vanoxerine [Ligand Id: 9983] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL281594 (GBR 12909, GBR-12909, Vanoxerine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Displacement of [3H]WIN35428 from DAT after 1.5 hrs by scintillation counting | B | 7.66 | pKi | 22 | nM | Ki | Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583] |
| ChEMBL | Displacement of [3H]-WIN35428 from human DAT expressed in HEK293 cells measured after 30 mins | B | 8.06 | pKi | 8.8 | nM | Ki | J Med Chem (2016) 59: 6329-6343 [PMID:27309376] |
| ChEMBL | Inhibition of [3H]dopamine reuptake at dopamine transporter | B | 8.29 | pKi | 5.07 | nM | Ki | J Med Chem (2009) 52: 5872-5879 [PMID:19791802] |
| ChEMBL | Displacement of [3H]-WIN35428 from human DAT expressed in HEK cell membrane assessed as inhibition constant by radioligand binding assay | B | 8.33 | pKi | 4.7 | nM | Ki | Bioorg Med Chem (2021) 51: 116509-116509 [PMID:34798381] |
| ChEMBL | Binding affinity towards dopamine transporter (DAT) by using [125I]RTI-55 radioligand | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2002) 45: 4371-4374 [PMID:12213078] |
| ChEMBL | Displacement of [125I]RTI55 from DAT | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki |
Eur J Pharmacol (1989) 166: 493-504 [PMID:2530094]; Eur J Pharmacol (1984) 103: 241-8 [PMID:6237922]; J Pharmacol Exp Ther (1991) 258: 626-32 [PMID:1678014] |
| ChEMBL | Competitive binding versus [N-methyl-3H]WIN-35428 in murine kidney cells transfected with human dopamine transporter | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (2000) 43: 639-648 [PMID:10691690] |
| ChEMBL | Inhibition of human DAT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 6.72 | pIC50 | 190 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Inhibition of [3H]-5-dopamine reuptake in human DAT expressed in HEK293 cells by microbeta liquid scintillation counting method | B | 7.37 | pIC50 | 43 | nM | IC50 | Bioorg Med Chem (2017) 25: 2266-2276 [PMID:28274674] |
| ChEMBL | Affinity was evaluated using [3H]WIN-35428 (radioligand) on Cloned human Dopamine transporter expressed in HEK cells | B | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (1998) 41: 3293-3297 [PMID:9703474] |
| ChEMBL | Inhibition of re-uptake of [3H]-DA at human DAT expressed in HEK293 cells by liquid scintillation counting | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2017) 25: 5278-5289 [PMID:28807575] |
| ChEMBL | Inhibition of human DAT | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Affinity was evaluated using [3H]DA (radioligand) on Cloned human Dopamine transporter expressed in HEK cells | B | 7.59 | pIC50 | 26 | nM | IC50 | J Med Chem (1998) 41: 3293-3297 [PMID:9703474] |
| ChEMBL | Inhibition of human dopamine transporter | B | 8.14 | pIC50 | 7.2 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | The inhibition of reuptake against dopamine transporter | F | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (2002) 45: 4371-4374 [PMID:12213078] |
| DAT/Dopamine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2799] [GtoPdb: 927] [UniProtKB: Q61327] | ||||||||
| ChEMBL | Displacement of [3H]RTI-121 from mouse DAT in striatal membranes | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem (2015) 23: 222-230 [PMID:25468036] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of [3H]DA uptake at DAT in rat brain striatal synaptosomes by liquid scintillation spectrophotometry | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2010) 18: 640-649 [PMID:20036131] |
| ChEMBL | Binding affinity to dopamine transporter (DAT) using [3H]WIN-35428 as a radioligand | B | 7.92 | pKi | 12.02 | nM | Ki | J Med Chem (2000) 43: 4151-4159 [PMID:11063611] |
| ChEMBL | Binding affinity at dopamine transporter from rat caudate-putamen tissue by [3H]WIN-35428 displacement. | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 629-632 [PMID:12639545] |
| ChEMBL | Displacement of [3H]WIN-35428 from dopamine transporter of rat caudate putamen tissue | B | 7.92 | pKi | 12 | nM | Ki | Bioorg Med Chem Lett (2002) 12: 2387-2390 [PMID:12161139] |
| ChEMBL | Binding affinity Sprague-Dawley rats using [3H]WIN-35428 ligand | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
| ChEMBL | Binding affinity against dopamine transporter was determined by the displacement of [3H]WIN-35428 radioligand in rat brain | B | 7.92 | pKi | 11.9 | nM | Ki | J Med Chem (2003) 46: 2589-2598 [PMID:12801223] |
| ChEMBL | Binding affinity at Dopamine transporter by displacing [3H]WIN-35428 from rat caudate putamen | B | 7.92 | pKi | 11.9 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867] |
