fentanyl [Ligand Id: 1626] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL596 (Abstral, Abstral-, Actiq, AD 923, AD-923, Breakyl, Duragesic-100, Duragesic-12, Duragesic-25, Duragesic-37, Duragesic-50, Duragesic-75, Durogesic, Durogesic d-trans, Durogesic dtrans, Effentora, En3267, EN-3267, Fencino, Fendrop, Fentalis reservoir, Fentanest, Fentanilo, Fentanyl, Fentanyl-100, Fentanyl-12, Fentanyl-25, Fentanyl-37, Fentanyl-50, Fentanyl-62, Fentanyl-75, Fentanyl-87, Fentanyl cii, Fentora, IDS-NF-001, Innovar, Ionsys, Leptanal, Matrifen, Mezolar matrix, Mylafent, N02AB03, Opiodur, Oralet, Osmach, Osmanil, Pecfent, Phentanyl, R 4263, Recivit, Recuvyra, Sublimase, Sublimaze, Subsys, Tilofyl, Victanyl, Yemex)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Mouse [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • Kappa opioid receptor in Guinea pig [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Mouse [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
  • Mu opioid receptor in Guinea pig [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
There should be some charts here, you may need to enable JavaScript!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Binding affinity against Opioid receptor delta 1 B 5.99 pKi 1035 nM Ki J Med Chem (2000) 43: 381-391 [PMID:10669565]
ChEMBL Binding affinity against Opioid receptor delta 1 in guinea pig brain membranes B 6.17 pKi 679 nM Ki Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL Displacement of [3H]DPDPE from human delta opioid receptor B 6.24 pKi 570 nM Ki Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
GtoPdb - - 6.8 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Binding affinity against delta-opiate receptor (human) using [3H]-DPDPE radioligand B 6.37 pIC50 431 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL In vitro binding activity against opioid receptor delta using [3DPDPE] as radioligand B 6.73 pIC50 187.4 nM IC50 J Med Chem (1991) 34: 827-841 [PMID:1847432]
ChEMBL Compound was tested in vitro for binding affinity towards delta opioid receptor by measuring displacement of [3H]DPDPE from guinea pig brain membranes B 6.73 pIC50 187 nM IC50 Bioorg Med Chem Lett (1995) 5: 1177-1182
δ receptor/Delta opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3222] [GtoPdb: 317] [UniProtKB: P32300]
ChEMBL Displacement of [3H]-DPDPE from Swiss Webster mouse neural membranes delta opioid receptor after 60 mins by liquid scintillation spectrometric analysis B 6.25 pKi 568 nM Ki Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electric stimulation-induced contraction B 5.03 pIC50 9400 nM IC50 Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically stimulated muscle contraction B 8.02 pIC50 9.5 nM IC50 Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL Agonist activity at delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction F 8.02 pIC50 9.45 nM IC50 J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL Inhibition of delta opioid receptor in mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction B 8.03 pIC50 9.4 nM IC50 Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL Agonist activity at delta opioid receptor in beta-funaltrexamine-treated mouse vas deferens B 8.46 pIC50 3.45 nM IC50 Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
ChEMBL Binding affinity towards Opioid receptor delta 1 using [3H]DADLE as radioligand. B 5.99 pKi 1035 nM Ki J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL Displacement of [3H]DSLET from delta opioid receptor in rat brain membrane B 6.25 pKi 568 nM Ki J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL Binding affinity of compound evaluated for Opioid receptor delta 1 isolated from rat brain B 6.4 pKi 400 nM Ki J Med Chem (2003) 46: 623-633 [PMID:12570383]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 4.68 pKi 21000 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 4.58 pKi 26200 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of [3H]-N-methylspiperone from human dopamine D4 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis B 6.26 pKi 554 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibitory concentration against potassium channel HERG B 5.74 pIC50 1819.7 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
ChEMBL Displacement of [3H]mepyramine from histamine H1 receptor in Sprague-Dawley rat brain membrane after 2 hr by scintillation counting B 4.7 pIC50 19952.62 nM IC50 J Med Chem (2012) 55: 7054-7060 [PMID:22793499]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Binding affinity against Opioid receptor kappa 1 B 6.71 pKi 196.5 nM Ki J Med Chem (2000) 43: 381-391 [PMID:10669565]
