancer drugs, , Volume: 7, Issue:5, 1996
Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Rational drug design of 6-substituted 4-anilino-2-phenylpyrimidines for exploration of novel ABCG2 binding site.European journal of medicinal chemistry, , Feb-15, Volume: 212, 2021
Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.European journal of medicinal chemistry, , Apr-15, Volume: 216, 2021
[no title available]Journal of medicinal chemistry, , 09-24, Volume: 63, Issue:18, 2020
Identification of Thienopyrimidine Scaffold as an Inhibitor of the ABC Transport Protein ABCC1 (MRP1) and Related Transporters Using a Combined Virtual Screening Approach.Journal of medicinal chemistry, , 05-09, Volume: 62, Issue:9, 2019
Synthesis and biological evaluation of quinazoline derivatives - A SAR study of novel inhibitors of ABCG2.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
Synthesis and biological investigation of 2,4-substituted quinazolines as highly potent inhibitors of breast cancer resistance protein (ABCG2).European journal of medicinal chemistry, , Oct-20, Volume: 139, 2017
4-Anilino-2-pyridylquinazolines and -pyrimidines as Highly Potent and Nontoxic Inhibitors of Breast Cancer Resistance Protein (ABCG2).Journal of medicinal chemistry, , 05-25, Volume: 60, Issue:10, 2017
Synthesis and Biological Evaluation of 4-Anilino-quinazolines and -quinolines as Inhibitors of Breast Cancer Resistance Protein (ABCG2).Journal of medicinal chemistry, , 06-09, Volume: 59, Issue:11, 2016
The combination of quinazoline and chalcone moieties leads to novel potent heterodimeric modulators of breast cancer resistance protein (BCRP/ABCG2).European journal of medicinal chemistry, , Jul-19, Volume: 117, 2016
Synthesis and Investigation of Tetrahydro-β-carboline Derivatives as Inhibitors of the Breast Cancer Resistance Protein (ABCG2).Journal of medicinal chemistry, , 07-14, Volume: 59, Issue:13, 2016
Phenyltetrazolyl-phenylamides: Substituent impact on modulation capability and selectivity toward the efflux protein ABCG2 and investigation of interaction with the transporter.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.Journal of medicinal chemistry, , Jun-11, Volume: 58, Issue:11, 2015
HM30181 Derivatives as Novel Potent and Selective Inhibitors of the Breast Cancer Resistance Protein (BCRP/ABCG2).Journal of medicinal chemistry, , May-14, Volume: 58, Issue:9, 2015
Structure-activity relationship study of permethyl ningalin B analogues as P-glycoprotein chemosensitizers.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Investigation of quinazolines as inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Synthesis and biological evaluation of flavones and benzoflavones as inhibitors of BCRP/ABCG2.European journal of medicinal chemistry, , Volume: 67, 2013
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
A novel approach for predicting P-glycoprotein (ABCB1) inhibition using molecular interaction fields.Journal of medicinal chemistry, , Mar-24, Volume: 54, Issue:6, 2011
From taxuspine x to structurally simplified taxanes with remarkable p-glycoprotein inhibitory activity.ACS medicinal chemistry letters, , Nov-11, Volume: 1, Issue:8, 2010
Synthesis and biological evaluation of a small molecule library of 3rd generation multidrug resistance modulators.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
A 4-aminobenzoic acid derivative as novel lead for selective inhibitors of multidrug resistance-associated proteins.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 18, Issue:17, 2008
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
Small P-gp modulating molecules: SAR studies on tetrahydroisoquinoline derivatives.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.Journal of medicinal chemistry, , Mar-13, Volume: 51, Issue:5, 2008
Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.Antimicrobial agents and chemotherapy, , Volume: 51, Issue:10, 2007
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Suppressor mutations in the transmembrane segments of P-glycoprotein promote maturation of processing mutants and disrupt a subset of drug-binding sites.The Journal of biological chemistry, , Nov-02, Volume: 282, Issue:44, 2007
Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance protein efflux transporter.Pharmaceutical research, , Volume: 20, Issue:2, 2003
Comparison of in vitro P-glycoprotein screening assays: recommendations for their use in drug discovery.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Cyclosporins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC transporter.Journal of medicinal chemistry, , Oct-10, Volume: 45, Issue:21, 2002
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?Pharmaceutical research, , Volume: 19, Issue:6, 2002
Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.Molecular pharmacology, , Volume: 61, Issue:5, 2002
C-7 analogues of progesterone as potent inhibitors of the P-glycoprotein efflux pump.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.Pharmaceutical research, , Volume: 18, Issue:12, 2001
Active transport of fluorescent P-glycoprotein substrates: evaluation as markers and interaction with inhibitors.Biochemical and biophysical research communications, , Nov-30, Volume: 289, Issue:2, 2001
Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-1 protease inhibitors into brain and testes.Drug metabolism and disposition: the biological fate of chemicals, , Volume: 28, Issue:6, 2000
Aureobasidins: structure-activity relationships for the inhibition of the human MDR1 P-glycoprotein ABC-transporter.Journal of medicinal chemistry, , Jun-29, Volume: 43, Issue:13, 2000
PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.Biochemical and biophysical research communications, , Apr-13, Volume: 257, Issue:2, 1999
Inhibitory effects of a cyclosporin derivative, SDZ PSC 833, on transport of doxorubicin and vinblastine via human P-glycoprotein.Japanese journal of cancer research : Gann, , Volume: 89, Issue:11, 1998
Relevance of p-glycoprotein for the enteral absorption of cyclosporin A: in vitro-in vivo correlation.British journal of pharmacology, , Volume: 118, Issue:7, 1996
Direct demonstration of high affinity interactions of immunosuppressant drugs with the drug binding site of the human P-glycoprotein.Molecular pharmacology, , Volume: 45, Issue:4, 1994
Human P-glycoprotein transports cyclosporin A and FK506.The Journal of biological chemistry, , Mar-25, Volume: 268, Issue:9, 1993
Structure-activity relationship and in vitro and in vivo evaluation of the potent cytotoxic anti-microtubule agent N-(4-methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium chloride and its analogues as antitumor agents.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Synthesis of N(4)-(substituted phenyl)-N(4)-alkyl/desalkyl-9H-pyrimido[4,5-b]indole-2,4-diamines and identification of new microtubule disrupting compounds that are effective against multidrug resistant cells.Bioorganic & medicinal chemistry, , Feb-15, Volume: 21, Issue:4, 2013
Structure-activity relationships, ligand efficiency, and lipophilic efficiency profiles of benzophenone-type inhibitors of the multidrug transporter P-glycoprotein.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2.Bioorganic & medicinal chemistry letters, , Dec-04, Volume: 10, Issue:23, 2000
PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.Biochemical and biophysical research communications, , Apr-13, Volume: 257, Issue:2, 1999
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.Journal of medicinal chemistry, , Oct-08, Volume: 41, Issue:21, 1998
[no title available]Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Tariquidar-related triazoles as potent, selective and stable inhibitors of ABCG2 (BCRP).European journal of medicinal chemistry, , Apr-01, Volume: 191, 2020
Triazole Bridged Flavonoid Dimers as Potent, Nontoxic, and Highly Selective Breast Cancer Resistance Protein (BCRP/ABCG2) Inhibitors.Journal of medicinal chemistry, , 09-26, Volume: 62, Issue:18, 2019
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Functional assay and structure-activity relationships of new third-generation P-glycoprotein inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Structure-activity relationships of new inhibitors of breast cancer resistance protein (ABCG2).Bioorganic & medicinal chemistry, , Sep-01, Volume: 16, Issue:17, 2008
New functional assay of P-glycoprotein activity using Hoechst 33342.Bioorganic & medicinal chemistry, , Dec-01, Volume: 15, Issue:23, 2007
Enables
This protein enables 14 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| ABC-type xenobiotic transporter activity | molecular function | Catalysis of the reaction: ATP + H2O + xenobiotic(in) = ADP + phosphate + xenobiotic(out). [EC:7.6.2.2] |
| efflux transmembrane transporter activity | molecular function | Enables the transfer of a specific substance or related group of substances from the inside of the cell to the outside of the cell across a membrane. [GOC:ai, GOC:mtg_transport, ISBN:0815340729] |
| ATP hydrolysis activity | molecular function | Catalysis of the reaction: ATP + H2O = ADP + H+ phosphate. ATP hydrolysis is used in some reactions as an energy source, for example to catalyze a reaction or drive transport against a concentration gradient. [RHEA:13065] |
| transmembrane transporter activity | molecular function | Enables the transfer of a substance, usually a specific substance or a group of related substances, from one side of a membrane to the other. [GOC:jid, GOC:mtg_transport, ISBN:0815340729] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| ATPase-coupled transmembrane transporter activity | molecular function | Primary active transporter of a solute across a membrane, via the reaction: ATP + H2O = ADP + phosphate, to directly drive the transport of a substance across a membrane. The transport protein may be transiently phosphorylated (P-type transporters), or not (ABC-type transporters and other families of transporters). Primary active transport occurs up the solute's concentration gradient and is driven by a primary energy source. [GOC:mtg_transport, ISBN:0815340729] |
| xenobiotic transmembrane transporter activity | molecular function | Enables the directed movement of a xenobiotic from one side of a membrane to the other. A xenobiotic is a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:go_curators, GOC:krc] |