| ChEMBL | Compound was evaluated for its ability to displace [3H]WIN-35428 binding in rat caudate-putamen | B | 7.94 | pKi | 11.6 | nM | Ki | J Med Chem (1994) 37: 2258-2261 [PMID:8057273] |
| ChEMBL | Affinity for rat dopamine transporter using [3H]WIN-35428 displacement. | B | 7.94 | pKi | 11.6 | nM | Ki | J Med Chem (1995) 38: 3933-3940 [PMID:7562926] |
| ChEMBL | Inhibition of DAT-mediated [3H]DA uptake in rat striatum | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2006) 49: 4239-4247 [PMID:16821783] |
| ChEMBL | Inhibition of rat brain dopamine transporter as accumulation of [3H]DA | F | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | Inhibition of [3H]dopamine uptake in DAT in rat striatum | B | 7.97 | pKi | 10.6 | nM | Ki | Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549] |
| ChEMBL | Inhibitory constant towards reuptake of [125I]-13 from dopamine transporter in rat striatal membranes | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
| ChEMBL | Displacement of [3H]WIN-from DAT in rat striatum | B | 7.99 | pKi | 10.2 | nM | Ki | Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549] |
| ChEMBL | Inhibition of [3H]WIN-35428 binding to rat striatum DAT | B | 8.07 | pKi | 8.56 | nM | Ki | J Med Chem (2006) 49: 4239-4247 [PMID:16821783] |
| ChEMBL | Inhibition of [3H]dopamine uptake via rat dopamine receptor. | B | 8.37 | pKi | 4.3 | nM | Ki | J Med Chem (2003) 46: 1465-1469 [PMID:12672246] |
| ChEMBL | Binding affinity against dopamine transporter labelled with [125I]- RTI-55 in rat. | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (1999) 42: 5029-5042 [PMID:10585212] |
| ChEMBL | Binding affinity for dopamine transporter | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2002) 45: 1321-1329 [PMID:11882001] |
| ChEMBL | Displacement of [125I]RTI55 from DAT in rat brain synaptosomes | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem (2007) 15: 1146-1159 [PMID:17127069] |
| ChEMBL | Affinity at rat dopamine transporter using [125I]RTI-55 displacement. | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2003) 46: 1465-1469 [PMID:12672246] |
| ChEMBL | Binding affinity against Dopamine transporter using [125]RTI-55 | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2001) 44: 3937-3945 [PMID:11689080] |
| ChEMBL | Binding affinity towards dopamine transporter (DAT) | B | 8.43 | pKi | 3.7 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288] |
| ChEMBL | Displacement of [3H]WIN-35428 from DAT in rat striatum membrane | B | 8.75 | pKi | 1.77 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292] |
| ChEMBL | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | B | 9.06 | pKi | 0.88 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
| ChEMBL | In vitro binding affinity towards dopamine transporter in rat striatal membranes by [3H]GBR-12395 displacement. | B | 10.22 | pKi | 0.06 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
| ChEMBL | Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]-5-HT on synaptosomes obtained from whole rat brain minus cerebellum. | F | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Inhibition of [3H]cocaine binding to the dopamine transporter. | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Inhibition of [3H]WIN-35428 binding to the dopamine transporter. | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Inhibition of [3H]WIN-35065-2 binding to the dopamine transporter. | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Displacement of [3H]WIN-35428 from DAT in Sprague-Dawley rat striatum | B | 7.68 | pIC50 | 21.1 | nM | IC50 | J Med Chem (2004) 47: 6128-6136 [PMID:15566284] |
| ChEMBL | IC50 value was evaluated using [3H]WIN-35428 (radioligand) on Dopamine transporter in rat striatum. | B | 7.71 | pIC50 | 19.3 | nM | IC50 | J Med Chem (1998) 41: 3293-3297 [PMID:9703474] |
| ChEMBL | Inhibition of rat brain Dopamine transporter uptake as [3H]DA accumulation | F | 7.85 | pIC50 | 14.2 | nM | IC50 | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | Inhibitory activity against dopamine transporter (DAT) labeled with [3H]WIN-35428 in rat brain striatal membrane. | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1998) 41: 699-705 [PMID:9513598] |
| ChEMBL | In vitro inhibition of [3H]WIN-35 428 binding to dopamine transporter on rat striatal membranes. | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1997) 40: 35-43 [PMID:9016326] |