GtoPdb - - 7.1 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Binding affinity against opioid receptor kappa 1 using [3H]- U-69,593 radioligand B 5.8 pIC50 1580 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144]
ChEMBL Binding affinity against Opioid receptor kappa 1 in guinea pig brain membranes B 5.95 pKi 1130 nM Ki Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane B 6.53 pKi 298 nM Ki J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL Binding affinity towards Opioid receptor kappa 1 using [3H]U-69593 as radioligand. B 6.71 pKi 196.5 nM Ki J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL In vitro binding activity against opioid receptor kappa using [3H]EKC as radioligand B 5.23 pIC50 5893 nM IC50 J Med Chem (1991) 34: 827-841 [PMID:1847432]
ChEMBL Compound was tested in vitro for binding affinity towards kappa opioid receptor by measuring displacement of [3H]EKC from guinea pig brain membranes B 5.23 pIC50 5893 nM IC50 Bioorg Med Chem Lett (1995) 5: 1177-1182
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in HEK293 cell membrane incubated for 60 mins by radioligand binding assay B 8.28 pKi 5.23 nM Ki J Med Chem (2021) 64: 7778-7808 [PMID:34011153]
ChEMBL Binding affinity against Opioid receptor mu 1 B 8.4 pKi 3.97 nM Ki J Med Chem (2000) 43: 381-391 [PMID:10669565]
ChEMBL Displacement of [3H]-DAMGO from human MOR expressed in CHO-K1 cell membranes incubated for 90 mins measured by MicroBeta scintillation counter method B 8.48 pKi 3.3 nM Ki Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
ChEMBL Displacement of [3H]DAMGO (2 nM ) from opioid receptor mu 1 in human brain B 8.54 pKi 2.9 nM Ki Bioorg Med Chem Lett (2004) 14: 491-493 [PMID:14698188]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor measured after 2 hrs by competitive binding assay B 8.87 pKi 1.35 nM Ki J Med Chem (2022) 65: 13483-13504 [PMID:36206553]
ChEMBL Binding affinity to mu opioid receptor (unknown origin) expressed in HEK cells at pH 7.4 B 8.96 pKi 1.1 nM Ki J Med Chem (2018) 61: 5822-5880 [PMID:29400967]
GtoPdb - - 9.2 pKi - - - NIDA Res Monogr (1998) 178: 440-66 [PMID:9686407]
ChEMBL Binding affinity to mu-opioid receptor (unknown origin) assessed as inhibition constant B 10.29 pKi 0.05 nM Ki J Med Chem (2023) 66: 6463-6497 [PMID:37145921]
ChEMBL Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 7.4 measured after 15 mins by Glo-Sensor assay F 7.97 pIC50 10.72 nM IC50 ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209]
ChEMBL Agonist activity at Gi-coupled mu opioid receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of cAMP production at pH 6.5 measured after 15 mins by Glo-Sensor assay F 8.26 pIC50 5.5 nM IC50 ACS Med Chem Lett (2019) 10: 1353-1356 [PMID:31531209]
ChEMBL Binding affinity against mu-opiate receptor (human) using [3H]DAMGO radioligand B 8.89 pIC50 1.3 nM IC50 J Med Chem (2001) 44: 3378-3390 [PMID:11585443]
ChEMBL Agonist activity at human mu opioid receptor expressed in human U2OS cells co-transfected with beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by BRET assay B 7.28 pEC50 53 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at human mu opioid receptor expressed in CHO cell membranes after 1 hr by [35S]-GTPgammaS binding assay F 7.37 pEC50 43 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay F 7.76 pEC50 17.38 nM EC50 J Med Chem (2020) 63: 15709-15725 [PMID:33271020]
ChEMBL Agonist activity at mu opioid receptor (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay F 7.76 pEC50 17.2 nM EC50 J Med Chem (2020) 63: 15709-15725 [PMID:33271020]
ChEMBL Agonist activity at mu-opioid receptor (unknown origin) expressed in CHO cells assessed as inhibition of intracellular cAMP production measured after 45 mins by HTRF-based assay F 8.72 pEC50 1.9 nM EC50 J Med Chem (2023) 66: 16257-16275 [PMID:38015878]
ChEMBL Agonist activity at mu-opioid receptor (unknown origin) F 8.72 pEC50 1.9 nM EC50 J Med Chem (2023) 66: 16257-16275 [PMID:38015878]
ChEMBL Agonist activity at human MOR expressed in CHO-K1 cells assessed as cAMP accumulation incubated for 30 mins and measured after 1 hr by Eu-cAMP tracer based TR-FRET assay F 9.29 pEC50 0.51 nM EC50 ACS Med Chem Lett (2019) 10: 1568-1572 [PMID:31749912]
μ receptor/Mu opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2858] [GtoPdb: 319] [UniProtKB: P42866]