| carboxylic acid transmembrane transporter activity | molecular function | Enables the transfer of carboxylic acids from one side of a membrane to the other. Carboxylic acids are organic acids containing one or more carboxyl (COOH) groups or anions (COO-). [GOC:ai] |
| phosphatidylcholine floppase activity | molecular function | Catalysis of the movement of phosphatidylcholine from the cytosolic to the exoplasmic leaftlet of a membrane, using energy from the hydrolysis of ATP. [GOC:ab, PMID:16452632, RHEA:38583] |
| phosphatidylethanolamine flippase activity | molecular function | Catalysis of the movement of phosphatidylethanolamine from the exoplasmic to the cytosolic leaftlet of a membrane, using energy from the hydrolysis of ATP. [GOC:ab, PMID:16452632, PMID:20043909, RHEA:36440] |
| ceramide floppase activity | molecular function | Catalysis of the movement of ceramide from the cytosolic to the exoplasmic leaftlet of a membrane, using energy from the hydrolysis of ATP. [GOC:BHF, GOC:dos, GOC:rl] |
| floppase activity | molecular function | Catalysis of the movement of a lipid from the cytosolic to the exoplasmic leaftlet of a membrane, using energy from the hydrolysis of ATP. [PMID:20043909, PMID:25284293, Wikipedia:Flippase] |
Located In
This protein is located in 7 target(s):
| Target | Category | Definition |
|---|
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
| external side of apical plasma membrane | cellular component | The leaflet the apical region of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:ab, GOC:dos] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 17 target(s):
| Target | Category | Definition |
|---|
| G2/M transition of mitotic cell cycle | biological process | The mitotic cell cycle transition by which a cell in G2 commits to M phase. The process begins when the kinase activity of M cyclin/CDK complex reaches a threshold high enough for the cell cycle to proceed. This is accomplished by activating a positive feedback loop that results in the accumulation of unphosphorylated and active M cyclin/CDK complex. [GOC:mtg_cell_cycle] |
| xenobiotic metabolic process | biological process | The chemical reactions and pathways involving a xenobiotic compound, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:cab2, GOC:krc] |
| response to xenobiotic stimulus | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| phospholipid translocation | biological process | The movement of a phospholipid molecule from one leaflet of a membrane bilayer to the opposite leaflet. [ISBN:0815316194, PMID:16452632, PMID:20043909, PMID:20302864] |
| terpenoid transport | biological process | The directed movement of terpenoids into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. Terpenoids are a class of compounds characterized by an isoprenoid chemical structure and include derivatives with various functional groups. [GOC:ai] |
| regulation of response to osmotic stress | biological process | Any process that modulates the rate or extent of the response to osmotic stress. [GOC:ai] |
| transmembrane transport | biological process | The process in which a solute is transported across a lipid bilayer, from one side of a membrane to the other. [GOC:dph, GOC:jid] |
| transepithelial transport | biological process | The directed movement of a substance from one side of an epithelium to the other. [GOC:mah, GOC:yaf, ISBN:0716731363] |
| stem cell proliferation | biological process | The multiplication or reproduction of stem cells, resulting in the expansion of a stem cell population. A stem cell is a cell that retains the ability to divide and proliferate throughout life to provide progenitor cells that can differentiate into specialized cells. [GOC:mtg_kidney_jan10] |
| ceramide translocation | biological process | The movement of a ceramide molecule from one leaflet of a membrane bilayer to the opposite leaflet. [GOC:BHF, GOC:rl] |
| export across plasma membrane | biological process | The directed movement of some substance from inside of a cell, across the plasma membrane and into the extracellular region. [GOC:pg] |
| transport across blood-brain barrier | biological process | The directed movement of substances (e.g. macromolecules, small molecules, ions) through the blood-brain barrier. [GOC:aruk, GOC:bc, PMID:29377008] |
| positive regulation of anion channel activity | biological process | Any process that activates or increases the frequency, rate or extent of anion channel activity. [GOC:TermGenie] |
| carboxylic acid transmembrane transport | biological process | The process in which carboxylic acid is transported across a membrane. [GO_REF:0000069, GOC:TermGenie, PMID:10869563] |
| xenobiotic detoxification by transmembrane export across the plasma membrane | biological process | A process that reduces or removes the toxicity of a xenobiotic by exporting it outside the cell. [PMID:28355133] |
| xenobiotic transport across blood-brain barrier | biological process | The directed movement of a xenobiotic through the blood-brain barrier. [PMID:25053619] |
| regulation of chloride transport | biological process | Any process that modulates the frequency, rate or extent of chloride transport. [GOC:dph] |