| ChEMBL | Inhibition of [3H]WIN-35428 binding to rat brain dopamine transporter | B | 7.97 | pIC50 | 10.6 | nM | IC50 | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | Inhibition of binding of 3[H] WIN-35 428 to Dopamine transporter (DAT) of rat striatum. | B | 7.97 | pIC50 | 10.6 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
| ChEMBL | Inhibition of binding of [3H]WIN-35 428 to (DAT) dopamine transporter in rat striatum | B | 7.97 | pIC50 | 10.6 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762] |
| ChEMBL | Binding affinity towards dopamine transporter in rat striatum using [3H]WIN-35 428 as radioligand | B | 7.97 | pIC50 | 10.6 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
| ChEMBL | Binding affinity at the dopamine transporter in rast striatum by [3H]WIN-35428 displacement. | B | 7.97 | pIC50 | 10.6 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
| ChEMBL | In vitro binding affinity at dopamine transporter in rat striatum by [3H]WIN-35428 displacement. | B | 7.97 | pIC50 | 10.6 | nM | IC50 | J Med Chem (2001) 44: 937-948 [PMID:11300876] |
| ChEMBL | Reuptake inhibition of [3H]-labeled dopamine (DA) in rat. | F | 8.14 | pIC50 | 7.3 | nM | IC50 | J Med Chem (1999) 42: 5029-5042 [PMID:10585212] |
| ChEMBL | Reuptake inhibition at the dopamine transporter labeled with radioligand [3H]dopamine on synaptosomes obtained from rat caudate. | F | 8.14 | pIC50 | 7.3 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Inhibition of [3H]DA reuptake in rat caudate homogenate. | F | 8.14 | pIC50 | 7.3 | nM | IC50 | J Med Chem (2000) 43: 4840-4849 [PMID:11123994] |
| ChEMBL | Inhibition of uptake from dopamine transporter in rat striatum using [3H]DA as radioligand | F | 8.18 | pIC50 | 6.63 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
| ChEMBL | Binding affinity at dopamine transporter from rat striatal membrane tissue by [3H]CFT displacement. | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (1996) 39: 749-756 [PMID:8576918] |
| ChEMBL | Binding against Dopamine transporter using radioligand as [3H]GBR 12935 | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
| ChEMBL | Inhibition of dopamine DA reuptake | B | 8.37 | pIC50 | 4.3 | nM | IC50 | J Med Chem (1996) 39: 4704-4716 [PMID:8941383] |
| ChEMBL | Compound was tested for its ability to inhibit the uptake of [3H]dopamine in DAT (dopamine transporter system) expressing cell line | F | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 261-266 [PMID:9871666] |
| ChEMBL | Compound was tested for its ability to inhibit the neurotransmitter dopamine-DA reuptake system using [3H]dopamine as radioligand | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2559-2564 |
| ChEMBL | Inhibition of [3H]BTCP binding to the dopamine transporter. | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Binding affinity for rat Dopamine transporter. | B | 8.43 | pIC50 | 3.7 | nM | IC50 | J Med Chem (2000) 43: 4840-4849 [PMID:11123994] |
| ChEMBL | Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55 | B | 8.43 | pIC50 | 3.7 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Inhibition of [3H]GBR-12935 binding to the dopamine transporter. | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Binding affinity was determined at the dopamine transporter labeled with radioligand [125 I] RTI-55 in nonstandard conditions | F | 8.58 | pIC50 | 2.63 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Inhibition of Dopamine uptake in male Sprague-Dawley rats using [3H]DA ligand | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
| ChEMBL | Reuptake inhibition was determined at the dopamine transporter labeled with radioligand [3H]dopamine in nonstandard conditions on brain membranes obtained from rat | F | 8.76 | pIC50 | 1.75 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Inhibition of [125I]RTI-55 cocaine binding to the dopamine transporter. | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1992) 35: 969-981 [PMID:1552510] |
| ChEMBL | Displacement of [125I]RTI-55 dopamine transporter binding in rat striatal membrane | B | 9.37 | pIC50 | 0.43 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 4915-4918 [PMID:16165350] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Inhibition of human NET expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 5.84 | pIC50 | 1460 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Inhibition of the Norepinephrine transporter (NET, SLC6A2) as assessed by GPCR-mediated changes in cell morphology using the impedance-based transporter activity through receptor activation (TRACT) assay in HEK-293 JumpIN-SLC6A2 cells (PubChem AID: 1745860) | F | 6.1 | pIC50 | 790 | nM | IC50 | Sci Rep (2021) 11: 12290-null [PMID:34112854] |