ChEMBL Displacement of [3H]-DAMGO from Swiss Webster mouse neural membranes mu opioid receptor after 60 mins by liquid scintillation spectrometric analysis B 8.23 pKi 5.9 nM Ki Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
ChEMBL Displacement of [3H] DAMGO from rat mu-opioid receptor B 6.24 pKi 570 nM Ki Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain membrane B 8.23 pKi 5.9 nM Ki J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL Displacement of [3H]DAMGO from mu opioid receptor in rat brain membranes B 8.23 pKi 5.9 nM Ki Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL Binding affinity towards Opioid receptor mu 1 using [3H]DAMGO as radioligand. B 8.4 pKi 3.97 nM Ki J Med Chem (1995) 38: 1547-1557 [PMID:7739013]
ChEMBL Displacement [3H]-naloxone from the Opioid receptor mu 1 isolated from rat brain membrane. B 8.67 pKi 2.16 nM Ki J Med Chem (1989) 32: 663-671 [PMID:2563773]
ChEMBL Ability to displace [3H]naloxone from the Opioid receptor mu 1 isolated from the rat brain membranes. B 8.67 pKi 2.16 nM Ki J Med Chem (1990) 33: 2876-2882 [PMID:2170652]
ChEMBL Inhibition of [3H]DAMGO binding to mu opioid receptor of rat brain membranes B 8.82 pKi 1.5 nM Ki J Med Chem (2003) 46: 623-633 [PMID:12570383]
GtoPdb - - 9.4 pKi - - - Mol Pharmacol (1994) 45: 330-4 [PMID:8114680]
ChEMBL Displacement of [3H] DAMGO from rat mu-opioid receptor B 5.9 pIC50 1258.93 nM IC50 Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL Displacement of [3H]DAMGO from rat brain mu opioid receptor incubated for 60 mins by microbeta scintillation counting method B 8.91 pIC50 1.23 nM IC50 Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
ChEMBL Compound was tested for its ability to stimulate [35S]GTP-gamma-S, binding to membranes from C6 glioma cells stably expressing rat mu opioid receptor F 7.49 pEC50 32.4 nM EC50 Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266]
ChEMBL Binding affinity against mu opioid receptor in guinea pig brain membranes B 8.07 pKi 8.45 nM Ki Bioorg Med Chem Lett (1998) 8: 2685-2688 [PMID:9873603]
ChEMBL Agonist activity at mu opioid receptor in guinea pig isolated ileum assessed as inhibition of electric stimulation-induced contraction B 5.47 pIC50 3400 nM IC50 Bioorg Med Chem (2016) 24: 85-91 [PMID:26712115]
ChEMBL Agonist activity at mu opioid receptor in beta-funaltrexamine-treated guinea pig isolated ileum B 8.02 pIC50 9.45 nM IC50 Bioorg Med Chem (2015) 23: 6185-6194 [PMID:26299827]
ChEMBL Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction F 8.46 pIC50 3.45 nM IC50 J Med Chem (2010) 53: 2875-2881 [PMID:20218625]
ChEMBL Inhibition of mu opioid receptor in guinea pig ileum assessed as inhibition of electrically-stimulated muscle contraction B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2013) 23: 3434-3437 [PMID:23623418]
ChEMBL Agonist activity at mu opioid receptor in guinea pig ileum assessed as inhibition of electrically stimulated muscle contraction B 8.47 pIC50 3.4 nM IC50 Bioorg Med Chem Lett (2015) 25: 4683-4688 [PMID:26323872]
ChEMBL Compound was tested in vitro for binding affinity towards mu opioid receptor by measuring displacement of [3H]DAGO from guinea pig brain membranes B 8.51 pIC50 3.1 nM IC50 Bioorg Med Chem Lett (1995) 5: 1177-1182
ChEMBL In vitro binding activity against opioid receptor mu using [3H]-DAGO as radioligand B 8.51 pIC50 3.1 nM IC50 J Med Chem (1991) 34: 827-841 [PMID:1847432]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells F 5.19 pIC50 6500 nM IC50 Anesthesiology (2002) 96: 913-920 [PMID:11964599]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membranes by microbeta scintillation counting method B 5.61 pKi 2474.3 nM Ki Eur J Med Chem (2022) 241: 114649-114649 [PMID:35961067]
ChEMBL Displacement of [3H]pentazocine from LAL/HA/BR guinea pig brain sigma1 receptor incubated for 90 mins by liquid scintillation counting method B 5.3 pIC50 4973 nM IC50 Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Inhibition of sigma 1 receptor (unknown origin) B 9.41 pKi 0.39 nM Ki Eur J Med Chem (2020) 191: 112144-112144 [PMID:32087465]
ChEMBL Displacement of [3H]PPP from sigma1 receptor (unknown origin) B 6.45 pIC50 354 nM IC50 Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H]SKF10047 from rat brain sigma1 receptor incubated for 35 mins by scintillation counting method B 6 pKi >1000 nM Ki Medchemcomm (2019) 10: 1187-1191 [PMID:31391893]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as reduction in ASP+ substrate uptake by microplate reader based analysis B 4.34 pIC50 46170 nM IC50 J Med Chem (2019) 62: 9890-9905 [PMID:31597043]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]