| ChEMBL | Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2017) 25: 2266-2276 [PMID:28274674] |
| ChEMBL | Inhibition of re-uptake of [3H]-NE at human NET expressed in HEK293 cells by liquid scintillation counting | B | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem (2017) 25: 5278-5289 [PMID:28807575] |
| ChEMBL | Compound was tested for the inhibition of norepinephrine (NE) reuptake | F | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2002) 45: 4371-4374 [PMID:12213078] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | In vitro binding affinity towards Norepinephrine transporter rat cerebral cortical homogenates by [3H]nisoxetine displacement. | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
| ChEMBL | Binding affinity at norepinephrine transporter using [3H]nisoxetine as radioligand from rat brain | B | 5.9 | pKi | 1270 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867] |
| ChEMBL | Displacement of [3H]nisoxetine from rat brain norepinephrine transporter | B | 5.9 | pKi | 1270 | nM | Ki | J Med Chem (2003) 46: 2589-2598 [PMID:12801223] |
| ChEMBL | The compound was tested for binding affinity nisoxatine ligand | B | 5.9 | pKi | 1270 | nM | Ki | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
| ChEMBL | Inhibition of [3H]NE uptake in NET in rat cerebral cortex | B | 6.99 | pKi | 102 | nM | Ki | Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549] |
| ChEMBL | Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]-NE | F | 6.99 | pKi | 102 | nM | Ki | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | Inhibition of NET-mediated [3H]NE uptake in rat cerebral cortex | B | 6.99 | pKi | 102 | nM | Ki | J Med Chem (2006) 49: 4239-4247 [PMID:16821783] |
| ChEMBL | Inhibition of [3H]norepinephrine uptake at the rat norepinephrine transporter. | B | 7.1 | pKi | 79 | nM | Ki | J Med Chem (2003) 46: 1465-1469 [PMID:12672246] |
| ChEMBL | Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement. | B | 6.3 | pIC50 | 496 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
| ChEMBL | Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum | B | 6.3 | pIC50 | 496 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762] |
| ChEMBL | Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex. | B | 6.3 | pIC50 | 496 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
| ChEMBL | Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand | B | 6.3 | pIC50 | 496 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
| ChEMBL | Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand | B | 6.3 | pIC50 | 496 | nM | IC50 | J Med Chem (2001) 44: 937-948 [PMID:11300876] |
| ChEMBL | Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]NE | F | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Displacement of [125I]RTI55 from SERT | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2008) 51: 2795-2806 [PMID:18393401] |
| ChEMBL | Binding affinity for serotonin transporter (SERT) using [125I]RTI-55 | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (2002) 45: 4371-4374 [PMID:12213078] |
| ChEMBL | Inhibition of human SERT expressed in HEK293 cells at incubated for 15 mins by neurotransmitter reuptake assay | B | 5.42 | pIC50 | 3840 | nM | IC50 | ACS Med Chem Lett (2014) 5: 999-1004 [PMID:25221656] |
| ChEMBL | Affinity was evaluated using [3H]citalopram (radioligand) on human serotonin transporter expressed in HEK cells | B | 6.13 | pIC50 | 741 | nM | IC50 | J Med Chem (1998) 41: 3293-3297 [PMID:9703474] |
| ChEMBL | The inhibition of reuptake against Serotonin transporter (5-HT) | F | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (2002) 45: 4371-4374 [PMID:12213078] |
| SERT/Serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] | ||||||||
| ChEMBL | Displacement of [3H]paroxetine from mouse SERT in whole brain membrane | B | 7.62 | pKi | 24.1 | nM | Ki | Bioorg Med Chem (2015) 23: 222-230 [PMID:25468036] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity for serotonin transporter | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2002) 45: 1321-1329 [PMID:11882001] |
| ChEMBL | Binding affinity against serotonin transporter using [125]RTI-55 | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2001) 44: 3937-3945 [PMID:11689080] |
| ChEMBL | Binding affinity against Serotonin transporter (SERT) labelled with [125I]RTI-55 in rat. | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (1999) 42: 5029-5042 [PMID:10585212] |
| ChEMBL | Displacement of [125I]RTI55 from SERT in rat brain synaptosomes | B | 6.9 | pKi | 126 | nM | Ki | Bioorg Med Chem (2007) 15: 1146-1159 [PMID:17127069] |
| ChEMBL | Binding affinity towards rat serotonin transporter (SERT) | B | 6.9 | pKi | 126 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 1385-1389 [PMID:12657288] |
| ChEMBL | Affinity at rat serotonin transporter using [125I]RTI-55 displacement. | B | 6.9 | pKi | 126 | nM | Ki | J Med Chem (2003) 46: 1465-1469 [PMID:12672246] |
| ChEMBL | Binding affinity against serotonin transporter by displacement of [3H]citalopram in rat brain | B | 6.98 | pKi | 105 | nM | Ki | J Med Chem (2003) 46: 2589-2598 [PMID:12801223] |
| ChEMBL | Binding affinity at Serotonin transporter using [3H]citalopram as radioligand from rat brain | B | 6.98 | pKi | 105 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3169-3173 [PMID:11720867] |
| ChEMBL | Displacement of [3H]citalopram from SERT in rat brain stem membrane | B | 6.98 | pKi | 104 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 5238-5241 [PMID:18774292] |
| ChEMBL | Inhibition of rat brain Serotonin transporter as accumulation of [3H]5-HT | F | 7.04 | pKi | 91.1 | nM | Ki | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | Inhibition of SERT-mediated [3H]5-HT uptake in rat cerebral cortex | B | 7.04 | pKi | 91.1 | nM | Ki | J Med Chem (2006) 49: 4239-4247 [PMID:16821783] |
| ChEMBL | Inhibition of [3H]5HT uptake in SERT in rat cerebral cortex | B | 7.04 | pKi | 91.1 | nM | Ki | Bioorg Med Chem (2008) 16: 2769-2778 [PMID:18249549] |
| ChEMBL | Inhibition of [3H]5-HT uptake at the rat serotonin transporter. | B | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2003) 46: 1465-1469 [PMID:12672246] |
| ChEMBL | In vitro binding affinity towards serotonin transporter in rat cerebral cortical homogenates by [3H]paroxetine displacement. | B | 7.28 | pKi | 52.8 | nM | Ki | J Med Chem (1996) 39: 543-548 [PMID:8558525] |
| ChEMBL | Binding affinity against Serotonin transporter in male Sprague-Dawley rats using [3H]paroxetine ligand | B | 7.62 | pKi | 24.1 | nM | Ki | J Med Chem (1999) 42: 4446-4455 [PMID:10543888] |
| ChEMBL | In vitro binding affinity at serotonin transporter in rat striatum by [3H]- citalopram displacement. | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2001) 44: 937-948 [PMID:11300876] |
| ChEMBL | Inhibition of binding of [3H]- citalopram to Serotonin transporter (SERT) of rat cerebral cortex. | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2002) 45: 654-662 [PMID:11806716] |
| ChEMBL | Inhibition of binding of [3H]citalopram to (SERT) serotonin transporter in rat striatum | B | 6.88 | pIC50 | 132 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1591-1595 [PMID:12699762] |
| ChEMBL | Binding affinity at serotonin transporter in rat striatum by [3H]citalopram displacement. | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2003) 46: 2205-2215 [PMID:12747792] |
| ChEMBL | Binding affinity towards serotonin transporter in rat striatum using [3H]citalopram as radioligand | B | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2003) 46: 1220-1228 [PMID:12646032] |
| ChEMBL | Binding affinity was determined at the Serotonin transporter labeled with radioligand [125 I] RTI-55 | B | 6.9 | pIC50 | 126 | nM | IC50 | J Med Chem (1997) 40: 705-716 [PMID:9057857] |
| ChEMBL | Binding affinity for rat 5-hydroxytryptamine transporter. | B | 6.9 | pIC50 | 126 | nM | IC50 | J Med Chem (2000) 43: 4840-4849 [PMID:11123994] |
| ChEMBL | Inhibition of rat brain Serotonin transporter uptake as [3H]5-HT accumulation | B | 6.99 | pIC50 | 101.4 | nM | IC50 | J Med Chem (2005) 48: 4962-4971 [PMID:16033275] |
| ChEMBL | IC50 value was evaluated using [3H]citalopram (radioligand) on serotonin transporter in rat striatum. | B | 7.06 | pIC50 | 87 | nM | IC50 | J Med Chem (1998) 41: 3293-3297 [PMID:9703474] |
| ChEMBL | Inhibitory activity against serotonin transporter (SERT) labeled with [3H]-citalopram in rat brain striatal membrane. | B | 7.06 | pIC50 | 86.6 | nM | IC50 | J Med Chem (1998) 41: 699-705 [PMID:9513598] |
| ChEMBL | Binding affinity at serotonin transporter from rat brain striatal membrane by [3H]citalopram displacement. | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (1996) 39: 749-756 [PMID:8576918] |
| ChEMBL | In vitro inhibition of [3H]citalopram binding to serotonin transporter on rat striatal membranes. | B | 7.09 | pIC50 | 82 | nM | IC50 | J Med Chem (1997) 40: 35-43 [PMID:9016326] |
| ChEMBL | Reuptake inhibition of [3H]-5-HT (5-HT) in rat. | F | ||||||